L
labetalol
la-bayt-a-lol
(Apo-Labetalol
, Normodyne
, Trandate
)
Do not confuse labetalol with betaxolol, metoprolol or propranolol, or Trandate with tramadol or Trental.
FIXED-COMBINATION(S)
Normozide: labetalol/hydrochlorothiazide (a diuretic): 100 mg/25 mg, 200 mg/25 mg, 300 mg/25 mg.
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: Alpha-, beta-adrenergic blocker. CLINICAL: Antihypertensive.
USES
Management of mild to severe hypertension. IV for severe hypertension. OFF-LABEL: Management of preeclampsia, severe hypertension in pregnancy, hypertension during acute ischemic stroke, pediatric hypertension.
PRECAUTIONS
Contraindications: Hypersensitivity to labetalol. Bronchial asthma, cardiogenic shock, uncompensated HF, second- or third-degree heart block (except in pts with functioning pacemaker), severe bradycardia, conditions associated with severe, prolonged hypotension. Cautions: Compensated HF, severe anaphylaxis to allergens, myasthenia gravis, psychiatric disease, hepatic impairment, pheochromocytoma, diabetes mellitus; concurrent use with digoxin, verapamil, or diltiazem; arterial obstruction, elderly. Pts with peripheral vascular disease, Raynaud’s disease.
ACTION
Blocks alpha1-, beta1-, beta2- (large doses) adrenergic receptor sites. Therapeutic Effect: Slows sinus heart rate; decreases peripheral vascular resistance, B/P.
PHARMACOKINETICS
| Route | Onset | Peak | Duration |
| PO | 0.5–2 hrs | 2–4 hrs | 8–12 hrs |
| IV | 2–5 min | 5–15 min | 2–4 hrs |
Incompletely absorbed from GI tract. Bioavailability: 25%. Protein binding: 50%. Metabolized in liver. Primarily excreted in urine. Not removed by hemodialysis. Half-life: 6–8 hrs.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Drug crosses placenta. Small amount distributed in breast milk. Children: Safety and efficacy not established. Elderly: Age-related peripheral vascular disease may increase susceptibility to decreased peripheral circulation.
INTERACTIONS
DRUG: May decrease effects of beta2-adrenergic agonists (e.g., arformoterol, salmeterol), theophylline. Beta blockers (e.g., carvedilol, metoprolol), digoxin may increase risk of bradycardia. HERBAL: Ephedra, ginseng, yohimbe may worsen hypertension. Garlic may increase antihypertensive effect. Licorice may cause water retention, increased serum sodium, decreased serum potassium. FOOD: None known. LAB VALUES: May increase serum antinuclear antibody titer (ANA), BUN, LDH, alkaline phosphatase, bilirubin, creatinine, potassium, triglycerides, lipoprotein, uric acid, ALT, AST.
AVAILABILITY (Rx)
Injection Solution: 5 mg/ml. Tablets (Trandate): 100 mg, 200 mg, 300 mg.
ADMINISTRATION/HANDLING
IV
◀ ALERT ▶ Prolonged duration of action: Monitor several hrs after administration. Excessive administration may result in prolonged hypotension and/or bradycardia.
Reconstitution • For IV infusion, dilute in D5W to provide concentration of 1–2 mg/ml.
Rate of Administration • For IV push, administer at a rate of 10 mg/min. • For IV infusion, administer at rate of 2 mg/min initially. Rate is adjusted according to B/P. • Monitor B/P immediately before and q5–10min during IV administration (maximum effect occurs within 5 min).
Storage • Store at room temperature. • After dilution, IV solution is stable for 72 hrs. • Solution appears clear, colorless to light yellow. • Discard if discolored or precipitate forms.
PO
• Give without regard to food. • Tablets may be crushed.
IV INCOMPATIBILITIES
Amphotericin B complex (Abelcet, AmBisome, Amphotec), ceftaroline (Teflaro), ceftriaxone (Rocephin), furosemide (Lasix), heparin, nafcillin (Nafcil).
IV COMPATIBILITIES
Amiodarone (Cordarone), calcium gluconate, dexmedetomidine (Precedex), diltiazem (Cardizem), dobutamine (Dobutrex), dopamine (Intropin), enalapril (Vasotec), fentanyl (Sublimaze), hydromorphone (Dilaudid), lidocaine, lorazepam (Ativan), magnesium sulfate, midazolam (Versed), milrinone (Primacor), morphine, nitroglycerin, norepinephrine (Levophed), potassium chloride, potassium phosphate, propofol (Diprivan).
INDICATIONS/ROUTES/DOSAGE
Hypertension
PO: ADULTS, ELDERLY: Initially, 100 mg twice daily. Adjust in increments of 100 mg twice daily q2–3days, Usual dose: 100–300 mg twice daily. Maximum: 2.4 g/day. CHILDREN: 1–3 mg/kg/day in 2 divided doses. Maximum: 10–12 mg/kg/day up to 1,200 mg/day.
Severe Hypertension, Hypertensive Crisis
IV: ADULTS: Initially, 20 mg (bolus over 2 min). Additional doses of 40–80 mg may be given at 10-min intervals, up to total dose of 300 mg.
IV Infusion: ADULTS: Initially, 2 mg/min up to total dose of 300 mg. CHILDREN: 0.4–1 mg/kg/hr. Maximum: 3 mg/kg/hr.
Dosage in Renal Impairment
No dose adjustment.
Dosage in Hepatic Impairment
Use caution.
SIDE EFFECTS
Frequent (20%–11%): Drowsiness, dizziness, excessive fatigue. Occasional (10% or less): Dyspnea, peripheral edema, depression, anxiety, constipation, diarrhea, nasal congestion, weakness, diminished sexual function, transient scalp tingling, insomnia, nausea, vomiting, abdominal discomfort. Rare: Altered taste, dry eyes, increased urination, paresthesia.
ADVERSE EFFECTS/TOXIC REACTIONS
May precipitate, aggravate HF due to decreased myocardial stimulation. Abrupt withdrawal may precipitate myocardial ischemia, producing chest pain, diaphoresis, palpitations, headache, tremor. May mask signs, symptoms of acute hypoglycemia (tachycardia, B/P changes) in diabetic pts.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Assess baseline renal function, LFT. Assess B/P, apical pulse immediately before drug administration (if pulse is 60/min or less or systolic B/P is lower than 90 mm Hg, withhold medication, contact physician).
INTERVENTION/EVALUATION
Monitor B/P for hypotension. Assess pulse for quality, irregular rate, bradycardia. Monitor EKG for cardiac arrhythmias. Assist with ambulation if dizziness occurs. Assess for evidence of HF: dyspnea (particularly on exertion or lying down), night cough, peripheral edema, distended neck veins. Monitor I&O (increase in weight, decrease in urine output may indicate HF).
PATIENT/FAMILY TEACHING
• Do not discontinue drug except upon advice of physician (abrupt discontinuation may precipitate heart failure). • Slowly go from lying to standing. • Compliance with therapy regimen is essential to control hypertension, arrhythmias. • Avoid tasks that require alertness, motor skills until response to drug is established. • Report shortness of breath, excessive fatigue, weight gain, prolonged dizziness, headache. • Do not use nasal decongestants, OTC cold preparations (stimulants) without physician approval. • Limit alcohol.
lacosamide
la-koe-sa-myde
(Vimpat)
Do not confuse lacosamide with zonisamide.
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: Succinimide (Schedule V). CLINICAL: Anticonvulsant.
USES
Monotherapy or adjuctive therapy for treatment of partial-onset seizures in pts 17 yrs and older.
PRECAUTIONS
Contraindications: Hypersensitivity to lacosamide. Cautions: Renal/hepatic impairment, cardiac conduction problems (e.g., marked first-degree AV block, second-degree or higher AV block, sick sinus syndrome without pacemaker), myocardial ischemia, HF, pts at risk of suicide.
ACTION
Selectively enhances slow inactivation of sodium channels, stabilizing hyperexcitable neuronal membranes and inhibits neuronal firing. Therapeutic Effect: Produces anticonvulsant effect.
PHARMACOKINETICS
Completely absorbed following PO administration. Protein binding: 15%. Peak plasma concentration: 1–4 hrs after oral dosing and is reached at the end of IV infusion. Primarily excreted in urine. Steady-state levels achieved in 3 days. Removed by hemodialysis. Half-life: 13 hrs.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown if distributed in breast milk. Children: Safety and efficacy not established in pts younger than 17 yrs. Elderly: No age-related precautions noted.
INTERACTIONS
DRUG: Strong CYP2C9 inhibitors (e.g., fluconazole), strong CYP3A4 inhibitors (e.g., clarithromycin, ketoconazole) may increase concentration/effects. HERBAL: None significant. FOOD: None known. LAB VALUES: May increase serum ALT; proteinuria.
AVAILABILITY (Rx)
Injection Solution: 10 mg/ml (20 ml). Oral Solution: 10 mg/ml.
Tablets: 50 mg, 100 mg, 150 mg, 200 mg.
ADMINISTRATION/HANDLING
PO
• Give without regard to meals. • Do not break, crush, dissolve, or divide film-coated tablets. • Oral solution should be administered with a calibrated measuring device. • Discard any unused portion after 7 wks.
IV
• Appears as a clear, colorless solution. • Discard unused portion or if precipitate or discoloration is present. May give without further dilution. • If mixing with diluent, may be stored for 24 hrs at room temperature. Infuse over 30–60 min.
IV COMPATIBILITIES
INDICATIONS/ROUTES/DOSAGE
Note: IV dose is same as oral dose. May give undiluted or mixed in compatible diluent and infused over 30–60 min.
Partial-Onset Seizures
Monotherapy
PO/IV: ADULTS, CHILDREN 17 YRS AND OLDER: Initially, 100 mg twice daily. May increase by 50 mg twice daily at wkly intervals. Maintenance: 150–200 mg twice daily.
Adjunctive Therapy
PO/IV: ADULTS, CHILDREN 17 YRS AND OLDER: Initially, 50 mg twice daily. May increase by 50 mg twice daily at wkly intervals. Maintenance: 100–200 mg twice daily.
Switch from IV to PO
When switching from IV to PO form, use same equivalent daily dosage and frequency as IV administration.
Switch from PO to IV
When switching from PO to IV form, initial total daily IV dosage should be equivalent to total daily dosage and frequency of PO form and should be infused IV over 30–60 min.
Dosage in Renal Impairment
Use caution when titrating. Mild to moderate impairment: No dose adjustment. Severe impairment, end-stage renal disease: Maxiumum: 300 mg/day.
Dosage in Hepatic Impairment
Use caution when titrating. Mild to moderate impairment: Maximum: 300 mg/day. Severe impairment: Not recommended.
SIDE EFFECTS
Frequent (31%–13%): Dizziness, headache. Occasional (11%–5%): Nausea, double vision, vomiting, fatigue, blurred vision, ataxia, tremor, nystagmus. Rare (4%–2%): Vertigo, diarrhea, gait disturbances, memory impairment, depression, pruritus, injection site discomfort.
ADVERSE EFFECTS/TOXIC REACTIONS
Increased risk of suicidal ideation, behavior. Dose-dependent prolongations in PR interval noted. Leukopenia, anemia, thrombocytopenia occur rarely.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Review history of seizure disorder (intensity, frequency, duration, level of consciousness). Initiate seizure precautions. Renal function, LFT, CBC should be performed before therapy begins and periodically during therapy.
INTERVENTION/EVALUATION
Observe for recurrence of seizure activity. Assess for clinical improvement (decrease in intensity/frequency of seizures). Assist with ambulation if dizziness occurs. Assess for suicidal ideation, depression, behavioral changes. Drug should be withdrawn gradually (over a minimum of 1 wk) to minimize potential for increased seizure frequency.
PATIENT/FAMILY TEACHING
• Strict maintenance of drug therapy is essential for seizure control. • Avoid tasks that require alertness, motor skills until response to drug is established. • Avoid alcohol. • Report depression, suicidal ideation, unusual behavioral changes.
lactulose
lak-tyoo-lose
(Apo-Lactulose
, Constulose, Enulose, Generlac, Kristalose)
Do not confuse lactulose with lactose.
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: Lactose derivative. CLINICAL: Hyperosmotic laxative, ammonia detoxicant.
USES
Prevention, treatment of portal-systemic encephalopathy (including hepatic precoma, coma); treatment of constipation.
PRECAUTIONS
Contraindications: Hypersensitivity to lactulose. Pts requiring a low-galactose diet. Cautions: Diabetes mellitus, hepatic impairment, dehydration.
ACTION
Inhibits diffusion of NH3 into blood by converting NH3 to NH4+; enhances diffusion of NH3 from blood to gut, where it is converted to NH4+; produces osmotic effect in colon. Therapeutic Effect: Promotes increased peristalsis, bowel evacuation; decreases serum ammonia concentration.
PHARMACOKINETICS
Poorly absorbed from GI tract. Extensively metabolized in colon. Primarily excreted in feces.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown if drug crosses placenta or is distributed in breast milk. Children: Avoid use in pts younger than 6 yrs (usually unable to describe symptoms). Elderly: No age-related precautions noted.
INTERACTIONS
DRUG: None significant. HERBAL: None significant. FOOD: None known. LAB VALUES: May decrease serum potassium (GI loss).
AVAILABILITY (Rx)
Packets (Kristalose): 10 g, 20 g. Solution, Oral: 10 g/15 ml.
ADMINISTRATION/HANDLING
PO
• Store solution at room temperature. • Solution appears pale yellow to yellow, viscous liquid. Cloudiness, darkened solution does not indicate potency loss. • Drink water, juice, milk with each dose (aids stool softening, increases palatability). • Mix packets with 4 oz water.
Rectal
• Lubricate anus with petroleum jelly before enema insertion. • Insert carefully (prevents damage to rectal wall) with nozzle toward navel. • Squeeze container until entire dose expelled. • Instruct pt to retain 30–60 min in divided doses. Maximum: 60 ml/day (40 g/day).
INDICATIONS/ROUTES/DOSAGE
Constipation
PO: ADULTS, ELDERLY: 15–30 ml (10–20 g)/day, up to 60 ml (40 g)/day. CHILDREN: 1–3 ml/kg/day (0.7–2 g/kg/day). Maximum: 40 g/day (60 ml/day).
Prevention of Portal-Systemic Encephalopathy
ADULTS, ELDERLY: 30–45 ml (20–30 g) 3–4 times/day. Adjust dose q1–2 days to produce 2–3 soft stools/day. CHILDREN: 40–90 ml/day in divided doses 3–4 times/day. INFANTS: 2.5–10 ml/day in 3–4 divided doses. Adjust dose q1–2 days to produce 2–3 soft stools/day.
Treatment of Portal-Systemic Encephalopathy
PO: ADULTS, ELDERLY: Initially, 30–45 ml (20–30 g) every hr to induce rapid laxation. Then, 30–45 ml 3–4 times/day. Adjust dose q1–2days to produce 2–3 soft stools/day.
Rectal Administration (as Retention Enema)
200 g (300 ml) diluted with 700 ml water or NaCl via rectal balloon catheter. Retain 30–60 min q4–6h. (Transition to oral prior to stopping rectal administration.)
Dosage in Renal/Hepatic Impairment
SIDE EFFECTS
Occasional: Abdominal cramping, flatulence, increased thirst, abdominal discomfort. Rare: Nausea, vomiting.
ADVERSE EFFECTS/TOXIC REACTIONS
Severe diarrhea indicates overdose. Long-term use may result in laxative dependence, chronic constipation, loss of normal bowel function.
NURSING CONSIDERATIONS
INTERVENTION/EVALUATION
Encourage adequate fluid intake. Assess bowel sounds for peristalsis. Monitor daily pattern of bowel activity, stool consistency; record time of evacuation. Assess for abdominal disturbances. Monitor serum electrolytes in pts with prolonged, frequent, excessive use of medication.
PATIENT/FAMILY TEACHING
• Evacuation occurs in 24–48 hrs of initial dose. • Institute measures to promote defecation: increase fluid intake, exercise, high-fiber diet.
*lamiVUDine
la-miv-yoo-deen
(Apo-Lamivudine
, Epivir, Epivir-HBV, Heptovir
)
BLACK BOX ALERT Serious, sometimes fatal lactic acidosis, severe hepatomegaly with steatosis (fatty liver) have occurred. Pts must be monitored for chronic hepatitis B infection for several months following therapy. Do not use Epivir-HBV for treatment of HIV infection.
Do not confuse Epivir with Combivir, or lamivudine with lamotrigine.
FIXED-COMBINATION(S)
Combivir: lamivudine/zidovudine (an antiviral): 150 mg/300 mg. Epzicom: lamivudine/abacavir (an antiviral): 300 mg/600 mg. Triumeq: lamivudine/abacavir (antiretroviral)/dolutegravir (integrase inhibitor): 300 mg/600 mg/50 mg. Trizivir: lamivudine/zidovudine/abacavir (an antiviral): 150 mg/300 mg/300 mg.
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: Nucleoside reverse transcriptase inhibitor. CLINICAL: Antiviral.
USES
Epivir: Treatment of HIV infection in combination with at least two other antiretroviral agents. Epivir-HBV: Treatment of chronic hepatitis B infection associated with evidence of hepatitis B viral replication and active hepatic inflammation. OFF-LABEL: Prophylaxis in health care workers at risk of acquiring HIV after occupational exposure to virus. Use as part of multidrug regimen.
PRECAUTIONS
Contraindications: Hypersensitivity to lamivudine. Cautions: Use in children with history of pancreatitis or risk factors for developing pancreatitis. Use in combination with interferon alfa with or without ribavirin in HIV/HBV coinfected pts; renal/hepatic impairment.
ACTION
Inhibits HIV reverse transcriptase by viral DNA chain termination. Inhibits RNA-, DNA-dependent DNA polymerase, an enzyme necessary for HIV, hepatitis B replication. Therapeutic Effect: Slows HIV replication, reduces progression of HIV infection, chronic hepatitis B.
PHARMACOKINETICS
Rapidly, completely absorbed from GI tract. Protein binding: less than 36%. Widely distributed (crosses blood-brain barrier). Primarily excreted unchanged in urine. Not removed by hemodialysis or peritoneal dialysis. Half-life: Children: 2 hrs. Adults: 5–7 hrs.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Drug crosses placenta. Unknown if distributed in breast milk. Breastfeeding not recommended (possibility of HIV transmission). Children: Safety and efficacy not established in pts younger than 3 mos. Elderly: Age-related renal impairment may require dosage adjustment.
INTERACTIONS
DRUG: Zalcitabine may inhibit absorption of both drugs; avoid concurrent administration. HERBAL: None significant. FOOD: None known. LAB VALUES: May increase Hgb, neutrophil count; serum amylase, ALT, AST, bilirubin.
AVAILABILITY (Rx)
Oral Solution: 5 mg/ml (Epivir-HBV), 10 mg/ml (Epivir). Tablets: 100 mg (Epivir-HBV), 150 mg (Epivir), 300 mg (Epivir).
ADMINISTRATION/HANDLING
PO
• Give without regard to meals.
INDICATIONS/ROUTES/DOSAGE
HIV Infection
PO: ADULTS, ELDERLY: 150 mg twice daily or 300 mg once daily. CHILDREN 4 MOS–16 YRS: (Oral Solution): 4 mg/kg twice daily (up to 150 mg/dose). INFANTS 1–3 MOS: 4 mg/kg twice daily. NEONATES YOUNGER THAN 30 DAYS: 2 mg/kg twice daily. (Tablets): 25 KG OR MORE: 150 mg 2 times/day or 300 mg once daily. 20–24 KG: 75 mg in am and 150 mg in pm or 225 mg once daily. 14–19 KG: 75 mg 2 times/day or 150 mg once daily.
Chronic Hepatitis B
PO: ADULTS: 100 mg/day. CHILDREN 2–17 YRS: 3 mg/kg/day. Maximum: 100 mg/day.
Dosage in Renal Impairment
Dosage and frequency are modified based on creatinine clearance.
| Creatinine Clearance | Dosage HIV | Dosage Hepatitis B |
| 30–49 ml/min | 150 mg once/daily | 100 mg first dose, then 50 mg once/daily |
| 15–29 ml/min | 150 mg first dose, then 100 mg once/daily | 100 mg first dose, then 25 mg once/daily |
| 5–14 ml/min | 150 mg first dose, then 50 mg once/daily | 35 mg first dose, then 15 mg once/daily |
| Less than 5 ml/min | 50 mg first dose, then 25 mg once/daily | 35 mg first dose, then 10 mg once/daily |
Hemodialysis: Dosing post-HD recommended.
Dosage in Hepatic Impairment
No dose adjustment.
SIDE EFFECTS
Frequent (35%–10%): Headache, nausea, malaise, fatigue, nasal disturbances, diarrhea, cough, musculoskeletal pain, neuropathy, insomnia, anorexia, dizziness, fever, chills. Occasional (9%–5%): Depression, myalgia, abdominal cramps, dyspepsia, arthralgia.
ADVERSE EFFECTS/TOXIC REACTIONS
Pancreatitis occurs in 13% of pediatric pts. Anemia, neutropenia, thrombocytopenia occur rarely. Lactic acidosis, severe hepatomegaly with steatosis have been reported.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Obtain baseline renal function test, LFT. Screen HIV pts for hepatitis B infection before initiating therapy.
INTERVENTION/EVALUATION
Monitor serum BUN, creatinine, amylase, lipase, ALT, AST, bilirubin. Assess for headache, nausea, cough. Monitor daily pattern of bowel activity, stool consistency. Modify diet or administer laxative as needed. Assess for dizziness, sleep pattern. If pancreatitis in children occurs, movement aggravates abdominal pain; sitting up, flexing at the waist may relieve the pain.
PATIENT/FAMILY TEACHING
• Continue therapy for full length of treatment. • Doses should be evenly spaced. • Lamivudine is not a cure for HIV infection, nor does it reduce risk of transmission to others. • Avoid tasks requiring alertness, motor skills until response to drug is established. • Avoid alcohol. • Closely monitor for symptoms of pancreatitis (severe, steady abdominal pain often radiating to the back, clammy skin, hypotension; nausea/vomiting may accompany abdominal pain).
*lamoTRIgine
la-moe-tri-jeen
(Apo-Lamotrigine
, Lamictal, Lamictal ODT, Lamictal XR)
BLACK BOX ALERT Severe, potentially life-threatening skin rashes have been reported, including Stevens-Johnson syndrome. Risk increased with coadministration with valproic acid and rapid-dose titration.
Do not confuse Lamictal with Lamisil or Lomotil, or lamotrigine with labetalol or lamivudine.
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: Phenyltriazine. CLINICAL: Anticonvulsant.
USES
Immediate-Release: Adjunctive therapy in adults and children with generalized tonic-clonic seizures and partial seizures, treatment of adults and children with generalized seizures of Lennox-Gastaut syndrome. Conversion to monotherapy in adults treated with another enzyme-inducing antiepileptic drug (EIAED) (e.g., valproic acid, carbamazepine, phenytoin, phenobarbital, primidone). Long-term maintenance treatment of bipolar disorder. Treatment of pts 2 yrs and older with primary generalized tonic-clonic seizures. Extended-release: Adjunctive therapy for primary generalized tonic-clonic and partial-onset seizures in pts 13 yrs and older. Conversion to monotherapy in pt 13 yrs and older with partial seizures receiving treatment with a single antiepileptic drug (AED).
