O

Obesity Management

USES

Adjunct to diet and physical activity in the treatment of chronic, relapsing obesity.

ACTIONS

Two categories of medications are used for weight control.

Appetite suppressants: Block neuronal uptake of norepinephrine, serotonin, dopamine, causing a feeling of fullness or satiety.

Digestion inhibitors: Reversible lipase inhibitors that block the breakdown and absorption of fats, decreasing appetite and reducing calorie intake.

ANOREXIANTS

Name	Availability	Dosage	Side Effects
Diethylpropion (Tenuate, Tenuate Dospan)	T: 25 mg, T (CR): 75 mg	25 mg 3–4 times/day or 75 mg once daily in midmorning	Headaches, euphoria, palpitations, hypertension, pulmonary hypertension, valvular heart disease, seizures, bone marrow depression, dependence, withdrawal psychosis
Liraglutide (Victoza)	I: 18 mg/3 ml	SQ: Initially, 0.6 mg/day. May increase by 0.6 mg/day weekly up to 3 mg/day	Diarrhea, constipation, dyspepsia, fatigue, vomiting, increased heart rate, renal impairment
Lorcaserin (BelViq, Belviq XR)	C: 10 mg T: 20 mg	(Belviq) 10 mg 2 times/day (Belviq XR): 20 mg once daily	Nausea, headache, dizziness, fatigue, dry mouth, diarrhea, constipation, hypoglycemia, hallucinations, decreased white/red blood cells, euphoria, cognitive impairment
Naltrexone/bupropion (Contrave)	T: 8 mg/90 mg	Titrate weekly up to 2 tablets 2 times/day (1 tablet once daily, then 1 tablet 2 times/day, then 2 tablets in am and 1 in pm, then 2 tablets 2 times/day)	Suicidal ideation, mood changes, seizures, increased HR with or without B/P, allergic reactions, hepatic toxicity, nausea, vomiting, headache, dizziness, dry mouth, angle closure glaucoma
Orlistat (Alli, Xenical)	C: 60 mg, 120 mg	Alli: 60 mg up to tid with meals Xenical: 120 mg tid with each meal containing fat	Flatulence, rectal incontinence, oily stools, cholelithiasis, abdominal/rectal pain, hepatitis, pancreatitis, nausea
Phenteramine (Apidex-P, Suprenza)	C: 15 mg, 30 mg, 37.5 mg T: 37.5 mg T (ODT): 15 mg, 30 mg, 37.5 mg	15–37.5 mg/day in 1 or 2 divided doses ODT: 15–37.5 mg once daily in morning	Headaches, euphoria, palpitations, hypertension, pulmonary hypertension, valvular heart disease, tremor, dependence, withdrawal psychosis, CNS stimulation, GI complaints
Phenteramine/topiramate (Qsymia)	C: 13.75 mg/23 mg	3.75 mg/23 mg to 15 mg/92 mg once daily in the morning	Paresthesia, dizziness, insomnia, depression, tachycardia, cognitive impairment, angle-closure glaucoma, hypokalemia, metabolic acidosis, constipation, dry mouth, suicidal ideation, kidney stones

AS, Appetite suppressant; B/P, blood pressure; C, capsules; CNS, central nervous system; CR, controlled-release; DI, digestion inhibitor; GI, gastrointestinal; HR, heart rate; I, injection; ODT, orally disintegrating tablets; SQ, subcutaneously; T, tablets.

Osteoporosis

HISTORY

Osteoporosis is a bone disease that can lead to fractures. Bone mineral density (BMD) is reduced, bone micro-architecture is disrupted, and the amount and variety of proteins in bone are altered. Osteoporosis primarily affects women after menopause (postmenopausal osteoporosis) but may develop in men, in anyone in the presence of particular hormonal disorders (e.g., parathyroid glands), after overconsumption of dietary proteins, or as a result of medications (e.g., glucocorticoids). Several pharmacologic options, along with lifestyle changes, that can be used to prevent and/or treat osteoporotic fractures include bisphosphonates, selective estrogen receptor modulator (SERM), parathyroid hormone (PTH), calcitonin, and monoclonal antibodies.

