classification

PHARMACOTHERAPEUTIC: Proton pump inhibitor. CLINICAL: Gastric acid inhibitor (see p. 147C).

Action

Converts to active metabolites that irreversibly bind to, inhibit hydrogen-potassium adenosine triphosphate, an enzyme on surface of gastric parietal cells. Actively secretes hydrogen ions for potassium ions, resulting in accumulation of hydrogen ions in gastric lumen. Therapeutic Effect: Increases gastric pH, reducing gastric acid production.

Pharmacokinetics

Rapidly absorbed from GI tract after passing through stomach relatively intact as delayed-release tablet. Protein binding: 96%. Metabolized in liver. Primarily excreted in urine. Unknown if removed by hemodialysis. Half-life: 1–2 hrs (increased with hepatic impairment).

Uses

Short-term treatment (4–8 wks), maintenance of erosive or ulcerative gastroesophageal reflux disease (GERD). Treatment of daytime/nighttime heartburn, other symptoms of GERD. Short-term treatment (4 wks or less) in healing, symptomatic relief of duodenal ulcers. Long-term treatment of pathologic hypersecretory conditions, including Zollinger-Ellison syndrome. Treatment of H. pylori (in combination with other medication). Sprinkle dose form approved for treatment of GERD in children 1–11 yrs. OFF-LABEL: Maintenance of healing and prevention of relapse of duodenal ulcers. Treatment of NSAID-induced ulcers.

Precautions

Contraindications: Hypersensitivity to proton pump inhibitors (e.g., omeprazole). Cautions: Severe hepatic impairment. May increase risk of fractures, GI infections.

 ​Lifespan considerations

Pregnancy/Lactation: Unknown if drug crosses placenta or is distributed in breast milk. Pregnancy Category B. Children: Safety and efficacy not established. Elderly: No age-related precautions noted.

Interactions

DRUG: May increase concentration/effects of cyclosporine, warfarin. May decrease concentration of ketoconazole, clopidogrel, atazanavir. HERBAL: St. John’s wort may decrease concentration/effects. FOOD: None known. LAB VALUES: May increase serum AST, ALT, thyroid stimulating hormone (TSH).

Availability (Rx)

Tablets (Delayed-Release): 10 mg, 20 mg.

• May give without regard to meals; best taken before breakfast. • Do not crush, break, split tablet; give whole.

PO: ADULTS, ELDERLY: 20 mg/day for 4–8 wks. Maintenance: 20 mg/day.

Side effects

Rare (less than 2%): Headache, nausea, dizziness, rash, diarrhea, malaise.

Adverse effects/toxic reactions

Hyperglycemia, hypokalemia, hyponatremia, hyperlipemia occur rarely.

Obtain baseline lab values, esp. serum chemistries.

classification

PHARMACOTHERAPEUTIC: Selective estrogen receptor modulator. CLINICAL: Osteoporosis preventive (see p. 143C).

Action

Selective estrogen receptor modulator that binds to estrogen receptors, increasing bone mineral density. Therapeutic Effect: Reduces bone resorption, decreases bone turnover, prevents bone loss.

Pharmacokinetics

Rapidly absorbed after PO administration. Protein binding: 95%. Metabolized in liver. Excreted mainly in feces and, to a lesser extent, in urine. Unknown if removed by hemodialysis. Half-life: 27.7–32.5 hrs.

Uses

Prevention/treatment of osteoporosis in postmenopausal women. Reduces risk of invasive breast cancer in postmenopausal women with osteoporosis and postmenopausal women at high risk for invasive breast cancer.

Precautions

Contraindications: Active or history of venous thromboembolic events, such as deep vein thrombosis (DVT), pulmonary embolism, retinal vein thrombosis; women who are or may become pregnant, or are breastfeeding. Cautions: Cardiovascular disease, renal/hepatic impairment, risk for venous thromboembolism, unexplained uterine bleeding, elevated triglycerides in response to oral estrogen therapy.

 ​Lifespan considerations

Pregnancy/Lactation: Unknown if distributed in breast milk. Not recommended for breastfeeding mothers. Pregnancy Category X. Children: Not used in this population. Elderly: No age-related precautions noted.

