H

H2 Antagonists


H2 ANTAGONISTS

NameAvailabilityDosage RangeSide Effects
Cimetidine (Tagamet)

T: 200 mg, 300 mg, 400 mg, 800 mg

L: 300 mg/5 ml

Treatment of DU: 800 mg at bedtime, 400 mg 2 times/day or 300 mg 4 times/day

Maintenance of DU: 400 mg at bedtime

Treatment of GU: 800 mg at bedtime or 300 mg 4 times/day

GERD: 400 mg 4 times/day or 800 mg 2 times/day

Hypersecretory: 300 mg 4 times/day.

Maximum: 2,400 mg/day

Headaches, fatigue, dizziness, confusion, diarrhea, gynecomastia
Famotidine (Pepcid)

T: 10 mg, 20 mg, 40 mg

OS: 40 mg/5 ml

I: 10 mg/ml

Treatment of DU: 40 mg/day in 1 or 2 divided doses

Maintenance of DU: 20 mg/day

Treatment of GU: 40 mg/day at bedtime

GERD: 20 mg 2 times/day for 6 wks

Hypersecretory: Initially, 20 mg q6h. May increase up to 160 mg q6h

Headaches, dizziness, diarrhea, constipation, abdominal pain, tinnitus
Nizatidine (Axid)

OS: 15 mg/ml

C: 75 mg, 150 mg, 300 mg

Treatment of GU: 300 mg at hs or 150 mg 2 times/day

GERD: 150 mg 2 times/day

Treatment of DU: 300 mg at hs or 150 mg 2 times/day

Maintenance of DU: 150 mg/day at bedtime

Fatigue, urticaria, abdominal pain, constipation, nausea
Ranitidine (Zantac)

T: 75 mg, 150 mg, 300 mg

C: 150 mg, 300 mg

Syrup: 15 mg/ml

I: 25 mg/ml

Treatment of DU: 300 mg at hs or 150 mg 2 times/day

Maintenance of DU: 150 mg/day at bedtime

Treatment of GU: 150 mg 2 times/day

GERD: 150 mg 2 times/day

Hypersecretory: 150 mg 2 times/day. Maximum: 6 g/day

Erosive Esophagitis: Treatment: 150 mg 4 times/day. Maintenance: 150 mg 2 times/day

Blurred vision, constipation, nausea, abdominal pain

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C, Capsules; DT, disintegrating tablets; DU, duodenal ulcer; GERD, gastroesophageal reflux disease; GU, gastric ulcer; I, injection; L, liquid; OS, oral suspension; T, tablets.

Hepatitis C Virus


ANTI-HEPATITIS C VIRUS PREPARATIONS

NameTypeGenotypeDosageSide Effects
Elbasvir, grazoprevir (Zepatier)

DAA

NS5A/NS3/4A protease inhibitor

1, 4

Genotype 1a: One tablet daily for 12 wks (16 wks with baseline NS5A polymorphins)

Genotype 1b: One tablet daily for 12 wks

Genotype 4: One tablet daily for 12 wks (16 wks peginterferon/ribavirin experienced)

Fatigue, headache, nausea
Simeprevir (Olysio)

DAA

(NS3/4A-PI)

1, 4

150 mg once daily plus peginterferon and ribavirin for 12 wks, then additional 12–36 wks of peginterferon and ribavirin)

150 mg once daily plus sofosbuvir for 12 wks without cirrhosis or 24 wks with cirrhosis

(With peginterferon, ribavirin): rash, itching, nausea, photosensitivity

(With sofosbuvir): fatigue, headache, nausea, insomnia, pruritus, rash, dizziness, diarrhea

Sofosbuvir (Sovaldi)

DAA

(NS5B)

1, 2, 3, 4

Genotypes 1, 4:

400 mg once daily plus peginterferon and ribavirin for 12 wks

400 mg once daily plus simeprevir for 12 wks without cirrhosis or 24 wks with cirrhosis

Genotypes 2, 3:

400 mg once daily plus ribavirin for 12 wks for genotype 2 or 24 wks for genotype 3

(With peginterferon, ribavirin):Fatigue, headache, nausea, insomnia, anemia

(With simeprevir): fatigue, headache, nausea, insomnia, pruritus, rash, dizziness, diarrhea

Ledipasvir, Sofosbuvir (Harvoni)

DAA

(NS5A/NS5B)