ACTION

Bisphosphonates: Inhibit bone resorption via actions on osteoclasts or osteoclast precursors, decrease rate of bone resorption, leading to an indirect increase in BMD.

Selective estrogen receptor modulator (SERM): Decreases bone resorption, increasing BMD and decreasing the incidence of fractures.

Parathyroid hormone: Stimulates osteoblast function, increasing gastrointestinal calcium absorption and increasing renal tubular reabsorption of calcium. This increases BMD, bone mass, and strength, resulting in a decrease in osteoporosis-related fractures.

Calcitonin: Inhibitor of bone resorption. Efficacy not observed in early postmenopausal women and is used only in women with osteoporosis who are at least 5 yrs beyond menopause.

Monoclonal antibody: Inhibits the RANK ligand (RANKL), a cytokine member of the tumor necrosis factor family. This inhibits osteoclast formation, function, and survival, which decreases bone resorption and increases bone mass and strength in cortical and trabecular bone.

BISPHOSPHONATES

Name	Availability	Dosage	Side Effects
Alendronate (Binosto, Fosamax)	T: 5 mg, 10 mg, 35 mg, 40 mg, 70 mg S: 70 mg/75ml	Prevention: 5 mg/day or 35 mg/wk Treatment: 10 mg/day or 70 mg/wk	Transient, mild hypocalcemia, hypophosphatemia, dysphagia, esophagitis, esophageal and gastric ulcer, abdominal pain, diarrhea, musculoskeletal pain
Ibandronate (Boniva)	T: 150 mg I: 1 mg/ml	Prevention and treatment: 150 mg/mo IV Injection: Treatment: 3 mg/3 mos	Dyspepsia, back pain, dysphagia, esophagitis, esophageal and gastric ulcer, abdominal pain, diarrhea, musculoskeletal pain
Risedronate (Actonel)	T: 5 mg, 30 mg, 35 mg, 150 mg T (DR): 35 mg	Prevention and treatment: 5 mg/day, 35 mg/wk, or 150 mg/mo	Hypertension, headache, rash, dysphagia, esophagitis, esophageal and gastric ulcer, abdominal pain, diarrhea, musculoskeletal pain
Zoledronic acid (Reclast)	I: 5 mg	Prevention: IV: 5 mg every 2 yrs Treatment: IV: 5 mg every yr	Hypertension, pain, fever, headache, chills, fatigue, nausea, musculoskeletal pain

SERM

Name	Availability	Dosage	Side Effects
Raloxifene (Evista)	T: 60 mg	Prevention and treatment: 60 mg/day	Peripheral edema, hot flashes, arthralgia, leg cramps, muscle spasms, flu syndrome, infection

PARATHYROID HORMONE

Name	Availability	Dosage	Side Effects
Teriparatide (Forteo)	I: 250 mcg/ml syringe delivers 20 mcg/dose	Treatment: 20 mcg subcutaneously once daily	Hypercalcemia, muscle cramps, nausea, dizziness, headache

CALCITONIN

Name	Availability	Dosage	Side Effects
Calcitonin (Fortical, Miacalcin)	I (Miacalcin): 200 units/ml Nasal (Fortical, Miacalcin): 200 units/activation	Treatment: IM/Subcutaneous (Miacalcin): 100 units every other day Nasal: 200 units in 1 nostril daily	Rhinitis, local nasal irritation. Injection: nausea, local inflammation, flushing of face, hands

MONOCLONAL ANTIBODY RANKL INHIBITOR

Name	Availability	Dosage	Side Effects
Denosumab (Prolia)	I: 60 mg/ml	Subcutaneous: 60 mg once every 6 mos	Back pain, pain in extremity, hypercholesterolemia, musculoskeletal pain, cystitis

DR, Delayed-release; I, injection; S, solution (oral); T, tablet.