PRECAUTIONS
Contraindications: Hypersensitivity to lamotrigine. Cautions: Renal/hepatic impairment, pts at high risk of suicide, pts taking estrogen-containing oral contraceptives, history of adverse hematologic reaction.
ACTION
May block voltage-sensitive sodium channels, stabilizing neuronal membranes, regulating presynaptic transmitter release of excitatory amino acids. Therapeutic Effect: Produces anticonvulsant activity. Delays time to occurrence of acute mood episodes (mania, depression, hypomania).
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Distributed in breast milk. Breastfeeding not recommended. Increased fetal risk of oral cleft formation has been noted with use during pregnancy. Children: Safety and efficacy in pts 18 yrs and younger with bipolar disorder, younger than 13 yrs with epilepsy not established. Elderly: Age-related renal impairment may require dosage adjustment.
INTERACTIONS
DRUG: Carbamazepine, phenobarbital, primidone, phenytoin, rifampin may decrease concentration. Valproic acid may increase concentration/effects. May decrease effects of oral contraceptives. HERBAL: Evening primrose may decrease seizure threshold. FOOD: None known. LAB VALUES: None significant.
AVAILABILITY (Rx)
Tablets: 25 mg, 100 mg, 150 mg, 200 mg. Tablets (Chewable): 5 mg, 25 mg. Tablets (Orally Disintegrating): 25 mg, 50 mg, 100 mg, 200 mg.
Tablets (Extended-Release): 25 mg, 50 mg, 100 mg, 200 mg, 250 mg, 300 mg.
ADMINISTRATION/HANDLING
PO
• Give without regard to food. • Chewable tablets may be dispensed in water or diluted fruit juice, or swallowed whole. • Extended-release tablets must be swallowed whole; do not break, crush, dissolve, or divide. • Place orally disintegrating tablet on tongue, allow to dissolve. Pt must not break, cut, or chew. Can be swallowed without regard to food or water.
INDICATIONS/ROUTES/DOSAGE
Lennox-Gastaut, Primary Generalized Tonic-Clonic Seizures, Partial Seizures
PO: ADULTS, ELDERLY, CHILDREN OLDER THAN 12 YRS: Initially, 25 mg/day for 2 wks, then increase to 50 mg/day for 2 wks. After 4 wks, may increase by 50 mg/day at 1- to 2-wk intervals. Maintenance: 225–375 mg/day in 2 divided doses. CHILDREN 2–12 YRS: Initially, 0.3 mg/kg/day in 1–2 divided doses for 2 wks, then increase to 0.6 mg/kg/day in 1–2 divided doses for 2 wks. After 4 wks, may increase by 0.6 mg/kg/day at 1- to 2-wk intervals. Maintenance: 4.5–7.5 mg/kg/day in 2 divided doses. Maximum: 300 mg/day in 2 divided doses.
Adjusted Dosage with Antiepileptic Drugs Containing Valproic Acid
PO: ADULTS, ELDERLY, CHILDREN OLDER THAN 12 YRS: Initially, 25 mg every other day for 2 wks, then increase to 25 mg/day for 2 wks. After 4 wks, may increase by 25–50 mg/day at 1- to 2-wk intervals. Maintenance: 100–400 mg/day in 2 divided doses (100–200 mg/day when taking lamotrigine with valproic acid alone). CHILDREN 2–12 YRS: Initially, 0.15 mg/kg/day in 1–2 divided doses for 2 wks, then increase to 0.3 mg/kg/day in 1–2 divided doses for 2 wks. After 4 wks, may increase by 0.3 mg/kg/day at 1- to 2-wk intervals. Maintenance: 1–5 mg/kg/day in 2 divided doses. Maximum: 200 mg/day in 2 divided doses.
Adjusted Dosage with EIAED without Valproic Acid
PO: ADULTS, ELDERLY, CHILDREN OLDER THAN 12 YRS: Initially, 50 mg/day for 2 wks, then increase to 100 mg/day in 2 divided doses for 2 wks. After 4 wks, may increase by 100 mg/day at 1- to 2-wk intervals. Maintenance: 300–500 mg/day in 2 divided doses. CHILDREN 2–12 YRS: Initially, 0.6 mg/kg/day in 1–2 divided doses for 2 wks, then increase to 1.2 mg/kg/day in 1–2 divided doses for 2 wks. After 4 wks, may increase by 1.2 mg/kg/day at 1- to 2-wk intervals. Maintenance: 5–15 mg/kg/day in 2 divided doses. Maximum: 400 mg/day in 2 divided doses.
Usual Maintenance Range for Extended-Release Tablets
PT TAKING VALPROIC ACID: 200–250 mg once daily. PT TAKING EIAED WITHOUT VALPROIC ADIC: 400–600 mg once daily. PT NOT TAKING EIAED: 300–400 mg once daily.
Conversion to Monotherapy for Pts Receiving EIAEDs
PO: ADULTS, ELDERLY, CHILDREN 16 YRS AND OLDER: 500 mg/day in 2 divided doses. Titrate to desired dose while maintaining EIAED at fixed level, then withdraw EIAED by 20% each wk over a 4-wk period.
Conversion to Monotherapy for Pts Receiving Valproic Acid
PO: ADULTS, ELDERLY, CHILDREN 16 YRS AND OLDER: Titrate lamotrigine to 200 mg/day, maintaining valproic acid dose. Maintain lamotrigine dose and decrease valproic acid to 500 mg/day, no greater than 500 mg/day/wk, then maintain 500 mg/day for 1 wk. Increase lamotrigine to 300 mg/day and decrease valproic acid to 250 mg/day. Maintain for 1 wk, then discontinue valproic acid and increase lamotrigine by 100 mg/day each wk until maintenance dose of 500 mg/day reached.
Bipolar Disorder
PO: ADULTS, ELDERLY: Initially, 25 mg/day for 2 wks, then 50 mg/day for 2 wks, then 100 mg/day for 1 wk, then 200 mg/day beginning with wk 6.
Bipolar Disorder in Pts Receiving EIAEDs
PO: ADULTS, ELDERLY: 50 mg/day for 2 wks, then 100 mg/day for 2 wks, then 200 mg/day for 1 wk, then 300 mg/day for 1 wk, then up to usual maintenance dose 400 mg/day in divided doses.
Bipolar Disorder in Pts Receiving Valproic Acid
PO: ADULTS, ELDERLY: 25 mg/day every other day for 2 wks, then 25 mg/day for 2 wks, then 50 mg/day for 1 wk, then 100 mg/day. Usual maintenance dose with valproic acid: 100 mg/day.
Usual Dosage for Lamictal XR
Adjunct Therapy: Range: 200–600 mg/day.
Conversion to Monotherapy: Range: 250–500 mg/day.
Discontinuation Therapy
◀ ALERT ▶ A dosage reduction of approximately 50%/wk over at least 2 wks is recommended.
Dosage in Renal Impairment
◀ ALERT ▶ Decreased dosage may be effective in pts with significant renal impairment.
Dosage in Hepatic Impairment
Mild impairment: No dose adjustment. Moderate to severe impairment without ascites: Reduce dose by 25%. Severe impairment with ascites: Reduce dose by 50%.
SIDE EFFECTS
Frequent (38%–14%): Dizziness, headache, diplopia, ataxia, nausea, blurred vision, drowsiness, rhinitis. Occasional (10%–5%): Rash, pharyngitis, vomiting, cough, flu-like symptoms, diarrhea, dysmenorrhea, fever, insomnia, dyspepsia. Rare: Constipation, tremor, anxiety, pruritus, vaginitis, hypersensitivity reaction.
ADVERSE EFFECTS/TOXIC REACTIONS
Abrupt withdrawal may increase seizure frequency. Serious rashes, including Stevens-Johnson syndrome, have been reported.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Review history of seizure disorder (type, onset, intensity, frequency, duration, LOC), medication history (esp. other anticonvulsants), other medical conditions (e.g., renal impairment). Initiate seizure precautions. Assess baseline mood, behavior.
INTERVENTION/EVALUATION
Report occurrence of rash (drug discontinuation may be necessary). Assist with ambulation if dizziness, ataxia occurs. Assess for clinical improvement (decreased intensity/frequency of seizures). Assess for visual abnormalities, headache. Monitor for suicidal ideation, depression, behavioral changes.
PATIENT/ FAMILY TEACHING
• Take medication only as prescribed; do not abruptly discontinue medication after long-term therapy. • Avoid alcohol. • Avoid tasks that require alertness, motor skills until response to drug is established. • Carry identification card/bracelet to note anticonvulsant therapy. • Strict maintenance of drug therapy is essential for seizure control. • Report any rash, fever, swelling of glands, worsening depression, suicidal ideation, unusual changes in behavior, worsening of seizure control. • May cause photosensitivity reaction; avoid exposure to sunlight, ultraviolet light.
lansoprazole
lan-soe-pra-zole
(Apo-Lansoprazole
, First Lansoprazole, Prevacid, Prevacid Solu-Tab, Prevacid 24HR)
Do not confuse lansoprazole with aripiprazole or dexlansoprazole, or Prevacid with Pravachol, Prilosec, or Prinivil.
FIXED-COMBINATION(S)
Prevacid NapraPac: lansoprazole/naproxen (an NSAID): 15 mg/375 mg, 15 mg/500 mg. Prevpac: Combination card containing amoxicillin 500 mg (4 capsules), lansoprazole 30 mg (2 capsules), clarithromycin 500 mg (2 tablets).
♦ CLASSIFICATION
CLINICAL: Proton pump inhibitor.
USES
Short-term treatment (4 wks and less) of healing, symptomatic relief of active duodenal ulcer; short-term treatment (8 wks and less) for healing, symptomatic relief of erosive esophagitis. Long-term treatment of pathologic hypersecretory conditions, including Zollinger-Ellison syndrome. Short-term treatment (8 wks and less) of active benign gastric ulcer, H. pylori–associated duodenal ulcer (part of multidrug regimen), maintenance treatment for healed duodenal ulcer. Treatment of gastroesophageal reflux disease (GERD), NSAID-associated gastric ulcer. Reduce risk of NSAID- associated gastric ulcer in pts with history of gastric ulcer requiring NSAIDs. OTC: Relief of frequent heartburn (2 or more days/wk). IV: Short-term treatment of erosive esophagitis. OFF-LABEL: Stress ulcer prophylaxis in critically ill.
PRECAUTIONS
Contraindications: Hypersensitivity to lansoprazole, other proton pump inhibitors. Cautions: Hepatic impairment. May increase risk of hip, wrist, spine fractures; GI infections.
ACTION
Inhibits the (H+, K+)–ATPase enzyme system, blocking the final step in gastric acid secretion. Therapeutic Effect: Suppresses gastric acid secretion.
PHARMACOKINETICS
Rapid, complete absorption (food may decrease absorption) once drug has left stomach. Protein binding: 97%. Distributed primarily to gastric parietal cells. Metabolized in liver. Eliminated in bile and urine. Not removed by hemodialysis. Half-life: 1.5 hrs (increased in hepatic impairment, elderly).
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown if distributed in breast milk. Children: Safety and efficacy not established. Elderly: No age-related precautions noted but doses greater than 30 mg not recommended.
INTERACTIONS
DRUG: May decrease concentration of atazanavir. May interfere with absorption of ampicillin, digoxin, iron salts, ketoconazole. Sucralfate may delay absorption. May increase effect of warfarin. May decrease effect of clopidogrel. HERBAL: St. John’s wort may decrease concentration/effect. FOOD: Food may decrease absorption. LAB VALUES: May increase serum LDH, alkaline phosphatase, bilirubin, cholesterol, creatinine, ALT, AST, triglycerides, uric acid; Hgb, Hct. May produce abnormal albumin/globulin ratio, electrolyte balance, platelet, RBC, WBC count.
AVAILABILITY (Rx)
Tablets, Orally Disintegrating (Prevacid Solu-Tab): 15 mg, 30 mg. Powder for Oral Suspension (First Lansoprazole): 3 mg/ml.
Capsules (Delayed-Release): (Prevacid): 15 mg, 30 mg. (Prevacid 24HR): 15 mg.
ADMINISTRATION/HANDLING
PO
• Best if taken before breakfast • Do not cut/crush delayed-release capsules. • If pt has difficulty swallowing capsules, open capsules, sprinkle granules on 1 tbsp of applesauce, give immediately. Do not crush or allow pt to chew granules.
PO (Solu-Tab)
• Place tablet on tongue; allow to dissolve, then swallow. • May give via oral syringe or nasogastric tube. • May dissolve in 4 ml (15 mg) or 10 ml (30 mg) water.
INDICATIONS/ROUTES/DOSAGE
Duodenal Ulcer
PO: ADULTS, ELDERLY: 15 mg/day, before morning meal for up to 4 wks. Maintenance: 15 mg/day.
Erosive Esophagitis
PO: ADULTS, ELDERLY: 30 mg/day, before morning meal for up to 8 wks. If healing does not occur within 8 wks (in 5%–10% of cases), may give for additional 8 wks. Maintenance: 15 mg/day. CHILDREN 1–11 YRS, WEIGHING GREATER THAN 30 KG: 30 mg/day; WEIGHING 30 KG OR LESS: 15 mg/day.
Gastric Ulcer
PO: ADULTS: 30 mg/day for up to 8 wks.
Nsaid Gastric Ulcer
PO: ADULTS, ELDERLY: (Healing): 30 mg/day for up to 8 wks. (Prevention): 15 mg/day for up to 12 wks.
Gastroesophageal Reflux Disease (GERD)
PO: ADULTS: 15 mg/day for up to 8 wks.
CHILDREN 12–17 YRS: 30 mg/day up to 8 wks. CHILDREN 1–11 YRS, WEIGHING GREATER THAN 30 KG: 30 mg/day; WEIGHING 30 KG OR LESS: 15 mg/day.
H. Pylori Infection
PO: ADULTS, ELDERLY: (triple drug therapy including amoxicillin, clarithromycin) 30 mg q12h for 10–14 days or (with amoxicillin) 30 mg 3 times/day for 14 days.
Pathologic Hypersecretory Conditions (Including Zollinger-Ellison Syndrome)
PO: ADULTS, ELDERLY: Initially, 60 mg/day. Individualize dosage according to pt needs and for as long as clinically indicated. Administer doses greater than 120 mg/day in divided doses.
Heartburn (OTC)
PO: ADULTS, ELDERLY: 15 mg once daily for 14 days. May repeat q4mos.
Dosage in Renal Impairment
No dose adjustment.
Dosage in Hepatic Impairment
Consider dose reduction in severe impairment.
SIDE EFFECTS
Occasional (3%–2%): Diarrhea, abdominal pain, rash, pruritus, altered appetite. Rare (1%): Nausea, headache.
ADVERSE EFFECTS/TOXIC REACTIONS
Bilirubinemia, eosinophilia, hyperlipemia occur rarely. May increase risk of C. difficile infection.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Obtain baseline lab values. Assess for epigastric/abdominal pain, evidence of GI bleeding, ecchymosis.
INTERVENTION/EVALUATION
Monitor CBC, hepatic/renal function tests. Assess for therapeutic response (relief of GI symptoms). Question if diarrhea, abdominal pain, nausea occurs. Obtain C. difficile PCR test in pts with persistent diarrhea, fever, abdominal pain.
PATIENT/ FAMILY TEACHING
• Do not chew, crush delayed-release capsules. • For pts who have difficulty swallowing capsules, open capsules, sprinkle granules on 1 tbsp of applesauce, swallow immediately.
lapatinib
la-pa-tin-ib
(Tykerb)
BLACK BOX ALERT Hepatotoxicity (serum ALT or AST more than 3 times upper limit of normal [ULN] and total bilirubin more than 2 times ULN), possibly severe, has occurred.
Do not confuse lapatinib with dasatinib, erlotinib, or imatinib.
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: Tyrosine kinase inhibitor. CLINICAL: Antineoplastic.
USES
Combination treatment with capecitabine for treatment of human epidermal growth receptor type 2 (HER2) overexpressing advanced or metastatic breast cancer in pts who have received prior therapy including an anthracycline, a taxane, and trastuzumab. Combination treatment with letrozole for treatment of postmenopausal women with HER2 overexpressing hormone receptor-positive metastatic breast cancer for whom hormonal therapy is indicated. OFF-LABEL: Treatment (in combination with trastuzumab) of HER2-overexpressing metastatic breast cancer that progressed on prior trastuzumab-containing therapy. Treatment of HER2-overexpressing metastatic breast cancer with brain metastasis.
PRECAUTIONS
Contraindications: Hypersensitivity to lapatinib. Cautions: Left ventricular function abnormalities, prolonged QT interval or medications known to prolong QT interval, hepatic impairment. History of treatment with anthracyclines, chest wall irradiation. Avoid concurrent use with strong CYP3A4 inhibitors or inducers.
ACTION
Inhibitory action against kinases targeting intracellular components of epidermal growth factor receptor ErbB1 and a second receptor, human epidermal receptor (HER2 [ErbB2]). Therapeutic Effect: Inhibits ErbB-driven tumor cell growth, produces tumor regression, inhibits metastasis.
PHARMACOKINETICS
| Route | Onset | Peak | Duration |
| PO | 30 min | 4 hrs | — |
Steady-state level occurs within 6–7 days. Incomplete and variable oral absorption. Undergoes extensive metabolism. Protein binding: 99%. Minimally excreted in feces and plasma. Half-life: 24 hrs.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: May cause fetal harm. Unknown if distributed in breast milk. Children: Safety and efficacy not established. Elderly: No age-related precautions noted.
INTERACTIONS
DRUG: May increase digoxin levels. CYP3A4 inhibitors (e.g., clarithromycin, ketoconazole, ritonavir) may increase plasma concentration. CYP3A4 inducers (e.g., carbamazepine, phenytoin, rifampin) may decrease plasma concentration. HERBAL: St. John’s wort decreases plasma concentration. FOOD: Grapefruit products may increase plasma concentration (potential for torsades, myelotoxicity). LAB VALUES: May increase serum ALT, AST, bilirubin. May decrease neutrophils, Hgb, platelets.
AVAILABILITY (Rx)
Tablets: 250 mg.
ADMINISTRATION/HANDLING
PO
• Do not break, crush, dissolve, or divide film-coated tablets. • Give at least 1 hr before or 1 hr after food. Take full dose at same time each day.
INDICATIONS/ROUTES/DOSAGE
Breast Cancer
PO: ADULTS, ELDERLY: (With capecitabine): 1,250 mg (5 tablets) once daily. (With letrozole): 1,500 mg once daily continuously with letrozole. Continue until disease progresses or unacceptable toxicity.
Dose Modification
Cardiac Toxicity
Discontinue with decreased left ventricular ejection fraction grade 2 or higher, or in pts with an ejection fraction that drops to lower limit of normal. May be started at a reduced dose (1,000 mg/day) at a minimum of 2 wks when ejection fraction returns to normal and pt is asymptomatic.
Pulmonary Toxicity
Discontinue with symptoms indicative of interstitial lung disease or pneumonitis grade 3 or higher.
Severe Hepatic Impairment
With capecitabine: 750 mg/day. With letrozole: 1,000 mg/day.
CYP3A4 Inhibitors/Inducers
Concomitant use of CYP3A4 inhibitors may require dose reduction of lapatinib (e.g., decrease to 500 mg/day with careful monitoring); CYP3A4 inducers may require dose increase of lapatinib (e.g., increase to 4,500 mg with capecitabine or 5,500 mg with letrozole).
Dosage in Renal Impairment
No dose adjustment.
Dosage in Hepatic Impairment
Mild to moderate impairment: No dose adjustment. Severe impairment: See dose modification.
SIDE EFFECTS
Common (65%–44%): Diarrhea, hand-foot syndrome (blistering/rash/peeling of skin on palms of hands, soles of feet), nausea. Frequent (28%–26%): Rash, vomiting. Occasional (15%–10%): Mucosal inflammation, stomatitis, extremity pain, back pain, dry skin, insomnia.
ADVERSE EFFECTS/TOXIC REACTIONS
Decreases in left ventricular ejection grade 3 or higher have been observed; 20% decrease relative to baseline is considered toxic.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Question for possibility of pregnancy. Obtain baseline CBC, serum chemistries before treatment begins and monthly thereafter.
INTERVENTION/EVALUATION
Offer antiemetics to control nausea, vomiting. Monitor daily pattern of bowel activity, stool consistency. Monitor CBC (particularly Hgb, platelets, neutrophil count), LFT. Assess hands and feet for erythema/blistering/peeling. Monitor for shortness of breath, palpitations, fatigue (decreased cardiac ejection fraction).
PATIENT/FAMILY TEACHING
• Avoid crowds, those with known infection. • Avoid contact with those who recently received live virus vaccine. • Do not have immunizations without physician’s approval (drug lowers resistance). • Promptly report fever, unusual bruising/bleeding from any site. • Ensure use of appropriate birth control measures in women.
leflunomide
lee-floo-noe-myde
(Apo-Leflunomide
, Arava)
BLACK BOX ALERT Do not use during pregnancy. Women of childbearing potential must be counseled regarding fetal risk, use of reliable contraceptives confirmed, possibility of pregnancy excluded. Severe hepatic injury may occur.
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: Immunomodulatory agent. CLINICAL: Anti-inflammatory, antirheumatic.
USES
Treatment of active rheumatoid arthritis (RA). Improve physical function in pts with rheumatoid arthritis. OFF-LABEL: Treatment of cytomegalovirus (CMV) disease. Prevention of acute/chronic rejection in recipients of solid organ transplants.
PRECAUTIONS
Contraindications: Hypersensitivity to leflunomide. Pregnancy or plans for pregnancy. Severe hepatic impairment. Cautions: Hepatic/renal impairment, hepatitis B or C infection, pts with immunodeficiency or bone marrow dysplasias, breastfeeding mothers, history of new/recurrent infections, significant hematologic abnormalities, diabetes, concomitant use of neurotoxic medications, elderly.
ACTION
Inhibits pyrimidine synthesis, resulting in antiproliferative and anti-inflammatory effects. Therapeutic Effect: Reduces signs/symptoms of RA, retards structural damage.
PHARMACOKINETICS
Well absorbed after PO administration. Protein binding: greater than 99%. Metabolized in GI wall, liver. Excreted through renal, biliary systems. Not removed by hemodialysis. Half-life: 16 days.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Can cause fetal harm. Unknown if distributed in breast milk. Breastfeeding not recommended. Children: Safety and efficacy not established in pts younger than 18 yrs. Elderly: No age-related precautions noted.