1, 4, 5, 6

Genotype 1:

One tablet (90 mg/400 mg) for 12 wks in treatment-naïve pt with or without cirrhosis and treatment-experienced pt without cirrhosis; for 24 wks for treatment experienced pts with cirrhosis

Genotypes 4, 5, 6: One tablet daily for 12 wks

Fatigue, headache, nausea, diarrhea, insomnia; elevations in bilirubin, lipase, and creatinine kinase
Ombitasvir, Paritaprevir, Ritonavir, Dasabuvir (Viekira Pak)

DAA

(NS5A/protease inhibitor/CYP3A inhibitor/polymerase inhibitor)

1

Two ombitasvir, paritaprevir, ritonavir tablets (12.5 mg, 75 mg, 50 mg) once daily in the morning plus one dasabuvir 250 mg tablet 2 times/day

Patients with genotype 1a or 1b with cirrhosis will also receive ribavirin for 12 wks (genotype 1a with cirrhosis: 12–24 wks based on treatment history; liver transplant pts: 24 wks)

(With ribavirin): fatigue, nausea, itching, insomnia

(Without ribavirin): nausea, itching, insomnia

Peginterferon alfa 2a (Pegasys)

IAA

(Interferon)

1, 2, 3, 4180 mcg SQ wkly for 12–48 wks based on antiviral regimen, pt history, response(With ribavirin): fatigue, weakness, fever, myalgia, headache
Peginterferon alfa 2b (PegIntron)

IAA

(Interferon)

1, 2, 3, 41.5 mcg/kg SQ wkly for 12–48 wks based on antiviral regimen, pt history, response(With ribavirin): injection site reaction, fatigue, weakness, headache, rigors, fever, nausea, myalgia, insomnia, mood instability, hair loss
Ribavirin (Copegus, Ribasphere)

IAA

(Nucleoside analogue)

1, 2, 3, 4

Genotypes 2, 3

400 mg 2 times/day (with peginterferon)

Genotypes 1, 4

< 75 kg: 400 mg qam and 600 mg qpm

75kg or greater: 600 mg 2 times/day

(With peginterferon): fatigue, weakness, headache, rigors, fever, nausea, myalgia, insomnia, mood instability, hair loss
Daclatasvir (Daklinza)

DAA

(NS5A)

360 mg once daily with sofosbuvir for 12 wksHeadache, fatigue
Ombitasvir, paritaprevir, ritonavir (Technivie)

DAA

(NS5A/protease Inhibitor/CYP3A inhibitor)

4Two tablets once daily with ribavirin for 12 wksAsthenia, fatigue, nausea, insomnia
Sofosbuvir/velpatasvir (Epclusa)

DAA

(NS5B/NS5A)

1, 2, 3, 4, 5, 6One tablet daily for 12 wksInsomnia, anemia, headache, fatigue, nausea, diarrhea

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Hormones


USES

Functions of the body are regulated by two major control systems: the nervous system and the endocrine (hormone) system. Together they maintain homeostasis and control different metabolic functions in the body.

Hormones are concerned with control of different metabolic functions in the body (e.g., rates of chemical reactions in cells, transporting substances through cell membranes, cellular metabolism [growth/secretions]). By definition, a hormone is a chemical substance secreted into body fluids by cells and has control over other cells in the body.

Hormones can be local or general:

Some general hormones affect all or almost all cells of the body (e.g., thyroid hormone from the thyroid gland increases the rate of most chemical reactions in almost all cells of the body); other general hormones affect only specific tissue (e.g., ovarian hormones are specific to female sex organs and secondary sexual characteristics of the female).

ACTION

Endocrine hormones almost never directly act intracellularly affecting chemical reactions. They first combine with hormone receptors either on the cell surface or inside the cell (cell cytoplasm or nucleus). The combination of hormone and receptors alters the function of the receptor, and the receptor is the direct cause of the hormone effects. Altered receptor function may include the following:

◀ ALERT ▶ cAMP has effects inside the cell. It is not the hormone but cAMP that causes these effects.

Regulation of hormone secretion is controlled by an internal control system, the negative feedback system:

The endocrine system contains many glands and hormones. A summary of the important glands and their hormones secreted are as follows:

The pituitary gland (hypophysis) is a small gland found in the sella turcica at the base of the brain. The pituitary is divided into two portions physiologically: the anterior pituitary (adenohypophysis) and the posterior pituitary (neurohypophysis). Six important hormones are secreted from the anterior pituitary and two from the posterior pituitary.