Interactions

DRUG: Cholestyramine reduces peak levels, extent of absorption. Do not use concurrently with hormone replacement therapy, systemic estrogen. May decrease effect of warfarin (decreases INR). HERBAL: None significant. FOOD: None known. LAB VALUES: May lower serum total cholesterol, LDL. May decrease platelet count, serum inorganic phosphate, albumin, calcium, protein.

Availability (Rx)

Tablets: 60 mg.

• Give without regard to meals.

PO: ADULTS, ELDERLY: 60 mg a day.

Side effects

Frequent (25%–10%): Hot flashes, flu-like symptoms, arthralgia, sinusitis. Occasional (9%–5%): Weight gain, nausea, myalgia, pharyngitis, cough, dyspepsia, leg cramps, rash, depression. Rare (4%–3%): Vaginitis, UTI, peripheral edema, flatulence, vomiting, fever, migraine, diaphoresis.

Adverse effects/toxic reactions

Pneumonia, gastroenteritis, chest pain, vaginal bleeding, breast pain occur rarely.

Question for possibility of pregnancy (Pregnancy Category X). Drug should be discontinued 72 hrs before and during prolonged immobilization (postop recovery, prolonged bed rest). Therapy may be resumed only after pt is fully ambulatory. Determine serum total, LDL cholesterol before therapy and routinely thereafter.

classification

PHARMACOTHERAPEUTIC: Integrase inhibitor. CLINICAL: Antiviral (see p. 70C, 121C).

Action

Inhibits activity of HIV-1 integrase, an enzyme required for viral replication. Therapeutic Effect: Prevents integration and replication of viral HIV-1.

Pharmacokinetics

Variably absorbed following PO administration. Protein binding: 83%. Metabolized in liver, primarily hepatic glucouronidation mediated by UGT1A1. Eliminated mainly in feces (51%), urine (32%). Half-life: 9 hrs.

Uses

Treatment of HIV-1 infection in adults and children 2 yrs and older and weighing at least 10 kg. Used in combination with at least two other antiretroviral agents.

Precautions

Contraindications: None known. Cautions: Elderly, pts at increased risk for myopathy, rhabdomyolysis, medications that induce (e.g., rifampin) or inhibit (e.g., atazanavir) UGT1A1 glucouronidation.

 ​Lifespan considerations

Pregnancy/Lactation: May cross placenta. Breastfeeding not recommended. Pregnancy Category C. Children: Safety and efficacy not established in those younger than 16 yrs. Elderly: Age-related hepatic, renal, cardiac impairment requires strict monitoring.

Interactions

DRUG: Proton pump inhibitors may increase concentration. HERBAL: St. John’s wort may decrease concentration/effects. FOOD: None known. LAB VALUES: May increase serum glucose, bilirubin, aminotransferase, alkaline phosphatase, amylase, lipase, creatine kinase. May decrease lymphocytes/neutrophil count (ANC), Hgb, platelets.

Availability (Rx)

Tablets, Chewable: 25 mg, 100 mg.

Tablets, Film-Coated: 400 mg.

• Give without regard to food. • Do not break, crush, or divide film-coated tablets. • Chewable tablets may be chewed or taken whole.

PO: ADULTS, ELDERLY, CHILDREN 12 YRS AND OLDER: 400 mg twice a day. Dosage increased to 800 mg twice a day when given with rifampin. CHILDREN 2–11 YRS (CHEWABLE TABLETS): 40 KG OR GREATER: 300 mg twice daily. 28–39 KG: 200 mg twice daily. 20–27 KG: 150 mg twice daily. 14–19 KG: 100 mg twice daily. 10–13 KG: 75 mg twice daily. Note: Children 6–11 yrs and greater than 25 kg may use adult dosing.

Side effects

Frequent (17%–10%): Diarrhea, nausea, headache. Occasional (5%): Fever. Rare (2%–1%): Vomiting, abdominal pain, fatigue, dizziness.

Adverse effects/toxic reactions

Hypersensitivity, anemia, neutropenia, MI, gastritis, hepatitis, herpes simplex, toxic nephropathy, renal failure, chronic renal failure, renal tubular necrosis occur rarely.

Obtain baseline laboratory testing before beginning therapy and at periodic intervals during therapy. Offer emotional support. Obtain medication history.

classification

PHARMACOTHERAPEUTIC: Melatonin receptor agonist. CLINICAL: Hypnotic (see p. 149C).