INTERACTIONS
DRUG: Rifampin may increase concentration/effects. Hepatotoxic medications (e.g., acetaminophen, ketoconazole, simvastatin) may increase risk of side effects, hepatotoxicity. Use of live virus vaccine not recommended. HERBAL: Echinacea may decrease effects. FOOD: None known. LAB VALUES: May increase serum ALT, AST, alkaline phosphatase, bilirubin.
AVAILABILITY (Rx)
Tablets: 10 mg, 20 mg.
ADMINISTRATION/HANDLING
PO
• Give without regard to food.
INDICATIONS/ROUTES/DOSAGE
Rheumatoid Arthritis (RA)
PO: ADULTS, ELDERLY: Initially, 100 mg/day for 3 days, then 10–20 mg/day. (Loading dose may be omitted in pts at increased risk of hepatitis or toxicity.)
Dosage in Renal Impairment
Dosage in Hepatic Impairment
ALT 2–3 Times Upper Limit of Normal (ULN): Not recommended. Persistent ALT Level Greater Than 3 Times ULN: Discontinue and initiate accelerated drug elimination.
SIDE EFFECTS
Frequent (20%–10%): Diarrhea, respiratory tract infection, alopecia, rash, nausea.
ADVERSE EFFECTS/TOXIC REACTIONS
May cause immunosuppression. Transient thrombocytopenia, leukopenia, hepatotoxicity occur rarely.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Question for possibility of pregnancy. Obtain baseline CBC, LFT. Assess limitations in activities of daily living due to rheumatoid arthritis (RA).
INTERVENTION/EVALUATION
Monitor tolerance to medication. Assess symptomatic relief of RA (relief of pain; improved range of motion, grip strength, mobility). Monitor LFT.
PATIENT/FAMILY TEACHING
• May take without regard to food. • Improvement may take longer than 8 wks. • Avoid pregnancy.
lenalidomide
len-a-lid-o-myde
(Revlimid)
BLACK BOX ALERT Analogue to thalidomide. High potential for significant birth defects. Hematologic toxicity (thrombocytopenia, neutropenia) occurs in 80% of pts. Greatly increases risk for DVT, pulmonary embolism in multiple myeloma pts.
Do not confuse lenalidomide with thalidomide.
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: Isoxazole immunomodulator. CLINICAL: Immunosuppressive agent.
USES
Treatment of low- to intermediate-risk myelodysplastic syndrome (MDS) in pts with deletion 5q cytogenetic abnormality with transfusion-dependent anemia. Treatment of multiple myeloma (in combination with dexamethasone). Treatment of relapsed or refractory mantle cell lymphoma. OFF-LABEL: Systemic amyloidosis, lower-risk myelodysplastic syndrome, non-Hodgkin’s lymphoma, maintenance treatment for multiple myeloma (following autologous stem cell transplant). Relapsed or refractory chronic lymphocytic leukemia (CLL).
PRECAUTIONS
Contraindications: Hypersensitivity to lenalidomide. Pregnancy, women capable of becoming pregnant. Cautions: Renal/hepatic impairment. History of arterial thromboembolic events, hypertension, hyperlipidemia. Avoid use in pts with glucose intolerance, lactase deficiency.
ACTION
Inhibits secretion of pro-inflammatory cytokines, increases secretion of anti-inflammatory cytokines. Enhances cell-mediated immunity by stimulation of T-cells. Therapeutic Effect: Inhibits myeloma cell growth; induces cell cycle arrest and cell death.
PHARMACOKINETICS
Well absorbed following PO administration. Protein binding: 30%. Eliminated in urine. Half-life: 3 hrs (increased in renal impairment).
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Contraindicated in women who are or may become pregnant, who are not using two reliable forms of contraception, or who are not abstinent. Can cause severe birth defects, fetal death. Unknown if distributed in breast milk; breastfeeding not recommended. Children: Safety and efficacy not established in pts younger than 18 yrs. Elderly: Age-related renal impairment may require caution in dosage selection. Risk of toxic reactions greater in those with renal insufficiency.
INTERACTIONS
DRUG: Erythropoietin, dexamethasone, oral contraceptives may increase risk of deep vein thrombosis, pulmonary embolism. May increase concentration of digoxin. HERBAL: Avoid echinacea (has immunostimulant properties). FOOD: None known. LAB VALUES: May decrease WBC count, Hgb, Hct platelets, troponin I, serum creatinine, sodium, T3, T4. May decrease serum bilirubin, glucose, potassium, magnesium.
AVAILABILITY (Rx)
Capsules: 2.5 mg, 5 mg, 10 mg, 15 mg, 25 mg.
ADMINISTRATION/HANDLING
• Store at room temperature. • Do not break, crush, dissolve, or divide capsules. • Swallow whole with water.
INDICATIONS/ROUTES/DOSAGE
Myelodysplastic Syndrome
PO: ADULTS, ELDERLY: 10 mg once daily.
Dosage Adjustments for Myelodysplastic Syndrome
Platelets:
Thrombocytopenia within 4 wks with 10 mg/day
Baseline platelets 100,000/mm3 or greater: If platelets less than 50,000/mm3, hold treatment. Resume at 5 mg/day when platelets return to 50,000/mm3 or greater. Baseline platelets less than 100,000/mm3: If platelets fall to 50% of baseline, hold treatment. Resume at 5 mg/day if baseline is 60,000/mm3 or greater and platelets return to 50,000/mm3 or greater. Resume at 5 mg/day if baseline is less than 60,000/mm3 and platelets return to 30,000/mm3 or greater.
Thrombocytopenia after 4 wks with 10 mg/day: If platelets less than 30,000/mm3 OR less than 50,000/mm3 with platelet transfusion, hold treatment. Resume at 5 mg/day when platelets return to 30,000/mm3 or greater.
Thrombocytopenia developing with 5 mg/day: If platelets less than 30,000/mm3 OR less than 50,000/mm3 with platelet transfusion, hold treatment. Resume at 5 mg every other day when platelets return to 30,000/mm3 or greater.
Neutrophils:
Neutropenia within 4 wks with 10 mg/day
Baseline absolute neutrophil count (ANC) 1,000/mcl or greater: If ANC less than 750/mm3, hold treatment. Resume at 5 mg/day when ANC 1,000/mm3 or greater. Baseline ANC less than 1,000/mm3: If ANC less than 500/mm3, hold treatment. Resume at 5 mg/day when ANC 500/mm3 or greater.
Neutropenia after 4 wks with 10 mg/day: If ANC less than 500/mm3 for 7 days or longer or associated with fever, hold treatment. Resume at 5 mg/day when ANC 500/mm3 or greater.
Neutropenia developing with 5 mg/day: If ANC less than 500/mm3 for 7 days or longer or associated with fever, hold treatment. Resume at 5 mg every other day when ANC 500/mm3 or greater.
Mantle Cell Lymphoma
PO: ADULTS, ELDERLY: 25 mg once daily on days 1–21 of repeated 28-day cycle.
Multiple Myeloma
PO: ADULTS, ELDERLY: 25 mg/day on days 1–21 of repeated 28-day cycle (in combination with dexamethasone).
Dosage Adjustments for Multiple Myeloma
Platelets:
Thrombocytopenia: If platelets fall to less than 30,000/mm3, hold treatment, monitor CBC. Resume at 15 mg/day when platelets 30,000/mm3 or greater. For each subsequent fall to less than 30,000/mm3, hold treatment and resume at 5 mg/day less than previous dose when platelets return to 30,000/mm3 or greater. Do not dose to less than 5 mg/day.
Neutrophils:
Neutropenia: If neutrophils fall to less than 1,000/mm3, hold treatment, add G-CSF, follow CBC wkly. Resume at 25 mg/day when neutrophils return to 1,000/mm3 and neutropenia is the only toxicity. Resume at 15 mg/day if other toxicity is present. For each subsequent fall to less than 1,000/mm3, hold treatment and resume at 5 mg/day less than previous dose when neutrophils return to 1,000/mm3 or greater. Do not dose to less than 5 mg/day.
Dosage in Renal Impairment
| Creatinine Clearance 30–59 ml/min | Creatinine Clearance Less Than 30 ml/min (Nondialysis Dependent) | Creatinine Clearance Less Than 30 ml/min (Dialysis Dependent) | |
| Myelodysplastic syndrome | 5 mg once daily | 2.5 mg once daily | 2.5 mg once daily (give after dialysis) |
| Multiple myeloma | 10 mg once daily | 15 mg q48h | 5 mg once daily (give after dialysis) |
Dosage in Hepatic Impairment
No dose adjustment.
SIDE EFFECTS
Frequent (49%–31%): Diarrhea, pruritus, rash, fatigue. Occasional (24%–12%): Constipation, nausea, arthralgia, fever, back pain, peripheral edema, cough, dizziness, headache, muscle cramps, epistaxis, asthenia, dry skin, abdominal pain. Rare (10%–5%): Extremity pain, vomiting, generalized edema, anorexia, insomnia, night sweats, myalgia, dry mouth, ecchymosis, rigors, depression, dysgeusia, palpitations.
ADVERSE EFFECTS/TOXIC REACTIONS
Significant increased risk of deep vein thrombosis (DVT), pulmonary embolism. Thrombocytopenia occurs in 62% of pts, neutropenia in 59% of pts, and anemia in 12% of pts. Upper respiratory infection (nasopharyngitis, pneumonia, sinusitis, bronchitis, rhinitis), UTI occur occasionally. Cellulitis, peripheral neuropathy, hypertension, hypothyroidism occur in approximately 6% of pts.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Obtain baseline CBC. Due to high potential for human birth defects/fetal death, female pts must avoid pregnancy 4 wks before therapy, during therapy, during dose interruptions, and 4 wks following therapy. Two reliable forms of contraception must be used even if pt has history of infertility unless it is due to hysterectomy or menopause that has occurred for at least 24 consecutive mos. Confirm two negative pregnancy tests before therapy initiation.
INTERVENTION/EVALUATION
Monitor CBC, BMP, serum magnesium as appropriate. Perform pregnancy tests on women of childbearing potential: wkly during the first 4 wks, then at 4-wk intervals in pts with regular menstrual cycles or q2wks in pts with irregular menstrual cycles. Monitor for hematologic toxicity; obtain CBC wkly during first 8 wks of therapy and at least monthly thereafter. Observe for signs, symptoms of thromboembolism (shortness of breath, chest pain, extremity pain, swelling, stroke-like symptoms).
PATIENT/FAMILY TEACHING
• Two reliable forms of birth control must be used before, during, and after therapy for female pts. • A pregnancy test must be performed within 10–14 days and 24 hrs before therapy begins. • Males must always use a latex condom during any sexual contact with females of childbearing potential even if they have undergone a successful vasectomy. • Avoid crowds; those with active infection. • Treatment may cause blood clots in the arms, legs, or lungs; report arm or leg pain/swelling, difficulty breathing, chest pain.
lenvatinib
len-va-ti-nib
(Lenvima)
Do not confuse lenvatinib with dasatinib, ibrutinib, imatinib.
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: Kinase inhibitor. CLINICAL: Antineoplastic.
USES
Treatment of locally recurrent or metastatic, progressive, radioactive iodine–refractory differentiated thyroid cancer. Treatment of advanced renal cell carcinoma (RCC) after one course of another antineoplastic.
PRECAUTIONS
Contraindications: Hypersensitivity to lenvatinib. Cautions: Electrolyte imbalance (hypokalemia, hypomagnesemia), hepatic/renal impairment. History of cardiac dysfunction (HF, pulmonary edema, right or left ventricular dysfunction), GI perforation/hemorrhage, hypertension, long-QT interval syndrome, medications that prolong QT interval, thromboembolic events (e.g., CVA, DVT), pituitary/thyroid disease.
ACTION
Inhibits tyrosine kinase receptor activity of vascular endothelial growth factor (VEGF) receptors. Inhibits tumor angiogenesis, growth, progression. Therapeutic Effect: Inhibits tumor cell growth and metastasis.
PHARMACOKINETICS
Readily absorbed. Metabolized in liver. Protein binding: 98%–99%. Peak plasma concentration: 1–4 hrs. Eliminated in feces (64%), urine (25%). Not removed by dialysis. Half-life: 28 hrs.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Avoid pregnancy; may cause fetal harm. Female pts of reproductive potential must use effective contraception during treatment for at least 2 mos after discontinuation. Potentially distributed in breast milk. Must either discontinue drug or discontinue breastfeeding. Treatment may reduce fertility in both female and male pts. Children: Safety and efficacy not established. Elderly: No age-related precautions noted.
INTERACTIONS
DRUG: CYP3A4 inhibitors (e.g., ketoconazole, ritonavir) may increase concentration/effect. CYP3A4 inducers (e.g., carbamazepine, rifampin) may decrease concentration/effect. Amiodarone, ciprofloxacin, quinidine may increase risk of QT interval prolongation. Hormonal contraceptives may increase risk of thromboembolic events. HERBAL: None significant. FOOD: None known. LAB VALUES: May increase serum alkaline phosphatase, ALT/AST, amylase, bilirubin, cholesterol, creatinine, lipase. May decrease serum albumin, glucose, magnesium; platelets. May increase or decrease serum calcium, potassium.
AVAILABILITY (Rx)
Capsules: 4 mg, 10 mg.
ADMINISTRATION/HANDLING
PO
• Give without regard to food. • Administer same time each day. • Do not cut, crush, divide, or open capsules.
INDICATIONS/ROUTES/DOSAGE
Thyroid Cancer
PO: ADULTS, ELDERLY: 24 mg once daily. Continue until disease progression or unacceptable toxicity.
RCC
PO: ADULTS, ELDERLY: 18 mg once daily (in combination with everolimus).
Dose Modification
Based on Common Terminology Criteria for Adverse Events (CTCAE).
| Adverse Reaction | Modification | Adjusted Dose |
| First occurrence | Interrupt until resolved to grade 0 or 1 or baseline | 20 mg once daily |
| Second occurrence | Interrupt until resolved to grade 0 or 1 or baseline | 14 mg once daily |
| Third occurrence | Interrupt until resolved to grade 0 or 1 or baseline | 10 mg once daily |
Arterial Thrombotic Event
Discontinue treatment.
Cardiac Dysfunction/Hemorrhagic Event
PO: ADULTS, ELDERLY: Interrupt treatment for grade 3 event until improved to grade 0 to 1 or baseline. Either resume at reduced dose or discontinue (depending on the severity and persistence). Discontinue for grade 4 event.
GI Perforation/Fistula Formation
Discontinue treatment.
Hypertension
PO: ADULTS, ELDERLY: Interrupt treatment for grade 3 hypertension that persists despite optimal antihypertensive therapy. Resume at reduced dose when hypertension is controlled at less than or equal to grade 2. Discontinue for life-threatening hypertension.
Proteinuria
PO: ADULTS, ELDERLY: Interrupt treatment for greater than or equal to 2 g proteinuria/24 hrs. Resume at reduced dose when proteinuria less than 2 g/24 hrs. Discontinue if nephrotic syndrome occurs.
QT Prolongation
PO: ADULTS, ELDERLY: Interrupt treatment for grade 3 or greater. Resume at reduced dose when QT prolongation resolved to grade 0 or 1 or baseline.
Renal Failure/Impairment or Hepatotoxicity
PO: ADULTS, ELDERLY: Interrupt treatment for grade 3 or 4 renal failure/impairment or hepatotoxicity until resolved to grade 0 or 1 or baseline. Either resume at reduced dose or discontinue (depending on the severity and persistence). Discontinue if hepatic failure occurs.
Reversible Posterior Leukoencephalopathy Syndrome (RPLS)
PO: ADULTS, ELDERLY: Interrupt treatment until fully resolved. Resume at reduced dose or discontinue (depending on the severity and persistence of neurologic symptoms).
Other Adverse Reactions
PO: ADULTS, ELDERLY: Reduce dose according to dose modification table. Due to limited data, there are no recommendations on resuming treatment in pts with grade 4 adverse events that resolve.
Dosage in Renal Impairment
Mild to moderate impairment: No dose adjustment. Severe impairment: 14 mg once daily.
Dosage in Hepatic Impairment
Mild to moderate impairment: No dose adjustment. Severe impairment: 14 mg once daily.
SIDE EFFECTS
Frequent (73%–29%): Hypertension, diarrhea, fatigue, asthenia, malaise, arthralgia, myalgia, decreased appetite, weight decreased, nausea, stomatitis, glossitis, mouth ulceration, mucosal inflammation, headache, vomiting, dysphonia, abdominal pain, constipation. Occasional (25%–7%): Oral pain, glossodynia, cough, peripheral edema, rash, dysgeusia, dry mouth, dizziness, dyspepsia, insomnia, alopecia, hypotension, dehydration, hyperkeratosis.
ADVERSE EFFECTS/TOXIC REACTIONS
Serious adverse effects may include: arterial thromboembolic events (5% of pts); cardiac dysfunction (7% of pts); dental and oral infections including gingivitis, parotitis, pericoronitis, periodenitis, sialoadenitis, tooth abscess, tooth infection (10% of pts); GI perforation/fistula formation (2% of pts); hemorrhagic events (35% of pts); hepatotoxicity (4% of pts); hypertension (73% of pts); grade 3 or greater hypocalcemia (9% of pts); impairment of thyroid-stimulating hormone (57% of pts); palmar-plantar erythrodysesthesia (32% of pts); proteinuria (34% of pts); QT interval prolongation (9% of pts); renal failure (14% of pts); urinary tract infection (11% of pts). Reverse posterior leukoencephalopathy occurs rarely. The median onset of hypertension was 16 days. The most frequently reported hemorrhagic event was epistaxis. The primary risk factor for renal failure was dehydration and hypovolemia related to diarrhea and vomiting.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Obtain baseline CBC, BMP, LFT; serum magnesium, phosphate, ionized calcium; urinalysis for proteinuria. Confirm negative pregnancy status before initiating treatment. Receive full medication history and screen for interactions. Question history of cardiac/pituitary/thyroid disease, CVA/DVT, hypertension, hepatic/renal impairment, long-QT interval syndrome. Assess oral cavity for lesions, poor dentation. Ensure B/P is controlled prior to initiation. Assess hydration status.
INTERVENTION/EVALUATION
Monitor B/P after 1 wk, then every 2 wks for the first 2 mos, then at least monthly thereafter. Monitor LFT every 2 wks for the first 2 mos, then at least monthly thereafter. Monitor for proteinuria periodically. If urine dipstick proteinuria is greater than or equal to 2+, obtain a 24-hr urine protein test. Monitor blood calcium levels at least monthly and replace as needed depending on severity, presence of EKG changes, persistence of hypocalcemia. Monitor and correct other electrolyte abnormalities as needed. Initiate medical management for nausea, vomiting, diarrhea prior to any interruption or dose reduction. Reversible posterior leukoencephalopathy syndrome should be considered in pts with altered mental status, confusion, headache, seizures, visual disturbances. Immediately report abdominal pain, GI bleeding, hemoptysis (may indicate GI perforation/fistula formation). Obtain cardiac echocardiogram, EKG if cardiac decompensation is suspected.
PATIENT/FAMILY TEACHING
• Blood levels will be monitored regularly. • Treatment may cause fetal harm. Female pts of childbearing potential should use effective contraception during treatment and up to 2 mos following discontinuation. Immediately report suspected pregnancy. • Therapy may reduce fertility in both female and male pts. • Report liver problems such as upper abdominal pain, bruising, dark or amber-colored urine, nausea, vomiting, or yellowing of the skin or eyes; heart problems such as chest tightness, dizziness, fainting, palpitations, shortness of breath; kidney problems such as dark-colored urine, decreased urine output, extremity swelling, flank pain; skin changes such as rash, skin bubbling, sloughing. • Neurologic changes including blurry vision, confusion, headache, one-sided weakness, seizures, trouble speaking may indicate high blood pressure crisis, stroke, or life-threatening brain swelling. • Report mouth ulceration, jaw pain. • Swallow capsules whole; do not chew, crush, cut, or open capsules. • Treatment may increase risk of GI bleeding, nosebleeds. • Drink plenty of fluids.
letrozole
let-roe-zole
(Apo-Letrozole
, Femara)
Do not confuse Femara with Famvir, Femhrt, or Provera, or letrozole with anastrozole.
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: Aromatase inhibitor, hormone. CLINICAL: Antineoplastic.
USES
First-line treatment of hormone receptor–positive or hormone receptor unknown locally advanced or metastatic breast cancer. Treatment of advanced breast cancer in postmenopausal women with disease progression following antiestrogen therapy. Postsurgical treatment for postmenopausal women with hormone receptor–positive early breast cancer. Extended treatment of early breast cancer after 5 yrs of tamoxifen. OFF-LABEL: Treatment of ovarian (epithelial), endometrial cancer.
PRECAUTIONS
Contraindications: Hypersensitivity to letrozole, other aromatase inhibitors. Use in women who are or may become pregnant. Cautions: Hepatic impairment, hyperlipidemia.
ACTION
Decreases circulating estrogen by inhibiting aromatase, an enzyme that catalyzes the final step in estrogen production. Therapeutic Effect: Inhibits growth of breast cancers stimulated by estrogens.
PHARMACOKINETICS
Rapidly, completely absorbed. Metabolized in liver. Primarily eliminated in urine. Unknown if removed by hemodialysis. Half-life: Approximately 2 days.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown if distributed in breast milk. May cause fetal harm. Children: Safety and efficacy not established. Elderly: No age-related precautions noted.
INTERACTIONS
DRUG: Tamoxifen may reduce concentration. HERBAL: None significant. FOOD: None known. LAB VALUES: May increase serum calcium, cholesterol, GGT, ALT, AST, bilirubin.
AVAILABILITY (Rx)
Tablets: 2.5 mg.
ADMINISTRATION/HANDLING
PO
• Give without regard to food.
INDICATIONS/ROUTES/DOSAGE
Breast Cancer (Advanced)
PO: ADULTS, ELDERLY: 2.5 mg/day. Continue until tumor progression is evident.
Breast Cancer (Early–Adjuvant Treatment)
PO: ADULTS, ELDERLY: (Postmenopausal): 2.5 mg/day for planned duration of 5 yrs. Discontinue at relapse.
Breast Cancer (Early–Extended Adjuvant Treatment)
PO: ADULTS, ELDERLY: (Postmenopausal): 2.5 mg/day for planned duration of 5 yrs (after 5 yrs of tamoxifen). Discontinue at relapse.
Dosage in Renal Impairment
No dose adjustment.
Dosage in Severe Hepatic Impairment
PO: ADULTS, ELDERLY: 2.5 mg every other day.
SIDE EFFECTS
Frequent (21%–9%): Musculoskeletal pain (back, arm, leg), nausea, headache. Occasional (8%–5%): Constipation, arthralgia, fatigue, vomiting, hot flashes, diarrhea, abdominal pain, cough, rash, anorexia, hypertension, peripheral edema. Rare (4%–1%): Asthenia, drowsiness, dyspepsia, weight gain, pruritus.
ADVERSE EFFECTS/TOXIC REACTIONS
Pleural effusion, pulmonary embolism, bone fracture, thromboembolic disorder, MI occur rarely.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Obtain baseline CBC, chemistries, renal function, LFT. Obtain pregnancy test prior to beginning therapy.