Anterior pituitary hormones:

Posterior pituitary hormones:

Almost all secretions of the pituitary hormones are controlled by hormonal or nervous signals from the hypothalamus. The hypothalamus is a center of information concerned with the well-being of the body, which in turn is used to control secretions of the important pituitary hormones just listed. Secretions from the posterior pituitary are controlled by nerve signals originating in the hypothalamus; anterior pituitary hormones are controlled by hormones secreted within the hypothalamus. These hormones are as follows:

Anterior Pituitary Hormones

All anterior pituitary hormones (except growth hormone) have as their principal effect stimulating target glands.

Growth Hormone (GH)

Growth hormone affects almost all tissues of the body. GH (somatopropin) causes growth in almost all tissues of the body (increases cell size, increases mitosis with increased number of cells, and differentiates certain types of cells). Metabolic effects include increased rate of protein synthesis, mobilization of fatty acids from adipose tissue, decreased rate of glucose utilization.

Thyroid-Stimulating Hormone (TSH)

Thyroid-stimulating hormone controls secretion of the thyroid hormones. The thyroid gland is located immediately below the larynx on either side of and anterior to the trachea and secretes two significant hormones, thyroxine (T4) and triiodothyroxine (T3), which have a profound effect on increasing the metabolic rate of the body. The thyroid gland also secretes calcitonin, an important hormone for calcium metabolism. Calcitonin promotes deposition of calcium in the bones, which decreases calcium concentration in the extracellular fluid.

Adrenocorticotropin

Adrenocorticotropin causes the adrenal cortex to secrete adrenocortical hormones. The adrenal glands lie at the superior poles of the two kidneys. Each gland is composed of two distinct parts: the adrenal medulla and the cortex. The adrenal medulla, related to the sympathetic nervous system, secretes the hormones epinephrine and norepinephrine. When stimulated, they cause constriction of blood vessels, increased activity of the heart, inhibitory effects on the GI tract, and dilation of the pupils. The adrenal cortex secretes corticosteroids, of which there are two major types: mineralocorticoids and glucocorticoids. Aldosterone, the principal mineralocorticoid, primarily affects electrolytes of the extracellular fluids. Cortisol, the principal glucocorticoid, affects glucose, protein, and fat metabolism.

Luteinizing Hormone (LH)

Luteinizing hormone plays an important role in ovulation and causes secretion of female sex hormones by the ovaries and testosterone by the testes.

Follicle-Stimulating Hormone (FSH)

Follicle-stimulating hormone causes growth of follicles in the ovaries before ovulation and promotes formation of sperm in the testes.

Ovarian sex hormones are estrogens and progestins. Estradiol is the most important estrogen; progesterone is the most important progestin.

Estrogens mainly promote proliferation and growth of specific cells in the body and are responsible for development of most of the secondary sex characteristics. Primarily cause cellular proliferation and growth of tissues of sex organs/other tissue related to reproduction. Ovaries, fallopian tubes, uterus, vagina increase in size. Estrogen initiates growth of breast and milk-producing apparatus, external appearance.

Progesterone stimulates secretion of the uterine endometrium during the latter half of the female sexual cycle, preparing the uterus for implantation of the fertilized ovum. Decreases the frequency of uterine contractions (helps prevent expulsion of the implanted ovum). Progesterone promotes development of breasts, causing alveolar cells to proliferate, enlarge, and become secretory in nature.

Testosterone is secreted by the testes and formed by the interstitial cells of Leydig. Testosterone production increases under the stimulus of the anterior pituitary gonadotropic hormones. It is responsible for distinguishing characteristics of the masculine body (stimulates the growth of male sex organs and promotes the development of male secondary sex characteristics, e.g., distribution of body hair, effect on voice, protein formation, and muscular development).

Prolactin

Prolactin promotes the development of breasts and secretion of milk.

POSTERIOR PITUITARY HORMONES

Antidiuretic Hormone (ADH) (Vasopressin)

ADH can cause antidiuresis (decreased excretion of water by the kidneys). In the presence of ADH, the permeability of the renal-collecting ducts and tubules to water increases, which allows water to be absorbed, conserving water in the body. ADH in higher concentrations is a very potent vasoconstrictor, constricting arterioles everywhere in the body, increasing B/P.