Action

Selectively targets melatonin receptors thought to be involved in maintenance of circadian rhythm underlying normal sleep-wake cycle. Therapeutic Effect: Prevents insomnia characterized by difficulty with sleep onset.

Pharmacokinetics

Rapidly absorbed following PO administration. Protein binding: 82%. Substantial tissue distribution. Metabolized in liver. Excreted in urine (84%), feces (4%). Half-life: 2–5 hrs.

Uses

Treatment of insomnia in pts who experience difficulty with sleep onset.

Precautions

Contraindications: Concurrent fluvoxamine therapy, history of angioedema with previous ramelteon therapy. Cautions: Clinical depression, other psychiatric conditions, alcohol consumption, other CNS depressants, moderate to severe hepatic impairment, severe sleep apnea, COPD.

 ​Lifespan considerations

Pregnancy/Lactation: Unknown if distributed in breast milk. Breastfeeding not recommended. Pregnancy Category C. Children: Safety and efficacy not established. Elderly: Age-related hepatic impairment may require dosage adjustment.

Interactions

DRUG: Concurrent use with alcohol may produce additive effect. Fluconazole, ketoconazole may increase serum concentration/effects. Donepezil, doxepin, fluvoxamine may cause marked increase in serum level, toxicity. Rifampin may decrease serum level, effects. HERBAL: Gotu kola, kava kava, St. John’s wort, valerian may increase CNS depression. FOOD: Onset of action may be reduced if taken with or immediately after a high-fat meal. LAB VALUES: May decrease serum cortisol.

Availability (Rx)

Tablets, Film-Coated: 8 mg (Rozerem).

• Administer within 30 min before bedtime. • Do not give with, or immediately following, a high-fat meal. • Do not break, crush, dissolve, or divide tablet.

PO: ADULTS, ELDERLY: 8 mg 30 min before bedtime.

Side effects

Frequent (7%–5%): Headache, dizziness, drowsiness (expected effect). Occasional (4%–3%): Fatigue, nausea, exacerbated insomnia. Rare (2%): Diarrhea, myalgia, depression, altered taste, arthralgia.

Adverse effects/toxic reactions

May affect reproductive hormones in adults (decreased testosterone levels, increased prolactin levels), resulting in unexplained amenorrhea, galactorrhea, decreased libido, impaired fertility.

Assess B/P, pulse, respirations. Raise bed rails, provide call light. Provide environment conducive to sleep (quiet environment, low/no lighting, TV off).

classification

PHARMACOTHERAPEUTIC: Renin-angiotensin system antagonist. CLINICAL: Antihypertensive (see pp. 10C, 61C).

Action

Suppresses renin-angiotensin-aldosterone system. Decreases plasma angiotensin II, increases plasma renin activity, decreases aldosterone secretion. Therapeutic Effect: Reduces peripheral arterial resistance, decreasing B/P.

Pharmacokinetics

Well absorbed from GI tract. Protein binding: 73%. Metabolized in liver. Primarily excreted in urine. Not removed by hemodialysis. Half-life: 5.1 hrs.

Uses

Treatment of hypertension. Used alone or in combination with other antihypertensives. Treatment of left ventricular dysfunction following MI. Reduce risk of heart attack, stroke in pts at increased risk for these events. OFF-LABEL: HF. Delay progression of nephropathy, reduce risks of cardiovascular events in hypertensive pts with type 1 or type 2 diabetes.

Precautions

Contraindications: Hypersensitivity to ACE inhibitors. History of ACE-inhibitor induced angioedema, concomitant use with aliskiren in pts with diabetes. Cautions: Renal impairment, collagen vascular disease, hyperkalemia, hypertrophic cardiomyopathy with outflow tract obstruction; unstented unilateral, bilateral renal artery stenosis; severe aortic stenosis; before, during, or immediately after major surgery.

 ​Lifespan considerations

Pregnancy/Lactation: Crosses placenta. Distributed in breast milk. May cause fetal or neonatal mortality or morbidity. Pregnancy Category C (D if used in second or third trimester). Children: Safety and efficacy not established. Elderly: May be more sensitive to hypotensive effects.