INTERVENTION/EVALUATION
Monitor for, assist with ambulation if asthenia, dizziness occurs. Assess for headache. Offer antiemetic for nausea, vomiting. Monitor CBC, thyroid function, electrolytes, renal function, LFT. Monitor for evidence of musculoskeletal pain; offer analgesics for pain relief.
PATIENT/FAMILY TEACHING
• Report if nausea, asthenia, hot flashes become unmanageable. • Discuss importance of negative pregnancy test prior to beginning therapy and nonhormonal methods of birth control. • Explain possible risk to fetus if pt is or becomes pregnant before or during therapy.
leucovorin
loo-koe-vor-in
Do not confuse leucovorin with Leukeran.
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: Folic acid antagonist. CLINICAL: Antidote.
USES
Antidote for folic acid antagonists (methotrexate, trimethoprim, pyrimethoamine). Treatment of megaloblastic anemias when folate deficient. Palliative treatment of advanced colon cancer (with fluorouracil). IV rescue therapy after high-dose methotrexate for osteosarcoma or orally to diminish toxicity and impaired methotrexate elimination. OFF-LABEL: Adjunctive cofactor therapy in methanol toxicity. Prevents pyrimethamine hematologic toxicity in HIV-positive pts.
PRECAUTIONS
Contraindications: Hypersensitivity to leucovorin. Pernicious anemia, other megaloblastic anemias secondary to vitamin B12 deficiency. Cautions: Renal impairment.
ACTION
Competes with methotrexate for same transport processes into cells (limits methotrexate action on normal cells). Therapeutic Effect: Reverses toxic effects of folic acid antagonists. Reverses folic acid deficiency.
PHARMACOKINETICS
Readily absorbed from GI tract. Widely distributed. Metabolized in liver, intestinal mucosa. Primarily excreted in urine. Half-life: 15 min; metabolite, 30–35 min.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown if drug crosses placenta or is distributed in breast milk. Children: May increase risk of seizures by counteracting anticonvulsant effects of barbiturates, hydantoins. Elderly: Age-related renal impairment may require dosage adjustment when used for rescue from effects of high-dose methotrexate therapy.
INTERACTIONS
DRUG: May decrease effects of anticonvulsants (e.g., phenytoin). May increase 5-fluorouracil toxicity/effects when taken in combination. HERBAL: None significant. FOOD: None known. LAB VALUES: May decrease platelets, WBCs (when used in combination with 5-fluorouracil).
AVAILABILITY (Rx)
Injection, Powder for Reconstitution: 50 mg, 100 mg, 200 mg, 350 mg, 500 mg. Injection, Solution: 10 mg/ml. Tablets: 5 mg, 10 mg, 15 mg, 25 mg.
ADMINISTRATION/HANDLING
IV
◀ ALERT ▶ Strict adherence to timing of 5-fluorouracil following leucovorin therapy must be maintained.
Reconstitution • Reconstitute each 50-mg vial with 5 ml Sterile Water for Injection or Bacteriostatic Water for Injection containing benzyl alcohol to provide concentration of 10 mg/ml. • Due to benzyl alcohol in 1-mg ampule and in Bacteriostatic Water for Injection, reconstitute doses greater than 10 mg/m2 with Sterile Water for Injection. • Further dilute with 100–1,000 ml D5W or 0.9% NaCl.
Rate of Administration • Do not exceed 160 mg/min if given by IV infusion (due to calcium content).
Storage • Store powdered vials for parenteral use at room temperature. • Refrigerate solution for injection vials. • Injection appears as clear, yellowish solution. • Use immediately if reconstituted with Sterile Water for Injection; stable for 7 days if reconstituted with Bacteriostatic Water for Injection. Diluted solutions stable for 24 hrs at room temperature or 4 days refrigerated.
PO
• Scored tablets may be crushed.
IV INCOMPATIBILITIES
Amphotericin B complex (Abelcet, AmBisome, Amphotec), droperidol (Inapsine), foscarnet (Foscavir).
IV COMPATIBILITIES
Cisplatin (Platinol AQ), cyclophosphamide (Cytoxan), doxorubicin (Adriamycin), etoposide (VePesid), filgrastim (Neupogen), 5-fluorouracil, gemcitabine (Gemzar), granisetron (Kytril), heparin, methotrexate, metoclopramide (Reglan), mitomycin (Mutamycin), piperacillin and tazobactam (Zosyn), vinblastine (Velban), vincristine (Oncovin).
INDICATIONS/ROUTES/DOSAGE
Rescue in High-Dose Methotrexate Therapy
PO, IV, IM: ADULTS, ELDERLY, CHILDREN: 15 mg (approximately 10 mg/m2) started 24 hrs after starting methotrexate infusion; continue q6h for 10 doses, until methotrexate level is less than 0.05 micromole/L.
Folic Acid Antagonist Overdose
PO: ADULTS, ELDERLY, CHILDREN: 5–15 mg/day.
Megaloblastic Anemia Secondary to Folate Deficiency
IM: ADULTS, ELDERLY, CHILDREN: 1 mg or less per day.
Colon Cancer
◀ ALERT ▶ For rescue therapy in cancer chemotherapy, refer to specific protocols used for optimal dosage and sequence of leucovorin administration.
IV: ADULTS, ELDERLY: (In Combination with 5-fluorouracil): 200 mg/m2 daily for 5 days. Repeat course at 4-wk intervals for 2 courses, then 4- to 5-wk intervals or 20 mg/m2 daily for 5 days. Repeat course at 4-wk intervals for 2 courses, then 4- to 5-wk intervals.
Dosage in Renal/Hepatic Impairment
No dose adjustment.
SIDE EFFECTS
Frequent: When combined with chemotherapeutic agents: diarrhea, stomatitis, nausea, vomiting, lethargy, malaise, fatigue, alopecia, anorexia. Occasional: Urticaria, dermatitis.
ADVERSE EFFECTS/TOXIC REACTIONS
Excessive dosage may negate chemotherapeutic effects of folic acid antagonists. Anaphylaxis occurs rarely. Diarrhea may cause rapid clinical deterioration.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Obtain baseline CBC, LFT, renal function. Give as soon as possible, preferably within 1 hr, for treatment of accidental overdosage of folic acid antagonists.
INTERVENTION/EVALUATION
Monitor for vomiting (may need to change from oral to parenteral therapy). Observe elderly, debilitated closely due to risk for severe toxicities. Assess CBC, BMP, LFT.
PATIENT/FAMILY TEACHING
• Explain purpose of medication in treatment of cancer. • Report allergic reaction, vomiting.
leuprolide
loo-proe-lide
(Eligard, Lupron
, Lupron Depot, Lupron Depot-Ped)
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: Gonadotropin-releasing hormone (GnRH) analogue. CLINICAL: Antineoplastic.
USES
Palliative treatment of advanced prostate carcinoma. Management of endometriosis. Treatment of anemia caused by uterine leiomyomata (fibroids). Treatment of central precocious puberty. OFF-LABEL: Treatment of breast cancer, infertility.
PRECAUTIONS
Contraindications: Hypersensitivity to leuprolide. Pregnancy, breastfeeding, undiagnosed vaginal bleeding. Eligard 7.5 mg is contraindicated in women, children; pts with hypersensitivity to GnRH, GnRH agonist analogues, or any of its components. 22.5 mg, 30 mg, 45 mg Lupron Depot contraindicated in women. Cautions: History of psychiatric illness, QTc prolongation or medications that prolong QTc interval, preexisting cardiac disease, chronic alcohol use, steroid therapy, seizures or medications that decrease seizures threshold.
ACTION
Inhibits gonadotropin secretion; suppresses ovarian and testicular steroidgenesis due to decreased LH/FSH levels. Decreases testosterone and estrogen. Therapeutic Effect: Produces pharmacologic castration, decreases growth of abnormal prostate tissue in males; causes endometrial tissue to become inactive, atrophic in females; decreases rate of pubertal development in children with central precocious puberty.
PHARMACOKINETICS
Rapidly, well absorbed after subcutaneous administration. Absorbed slowly after IM administration. Protein binding: 43%–49%. Half-life: 3–4 hrs.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Depot: Contraindicated in pregnancy. May cause spontaneous abortion. Children: Long-term safety not established. Elderly: No age-related precautions noted.
INTERACTIONS
DRUG: None significant. HERBAL: None significant. FOOD: None known. LAB VALUES: May increase serum prostatic acid phosphatase (PAP). Initially increases, then decreases, serum testosterone. May increase serum ALT, AST, alkaline phosphatase, glucose, LDH, LDL, cholesterol, triglycerides. May decrease platelets, WBC.
AVAILABILITY (Rx)
Injection Depot Formulation: Eligard: 7.5 mg, 22.5 mg, 30 mg, 45 mg. Lupron Depot-Ped: 7.5 mg, 11.25 mg (3-month), 11.25 (monthly), 15 mg, 30 mg. Lupron Depot: 3.75 mg, 11.25 mg, 22.5 mg, 30 mg, 45 mg. Injection Solution (Lupron): 5 mg/ml.
ADMINISTRATION/HANDLING
◀ ALERT ▶ May be carcinogenic, mutagenic, teratogenic. Handle with extreme care during preparation/administration.
IM
Lupron Depot • Store at room temperature. • Protect from light, heat. • Do not freeze vials. • Reconstitute only with diluent provided. Follow manufacturer’s instructions for mixing.
• Do not use needles less than 22 gauge; use syringes provided by the manufacturer (0.5-ml low-dose insulin syringes may be used as an alternative). • Administer immediately.
Eligard • Refrigerate. • Allow to warm to room temperature before reconstitution. • Follow manufacturer’s instructions for mixing. • Following reconstitution, administer within 30 min.
Subcutaneous
Lupron • Refrigerate vials. • Injection appears clear, colorless. • Discard if discolored or precipitate forms. • Administer into deltoid muscle, anterior thigh, abdomen.
INDICATIONS/ROUTES/DOSAGE
Advanced Prostatic Carcinoma
IM (Lupron Depot): ADULTS, ELDERLY: 7.5 mg q1mo, 22.5 mg q3mos, 30 mg q4mos, or 45 mg q6mos.
SQ (Eligard): ADULTS, ELDERLY: 7.5 mg every mo, 22.5 mg q3mos, 30 mg q4mos, or 45 mg q6mos.
SQ (Lupron): ADULTS, ELDERLY: 1 mg/day.
Endometriosis
IM (Lupron Depot): ADULTS, ELDERLY: 3.75 mg/mo for up to 6 mos or 11.25 mg q3mos for up to 2 doses.
Uterine Leiomyomata
IM (with Iron [Lupron Depot]): ADULTS, ELDERLY: 3.75 mg/mo for up to 3 mos or 11.25 mg as a single injection.
Precocious Puberty
IM (Lupron Depot-Ped): CHILDREN GREATER THAN 37.5 KG: 15 mg q mo. GREATER THAN 25 KG TO 37.5 KG: 11.25 mg q mo. 25 KG OR LESS: 7.5 mg q mo. Titrate dose upward by 3.75 mg/mo if down regulation not achieved. LUPRON DEPOT-PED (3 MOS): 11.25 mg or 30 mg q12wks.
SQ (Lupron): CHILDREN: Initially, 50 mcg/kg/day. Titrate upward by 10 mcg/kg/day if down regulation is not achieved.
Dosage in Renal/Hepatic Impairment
No dose adjustment.
SIDE EFFECTS
Frequent: Hot flashes (ranging from mild flushing to diaphoresis), migraines, hyperhidrosis. Females: Amenorrhea, spotting. Occasional: Arrhythmias, palpitations, blurred vision, dizziness, edema, headache, burning, pruritus, swelling at injection site, nausea, insomnia, weight gain. Females: Deepening voice, hirsutism, decreased libido, increased breast tenderness, vaginitis, altered mood. Males: Constipation, decreased testicle size, gynecomastia, impotence, decreased appetite, angina. Rare: Males: Thrombophlebitis.
ADVERSE EFFECTS/TOXIC REACTIONS
Occasionally, signs/symptoms of prostatic carcinoma worsen 1–2 wks after initial dosing (subsides during continued therapy). Increased bone pain and, less frequently, dysuria, hematuria, weakness, paresthesia of lower extremities may be noted. MI, pulmonary embolism occur rarely.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Question for possibility of pregnancy before initiating therapy. Obtain serum testosterone, prostatic acid phosphates (PAP) periodically during therapy. Serum testosterone, PAP should increase during first wk of therapy. Serum testosterone then should decrease to baseline level or less within 2 wks, PAP within 4 wks.
INTERVENTION/EVALUATION
Monitor for arrhythmias, palpitations. Assess for peripheral edema. Assess sleep pattern. Monitor for visual difficulties. Assist with ambulation if dizziness occurs. Offer antiemetics if nausea occurs.
PATIENT/ FAMILY TEACHING
• Hot flashes tend to decrease during continued therapy. • Temporary exacerbation of signs/symptoms of disease may occur during first few wks of therapy. • Use contraceptive measures. • Report persistent, regular menstration; pregnancy. • Avoid tasks that require alertness, motor skills until response to drug is established (potential for dizziness).
levalbuterol
lee-val-bue-ter-ole
(Xopenex, Xopenex HFA)
Do not confuse Xopenex with Xanax.
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: Sympathomimetic. CLINICAL: Bronchodilator.
USES
Treatment, prevention of bronchospasm due to reversible obstructive airway disease (e.g., asthma, bronchitis, emphysema).
PRECAUTIONS
Contraindications: History of hypersensitivity to albuterol or levalbuterol. Cautions: Cardiovascular disorders (cardiac arrhythmias, HF), seizures, hypertension, hyperthyroidism, diabetes mellitus, glaucoma, hypokalemia.
ACTION
Stimulates beta2-adrenergic receptors in lungs, resulting in relaxation of bronchial smooth muscle. Therapeutic Effect: Relieves bronchospasm, reduces airway resistance.
PHARMACOKINETICS
| Route | Onset | Peak | Duration |
| Inhalation | 5–10 min | 1.5 hrs | 5–6 hrs |
| Nebulization | 10–17 min | 1.5 hrs | 5–8 hrs |
Half-life: 3.3–4 hrs.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Crosses placenta. Unknown if distributed in breast milk. Pregnancy Category C. Children: Safety and efficacy not established in those younger than 12 yrs. Elderly: Lower initial dosages recommended.
INTERACTIONS
DRUG: Beta blockers (e.g., carvedilol, metoprolol) antagonize effects; may produce severe bronchospasm. May decrease digoxin concentration. MAOIs (e.g., phenelzine, tranylcypromine), tricyclic antidepressants (e.g., amitriptyline, desipramine) may potentiate cardiovascular effects. Diuretics (e.g., furosemide, HCTZ) may increase hypokalemia. HERBAL: None significant. FOOD: None known. LAB VALUES: May decrease serum potassium.
AVAILABILITY (Rx)
Inhalation Aerosol: 45 mcg/activation. Solution for Nebulization: 0.31 in 3-ml vials, 0.63 mg in 3-ml vials, 1.25 mg in 3-ml vials, 1.25 mg in 0.5-ml vials.
ADMINISTRATION/HANDLING
Nebulization
• No diluent necessary. • Protect from light, excessive heat. Store at room temperature. • Once foil is opened, use within 2 wks. • Use within 1 wk and protect from light after removal from pouch • Discard if solution is not colorless. • Do not mix with other medications. • Concentrated solution (1.25 mg in 0.5 ml) should be diluted with 2.5 ml 0.9% NaCl prior to use. • Give over 5–15 min.
Inhalation
• Shake well before inhalation. • Following first inhalation, wait 2 min before inhaling second dose (allows for deeper bronchial penetration). • Rinsing mouth with water immediately after inhalation prevents mouth/throat dryness.
INDICATIONS/ROUTES/DOSAGE
Treatment/Prevention of Bronchospasm
Nebulization: ADULTS, ELDERLY, CHILDREN 12 YRS AND OLDER: Initially, 0.63 mg 3 times/day 6–8 hrs apart. May increase to 1.25 mg 3 times/day with dose monitoring. CHILDREN 5–11 YRS: Initially, 0.31 mg 3 times/day. Maximum: 0.63 mg 3 times/day. CHILDREN 4 YRS OR YOUNGER: 0.31–1.25 mg q4–6h as needed.
Inhalation: ADULTS, ELDERLY, CHILDREN 4 YRS AND OLDER: 1–2 inhalations q4–6h.
Acute Asthma Exacerbation
Nebulization: ADULTS, ELDERLY, CHILDREN 12 YRS AND OLDER: 1.25–2.5 mg q20min for 3 doses, then 1.25–5 mg q1–4h as needed. CHILDREN YOUNGER THAN 12 YRS: 0.075 mg/kg (minimum dose: 1.25 mg) q20min for 3 doses, then 0.075–0.15 mg/kg q1–4h as needed.
Inhalation: ADULTS, ELDERLY, CHILDREN 12 YRS AND OLDER: 4–8 puffs q20min for up to 4 hrs, then q1–4h. CHILDREN YOUNGER THAN 12 YRS: 4–8 puffs q20min for 3 doses, then q1–4h.
Dosage in Renal/Hepatic Impairment
No dose adjustment.
SIDE EFFECTS
Occasional (11%–4%): Nervousness, tremor, rhinitis, flu-like illness. Rare (less than 3%): Tachycardia, dizziness, anxiety, viral infection, dyspepsia, dry mouth, headache, chest pain.
ADVERSE EFFECTS/TOXIC REACTIONS
Excessive sympathomimetic stimulation may produce palpitations, premature heart contraction, tachycardia, chest pain, slight increase in B/P followed by substantial decrease, chills, diaphoresis, blanching of skin. Too-frequent or excessive use may decrease bronchodilating effectiveness, lead to severe, paradoxical bronchoconstriction.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Offer emotional support (high incidence of anxiety due to difficulty in breathing, sympathomimetic response to drug). Assess lung sounds, pulse, B/P. Note color, amount of sputum.
INTERVENTION/EVALUATION
Monitor rate, depth, rhythm, type of respiration; quality/rate of pulse, EKG, serum potassium, ABG determinations. Assess lung sounds for wheezing (bronchoconstriction), rales. Observe for paradoxical bronchospasm.
PATIENT/ FAMILY TEACHING
• Increase fluid intake (decreases lung secretion viscosity). • Rinsing mouth with water immediately after inhalation may prevent mouth/throat dryness. • Avoid excessive use of caffeine derivatives (chocolate, coffee, tea, cola, cocoa). • Report if palpitations, tachycardia, chest pain, tremors, dizziness, headache occurs or shortness of breath is not relieved.
*levETIRAcetam
lee-ve-tye-ra-se-tam
(Apo-Levetiracetam
, Elepsia XR, Keppra, Keppra XR, Spritam)
Do not confuse Keppra with Kaletra, Keflex, or Keppra XR, or levetiracetam with levofloxacin.
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: Pyrrolidine derivative. CLINICAL: Anticonvulsant.
USES
Adjunctive therapy in treatment of partial-onset, myoclonic, and/or primary generalized tonic-clonic seizures.
PRECAUTIONS
Contraindications: Hypersensitivity to levetiracetam. Cautions: Renal impairment, pts with depression at high risk for suicide.
ACTION
Exact mechanism unknown. May inhibit voltage-dependent calcium channels, facilitate GABA inhibitory transmission, reduce potassium current, or bind to synaptic proteins that modulate neurotransmitter release. Therapeutic Effect: Prevents seizure activity.
PHARMACOKINETICS
Rapidly, completely absorbed following PO administration. Protein binding: less than 10%. Metabolized primarily by enzymatic hydrolysis. Primarily excreted in urine as unchanged drug. Half-life: 6–8 hrs.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Distributed in breast milk. Breastfeeding not recommended. Children: Safety and efficacy not established in children 4 yrs or younger. Elderly: Age-related renal impairment may require dosage adjustment.
INTERACTIONS
DRUG: None significant. HERBAL: None significant. FOOD: None known. LAB VALUES: May decrease Hgb, Hct, RBC, WBC counts.
AVAILABILITY (Rx)
Injection, Solution: 100 mg/ml. Oral Solution: 100 mg/ml. Tablets: 250 mg, 500 mg, 750 mg, 1,000 mg.
Tablets, Extended-Release: 500 mg, 750 mg.
ADMINISTRATION/HANDLING
IV
Rate of Infusion • Infuse over 15 min.
Reconstitution • Dilute with 100 ml 0.9% NaCl or D5W.
Storage • Store at room temperature. • Stable for 24 hrs following dilution.
IV INCOMPATIBILITIES
Data not available.
IV COMPATIBILITIES
Diazepam (Valium), lorazepam (Ativan), valproate (Depacon).
PO
• Give without regard to food. • Use oral solution for pts weighing 20 kg or less. • Use tablets or oral solution for pts weighing more than 20 kg. • Oral solution should be administered with a calibrated measuring device. • Swallow extended-release and immediate-release tablets whole; do not break, crush, dissolve, or divide.
INDICATIONS/ROUTES/DOSAGE
Partial-Onset Seizures
IV/PO: ADULTS, ELDERLY, CHILDREN 17 YRS AND OLDER: (Immediate-Release):Initially, 500 mg q12h. May increase by 1,000 mg/day q2wks. Maximum: 3,000 mg/day in 2 divided doses. Extended Release: 1,000 mg once daily. May increase in increments of 1,000 mg/day q2wks. Maximum: 3,000 mg once daily.
PO: CHILDREN 4–16 YRS: 20 mg/kg/day in 2 divided doses. May increase q2wks by 10 mg/kg/dose. Maximum: 60 mg/kg/day in 2 divided doses. CHILDREN 6 MOS TO YOUNGER THAN 4 YRS: 20 mg/kg/day in 2 divided doses. May increase q2wks by 10 mg/kg/dose. Maximum: 50 mg/kg/day in 2 divided doses. CHILDREN 1 MO TO YOUNGER THAN 6 MOS (ORAL SOLUTION): 14 mg/kg/day in 2 divided doses. May increase q2wks by 7 mg/kg/dose. Maximum: 42 mg/kg/day in 2 divided doses.
Myoclonic Seizures
PO/IV: ADULTS, ELDERLY, CHILDREN 12 YRS AND OLDER: (Immediate-Release):Initially, 500 mg q12h. May increase by 1,000 mg/day q2wks. Maximum: 3,000 mg/day in 2 divided doses.
Tonic-Clonic Seizures
PO: ADULTS, ELDERLY, CHILDREN 16 YRS AND OLDER: (Immediate-Release): Initially, 500 mg twice daily. May increase by 1,000 mg/day q2wks up to recommended dose of 1,500 mg 2 times/day. CHILDREN 6–15 YRS: Initially, 10 mg/kg twice daily. May increase by 20 mg/kg/day q2wks up to recommended dose of 30 mg/kg 2 times/day.