Oxytocin

Oxytocin contracts the uterus during the birthing process, esp. toward the end of the pregnancy, helping expel the baby. Oxytocin also contracts myoepithelial cells in the breasts, causing milk to be expressed from the alveoli into the ducts so that the baby can obtain it by suckling.

PANCREAS

The pancreas is composed of two tissue types: acini (secrete digestive juices in the duodenum) and islets of Langerhans (secrete insulin/glucagons directly into the blood). The islets of Langerhans contain three cells: alpha, beta, and delta. Alpha cells secrete glucagon, beta cells secrete insulin, and delta cells secrete somatostatin.

Insulin promotes glucose entry into most cells, thus controlling the rate of metabolism of most carbohydrates. Insulin also affects fat metabolism.

Glucagon effects are opposite those of insulin, the most important of which is increasing blood glucose concentration by releasing it from the liver into the circulating body fluids.

Somatostatin (same chemical as secreted by the hypothalamus) has multiple inhibitory effects: depresses secretion of insulin and glucagon, decreases GI motility, decreases secretions/absorption of the GI tract.

Human Immunodeficiency Virus (HIV) Infection


ANTIRETROVIRAL AGENTS FOR TREATMENT OF HIV INFECTION

NameAvailabilityDosage RangeSide Effects
Nucleoside Analogues
Abacavir (Ziagen)

T: 300 mg

OS: 20 mg/ml

A: 300 mg 2 times/day or 600 mg once dailyNausea, vomiting, malaise, rash, fever, headaches, asthenia, fatigue, hypersensitivity reactions
Didanosine (Videx EC)

DR: 125 mg, 200 mg, 250 mg, 400 mg

OS: 2 g/bottle, 4 g/bottle

DR (weighing 60 kg or more): 400 mg once daily; (weighing 25–59 kg): 250 mg once daily; (weighing 20–24 kg): 200 mg once daily

OS (weighing more than 60 kg): 200 mg q12h or 400 mg once daily; (weighing less than 60 kg): 125 mg q12h or 250 mg once daily

Peripheral neuropathy, pancreatitis, diarrhea, nausea, vomiting, headaches, insomnia, rash, hepatitis, seizures
Emtricitabine (Emtriva)

C: 200 mg

OS: 10 mg/ml

A: 200 mg/day (C)

240 mg/day (OS)

Headaches, insomnia, depression, diarrhea, nausea, vomiting, rhinitis, asthenia, rash
Lamivudine (Epivir)

T: 100 mg, 150 mg, 300 mg

OS: 5 mg/ml, 10 mg/ml

A: 150 mg 2 times/day or 300 mg once daily

C: 4 mg/kg 2 times/day

Diarrhea, malaise, fatigue, headaches, nausea, vomiting, abdominal pain, peripheral neuropathy, arthralgia, myalgia, skin rash
Stavudine (Zerit)

C: 15 mg, 20 mg, 30 mg, 40 mg

OS: 1 mg/ml

A (weighing more than 60 kg): 40 mg 2 times/day (20 mg 2 times/day if peripheral neuropathy occurs); (weighing 60 kg or less): 30 mg 2 times/day (15 mg 2 times/day if peripheral neuropathy occurs)Peripheral neuropathy, anemia, leukopenia, neutropenia
Zidovudine (Retrovir)

C: 100 mg

T: 300 mg

Syrup: 50 mg/5 ml, 10 mg/ml

A: 300 mg 2 times/dayAnemia, granulocytopenia, myopathy, nausea, malaise, fatigue, insomnia
Nucleotide Analogues
Tenofovir TAF (Vemlidy)T: 25 mgA: 25 mg once dailyHeadache, abdominal pain, fatigue, cough, nausea, back pain
Tenofovir TDF (Viread)T: 300 mgA: 300 mg once dailyNausea, vomiting, diarrhea, headache, fatigue
Non-nucleoside Analogues
Delavirdine (Rescriptor)T: 100 mg, 200 mgA: 200 mg 3 times/day for 14 days, then 400 mg 3 times/dayRash, nausea, headaches, elevated hepatic function tests
Efavirenz (Sustiva)