Dosage in Renal Impairment
Dosage is modified based on creatinine clearance. Note: CrCl less than 50 ml/min: Not recommended with Elepsia XR.
| Creatinine Clearance | Dosage (Immediate-Release, IV) | Dosage (Extended-Release) |
| Greater than 80 ml/min: | 500–1,500 mg q12h | 1,000–3,000 mg q24h |
| 50–80 ml/min: | 500–1,000 mg q12h | 1,000–2,000 mg q24h |
| 30–49 ml/min: | 250–750 mg q12h | 500–1,500 mg q24h |
| Less than 30 ml/min: | 250–500 mg q12h | 500–1,000 mg q24h |
| End-stage renal disease using dialysis: | 500–1,000 mg q24h, after dialysis, a 250- to 500-mg supplemental dose is recommended | NA |
| CRRT | 250–750 mg q12h |
Dosage in Hepatic Impairment
No dose adjustment.
SIDE EFFECTS
Frequent (15%–10%): Drowsiness, asthenia, headache, infection. Occasional (9%–3%): Dizziness, pharyngitis, pain, depression, anxiety, vertigo, rhinitis, anorexia. Rare (less than 3%): Amnesia, emotional lability, cough, sinusitis, anorexia, diplopia.
ADVERSE EFFECTS/TOXIC REACTIONS
Acute psychosis, seizures have been reported. Sudden discontinuance increases risk of seizure activity. Serious dermatological reactions, including Steven-Johnson syndrome and toxic epidermal necrolysis, have been reported.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Review history of seizure disorder (intensity, frequency, duration, LOC). Initiate seizure precautions. Assess for hypersensitivity to levetiracetam. Obtain renal function test.
INTERVENTION/EVALUATION
Observe for recurrence of seizure activity. Assess for clinical improvement (decrease in intensity/frequency of seizures). Monitor renal function tests. Observe for suicidal ideation, depression, behavioral changes. Assist with ambulation if dizziness occurs.
PATIENT/ FAMILY TEACHING
• Drowsiness usually diminishes with continued therapy. • Avoid tasks that require alertness, motor skills until response to drug is established. • Avoid alcohol. • Do not abruptly discontinue medication (may precipitate seizures). • Strict maintenance of drug therapy is essential for seizure control. • Report mood swings, hostile behavior, suicidal ideation, unusual changes in behavior.
*levoFLOXacin
lee-voe-flox-a-sin
(Apo-Levofloxacin
, Levaquin, Quixin)
BLACK BOX ALERT May increase risk of tendonitis, tendon rupture. (Risk increased with concurrent corticosteroids, organ transplant, pts older than 60 yrs.) May exacerbate myasthenia gravis.
Do not confuse Levaquin with Levoxyl, Levsin/SL, or Lovenox, or levofloxacin with levetiracetam or levothyroxine.
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: Fluoroquinolone. CLINICAL: Antibiotic.
USES
Treatment of susceptible infections due to S. pneumoniae, S. aureus, E. faecalis, H. influenzae, M. catarrhalis, Serratia marcescens, K. pneumoniae, E. coli, P. mirabilis, P. aeruginosa, C. pneumoniae, Legionella pneumophila, Mycoplasma pneumoniae, including acute bacterial exacerbation of chronic bronchitis, acute bacterial sinusitis, community-acquired pneumonia, nosocomial pneumonia, complicated and uncomplicated UTI, acute pyelonephritis, complicated and uncomplicated mild to moderate skin/skin structure infections, prostatitis. Inhalation anthrax (post-exposure); plague. Ophthalmic: Treatment of superficial infections to conjunctiva (0.5%), cornea (1.5%). OFF-LABEL: Urethritis, traveler’s diarrhea, diverticulitis, enterocolitis, Legionnaire’s disease, peritonitis. Treatment of prosthetic joint infection.
PRECAUTIONS
Contraindications: Hypersensitivity to levofloxacin, other fluoroquinolones. Cautions: Known or suspected CNS disorders, seizure disorder, renal impairment, bradycardia, rheumatoid arthritis, elderly, hypokalemia, hypomagnesemia, myasthenia gravis, severe cerebral arteriosclerosis, prolonged QT interval, medications that potentiate QT interval prolongation, diabetes.
ACTION
Inhibits DNA enzyme gyrase in susceptible microorganisms, interfering with bacterial cell replication, repair. Therapeutic Effect: Bactericidal.
PHARMACOKINETICS
Well absorbed after PO, IV administration. Protein binding: 50%. Widely distributed. Eliminated unchanged in urine. Partially removed by hemodialysis. Half-life: 6–8 hrs.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Distributed in breast milk. Avoid use in pregnancy. Children: Safety and efficacy not established in pts younger than 18 yrs. Elderly: Age-related renal impairment may require dosage adjustment.
INTERACTIONS
DRUG: Antacids, iron preparations, sucralfate, zinc decrease absorption. NSAIDs may increase risk of CNS stimulation, seizures. Medications that prolong QT interval (e.g., amiodarone, fluoxetine, haloperidol, sotalol, quinidine) may increase risk of arrhythmias. May increase effects of warfarin. HERBAL: None significant. FOOD: None known. LAB VALUES: May alter serum glucose.
AVAILABILITY (Rx)
Infusion Premix: 250 mg/50 ml, 500 mg/100 ml, 750 mg/150 ml. Injection, Solution: 25 mg/ml. Ophthalmic Solution: 0.5%. Oral Solution: 25 mg/ml. Tablets: 250 mg, 500 mg, 750 mg.
ADMINISTRATION/HANDLING
IV
Reconstitution • For infusion using single-dose vial, withdraw desired amount (10 ml for 250 mg, 20 ml for 500 mg). Dilute each 10 ml (250 mg) with minimum 40 ml 0.9% NaCl, D5W, providing a concentration of 5 mg/ml.
Rate of Administration • Administer no less than 60 min for 250 mg or 500 mg; 90 min for 750 mg.
Storage • Available in single-dose 20-ml (500-mg) vials and premixed with D5W, ready to infuse. • Diluted vials stable for 72 hrs at room temperature, 14 days if refrigerated.
PO
• Do not administer antacids (aluminum, magnesium), sucralfate, iron or multivitamin preparations with zinc within 2 hrs of administration (significantly reduces absorption). • Give tablets without regard to food. • Give oral solution 1 hr before or 2 hrs after meals.
Ophthalmic
• Place a gloved finger on lower eyelid and pull out until a pocket is formed between eye and lower lid. • Place prescribed number of drops into pocket. • Instruct pt to close eye gently (so medication will not be squeezed out of the sac) and to apply digital pressure to lacrimal sac for 1–2 min to minimize systemic absorption.
IV INCOMPATIBILITIES
Furosemide (Lasix), heparin, insulin, nitroglycerin, propofol (Diprivan).
IV COMPATIBILITIES
Dexmedetomidine (Precedex), dobutamine (Dobutrex), dopamine (Intropin), fentanyl (Sublimaze), lidocaine, (Ativan), magnesium, morphine.
INDICATIONS/ROUTES/DOSAGE
Usual Dosage Range
PO, IV: ADULTS, ELDERLY: 250–500 mg q24h; 750 mg q24h for severe or complicated infections.
Bacterial Conjunctivitis
Ophthalmic: ADULTS, ELDERLY, CHILDREN 1 YR AND OLDER (QUIXIN) (0.5%): 1–2 drops q2h for 2 days while awake (up to 8 times/day), then 1–2 drops q4h while awake up to 4 times/day.
Dosage in Renal Impairment
Normal renal function dosage of 250 mg/day:
| Creatinine Clearance | Dosage |
| 20–49 ml/min | No change |
| 10–19 ml/min | 250 mg initially, then 250 mg q48h |
Normal renal function dosage of 500 mg/day:
| Creatinine Clearance | Dosage |
| 50–80 ml/min | No change |
| 20–49 ml/min | 500 mg initially, then 250 mg q24h |
| 10–19 ml/min | 500 mg initially, then 250 mg q48h |
For pts undergoing dialysis, 500 mg initially, then 250 mg q48h.
Normal renal function dosage of 750 mg/day:
| Creatinine Clearance | Dosage |
| 50–80 ml/min | No change |
| 20–49 ml/min | Initially, 750 mg, then 750 mg q48h |
| 10–19 ml/min | Initially, 750 mg, then 500 mg q48h |
| Dialysis | 500 mg q48h (administer after dialysis on dialysis days) |
| Continuous Renal Replacement Therapy | |
| CVVH | 500–750 mg once, then 250 mg q24h |
| CVVHD | 500–750 mg once, then 250–500 mg q24h |
| CVVHDT | 500–750 mg once, then 250–750 mg q24h |
Dosage in Hepatic Impairment
No dose adjustment.
SIDE EFFECTS
Occasional (3%–1%): Diarrhea, nausea, abdominal pain, dizziness, drowsiness, headache. Ophthalmic: Local burning/discomfort, margin crusting, crystals/scales, foreign body sensation, ocular itching, altered taste. Rare (less than 1%): Flatulence; pain, inflammation, swelling in calves, hands, shoulder; chest pain, difficulty breathing, palpitations, edema, tendon pain. Ophthalmic: Corneal staining, keratitis, allergic reaction, eyelid swelling, tearing, reduced visual acuity.
ADVERSE EFFECTS/TOXIC REACTIONS
Antibiotic-associated colitis, other super-infections (abdominal cramps, severe watery diarrhea, fever) may occur. Superinfection (genital/anal pruritus, ulceration/changes in oral mucosa, moderate to severe diarrhea) may occur from altered bacterial balance in GI tract. Hypersensitivity reactions, including photosensitivity (rash, pruritus, blisters, edema, sensation of burning skin) have occurred in pts receiving fluoroquinolones.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Question for hypersensitivity to levofloxacin, other fluoroquinolones. Question history as listed in Precautions. Receive full medication history and screen for interactions, esp. medications that prolong QT interval.
INTERVENTION/EVALUATION
Monitor serum glucose, renal function, LFT. Monitor daily pattern of bowel activity, stool consistency. Report hypersensitivity reaction: skin rash, urticaria, pruritus, photosensitivity promptly. Be alert for superinfection: fever, vomiting, diarrhea, anal/genital pruritus, oral mucosal changes (ulceration, pain, erythema). Provide symptomatic relief for nausea. Evaluate food tolerance, altered taste.
PATIENT/ FAMILY TEACHING
• Drink 6–8 glasses of fluid a day (prevents formation of urine crystals). • Avoid tasks that require alertness, motor skills until response to drug is established (may cause dizziness, drowsiness). • Report tendon pain/swelling, palpitations, chest pain, difficulty breathing, persistent diarrhea occurs. • Avoid exposure to direct sunlight. • Report use of warfarin.
levothyroxine
lee-voe-thy-rox-een
(Eltroxin
, Levoxyl, Synthroid, Tirosint, Unithroid)
BLACK BOX ALERT Ineffective, potentially toxic for weight reduction. High doses increase risk of serious, life-threatening toxic effects, especially when used with some anorectic drugs.
Do not confuse levothyroxine with levofloxacin or liothyronine, or Synthroid with Symmetrel.
FIXED-COMBINATION(S)
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: Synthetic isomer of thyroxine. CLINICAL: Thyroid hormone (T4).
USES
PO: Treatment of hypothyroidism, pituitary thyroid-stimulating hormone (TSH) suppression. IV: Myxedema coma. OFF-LABEL: Management of hemodynamically unstable potential organ donors.
PRECAUTIONS
Contraindications: Hypersensitivity to levothyroxine. Acute MI, untreated subclinical or overt thyrotoxicosis, uncorrected adrenal insufficiency. Capsule: Inability to swallow capsules. Cautions: Elderly, angina pectoris, hypertension, other cardiovascular disease, adrenal insufficiency, myxedema, diabetes mellitus and insipidus, swallowing disorders.
ACTION
Converts to T3, then binds to thyroid receptor proteins exerting metabolic effects through DNA and protein synthesis. Therapeutic Effect: Involved in normal metabolism, growth and development. Increases basal metabolic rate, enhances gluconeogenesis, stimulates protein synthesis.
PHARMACOKINETICS
Variable, incomplete absorption from GI tract. Protein binding: greater than 99%. Widely distributed. Deiodinated in peripheral tissues, minimal metabolism in liver. Eliminated by biliary excretion. Half-life: 6–7 days.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Does not cross placenta. Minimal distribution in breast milk. Children: No age-related precautions noted. Caution in neonates in interpreting thyroid function tests. Elderly: May be more sensitive to thyroid effects; individualized dosage recommended.
INTERACTIONS
DRUG: Cholestyramine, colestipol, aluminum- and magnesium-containing antacids may decrease absorption. Estrogens may cause decrease in serum-free thyroxine. May enhance effects of oral anticoagulants (e.g, warfarin). Sympathomimetics (e.g., norepinephrine, phenylephrine) may increase risk of coronary insufficiency, effects of levothyroxine. May decrease effects of insulin, oral hypoglycemic agents. HERBAL: None significant. FOOD: None known. LAB VALUES: None known.
AVAILABILITY (Rx)
Capsules (Tirosint): 13 mcg, 25 mcg, 50 mcg, 75 mcg, 88 mcg, 100 mcg, 112 mcg, 125 mcg, 137 mcg, 150 mcg. Injection, Powder for Reconstitution (Synthroid): 100 mcg, 200 mcg, 500 mcg. Tablets (Synthroid, Unithroid): 25 mcg, 50 mcg, 75 mcg, 88 mcg, 100 mcg, 112 mcg, 125 mcg, 137 mcg, 150 mcg, 175 mcg, 200 mcg, 300 mcg.
ADMINISTRATION/HANDLING
◀ ALERT ▶ Do not interchange brands (known issues with bioequivalence between manufacturers).
IV
Reconstitution • Reconstitute 200-mcg or 500-mcg vial with 5 ml 0.9% NaCl to provide concentration of 40 or 100 mcg/ml, respectively; shake until clear.
Rate of Administration • Use immediately; discard unused portions. • Give each 100 mcg or less over 1 min.
Storage • Store vials at room temperature.
PO
• Administer in the morning on an empty stomach, 30 min before food. • Administer before breakfast to prevent insomnia. • Tablets may be crushed. • Take 4 hrs apart from antacids, iron, calcium supplements.
IV INCOMPATIBILITIES
Do not use or mix with other IV solutions.
INDICATIONS/ROUTES/DOSAGE
Note: IV dose is 50% of oral dose.
Hypothyroidism
PO: ADULTS, CHILDREN IN WHOM GROWTH AND PUBERTY ARE COMPLETE, OLDER ADULTS RECENTLY TREATED FOR HYPOTHYROIDISM OR WHO HAVE BEEN HYPOTHYROID FOR ONLY A FEW MOS: 1.7 mcg/kg/day as single daily dose. Usual maintenance: 100–125 mcg/day. ADULTS YOUNGER THAN 50 YRS WITH CARDIAC DISEASE, OLDER THAN 50 YRS WITHOUT CARDIAC DISEASE: Initially, 25–50 mcg/day. Adjust dose by 12.5–25 mcg at 6–8-wk intervals. ADULTS (OLDER THAN 50 YRS WITH CARDIAC DISEASE): Initially, 12.5–50 mcg/day. Adjust dose by 12.5–25 mcg/day at 4–8-wk intervals. CHILDREN OLDER THAN 12 YRS, GROWTH AND PUBERTY INCOMPLETE: 2–3 mcg/kg/day. CHILDREN 6–12 YRS: 4–5 mcg/kg/day. CHILDREN 1–5 YRS: 5–6 mcg/kg/day. CHILDREN 6–12 MOS: 6–8 mcg/kg/day. CHILDREN 3–5 MOS: 8–10 mcg/kg/day. CHILDREN YOUNGER THAN 3 MOS: 10–15 mcg/kg/day.
Myxedema Coma
IV: ADULTS, ELDERLY: Initially, 300–500 mcg, then 50–100 mcg once daily until able to tolerate PO administration.
Pituitary Thyroid-Stimulating Hormone (TSH) Suppression
PO: ADULTS, ELDERLY: Doses greater than 2 mcg/kg/day usually required to suppress TSH below 0.1 milliunits/L.
Dosage in Renal/Hepatic Impairment
No dose adjustment.
SIDE EFFECTS
Occasional: Reversible hair loss at start of therapy in children. Rare: Dry skin, GI intolerance, rash, urticaria, pseudotumor cerebri, severe headache in children.
ADVERSE EFFECTS/TOXIC REACTIONS
Excessive dosage produces signs/symptoms of hyperthyroidism (weight loss, palpitations, increased appetite, tremors, anxiety, tachycardia, hypertension, headache, insomnia, menstrual irregularities). Cardiac arrhythmias occur rarely.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Obtain baseline TSH, T3, T4, weight, vital signs. Signs/symptoms of diabetes mellitus, diabetes insipidus, adrenal insufficiency, hypopituitarism may become intensified. Treat with adrenocortical steroids before thyroid therapy in coexisting hypothyroidism and hypoadrenalism.
INTERVENTION/EVALUATION
Monitor pulse for rate, rhythm (report pulse greater than 100 or marked increase). Observe for tremors, anxiety. Assess appetite, sleep pattern. Children: (Undertreatment): May decrease intellectual development, linear growth. (Overtreatment): Adversely affects brain maturation, accelerates bone age. Monitor thyroid function tests.
PATIENT/ FAMILY TEACHING
• Do not discontinue drug therapy; replacement for hypothyroidism is lifelong. • Follow-up office visits, thyroid function tests are essential. • Take medication at the same time each day, preferably in the morning. • Monitor pulse for rate, rhythm; report irregular rhythm or pulse rate over 100 beats/min. • Promptly report chest pain, weight loss, anxiety, tremors, insomnia. • Children may have reversible hair loss, increased aggressiveness during first few mos of therapy. • Full therapeutic effect may take 1–3 wks.
lidocaine
lye-doe-kane
(Lidoderm, Xylocaine)
FIXED-COMBINATION(S)
EMLA: lidocaine/prilocaine (an anesthetic): 2.5%/2.5%. Lidosite: lidocaine/epinephrine (a sympathomimetic): 10%/0.1%. Lidocaine with epinephrine: lidocaine/epinephrine (a sympathomimetic): 2%/1:50,000, 1%/1:100,000, 1%/1:200,000, 0.5%/1:200,000. Synéra: lidocaine/tetracaine (an anesthetic): 70 mg/70 mg.
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: Amide anesthetic. CLINICAL: Class 1B Antiarrhythmic, anesthetic.
USES
Antiarrhythmic: Rapid control of acute ventricular arrhythmias following MI, cardiac catheterization, cardiac surgery. Local Anesthetic: Infiltration/nerve block for dental/surgical procedures, childbirth. Topical Anesthetic: Local skin disorders (minor burns, insect bites, prickly heat, skin manifestations of chickenpox, abrasions). Mucous membranes (local anesthesia of oral, nasal, laryngeal mucous membranes; local anesthesia of respiratory, urinary tracts; relief of discomfort of pruritus ani, hemorrhoids, pruritus vulvae). Dermal patch: Relief of chronic pain in post-herpetic neuralgia, allodynia (painful hypersensitivity).
PRECAUTIONS
Contraindications: Hypersensitivity to lidocaine. Adams-Stokes syndrome, hypersensitivity to amide-type local anesthetics, supraventricular arrhythmias, Wolff-Parkinson-White syndrome. Severe degree of SA, AV, or intraventricular heart block (except in pts with functioning pacemaker). Cautions: Hepatic disease, marked hypoxia, severe respiratory depression, hypovolemia, incomplete heart. History of malignant hyperthermia, shock, elderly, HF.
ACTION
Anesthetic: Inhibits conduction of nerve impulses. Therapeutic Effect: Causes temporary loss of feeling/sensation. Antiarrhythmic: Suppresses automaticity of conduction tissue; increases electrical stimulation threshold of ventricle, His Purkinje system; and spontaneous depolarization of ventricle during diastole. Therapeutic Effect: Inhibits ventricular arrhythmias.
PHARMACOKINETICS
| Route | Onset | Peak | Duration |
| IV | 30–90 sec | N/A | 10–20 min |
| Local anesthetic | 2.5 min | N/A | 30–60 min |
Completely absorbed after IM administration. Protein binding: 60%–80%. Widely distributed. Metabolized in liver. Primarily excreted in urine. Minimally removed by hemodialysis. Half-life: 1–2 hrs.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Crosses placenta. Distributed in breast milk. Children: No age-related precautions noted. Elderly: More sensitive to adverse effects. Dose, rate of infusion should be reduced. Age-related renal impairment may require dosage adjustment.
INTERACTIONS
DRUG: Class 1 antiarrhythmics may increase cardiac effects. HERBAL: St. John’s wort may decrease concentration. FOOD: None known. LAB VALUES: IM lidocaine may increase creatine kinase (CK) level. Therapeutic serum level: 1.5 to 6 mcg/ml; toxic serum level: greater than 6 mcg/ml.
AVAILABILITY (Rx)
Cream, Topical: 4%. Infusion Premix: 0.4% (4 mg/ml in 250 ml, 500 ml); 0.8% (8 mg/ml in 250 ml, 500 ml). Injection, Solution: 0.5% (5 mg/ml), 1% (10 mg/ml), 2% (20 mg/ml). Jelly, Topical: 2%. Solution, Topical: 4%. Solution, Viscous: 2%. Transdermal, Topical (Lidoderm): 5%.
ADMINISTRATION/HANDLING
◀ ALERT ▶ Resuscitative equipment, drugs (including O2) must always be readily available when administering lidocaine by any route.
IV
◀ ALERT ▶ Use only lidocaine without preservative, clearly marked for IV use.
Reconstitution • For IV infusion, prepare solution by adding 2 g to 250–500 ml D5W or 0.9% NaCl to provide concentration of 8 mg/ml or 4 mg/ml, respectively. • Commercially available preparations of 0.4% and 0.8% may be used for IV infusion. Maximum concentration: 4 g/250 ml (16 mg/ml).
Rate of Administration • For IV push, use 1% (10 mg/ml) or 2% (20 mg/ml). • Administer IV push at rate of 25–50 mg/min. • Administer for IV infusion at rate of 1–4 mg/min (1–4 ml); use volume control IV set.
Storage • Store premix solutions at room temperature.
Topical
• Not for ophthalmic use. • For skin disorders, apply directly to affected area or put on gauze or bandage, which is then applied to the skin. • For mucous membrane use, apply to desired area per manufacturer’s insert. • Administer lowest dosage possible that still provides anesthesia.
Dermal Patch
Patch may be cut to appropriate size.
IV INCOMPATIBILITIES
Amphotericin B complex (Abelcet, AmBisome, Amphotec).
IV COMPATIBILITIES
Amiodarone (Cordarone), calcium gluconate, dexmedetomidine (Precedex), digoxin (Lanoxin), diltiazem (Cardizem), dobutamine (Dobutrex), dopamine (Intropin), enalapril (Vasotec), furosemide (Lasix), heparin, insulin, nitroglycerin, potassium chloride.