C: 50 mg, 200 mg

T: 600 mg

A: 600 mg/day

C: 200–600 mg/day based on weight

Headaches, dizziness, insomnia, fatigue, rash, nightmares
Etravirine (Intelence)T: 100 mg, 200 mgA: 200 mg 2 times/daySkin reactions (e.g., Stevens-Johnson syndrome, erythema multiforme), nausea, abdominal pain, vomiting
Nevirapine (Viramune, Viramune XR)

T: 200 mg

T (ER): 400 mg

S: 50 mg/ml

A: 200 mg/day for 14 days, then (if no rash) 200 mg 2 times/dayRash, nausea, fatigue, fever, headaches, abnormal hepatic function tests
Rilpivirine (Edurant)T: 25 mgA: 25 mg once daily with a mealDepression, insomnia, headache, rash
Protease Inhibitors
Atazanavir (Reyataz)C: 100 mg, 150 mg, 200 mg, 300 mgA: 400 mg/day or 300 mg (with 100 mg ritonavir) once dailyHeadaches, diarrhea, abdominal pain, nausea, rash
Darunavir (Prezista)T: 400 mg, 600 mgA: 600 mg 2 times/day (with ritonavir 100 mg) or 800 mg once daily with ritonavir 100 mgDiarrhea, nausea, vomiting, headaches, skin rash, constipation
Fosamprenavir (Lexiva)

T: 700 mg

OS: 50 mg/ml

A: 1,400–2,800 mg/day with 100 mg ritonavirHeadaches, fatigue, rash, nausea, diarrhea, vomiting, abdominal pain
Indinavir (Crixivan)C: 200 mg, 400 mgA: 800 mg q8h or 800 mg 2 times/day with ritonavir 100 mgNephrolithiasis, hyperbilirubinemia, abdominal pain, asthenia, fatigue, flank pain, nausea, vomiting, diarrhea, headaches, insomnia, dizziness, altered taste
Lopinavir/ritonavir (Kaletra)

C: 133/33 mg

OS: 80/20 mg

A: 400 mg/100 mg 2 times/day or 800 mg/200 mg once daily

C (4–12 yrs): 10–13 mg/kg 2 times/day

Diarrhea, nausea, vomiting, abdominal pain, headaches, rash
Nelfinavir (Viracept)

T: 250 mg

Oral Powder: 50 mg/g

A: 750 mg q8h or 1,250 mg 2 times/day

C: 20–25 mg/kg q8h

Diarrhea, fatigue, asthenia, headaches, hypertension, impaired concentration
Ritonavir (Norvir)

C: 100 mg

OS: 80 mg/ml

A: Titrate up to 800 mg/day based on protease inhibitorNausea, vomiting, diarrhea, altered taste, fatigue, elevated LFT and triglyceride levels
Saquinavir (Invirase)

C: 200 mg

T: 500 mg

A: 1,000 mg 2 times/day with ritonavir 100 mgDiarrhea, elevated LFTs, hypertriglycerides, cholesterol, abnormal fat accumulation, hyperglycemia
Tipranavir (Aptivus)

C: 250 mg

OS: 100 mg/ml

A: 500 mg (with 200 mg ritonavir) 2 times/dayDiarrhea, nausea, fatigue, headaches, vomiting
Fusion Inhibitors
Enfuvirtide (Fuzeon)I: 108 mg (90 mg when reconstituted)Subcutaneous: 90 mg 2 times/dayInsomnia, depression, peripheral neuropathy, decreased appetite, constipation, asthenia, cough
CCR5 Antagonists
Maraviroc (Selzentry)T: 150 mg, 300 mg

A: 300 mg 2 times/day

CYP3A4 inducers: 600 mg 2 times/day

CYP3A4 inhibitors: 150 mg 2 times/day

Cough, pyrexia, upper respiratory tract infections, rash, musculoskeletal symptoms, abdominal pain, dizziness
Integrase Inhibitor
Raltegravir (Isentress)T: 400 mgA: 400 mg 2 times/dayNausea, headache, diarrhea, pyrexia
Dolutegravir (Tivicay)T: 50 mgA: 50 mg once daily or 50 mg bid (with CYP3A inducers or resistance)Insomnia, headache

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A, Adults; C, capsules; C (dosage), children; DR, delayed-release; ER, extended-release; I, injection; OS, oral solution; S, suspension; T, tablets; TAF, tenofovir alafenamide; TDF, tenofovir disoproxil fumarate.

FIXED-COMBINATION THERAPIES