INDICATIONS/ROUTES/DOSAGE
Ventricular Arrhythmias
IV: ADULTS, ELDERLY: Initially, 1–1.5 mg/kg. Refractory ventricular tachycardia, fibrillation: Repeat dose at 0.5–0.75 mg/kg q10–15min after initial dose for a maximum of 3 doses. Total dose not to exceed 3 mg/kg. Follow with continuous infusion (1–4 mg/min) after return of perfusion. Reappearance of arrhythmia during infusion: 0.5 mg/kg, reassess infusion. CHILDREN, INFANTS: Initially, 1 mg/kg (maximum: 100 mg). May repeat second dose of 0.5–1 mg/kg if start of infusion longer than 15 min. Maintenance: 20–50 mcg/kg/min as IV infusion.
Local Anesthesia
Infiltration, Nerve Block: ADULTS: Local anesthetic dosage varies with procedure, degree of anesthesia, vascularity, duration. Maximum dose: 4.5 mg/kg. Do not repeat within 2 hrs.
Topical Local Anesthesia
Topical: ADULTS, ELDERLY: Apply to affected areas as needed.
Treatment of Localized Pain
◀ ALERT ▶ Transdermal patch may contain conducting metal (e.g., aluminum). Remove patch prior to MRI.
Topical (Dermal Patch): ADULTS, ELDERLY: Apply to intact skin over most painful area (up to 3 applications once for up to 12 hrs in a 24-hr period).
Dosage in Renal Impairment
No dose adjustment.
Dosage in Hepatic Impairment
SIDE EFFECTS
CNS effects generally dose-related and of short duration. Occasional: IM: Pain at injection site. Topical: Burning, stinging, tenderness at application site. Rare: Generally associated with high dose: Drowsiness, dizziness, disorientation, light-headedness, tremors, apprehension, euphoria, sensation of heat, cold, numbness; blurred or double vision, tinnitus, nausea.
ADVERSE EFFECTS/TOXIC REACTIONS
Serious adverse reactions to lidocaine are uncommon, but high dosage by any route may produce cardiovascular depression, bradycardia, hypotension, arrhythmias, heart block, cardiovascular collapse, cardiac arrest. Potential for malignant hyperthermia, CNS toxicity may occur, esp. with regional anesthesia use, progressing rapidly from mild side effects to tremors, drowsiness, seizures, vomiting, respiratory depression. Methemoglobinemia (evidenced by cyanosis) has occurred following topical application of lidocaine for teething discomfort and laryngeal anesthetic spray.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Question for hypersensitivity to lidocaine, amide anesthetics. Obtain baseline B/P, pulse, respiratory rate, EKG, serum electrolytes.
INTERVENTION/EVALUATION
Monitor EKG, vital signs closely during and following drug administration for cardiac performance. If EKG shows arrhythmias, prolongation of PR interval or QRS complex, inform physician immediately. Assess pulse for rhythm, rate, quality. Assess B/P for evidence of hypotension. Monitor for therapeutic serum level (1.5–6 mcg/ml). For lidocaine given by all routes, monitor vital signs, LOC. Drowsiness should be considered a warning sign of high serum levels of lidocaine. Therapeutic serum level: 1.5–6 mcg/ml; toxic serum level: greater than 6 mcg/ml.
PATIENT/ FAMILY TEACHING
• Local anesthesia: Due to loss of feeling/sensation, protective measures may be needed until anesthetic wears off (no ambulation, including special positions for some regional anesthesia). • Oral mucous membrane anesthesia: Do not eat, drink, chew gum for 1 hr after application (swallowing reflex may be impaired, increasing risk of aspiration; numbness of tongue, buccal mucosa may lead to bite trauma). • IV infusions: Report dizziness, numbness, double vision, nausea, pain/burning, respiratory difficulty. • Topical: Report irritation, pain, numbness, swelling, blurred vision, tinnitus, respiratory difficulty.
linaclotide
lin-a-kloe-tide
(Constella
, Linzess)
BLACK BOX ALERT Contraindicated in pediatric pts 6 yrs of age and younger. Avoid use in pediatric patients 7 yrs through 17 yrs old.
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: Guanylate cyclase-C (cGMP) agonist. CLINICAL: Anti-constipation agent.
USES
Treatment of irritable bowel syndrome with constipation, chronic idiopathic constipation.
PRECAUTIONS
Contraindications: Hypersensitivity to linaclotide. Pediatric patients 6 yrs and younger, known or suspected mechanical GI obstruction. Cautions: Diarrhea.
ACTION
Binds on the luminal surface of GI epithelium. Increase cGMP which stimulates chloride and bicarbonate into intestinal lumen. Therapeutic Effect: Increase intestinal fluid, accelerates transit.
PHARMACOKINETICS
Metabolized within GI tract. Minimal distribution beyond GI tissue. Minimal systemic absorption. Half-life: N/A.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown if distributed in breast milk. Children: Avoid use in pediatric pts 7 yrs through 17 yrs. Contraindicated in pediatric pts 6 yrs and younger. Elderly: No age-related precautions noted.
INTERACTIONS
DRUG: None significant. HERBAL: None significant. FOOD: None known. LAB VALUES: None significant.
AVAILABILITY (Rx)
Capsules: 145 mcg, 290 mcg.
ADMINISTRATION/HANDLING
PO
• Give on empty stomach at least 30 min prior to first meal of day. • Do not break, crush, or open capsule.
INDICATIONS/ROUTES/DOSAGE
Irritable Bowel Syndrome With Constipation
PO: ADULTS 18 YRS AND OLDER, ELDERLY: 290 mcg once Daily.
Chronic Idiopathic Constipation
PO: ADULTS 18 YRS AND OLDER, ELDERLY: 145 mcg once daily.
Dosage in Renal/Hepatic Impairment
No dose adjustment.
SIDE EFFECTS
Frequent (16%): Diarrhea (may begin within first 2 wks of initiation of treatment). Occasional (7%–2%): Abdominal pain, flatulence, headache, abdominal distention. Rare (1% and Less): Gastroesophageal reflux, vomiting.
ADVERSE EFFECTS/TOXIC REACTIONS
Severe diarrhea was reported in 2% of pts. Viral gastroenteritis was noted in 3% of pts. Fecal incontinence, dehydration was reported in 1%. Dose reduced or suspended secondary to diarrhea, other GI adverse reaction.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Encourage adequate fluid intake. Assess bowel sounds for peristalsis. Assess for abdominal disturbances.
INTERVENTION/EVALUATION
For pts with irritable bowel syndrome, assess for improvement in symptoms (relief from bloating, cramping, urgency, abdominal discomfort). Monitor daily bowel activity, stool consistency. Monitor serum electrolytes in pts with prolonged, frequent, or excessive use of medication.
PATIENT/FAMILY TEACHING
• Institute measures to promote defecation: increase fluid intake, exercise, high-fiber diet. • Report new/worsening episodes of abdominal pain, severe diarrhea. • Do not break, crush, or open capsule. Take whole.
linagliptin
lin-a-glip-tin
(Tradjenta)
Do not confuse linagliptin with saxagliptin or sitagliptin.
FIXED-COMBINATION(S)
Glyxambi: linagliptin/empagliflozin (an antidiabetic): 5 mg/10 mg, 5 mg/25 mg. Jentadueto: linagliptin/metformin (an antidiabetic): 2.5 mg/500 mg; 2.5 mg/850 mg; 2.5 mg/1,000 mg. Jentadueto XR: linagliptin/metformin (extended-release): 2.5 mg/1,000 mg; 5 mg/1,000 mg.
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: Dipeptidyl peptidase-4 (DDP-4) inhibitor (gliptan). CLINICAL: Antidiabetic agent.
USES
Adjunctive treatment to diet and exercise to improve glycemic controls in pts with type 2 diabetes mellitus alone or in combination with other antidiabetic agents.
PRECAUTIONS
Contraindications: Hypersensitivity to linagliptin, other DD4 inhibitors. Cautions: Concurrent use of other hypoglycemics. Not recommended for use in type 1 diabetes, diabetic ketoacidosis, history of pancreatitis, HF.
ACTION
Slows inactivation of incretin hormones by inhibiting DDP-4 enzyme. Therapeutic Effect: Incretin hormones increase insulin synthesis/release from pancreas and decrease glucagon secretion. Lowers serum glucose levels.
PHARMACOKINETICS
Rapidly absorbed following PO administration. Peak plasma concentration: 1.5 hrs. Extensive tissue distribution. Protein binding: 70%–99%. Minimal metabolism (90% excreted as unchanged metabolite). Excreted primarily in enterohepatic system (80%), urine (5%). Half-life: 12 hrs.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown if distributed in breast milk. Children: Safety and efficacy not established. Elderly: No age-related precautions noted.
INTERACTIONS
DRUG: CYP3A4 inducers (e.g., rifampin) may decrease concentration. Insulin, metformin, saxagliptin, sitagliptin, sulfonylureas may increase risk of hypoglycemia. HERBAL: Ginseng, ginger, other herbs with hypoglycemic activity may increase risk of hypoglycemia. FOOD: None known. LAB VALUES: Decreases serum glucose. May increase serum uric acid.
AVAILABILITY (Rx)
Tablets: 5 mg.
ADMINISTRATION/HANDLING
PO
• May give without regard to food.
INDICATIONS/ROUTES/DOSAGE
Note: Dose reduction of insulin and/or insulin secretagogues may be needed.
Type 2 Diabetes Mellitus
PO: ADULTS, ELDERLY: 5 mg once daily.
Dosage in Renal/Hepatic Impairment
No dose adjustment.
SIDE EFFECTS
Occasional (5%): Nasopharyngitis. Rare (less than 2%): Cough, headache.
ADVERSE EFFECTS/TOXIC REACTIONS
Hypoglycemia reported in 7% of pts. Concomitant use of hypoglycemic medication may increase hypoglycemic risk. Pancreatitis, hypersensitivity reactions (angioedema, rash, urticaria, pruritus, bronchospasm) occur rarely.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Check blood glucose, hemoglobin A1c level. Assess pt’s understanding of diabetes management, routine glucose monitoring. Receive full medication history including herbal products.
INTERVENTION/EVALUATION
Monitor blood glucose, hemoglobin A1c level. Assess for hypoglycemia (diaphoresis, tremors, dizziness, anxiety, headache, tachycardia, perioral numbness, hunger, diplopia, difficulty concentrating), hyperglycemia (polyuria, polyphagia, polydipsia, nausea, vomiting, fatigue, Kussmaul breathing). Screen for glucose-altering conditions: fever, increased activity or stress, surgical procedures. Dietary consult for nutritional education.
PATIENT/FAMILY TEACHING
• Diabetes mellitus requires lifelong control. • Diet and exercise is principal part of treatment; do not skip or delay meals. • Test blood glucose regularly. • When taking combination drug therapy or when glucose demands are altered (fever, infection, trauma, stress, heavy physical activity), have hypoglycemic treatment available (glucagon, oral dextrose). • Monitor daily calorie intake.
linezolid
lin-ez-oh-lid
Apo-Linezolid
, (Zyvox, Zyvoxam
)
Do not confuse Zyvox with Zosyn or Zovirax.
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: Oxazolidinone. CLINICAL: Antibiotic.
USES
Treatment of susceptible infections due to aerobic and facultative, gram-positive microorganisms, including E. faecium (vancomycin-resistant strains only), S. aureus (including methicillin-resistant strains), S. agalactiae, S. pneumoniae (including multidrug-resistant strains), S. pyogenes. Treatment of pneumonia (community-acquired and hospital acquired), skin, soft tissue infections (including diabetic foot infections), bacteremia caused by susceptible vancomycin-resistant organisms. OFF-LABEL: Treatment of prosthetic joint infection. Septic arthritis.
PRECAUTIONS
Contraindications: Hypersensitivity to linezolid. Concurrent use or within 2 wks of MAOIs. Cautions: History of seizures, preexisting myelosuppression, medications that may cause bone marrow depression, uncontrolled hypertension, pheochromocytoma, carcinoid syndrome, untreated hyperthyroidism, diabetes, chronic infection; concurrent use of SSRIs, SNRIs, tricyclic antidepressants, triptans, bupropion.
ACTION
Binds to bacterial ribosomal RNA sites preventing formation of a complex essential for bacterial translation. Therapeutic Effect: Bacteriostatic against enterococci, staphylococci; bactericidal against streptococci.
PHARMACOKINETICS
Rapidly, extensively absorbed after PO administration. Protein binding: 31%. Metabolized in liver by oxidation. Excreted in urine. Half-life: 4–5.4 hrs.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown if distributed in breast milk. Children: Safety and efficacy not established. Elderly: No age-related precautions noted.
INTERACTIONS
DRUG: CYP3A4 inducers (e.g., carbamazepine, phenytoin) may decrease concentration/effects. Adrenergic medications (sympathomimetics) may increase effects. SSRIs may increase risk of serotonin syndrome. HERBAL: Supplements containing caffeine, tyrosine, or tryptophan may precipitate hypertensive crisis. FOOD: Excessive amounts of tyramine-containing foods, beverages may cause significant hypertension. LAB VALUES: May decrease Hgb, neutrophils, platelets, WBC. May increase serum ALT, AST, alkaline phosphatase, amylase, bilirubin, BUN, creatinine, LDH, lipase.
AVAILABILITY (Rx)
Injection Premix: 2 mg/ml in 100-ml, 300-ml bags. Powder for Oral Suspension: 100 mg/5 ml. Tablets: 600 mg.
ADMINISTRATION/HANDLING
IV
Rate of Administration • Infuse over 30–120 min. • Should be administered without further dilution.
Storage • Store at room temperature. • Protect from light. • Yellow color does not affect potency.
PO
• Give without regard to meals. • Use suspension within 21 days after reconstitution. Gently invert 3–5 times before administration. • Do not shake.
IV INCOMPATIBILITIES
Amphotericin B complex (Abelcet, AmBisome, Amphotec), co-trimoxazole (Bactrim), diazepam (Valium), erythromycin (Erythrocin), pentamidine (Pentam IV), phenytoin (Dilantin).
IV COMPATIBILITIES
Calcium gluconate, dexmedetomidine (Precedex), heparin, magnesium, potassium chloride.
INDICATIONS/ROUTES/DOSAGE
Vancomycin-Resistant Infections (VRI)
PO, IV: ADULTS, ELDERLY, CHILDREN OLDER THAN 11 YRS: 600 mg q12h for 14–28 days. CHILDREN 11 YRS AND YOUNGER: 10 mg/kg q8–12h for 14–28 days.
Pneumonia, Complicated Skin/Skin Structure Infections
PO, IV: ADULTS, ELDERLY, CHILDREN OLDER THAN 11 YRS: 600 mg q12h for 10–14 days. CHILDREN 11 YRS AND YOUNGER: 10 mg/kg q8h for 10–14 days.
Uncomplicated Skin/Skin Structure Infections
PO: ADULTS, ELDERLY: 400 mg q12h for 10–14 days. CHILDREN OLDER THAN 11 YRS: 600 mg q12h for 10–14 days. CHILDREN 5–11 YRS: 10 mg/kg/dose q12h for 10–14 days. CHILDREN YOUNGER THAN 5 YRS: 10 mg/kg q8h for 10–14 days.
Usual Neonate Dosage
PO, IV: NEONATES: 10 mg/kg/dose q8–12h.
Dosage in Renal/Hepatic Impairment
No dose adjustment. Administer after HD on dialysis days.
SIDE EFFECTS
Occasional (9%–2%): Diarrhea, nausea, vomiting, insomnia, constipation, rash, dizziness, fever, headache. Rare (less than 2%): Altered taste, vaginal candidiasis, fungal infection, tongue discoloration.
ADVERSE EFFECTS/TOXIC REACTIONS
Thrombocytopenia, myelosuppression occur rarely. Antibiotic-associated colitis, other superinfections (abdominal cramps, severe watery diarrhea, fever) may result from altered bacterial balance in GI tract.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Obtain appropriate culture specimens for sensitivity testing prior to therapy. Obtain baseline CBC, chemistries.
INTERVENTION/EVALUATION
Monitor daily pattern of bowel activity, stool consistency. Mild GI effects may be tolerable, but increasing severity may indicate onset of antibiotic-associated colitis. Be alert for superinfection: fever, vomiting, diarrhea, anal/genital pruritus, oral mucosal changes (ulceration, pain, erythema). Monitor CBC, platelets, Hgb, chemistries.
PATIENT/ FAMILY TEACHING
• Continue therapy for full length of treatment. • Doses should be evenly spaced. • May cause GI upset (may take with food, milk). • Excessive amounts of tyramine-containing foods (red wine, aged cheese) may cause severe reaction (severe headache, neck stiffness, diaphoresis, palpitations). • Avoid alcohol. • Report persistent diarrhea, nausea, vomiting.
liraglutide
leer-a-gloo-tide
(Saxenda, Victoza)
BLACK BOX ALERT Causes dose-dependent and treatment duration–dependent thyroid C-cell tumors, including medullary thyroid cancer.
FIXED COMBINATION(S)
Xultophy: liraglutide 3.6 mg/ml and insulin degludec 100 units/ml.
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: Antihyperglycemic (glucagon-like peptide-1 [GLP-1] receptor agonist. CLINICAL: Antidiabetic agent.
USES
Saxenda: Adjunct to diet and increased physical activity for chronic weight management in adults with body mass index (BMI) of 30 kg/m2 or greater, or 27 kg/m2 or greater, with at least one co-morbid condition (e.g., hypertension, diabetes, dyslipidemia). Victoza: Adjunct to diet and exercise to improve glycemic control in adult pts with type 2 diabetes mellitus.
PRECAUTIONS
Contraindications: Hypersensitivity to liraglutide. Personal or family history of medullary thyroid carcinoma (MTC), pts with multiple endocrine neoplasia syndrome type 2 (MEN2). (Saxenda): Pregnancy. Cautions: History of pancreatitis, cholelithiasis, alcohol abuse, renal/hepatic impairment. History of angioedema to other GLP-1 receptor agonists. Do not use in type 1 diabetes or diabetic ketoacidosis. Medications with narrow therapeutic index or requiring rapid GI absorption.
ACTION
Stimulates release of insulin from pancreatic beta cells, mimics enhancement of glucose-dependent insulin secretion, suppresses elevated glucagon secretion, slows gastric emptying. Therapeutic Effect: Improves glycemic control by increasing postmeal insulin secretion, emptying, increasing satiety.
PHARMACOKINETICS
Maximum concentration achieved in 8–12 hrs. Protein binding: 98%. Metabolized to large proteins without a specific organ as major route of elimination. Half-life: 13 hrs.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown if distributed in breast milk. Children: Safety and efficacy not established. Elderly: No age-related precautions noted.
INTERACTIONS
DRUG: Liraglutide has potential to alter absorption of concurrently administered oral medications. HERBAL: None significant. FOOD: None known. LAB VALUES: Decreases glucose serum levels (when used in combination with insulin secretagogues [e.g., sulfonylureas]).
AVAILABILITY (Rx)
Subcutaneous, Solution (Prefilled Pen): (Victoza): 18 mg/3 ml. (Saxenda): (Prefilled Pen) 18 mg/3 ml. Delivers doses of 0.6 mg, 1.2 mg,1.8 mg, 2.4 mg, or 3 mg.
ADMINISTRATION/HANDLING
Subcutaneous
• May be given in thigh, abdomen, upper arm. • Rotation of injection sites is essential; maintain careful records. • Give at any time without regard to meals.
Storage • Refrigerate prefilled pens. • Discard if freezing occurs. • Discard pen 30 days after initial use.
INDICATIONS/ROUTES/DOSAGE
Diabetes Mellitus (Victoza)
SQ: ADULTS, ELDERLY: Initial dose: 0.6 mg subcutaneously once per day for at least 1 wk. (Note: This dose is intended to reduce GI symptoms during initial titration; it is not effective for glycemic control.) After 1 wk, increase dose to 1.2 mg. If 1.2-mg dose does not result in acceptable glycemic control, dose can be increased to 1.8 mg.
Weight Management (Saxenda)
SQ: ADULTS, ELDERLY: Initially, 0.6 mg daily for one week. Increase wkly by 0.6 mg/day to a target dose of 3 mg once daily. Note: Evaluate change in weight 16 wks after initiation. Discontinue if less than 4% of baseline weight not achieved.
Dosage in Renal/Hepatic Impairment
Use caution.
SIDE EFFECTS
Frequent (greater than 13%): Headache, nausea, diarrhea, liraglutide antibody resistance. Occasional (13%–6%): Diarrhea, vomiting, dizziness, nervousness, dyspepsia. Rare (less than 6%): Weakness, decreased appetite.
ADVERSE EFFECTS/TOXIC REACTIONS
Serious hypoglycemia may occur when used concurrently with insulin analogue (e.g., sulfonylurea); consider lowering dose.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Check blood glucose concentration before administration. Discuss pt’s lifestyle to determine extent of learning, emotional needs. Ensure follow-up instruction if pt/family does not thoroughly understand diabetes management or glucose testing technique. Dose is gradually increased to improve GI tolerance.
INTERVENTION/EVALUATION
Monitor blood glucose level, food intake. Assess for hypoglycemia (cool wet skin, tremors, dizziness, anxiety, headache, tachycardia, numbness in mouth, hunger, diplopia) or hyperglycemia (polyuria, polyphagia, polydipsia, nausea, vomiting, dim vision, fatigue, deep rapid breathing). Be alert to conditions that alter glucose requirements (fever, increased activity/stress, surgical procedures). Consider lowering dose of insulin analogue to reduce risk of hypoglycemia.
PATIENT/FAMILY TEACHING
• Diabetes mellitus requires lifelong control. • Prescribed diet, exercise are principal parts of treatment; do not skip/delay meals. • Continue following dietary instructions, regular exercise program, regular testing of blood glucose level. • Serious hypoglycemia may occur when used concurrently with insulin analogue (e.g., sulfonylurea). • Have source of glucose available to treat symptoms of low blood sugar.
lisdexamfetamine
lis-dex-am-fet-a-meen
(Vyvanse)
BLACK BOX ALERT Potential for drug abuse dependency exists.
Do not confuse lisdexamfetamine with dextroamphetamine, or Vyvanse with Glucovance, Vivactil, or Vytorin.
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: Amphetamine (Schedule II). CLINICAL: CNS stimulant.
USES
Treatment of attention-deficit/hyperactivity disorder (ADHD), moderate to severe binge eating disorder (BED).
PRECAUTIONS
Contraindications: Hypersensitivity to lisdexamfetamine, amphetamine products. Concurrent use or within 2 wks of use of MAOI. Cautions: Hyperthyroidism, glaucoma, agitated states, cardiovascular conditions (hypertension, recent MI, ventricular arrhythmias), elderly, psychiatric/seizures, preexisting psychosis or bipolar disorder, Tourette syndrome. Avoid use in pts with serious structural cardiac abnormalities, cardiomyopathy, arrhythmias, CAD. History of alcohol or drug abuse.
ACTION
Enhances action of dopamine, norepinephrine by blocking reuptake from synapses, increasing levels in extraneuronal space. Therapeutic Effect: Improves attention span in ADHD.
PHARMACOKINETICS
Rapidly absorbed. Converted to dextroamphetamine. Excreted in urine. Half-life: Less than 1 hr.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Has potential for fetal harm. Unknown if distributed in breast milk. Children: Safety and efficacy not established in pts younger than 6 yrs. Elderly: No age-related precautions noted.
INTERACTIONS
DRUG: MAOIs may prolong/intensify effects. May decrease sedative effect of antihistamines (e.g., diphenhydramine). May decrease hypotensive effects of antihypertensives (e.g., amlodipine, lisinopril, valsartan). Effects may be decreased by chlorpromazine, haloperidol, lithium, urinary acidifying agents (ammonium chloride, sodium acid phosphate). May increase absorption of phenobarbital, phenytoin. Tricyclic antidepressants (e.g., amitriptyline, doxepin) may increase cardiovascular effects. HERBAL: None significant. FOOD: None known. LAB VALUES: May increase plasma corticosteroid.
AVAILABILITY (Rx)
Capsules: 10 mg, 20 mg, 30 mg, 40 mg, 50 mg, 60 mg, 70 mg.
ADMINISTRATION/HANDLING
PO
• May be given in the morning without regard to food. • Administer capsule whole; pt must not chew. • Capsules may be opened and dissolved in water and taken immediately.
INDICATIONS/ROUTES/DOSAGE
ADHD
PO: ADULTS, CHILDREN 6 YRS AND OLDER: Initially, 30 mg once daily in the morning. May increase dosage in increments of 10 or 20 mg/day at wkly intervals. Maximum: 70 mg/day.
BED
PO: ADULTS, ELDERLY: Initially, 30 mg once daily in morning. May increase by 20 mg/day at wkly intervals to a target dose of 50–70 mg once daily. Maximum: 70 mg/day.
Dosage in Renal Impairment
CrCl 30 ml/min or greater: Maximum: 70 mg/day. CrCl 15–29 ml/min: Maximum: 50 mg/day. CrCl less than 15 ml/min or end-stage renal disease: Maximum: 30 mg/day.
Dosage in Hepatic Impairment
No dose adjustment.
SIDE EFFECTS
Frequent (39%): Decreased appetite. Occasional (19%–9%): Insomnia, upper abdominal pain, headache, irritability, vomiting, weight decrease. Rare (6%–2%): Nausea, dry mouth, dizziness, rash, affect change, fatigue, tic.
ADVERSE EFFECTS/TOXIC REACTIONS
Abrupt withdrawal following prolonged administration of high dosage may produce extreme fatigue (may last for wks). Prolonged administration to children with ADHD may produce a suppression of weight and/or height patterns. May produce cardiac irregularities, psychotic syndrome.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Assess attention span, impulse control, interaction with others.
INTERVENTION/EVALUATION
Monitor for CNS stimulation, increase in B/P, weight loss, pulse, sleep pattern, appetite. Observe for signs of hostility, aggression, depression.
PATIENT/FAMILY TEACHING
• Take early in day. • May mask extreme fatigue. • Report pronounced dizziness, decreased appetite, dry mouth, weight loss, new or worsened psychiatric problems, palpitations, dyspnea.
lisinopril
lye-sin-o-pril
(Apo-Lisinopril
, Prinivil, Qbrelis, Zestril)
BLACK BOX ALERT May cause fetal injury, mortality. Discontinue as soon as possible once pregnancy is detected.
Do not confuse lisinopril with fosinopril, or Prinivil with Plendil, Pravachol, Prevacid, Prilosec, Proventil, or Restoril, or Zestril with Desyrel, Restoril, Vistaril, Zetia, or Zostrix. Do not confuse lisinopril’s combination form Zestoretic with Prilosec.
FIXED-COMBINATION(S)
Prinzide/Zestoretic: lisinopril/hydrochlorothiazide (a diuretic): 10 mg/12.5 mg, 20 mg/12.5 mg, 20 mg/25 mg.
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: ACE inhibitor. CLINICAL: Antihypertensive.
USES
Treatment of hypertension in adults and children 6 yrs and older. Used alone or in combination with other antihypertensives. Adjunctive therapy in management of heart failure. Treatment of acute MI within 24 hrs in hemodynamically stable pts to improve survival. Treatment of left ventricular dysfunction following MI.
PRECAUTIONS
Contraindications: Hypersensitivity to lisinopril, other ACE inhibitors. History of angioedema from treatment with ACE inhibitors, idiopathic or hereditary angioedema. Concomitant use with aliskiren in pts with diabetes. Cautions: Renal impairment, unstented unilateral/bilateral renal artery stenosis, volume depletion, ischemic heart disease, cerebrovascular disease, severe aortic stenosis, hypertrophic cardiomyopathy, HF, systolic B/P less than 100, dialysis, hyponatremia; before, during, or immediately after major surgery. Concomitant use of potassium supplements.
ACTION
Suppresses renin-angiotensin-aldosterone system (prevents conversion of angiotensin I to angiotensin II, a potent vasoconstrictor; may inhibit angiotensin II at local vascular, renal sites). Decreases plasma angiotensin II, increases plasma renin activity, decreases aldosterone secretion. Therapeutic Effect: Reduces blood pressure.
PHARMACOKINETICS
| Route | Onset | Peak | Duration |
| PO | 1 hr | 6 hrs | 24 hrs |
Incompletely absorbed from GI tract. Protein binding: 25%. Primarily excreted unchanged in urine. Removed by hemodialysis. Half-life: 12 hrs (increased in renal impairment).
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Crosses placenta. Unknown if distributed in breast milk. Children: Safety and efficacy not established. Elderly: May be more sensitive to hypotensive effects.
INTERACTIONS
DRUG: Diuretics (e.g., furosemide, HCTZ) may increase hypotensive effects. May increase concentration, risk of toxicity of lithium. NSAIDs may decrease effects. Potassium-sparing diuretics (e.g., spironolactone, triamterene), potassium supplements may cause hyperkalemia. May increase hypoglycemic effect of oral hypoglycemic agents (e.g., glyburide, metformin). HERBAL: Ephedra, ginseng, licorice, yohimbe may worsen hypertension. Black cohosh, periwinkle may increase antihypertensive effect. FOOD: None known. LAB VALUES: May increase serum BUN, alkaline phosphatase, bilirubin, creatinine, potassium, ALT, AST. May decrease serum sodium. May cause positive ANA titer.
AVAILABILITY (Rx)
Solution, Oral: (Qbrelis) 1 mg/ml. Tablets: 2.5 mg, 5 mg, 10 mg, 20 mg, 30 mg, 40 mg.
ADMINISTRATION/HANDLING
PO
• Give without regard to food. • Tablets may be crushed.
INDICATIONS/ROUTES/DOSAGE
Hypertension (Used Alone)
PO: ADULTS: Initially, 10 mg/day. May increase by 5–10 mg/day at 1- to 2-wk intervals. Range: 10–40 mg/day. ELDERLY: Initially, 2.5–5 mg/day. May increase by 2.5–5 mg/day at 1- to 2-wk intervals. Maximum: 40 mg/day. CHILDREN 6 YRS OR OLDER: Initially, 0.07 mg/kg once daily (up to 5 mg). Titrate at 1- to 2-wk intervals. Maximum: 40 mg/day.
Hypertension (in Combination with Other Antihypertensives)
◀ ALERT ▶ If possible, discontinue diuretics 48–72 hrs prior to initiating lisinopril therapy.
PO: ADULTS, ELDERLY: Initially, 2.5–5 mg/day titrated to pt’s needs. Range: 10–40 mg/day.
HF
PO: ADULTS, ELDERLY: Initially, 2.5–5 mg/day. May increase by no more than 10 mg/day at intervals of at least 2 wks to a target dose of 20–40 mg once daily.
Improve Survival in Pts after MI
PO: ADULTS, ELDERLY: Initially, 5 mg, then 5 mg after 24 hrs, 10 mg after 48 hrs, then 10 mg/day for 6 wks. For pts with low systolic B/P, give 2.5 mg/day for 3 days, then 2.5–5 mg/day. Discontinue if systolic B/P less than 90 mm Hg for more than 1 hr.
Dosage in Renal Impairment
CrCl less than 30 ml/min: Not recommended in children. Titrate to pt’s needs after giving the following initial dose:
Hypertension
| Creatinine Clearance | Initial Dose |
| 10–30 ml/min | 5 mg |
| Less than 10 ml/min or Dialysis | 2.5 mg |
HF
CrCl less than 30 ml/min or serum creatinine greater than 3 mg/dL: Initial dose: 2.5 mg.
Acute MI
Creatinine clearance 30 ml/min or less: Initial dose: 2.5 mg.
Dosage in Hepatic Impairment
No dose adjustment.
SIDE EFFECTS
Frequent (12%–5%): Headache, dizziness, postural hypotension. Occasional (4%–2%): Chest discomfort, fatigue, rash, abdominal pain, nausea, diarrhea, upper respiratory infection. Rare (1% or less): Palpitations, tachycardia, peripheral edema, insomnia, paresthesia, confusion, constipation, dry mouth, muscle cramps.
ADVERSE EFFECTS/TOXIC REACTIONS
Excessive hypotension (“first-dose syncope”) may occur in pts with HF, severe salt/volume depletion. Angioedema (swelling of face and lips), hyperkalemia occur rarely. Agranulocytosis, neutropenia may be noted in pts with collagen vascular disease (scleroderma, systemic lupus erythematosus). Nephrotic syndrome may be noted in pts with history of renal disease.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Obtain B/P, apical pulse immediately before each dose, in addition to regular monitoring (be alert to fluctuations). In pts with renal impairment, autoimmune disease, taking drugs that affect leukocytes or immune response, CBC and differential count should be performed before beginning therapy and q2wks for 3 mos, then periodically thereafter.
INTERVENTION/EVALUATION
Assess for edema. Auscultate lungs for rales. Monitor I&O; weigh daily. Monitor daily pattern of bowel activity, stool consistency. Assist with ambulation if dizziness occurs. Monitor B/P, renal function tests, WBC, serum potassium. If excessive reduction in B/P occurs, place pt in supine position, feet slightly elevated.
PATIENT/ FAMILY TEACHING
• To reduce hypotensive effect, go from lying to standing slowly. • Limit alcohol intake. • Report vomiting, diarrhea, diaphoresis, swelling of face/lips/tongue, difficulty in breathing, persistent cough. • Limit salt intake.
lithium
lith-ee-um
(Apo-Lithium
, Lithobid)
BLACK BOX ALERT Lithium toxicity is closely related to serum lithium levels and can occur at therapeutic doses. Routine determination of serum lithium levels is essential during therapy.
Do not confuse Lithobid with Levbid or Lithostat.
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: Psychotherapeutic. CLINICAL: Antimanic, antidepressant, vascular headache prophylactic.
USES
Management of bipolar disorder. Treatment of mania in pts with bipolar disorder. OFF-LABEL: Augmenting agent for depression.
PRECAUTIONS
Contraindications: Hypersensitivity to lithium. Severely debilitated pts, severe cardiovascular disease, severe dehydration, severe renal disease, severe sodium depletion or dehydration. Cautions: Mild to moderate cardiovascular disease, thyroid disease, elderly, mild to moderate renal impairment, medications altering sodium excretion, pregnancy, pts at risk for suicide, pts with significant fluid loss, pts receiving neuromuscular blocking agents.
ACTION
Changes cation transport across cell membrane in nerve/muscle cells; influences reuptake of serotonin/norepinephrine. Therapeutic Effect: Produces antimanic, antidepressant effects.
PHARMACOKINETICS
Rapidly, completely absorbed from GI tract. Protein binding: None. Primarily excreted unchanged in urine. Removed by hemodialysis. Half-life: 18–24 hrs (increased in elderly).
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Freely crosses placenta. Distributed in breast milk. Children: May increase bone formation or density (alter parathyroid hormone concentrations). Elderly: More susceptible to develop lithium-induced goiter or clinical hypothyroidism, CNS toxicity. Increased thirst, urination noted more frequently; lower dosage recommended.
INTERACTIONS
DRUG: Diuretics (e.g., furosemide), NSAIDs, metronidazole, ACE inhibitors (e.g., enalapril, lisinopril), angiotensin II antagonists, SSRIs, calcium channel blockers (e.g., losartan, valsartan) may increase lithium concentration, risk of toxicity. HERBAL: None significant. FOOD: None known. LAB VALUES: May increase serum glucose, immunoreactive parathyroid hormone, calcium. Therapeutic serum level: 0.6–1.2 mEq/L; toxic serum level: greater than 1.5 mEq/L.
AVAILABILITY (Rx)
Capsules: 150 mg, 300 mg, 600 mg. Oral Solution: 300 mg/5 ml. Tablets: 300 mg.
Tablets (Extended-Release): 300 mg, 450 mg.
ADMINISTRATION/HANDLING
PO
• Administer with meals, milk to decrease GI upset. • Do not break, crush, dissolve, or divide extended-release tablets.
INDICATIONS/ROUTES/DOSAGE
◀ ALERT ▶ During acute phase, a therapeutic serum lithium concentration of 0.6–1.2 mEq/L is required. For long-term control, desired level is 0.8–1 mEq/L. Monitor serum drug concentration, clinical response to determine proper dosage.
Usual Dosage
PO: ADULTS, ELDERLY, CHILDREN OLDER THAN 12 YRS: (Immediate-Release):300 mg 3–4 times/day.(Extended-Release):450 mg twice daily. Gradually increase based on response/tolerability. Usual dose: (Immediate-Release): 900–1,800 mg/day in 3–4 divided doses. (Extended-Release): 900–1,800 mg in 2 divided doses. CHILDREN 6–12 YRS: (Immediate-Release):15–60 mg/kg/day in 3–4 divided doses not to exceed usual adult dose.
Dosage in Renal Impairment
| Creatinine Clearance | Dosage |
| 10–50 ml/min | 50%–75% normal dose |
| Less than 10 ml/min | 25%–50% normal dose |
| End-stage renal disease with HD | Dose after HD |
Dosage in Hepatic Impairment
No dose adjustment.
SIDE EFFECTS
◀ ALERT ▶ Side effects are dose related and seldom occur at lithium serum levels less than 1.5 mEq/L. Occasional: Fine hand tremor, polydipsia, polyuria, mild nausea. Rare: Weight gain, bradycardia, tachycardia, acne, rash, muscle twitching, peripheral cyanosis, pseudotumor cerebri (eye pain, headache, tinnitus, vision disturbances).
ADVERSE EFFECTS/TOXIC REACTIONS
Lithium serum concentration of 1.5–2.0 mEq/L may produce vomiting, diarrhea, drowsiness, confusion, incoordination, coarse hand tremor, muscle twitching, T-wave depression on EKG. Lithium serum concentration of 2.0–2.5 mEq/L may result in ataxia, giddiness, tinnitus, blurred vision, clonic movements, severe hypotension. Acute toxicity may be characterized by seizures, oliguria, circulatory failure, coma, death.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Assess mental status (e.g., mood, behavior). Serum lithium levels should be tested q3–4days during initial phase of therapy, q1–2mos thereafter, and wkly if there is no improvement of disorder or adverse effects occur.
INTERVENTION/EVALUATION
Clinical assessment of therapeutic effect, tolerance to drug effect is necessary for correct dosing-level management. Assess behavior, appearance, emotional status, response to environment, speech pattern, thought content. Monitor serum lithium concentrations, CBC with differential, urinalysis, creatinine clearance. Monitor renal, hepatic, thyroid, cardiovascular function; serum electrolytes. Assess for increased urinary output, persistent thirst. Report polyuria, prolonged vomiting, diarrhea, fever to physician (may need to temporarily reduce or discontinue dosage). Monitor for signs of lithium toxicity. Assess for therapeutic response (interest in surroundings, improvement in self-care, increased ability to concentrate, relaxed facial expression). Monitor lithium levels q3–4days at initiation of therapy (then q1–2mos). Obtain lithium levels 8–12 hrs postdose. Therapeutic serum level: 0.6–1.2 mEq/L; toxic serum level: greater than 1.5 mEq/L.
PATIENT/ FAMILY TEACHING
• Limit alcohol, caffeine intake. • Avoid tasks requiring coordination until CNS effects of drug are known. • May cause dry mouth. • Maintain steady salt, fluid intake (avoid dehydration). • Report vomiting, diarrhea, muscle weakness, tremors, drowsiness, ataxia. • Serum level monitoring is necessary to determine proper dose.
lixisenatide
lix-i-sen-a-tide
(Adlyxin)
Do not confuse lixisenatide with exenatide, liraglutide.
FIXED-COMBINATION(S)
Soliqua: lixisenatide 33 mcg/ml and insulin glargine 100 units/ml.
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: Antihyperglycemic (glucagon-like peptide-1 [GLP-1]) receptor agonist. CLINICAL: Antidiabetic agent.
USES
Adjunct to diet and exercise to improve glycemic controls in pts with type 2 diabetes mellitus.
PRECAUTIONS
Contraindications: Hypersensitivity to lixisenatide. Cautions: Renal impairment, severe gastroparesis, history of pancreatitis. Not recommended in pts with diabetic ketoacidosis, type 1 diabetes mellitus. Not a substitute for insulin. Medications with narrow therapeutic index or requiring rapid GI absorption.
ACTION
Increases glucose-dependent insulin secretion; decreases glucagon secretion. Slows gastric emptying. Therapeutic Effect: Improves glycemic control by lowering fasting glucose and postprandial blood glucose.
PHARMACOKINETICS
Widely distributed. Protein binding: not specified. Peak plasma concentration: 1–3.5 hrs. Eliminated through glomerulus filtration and proteolytic degradation. Half-life: 3 hrs.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown if distributed in breast milk. Children: Safety and efficacy not established in pts younger than 18 yrs. Elderly: No age-related precautions noted.
INTERACTIONS
DRUG: May increase hypoglycemic effect when added to insulin or sulfonylureas. May decrease the rate of absorption of oral medications due to delayed gastric emptying. Oral contraceptive should be taken 1 hr before or 11 hrs after lixisenatide. HERBAL: None significant. FOOD: None known. LAB VALUES: Expected to decreased serum glucose, Hgb A1c.
AVAILABILITY (Rx)
Prefilled Injector Pens: 50 mcg/ml in 3 ml (for 14 preset doses of 10 mcg/dose), 100 mcg/ml in 3 ml (for 14 preset doses of 20 mcg/dose).
ADMINISTRATION/HANDLING
Subcutaneous
Preparation • Follow instructions for preparation according to manufacturer guidelines. • Visually inspect for particulate matter or discoloration. Solution should appear clear and colorless. • Do not use if solution is cloudy or discolored or if visible particles are observed.
Administration • Administer within 1 hr before the first meal of the day, preferably the same time each day. If a dose is missed, administer within 1 hr prior to next meal. • Insert needle subcutaneously into upper arms, outer thigh, or abdomen and inject solution. • Do not inject into areas of active skin disease or injury such as sunburns, skin rashes, inflammation, skin infections, or active psoriasis. • Rotate injection sites.
Storage • Refrigerate unused injector pens. • Once injector pen is activated, store at room temperature for up to 14 days. • Do not freeze. • Protect from light.
INDICATIONS/ROUTES/DOSAGE
Type 2 Diabetes Mellitus
SQ: ADULTS, ELDERLY: 10 mcg once daily for 14 days. Maintenance: Increase to 20 mcg once daily on day 15.
Dosage in Renal Impairment
Use caution.
Dosage in Hepatic Impairment
No dose adjustment.
SIDE EFFECTS
Frequent (25%–10%): Nausea, vomiting.
Occasional (9%–1%): Headache, diarrhea, dizziness, dyspepsia, constipation, abdominal distention, abdominal pain.
ADVERSE EFFECTS/TOXIC REACTIONS
May increase risk of acute renal failure or worsening of chronic renal impairment (esp. in pts with vomiting, dehydration). May increase risk of hypoglycemia when used with other hypoglycemic agents or insulin. Anaphylaxis reported in less than 1% of pts. Other hypersensitivity reactions including angioedema, bronchospasm, laryngeal edema occur rarely. Acute pancreatitis, hemorrhagic or necrotizing pancreatitis were reported. Immunogenicity (auto-lixisenatide antibodies) occurred in 70% of pts.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Obtain baseline fasting glucose level, Hgb A1c; BMP. Question history of renal impairment, gastroparesis, hypersensitivity reaction. Screen for use of other hypoglycemic agents or insulin. Assess pt’s understanding of diabetes management, routine home glucose monitoring, medication self-administration. Assess hydration status. Obtain dietary consult for nutritional education.
INTERVENTION/EVALUATION
Monitor capillary blood glucose levels, Hgb A1c; renal function test (esp. in pts with renal impairment who report diarrhea, gastroparesis, vomiting). Assess for hypoglycemia (anxiety, confusion, diaphoresis, diplopia, dizziness, headache, hunger, perioral numbness, tachycardia, tremors), hyperglycemia (confusion, fatigue, Kussmaul breathing, nausea, polyuria, vomiting). Screen for glucose-altering conditions: fever, stress, surgical procedures, trauma. Monitor for hypersensitivity reactions; abdominal pain that radiates to the back. Encourage PO intake. Monitor I&Os.
PATIENT/FAMILY TEACHING
• Diabetes mellitus requires lifelong control. Diet and exercise is principal part of treatment; do not skip or delay meals. • Test blood sugar regularly. • Monitor daily calorie intake. • When taking additional medications to lower blood sugar or when glucose demands are altered (fever, infection, stress trauma), have low blood sugar treatment available (glucagon, oral dextrose).
• Persistent, severe abdominal pain that radiates to the back (with or without vomiting) may indicate acute pancreatitis. • Report allergic reactions of any kind, esp. difficulty breathing, itching, rash, swelling of the face or throat. • Oral contraceptives should be taken at least 1 hr before or 11 hrs after dose. • Therapy may cause acute kidney injury or kidney failure; report decreased urine output, amber-colored urine, flank pain.
lomitapide
lom-i-ta-pide
(Juxtapid)
Do not confuse lomitapide with loperamide.
BLACK BOX ALERT May cause hepatotoxicity. May cause hepatic steatosis (increase in hepatic fat) regardless of serum ALT, AST elevation; may be risk factor for progressive hepatic disease, including steatohepatitis and cirrhosis.
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: Microsomal triglyceride transfer protein inhibitor. CLINICAL: Antihyperlipidemic.
USES
Treatment of homozygous familial hypercholesterolemia (HoFH) in combination with low-fat diet and other lipid-lowering therapies, including LDL-C apheresis, to reduce LDL, total cholesterol, apoprotein B, non–HDL-C.
PRECAUTIONS
Contraindications: Hypersensitivity to lomitapide. Pregnancy, breastfeeding, moderate to severe hepatic impairment, active hepatic disease including unexplained persistent elevation of serum transaminases, concomitant use of strong CYP3A4 inhibitors (e.g., ketoconazole, protease inhibitors). Cautions: Mild to moderate renal impairment, end-stage renal disease, mild hepatic impairment, alcohol consumption. Avoid use in pts with history of glucose-galactose malabsorption, other agents having hepatotoxic potential (e.g., acetaminophen).
ACTION
Inhibits microsomal triglyceride transfer protein in lumen of endoplasmic reticulum. Prevents assembly of apo-B-containing lipoproteins in enterocytes, hepatocytes; inhibits synthesis of chylomicrons, very low density lipoprotein (VLDL). Therapeutic Effect: Decreases plasma low-density lipoprotein cholesterol (LDL-C).
PHARMACOKINETICS
Well absorbed in GI tract. Metabolized in liver. Protein binding: 99%. Peak plasma concentration: 6 hrs. Primarily excreted in feces. Half-life: 40 hrs.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Contraindicated in pregnancy. May cause fetal harm. Must use effective contraception in addition to barrier methods. Unknown if distributed in breast milk. Must either discontinue breastfeeding or discontinue therapy. Children: Safety and efficacy not established. Elderly: Increased risk for side effects, adverse reactions.
INTERACTIONS
DRUG: Acetaminophen, amiodarone, isotretinoin, methotrexate, tamoxifen, tetracycline may increase risk for hepatotoxicity. Strong CYP3A4 inhibitors (e.g., ketoconazole, protease inhibitors) contraindicated due to increased risk for myopathy, rhabdomyolysis. Moderate CYP3A4 inhibitors (e.g., atorvastatin, oral contraceptives) may increase concentration. May increase concentration of warfarin. May increase effects of P-glycoprotein substrates (e.g., digoxin, sitagliptin). HERBAL: None known. FOOD: Grapefruit products may increase absorption, toxicity. LAB VALUES: May increase serum alkaline phosphatase, bilirubin, ALT, AST.
AVAILABILITY (Rx)
Capsules: 5 mg, 10 mg, 20 mg, 30 mg, 40 mg, 60 mg.
ADMINISTRATION/HANDLING
PO
• Give with water only. • Administer without food (at least 2 hrs after evening meal). • Administer whole; do not break, crush, or open capsules.
INDICATIONS/ROUTES/DOSAGE
◀ ALERT ▶ To reduce risk for fat-soluble nutrient deficiency, recommend supplemental coadministration: vitamin E 400 international units PO daily, linolenic acid 200 mg PO daily, alpha-linolenic acid (ALA) 210 mg PO daily, eicosapentaenoic acid (EPA) 110 mg PO daily, docosahexaenoic acid (DHA) 80 mg PO daily. Because of risk for myopathy, concurrent use of simvastatin should not exceed 20–40 mg/day.
Homozygous Familial Hypercholesterolemia
PO: ADULTS, ELDERLY: Initially, 5 mg once daily for minimum of 2 wks. Gradually increase dose at 4-wk (minimum) intervals to 10 mg once daily, then 20 mg once daily, then 40 mg once daily, then 60 mg once daily based on tolerability. Maximum: 60 mg/day.
Dose Modification
Elevated Hepatic Enzymes
If ALT, AST is between 3–5 times upper limit of normal (ULN), reduce dose until ALT, AST less than 3 times ULN. If ALT, AST is greater than 5 times ULN, withhold dose until less than 3 times ULN, then restart at reduced dose. If hepatotoxicity occurs or bilirubin level rises greater than 2 times ULN, discontinue treatment.
End-Stage Renal Disease Receiving Dialysis, Mild Hepatic Impairment
Do not exceed 40 mg/day.
Concurrent Use of Weak CYP3A4 Inhibitors
Do not exceed 30 mg/day.
Concurrent Use of Oral Contraception
Do not exceed 30 mg/day.
Dosage in Renal Impairment
No dose adjustment. End-stage renal disease: Maximum: 40 mg/day.
Dosage in Hepatic Impairment
Mild impairment: Maximum: 40 mg/day. Moderate to severe impairment: Contraindicated.
SIDE EFFECTS
Frequent (79%–65%): Diarrhea, nausea. Occasional (38%–10%): Dyspepsia, vomiting, abdominal pain, weight loss, abdominal distention, constipation, flatulence, fatigue, back pain, gastric reflux, headache, dizziness.
ADVERSE EFFECTS/TOXIC REACTIONS
Progressive hepatic disease including steatohepatitis, cirrhosis has been reported in 6% of pts due to increased hepatic fat. May reduce absorption of fat-soluble nutrients; recommend daily supplemental replacement. Increased risk for myopathy including rhabdomyolysis (muscle pain/tenderness, weakness, dark or decreased urine output, elevated serum creatinine, CPK) when used with other antihyperlipidemics. May increase risk for supratherapeutic INR with warfarin. Infections including influenza, nasopharyngitis, gastroenteritis reported in 5% of pts. Palpitations, angina pectoris report in 3% of pts. Increased risk for dehydration/malabsorption with galactose intolerance hereditary disorder, pancreatic disease, diarrhea.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Obtain detailed dietary history, esp. fat consumption. Confirm negative pregnancy test before initiating treatment. Obtain baseline laboratory studies: ALT, AST, alkaline phosphatase, bilirubin, serum cholesterol, triglycerides, PT/INR (if pt is on warfarin). Confirm positive history of homozygous familial hypercholesterolemia (HoFH). Receive full medication history including vitamins, minerals, herbal products. Screen for history of galactose intolerance, renal/hepatic impairment, angina.
INTERVENTION/EVALUATION
Maintain hydration; offer fluids frequently. Monitor INR routinely (with anticoagulants). Monitor LFT with any dosage change, then every month for first year when maintenance goal reached, then every 3 mos. Obtain EKG for palpitations, shortness of breath, dizziness. Monitor for bruising, hematuria, jaundice, right upper abdominal pain, fever, lethargy, melena.
PATIENT/FAMILY TEACHING
• Avoid pregnancy. • Use appropriate contraception measures, including barrier precautions. • If pregnancy occurs, inform physician immediately. • Diarrhea may decrease effectiveness of oral contraception. • Do not breastfeed. • Maintain low-fat diet. • Report yellowing of skin, bruising, black/tarry stool, right upper quadrant pain, fever, lethargy, chest pain, palpitations. • Avoid alcohol. • Avoid grapefruit products. • Do not chew, crush, or open capsules. • Report any newly prescribed medications.
loperamide
loe-per-a-myde
(Apo-Loperamide
, Diamode, Diarr-Eze
, Imodium A-D, Loperacap
, Novo-Loperamide
)
Do not confuse Imodium with Indocin, or loperamide with furosemide.
FIXED-COMBINATION(S)
Imodium Advanced: loperamide/simethicone (an antiflatulent): 2 mg/125 mg.
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: Antidiarrheal agent. CLINICAL: Antidiarrheal.
USES
Controls, provides symptomatic relief of acute nonspecific diarrhea, chronic diarrhea associated with inflammatory bowel disease, reduce volume of ileostomy discharge. OTC: Control symptoms of diarrhea, including traveler’s diarrhea. OFF-LABEL: Chemotherapy-induced diarrhea, irinotecan-induced delayed diarrhea.
PRECAUTIONS
Contraindications: Hypersensitivity to loperamide. Abdominal pain without diarrhea, children younger than 2 yrs. Cautions: Hepatic impairment, use in young children. Avoid use when inhibition of peristalsis is undesirable (e.g., potential for ileus, megacolon).
ACTION
Directly affects intestinal wall muscles through opioid receptor. Therapeutic Effect: Slows intestinal motility, prolongs transit time of intestinal contents by reducing fecal volume, diminishing loss of fluid, electrolytes, increasing viscosity, bulk of stool. Increases tone of anal sphincter.
PHARMACOKINETICS
Poorly absorbed from GI tract. Protein binding: 97%. Metabolized in liver. Excreted in feces (30%), urine (less than 2%). Not removed by hemodialysis. Half-life: 7–14 hrs.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown if drug crosses placenta or is distributed in breast milk. Children: Not recommended for pts younger than 6 yrs (infants younger than 3 mos more susceptible to CNS effects). Elderly: May mask dehydration, electrolyte depletion.
INTERACTIONS
DRUG: Ritonavir may increase concentration, side effects. May decrease concentration of saquinavir. HERBAL: None significant. FOOD: None known. LAB VALUES: None significant.
AVAILABILITY (Rx)
Capsules: 2 mg. Liquid: 1 mg/5 ml, 1 mg/7.5 ml. Suspension, Oral: 1 mg/7.5 ml. Tablet: 2 mg. Tablet, Chewable: 2 mg.
ADMINISTRATION/HANDLING
Liquid
• When administering to children, use accompanying plastic dropper to measure the liquid.
INDICATIONS/ROUTES/DOSAGE
Acute Diarrhea
PO (Capsules): ADULTS, ELDERLY: Initially, 4 mg, then 2 mg after each unformed stool. Maximum: 16 mg/day. CHILDREN 9–12 YRS, WEIGHING MORE THAN 30 KG: Initially, 2 mg 3 times/day for 24 hrs. CHILDREN 6–8 YRS, WEIGHING 20–30 KG: Initially, 2 mg twice daily for 24 hrs. CHILDREN 2–5 YRS, WEIGHING 13–20 KG: Initially, 1 mg 3 times/day for 24 hrs. Maintenance: 1 mg/10 kg only after loose stool but not exceeding initial dose.
Chronic Diarrhea
PO: ADULTS, ELDERLY: Initially, 4 mg, then 2 mg after each unformed stool until diarrhea is controlled. Average maintenance dose: 4–8 mg/day. Maximum: 16 mg/day. CHILDREN: 0.08–0.24 mg/kg/day in 2–3 divided doses. Maximum: 2 mg/dose.
Traveler’s Diarrhea
PO: ADULTS, ELDERLY: Initially, 4 mg, then 2 mg after each loose bowel movement (LBM). Maximum: 8 mg/day for 2 days. CHILDREN 9–11 YRS: Initially, 2 mg, then 1 mg after each LBM. Maximum: 6 mg/day for 2 days. CHILDREN 6–8 YRS: Initially, 2 mg, then 1 mg after each LBM. Maximum: 4 mg/day for 2 days.
Dosage in Renal/Hepatic Impairment
No dose adjustment.
SIDE EFFECTS
Rare: Dry mouth, drowsiness, abdominal discomfort, allergic reaction (rash, pruritus).
ADVERSE EFFECTS/TOXIC REACTIONS
Toxicity results in constipation, GI irritation (nausea, vomiting), CNS depression. Activated charcoal is used to treat loperamide toxicity.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Do not administer in presence of bloody diarrhea, temperature greater than 101°F.
INTERVENTION/EVALUATION
Encourage adequate fluid intake. Assess bowel sounds for peristalsis. Monitor daily pattern of bowel activity, stool consistency. Withhold drug, notify physician promptly in event of abdominal pain, distention, fever.
PATIENT/FAMILY TEACHING
• Do not exceed prescribed dose. • May cause dry mouth. • Avoid alcohol. • Avoid tasks that require alertness, motor skills until response to drug is established. • Report diarrhea lasting more than 3 days, abdominal pain with distention, new-onset fever.
lopinavir/ritonavir
loe-pin-a-veer/rit-oh-na-veer
(Kaletra)
Do not confuse Kaletra with Keppra.
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: Protease inhibitor combination. CLINICAL: Antiretroviral.
USES
In combination with other antiretroviral agents for treatment of HIV infection.
PRECAUTIONS
Contraindications: Hypersensitivity to lopinavir, ritonavir. Concomitant use of potent CYP3A inducers: alfuzosin, ergot derivatives (causes vasospasm, peripheral ischemia of extremities), lovastatin, midazolam (oral), pimozide, rifampin, sildenafil (for treatment of pulmonary arterial hypertension), simvastatin, St. John’s wort, triazolam (increased sedation, respiratory depression); co-administration of medications highly dependent on CYP3A for clearance and increased concentrations associated with serious adverse reactions. Cautions: Hepatic impairment, hepatitis B or C infection, cardiac disease with underlying conduction abnormalities or structural heart defects, ischemic heart disease, cardiomyopathies, congenital long QT syndrome or medications that prolong QT interval, hypokalemia, history of pancreatitis, diabetes.
ACTION
Lopinavir inhibits activity of protease, an enzyme, late in HIV replication process; ritonavir increases plasma levels of lopinavir. Therapeutic Effect: Formation of immature, noninfectious viral particles.
PHARMACOKINETICS
Readily absorbed after PO administration (absorption increased when taken with food). Protein binding: 98%–99%. Metabolized in liver. Eliminated primarily in feces. Not removed by hemodialysis. Half-life: 5–6 hrs.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown if distributed in breast milk. Breastfeeding by HIV-infected mothers not recommended. Children: Safety and efficacy not established in pts younger than 6 mos. Elderly: Age-related renal/hepatic/cardiac impairment requires caution.
INTERACTIONS
DRUG: May increase concentration/toxicity of amiodarone, atorvastatin, bepridil, clarithromycin, cyclosporine, felodipine, fluticasone, ketoconazole, lidocaine, lovastatin, midazolam, nelfinavir, nicardipine, nifedipine, sildenafil, simvastatin, tacrolimus, trazodone, triazolam, warfarin. May decrease concentration/effects of oral contraceptives. CYP3A4 inducers (e.g., carbamazepine, phenytoin, rifampin) may decrease concentration/effects. May cause disulfiram-like reaction with metronidazole. HERBAL: St. John’s wort may decrease concentration/effects. FOOD: None known. LAB VALUES: May increase serum glucose, GGT, amylase, bilirubin, total cholesterol, triglycerides, uric acid, ALT, AST. May decrease platelets, serum sodium.
AVAILABILITY (Rx)
Oral Solution: 80 mg/ml lopinavir/20 mg/ml ritonavir.
Tablets: 100 mg lopinavir/25 mg ritonavir, 200 mg lopinavir/50 mg ritonavir.
ADMINISTRATION/HANDLING
PO
• Give tablets whole; do not break, crush, dissolve, or divide. • Does not require refrigeration. • Give tablets without regard to food. • Solution should be given with food. • Administer solution using calibrated oral syringe.
INDICATIONS/ROUTES/DOSAGE
HIV Infection
Doses based on lopinavir component.
PO:ADULTS: 800 mg once daily or 400 mg twice daily. Pregnant Women: 400 mg twice daily. CHILDREN 6 MOS–18 YRS, WEIGHING GREATER THAN 40 KG:(Oral Solution):400 mg twice daily. WEIGHING 15–40 KG: 10 mg/kg twice daily. WEIGHING LESS THAN 15 KG: 12 mg/kg twice daily. CHILDREN 14 DAYS–6 MOS: 16 mg/kg twice daily. (Tablets):WEIGHING GREATER THAN 35 KG: 400 mg twice daily. WEIGHING 26–35 KG: 300 mg twice daily. WEIGHING 15–25 KG: 200 mg twice daily. WEIGHING LESS THAN 15 KG: Not recommended.
Dosage Adjustment for Combination Therapy
Efavirenz, Fosamprenavir, Nelfinavir, Nevirapine: ADULTS, CHILDREN 6 MOS–18 YRS, WEIGHING GREATER THAN 45 KG: 500 mg (533-mg solution) twice daily. (Solution): 15–45 KG: 11 mg/kg twice daily. LESS THAN 15 KG: 13 mg/kg twice daily. (Tablet): 31–45 KG: 400 mg twice daily. 21–30 KG: 300 mg twice daily. 15–20 KG: 200 mg twice daily. LESS THAN 15 KG: Not recommended.
Dosage in Renal Impairment
No dose adjustment. Avoid once daily dosing in HD pts.
Dosage in Hepatic Impairment
Use caution.
SIDE EFFECTS
Frequent (14%): Mild to moderate diarrhea. Occasional (6%–2%): Nausea, asthenia. Abdominal pain, headache, vomiting. Rare (less than 2%): Insomnia, rash.
ADVERSE EFFECTS/TOXIC REACTIONS
Anemia, leukopenia, lymphadenopathy, deep vein thrombosis (DVT), Cushing’s syndrome, pancreatitis, hemorrhagic colitis occur rarely.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Obtain baseline CBC, renal function, LFT viral load, CD4 count, cell count. Obtain baseline weight.
INTERVENTION/EVALUATION
Monitor daily pattern of bowel activity, stool consistency. Assess for opportunistic infections: onset of fever, oral mucosa changes, cough, other respiratory symptoms. Check weight at least 2 times/wk. Assess for nausea, vomiting. Observe for signs/symptoms of pancreatitis (nausea, vomiting, abdominal pain). Monitor electrolytes, serum glucose, cholesterol, LFT, CBC with differential, CD4 cell count, viral load.
PATIENT/ FAMILY TEACHING
• Explain correct administration of medication. • Eat small, frequent meals to offset nausea, vomiting. • Lopinavir/ritonavir is not a cure for HIV infection, nor does it reduce risk of transmission to others. • Pt must continue practices to prevent HIV transmission. • Illnesses, including opportunistic infections, may still occur.
loratadine
lor-at-a-deen
(Alavert, Apo-Loratadine
, Claritin, Claritin Reditabs, Loradamed)
Do not confuse Claritin with clarithromycin.
FIXED-COMBINATION(S)
Alavert Allergy and Sinus, Claritin-D: loratadine/pseudoephedrine (a sympathomimetic): 5 mg/120 mg, 10 mg/240 mg.
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: H1 antagonist. CLINICAL: Antihistamine.
USES
Relief of nasal, non-nasal symptoms of seasonal allergic rhinitis (hay fever). Treatment of itching due to hives (urticaria).
PRECAUTIONS
Contraindications: Hypersensitivity to loratadine. Cautions: Renal/hepatic impairment.
ACTION
Competes with histamine for H1 receptor sites on effector cells. Therapeutic Effect: Prevents allergic responses mediated by histamine (e.g., rhinitis, urticaria, pruritus).
PHARMACOKINETICS
| Route | Onset | Peak | Duration |
| PO | 1–3 hrs | 8–12 hrs | Longer than 24 hrs |
Rapidly, almost completely absorbed from GI tract. Protein binding: 97%; metabolite, 73%–77%. Distributed mainly to liver, lungs, GI tract, bile. Metabolized in liver. Eliminated in urine (40%) and feces (40%). Not removed by hemodialysis. Half-life: 8.4 hrs; metabolite, 28 hrs (increased in elderly, hepatic impairment).
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Distributed in breast milk. Children: Safety and efficacy not established in pts younger than 2 yrs. Elderly: More sensitive to anticholinergic effects (e.g., dry mouth, nose, throat).
INTERACTIONS
DRUG: Clarithromycin, erythromycin, fluconazole, ketoconazole may increase concentration. HERBAL: St. John’s wort may decrease concentration/effects. FOOD: All foods delay absorption. LAB VALUES: May suppress wheal, flare reactions to antigen skin testing unless drug is discontinued 4 days before testing.
AVAILABILITY (Rx)
Capsule: 5 mg. Solution, Oral: 5 mg/5 ml. Syrup: 5 mg/5 ml. Tablets (Alavert, Claritin, Loradamed): 10 mg. Tablets, Chewable (Claritin): 5 mg. Tablets (Orally Disintegrating [Alavert]): 5 mg, 10 mg.
ADMINISTRATION/HANDLING
PO
• May take without regard for food.
Orally Disintegrating Tablets
• Place under tongue. • Disintegration occurs within seconds, after which tablet contents may be swallowed with or without water.
INDICATIONS/ROUTES/DOSAGE
Allergic Rhinitis, Urticaria
PO: ADULTS, ELDERLY, CHILDREN 6 YRS AND OLDER: 10 mg once daily or 5 mg twice daily (Claritin Reditabs). CHILDREN 2–5 YRS: 5 mg once daily.
Dosage in Renal Impairment (CrCl Less Than 30 ml/min)
PO: ADULTS, ELDERLY, CHILDREN 6 YRS AND OLDER: 10 mg every other day. CHILDREN 2–5 YRS: No dose adjustment.
Dosage in Hepatic Impairment
No dose adjustment.
SIDE EFFECTS
Frequent (12%–8%): Headache, fatigue, drowsiness. Occasional (3%): Dry mouth, nose, throat. Rare: Photosensitivity.
ADVERSE EFFECTS/TOXIC REACTIONS
None significant.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Assess lung sounds for wheezing, skin for urticaria, other allergy symptoms.
INTERVENTION/EVALUATION
For upper respiratory allergies, increase fluids to decrease viscosity of secretions, offset thirst, replenish loss of fluids from increased diaphoresis. Monitor symptoms for therapeutic response.
PATIENT/FAMILY TEACHING
• Drink plenty of water (may cause dry mouth). • Avoid alcohol. • Avoid tasks that require alertness, motor skills until response to drug is established (may cause drowsiness). • May cause photosensitivity reactions (avoid direct exposure to sunlight).
*LORazepam
lor-az-e-pam
(Apo-Lorazepam
, Ativan, Lorazepam Intensol, Novo-Lorazem
)
Do not confuse Ativan with Ambien or Atarax, or lorazepam with alprazolam, diazepam, Lovaza, temazepam, or Zolpidem.
♦ CLASSIFICATION
PHARMACOTHERAPEUTIC: Benzodiazepine (Schedule IV). CLINICAL: Antianxiety, sedative-hypnotic, antiemetic, skeletal muscle relaxant, amnesiac, anticonvulsant, antitremor.
USES
PO: Management of anxiety disorders, short-term relief of symptoms of anxiety, anxiety associated with depressive symptoms. Insomnia due to anxiety or transient stress. IV: Status epilepticus, preanesthesia for amnesia, sedation. OFF-LABEL: Treatment of alcohol withdrawal, psychogenic catatonia, partial complex seizures, agitation (IV administration only), antiemetic for chemotherapy; rapid tranquilization of agitated pt, status epilepticus in children.
PRECAUTIONS
Contraindications: Hypersensitivity to lorazepam, other benzodiazepines. Acute narrow-angle glaucoma, IV administration in pts with sleep apnea, severe respiratory depression (except during mechanical ventilation). Cautions: Neonates, renal/hepatic impairment, compromised pulmonary function, concomitant CNS depressant use, depression, history of drug dependence, alcohol abuse, or significant personality disorder, pts at risk for suicide.
ACTION
Enhances action of inhibitory neurotransmitter gamma-aminobutyric acid (GABA) in CNS, affecting memory, motor, sensory, cognitive function. Therapeutic Effect: Produces anxiolytic, anticonvulsant, sedative, muscle relaxant, antiemetic effects.
PHARMACOKINETICS
| Route | Onset | Peak | Duration |
| PO | 30–60 min | N/A | 6–8 hrs |
| IV | 5–20 min | N/A | 6–8 hrs |
| IM | 20–30 min | N/A | 6–8 hrs |
Well absorbed after PO, IM administration. Protein binding: 85%. Widely distributed. Metabolized in liver. Primarily excreted in urine. Not removed by hemodialysis. Half-life: 10–20 hrs.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: May cross placenta. May be distributed in breast milk. May increase risk of fetal abnormalities if administered during first trimester of pregnancy. Chronic ingestion during pregnancy may produce fetal toxicity, withdrawal symptoms, CNS depression in neonates. Children: Safety and efficacy not established in pts younger than 12 yrs. Elderly: Use small initial doses with gradual increases to avoid ataxia, excessive sedation, or paradoxical CNS restlessness, excitement.