Interactions

DRUG: Alcohol, antihypertensives, diuretics may increase effects. May increase lithium concentration, risk of toxicity. NSAIDs may decrease effects. Potassium-sparing diuretics, potassium supplements may cause hyperkalemia. HERBAL: Black cohosh, periwinkle may increase antihypertensive effect. Ginseng, ginger, licorice, yohimbe may worsen hypertension. FOOD: None known. LAB VALUES: May increase BUN, serum alkaline phosphatase, bilirubin, creatinine, potassium, AST, ALT. May decrease serum sodium. May cause positive antinuclear antibody (ANA) titer.

Availability (Rx)

Capsules: 1.25 mg, 2.5 mg, 5 mg, 10 mg.

• Give without regard to food. • May mix with water, apple juice/sauce.

PO: ADULTS, ELDERLY: Initially, 2.5 mg/day. Maintenance: 2.5–20 mg/day as single dose or in 2 divided doses.

Side effects

Frequent (12%–5%): Cough, headache. Occasional (4%–2%): Dizziness, fatigue, nausea, asthenia (loss of strength, energy). Rare (less than 2%): Palpitations, insomnia, nervousness, malaise, abdominal pain, myalgia.

Adverse effects/toxic reactions

Excessive hypotension (“first-dose syncope”) may occur in pts with HF, severely salt or volume depleted. Angioedema, hyperkalemia occur rarely. Agranulocytosis, neutropenia may be noted in pts with collagen vascular disease (scleroderma, systemic lupus erythematosus), renal impairment. Nephrotic syndrome may be noted in those with history of renal disease.

Obtain B/P immediately before each dose, in addition to regular monitoring (be alert to fluctuations). If excessive reduction in B/P occurs, place pt in supine position with legs elevated. Renal function tests should be performed before beginning therapy. In pts with prior renal disease, urine test for protein (by dipstick method) should be made with first urine of day before beginning therapy and periodically thereafter. In pts with renal impairment, autoimmune disease, or taking drugs that affect leukocytes or immune response, CBC, differential count should be performed before beginning therapy and q2wks for 3 mos periodically thereafter.

classification

PHARMACOTHERAPEUTIC: Histamine H₂ receptor antagonist. CLINICAL: Antiulcer (see p. 111C).

Action

Inhibits histamine action at histamine 2 receptors of gastric parietal cells. Therapeutic Effect: Inhibits gastric acid secretion (fasting, nocturnal, when stimulated by food, caffeine, insulin). Reduces volume, hydrogen ion concentration of gastric juice.

Pharmacokinetics

Rapidly absorbed from GI tract. Protein binding: 15%. Widely distributed. Metabolized in liver. Primarily excreted in urine. Not removed by hemodialysis. Half-life: PO: 2.5 hrs; IV: 2–2.5 hrs (increased with renal impairment).

Uses

Short-term treatment of active duodenal ulcer. Prevention of duodenal ulcer recurrence. Treatment of active benign gastric ulcer, pathologic GI hypersecretory conditions, acute gastroesophageal reflux disease (GERD), including erosive esophagitis. Maintenance of healed erosive esophagitis. Part of regimen for H. pylori eradication to reduce risk of duodenal ulcer recurrence. OTC: Relieve heartburn, acid indigestion, sour stomach. OFF-LABEL: Prevention of aspiration pneumonia, treatment of recurrent postop ulcer, upper GI bleeding, prevention of acid aspiration pneumonitis during surgery, prevention of stress-induced ulcers.

Precautions

Contraindications: None known. Cautions: Renal/hepatic impairment, elderly, history of acute porphyria.

 ​Lifespan considerations

Pregnancy/Lactation: Unknown if drug crosses placenta or is distributed in breast milk. Pregnancy Category B. Children: No age-related precautions noted. Elderly: Confusion more likely with hepatic/renal impairment.

Interactions

DRUG: Magnesium or aluminum antacids may decrease absorption. May decrease absorption of atazanavir, itraconazole, ketoconazole. HERBAL: None significant. FOOD: None known. LAB VALUES: Interferes with skin tests using allergen extracts. May increase serum AST, ALT, gamma-glutamyl transpeptidase, creatinine.

Availability (Rx)

Capsules (Zantac): 150 mg, 300 mg. Injection Solution (Zantac): 25 mg/ml. Syrup (Zantac): 15 mg/ml. Tablets (Zantac): 75 mg, 150 mg, 300 mg. Tablet for Solution (Zantac EFFERdose): 25 mg.

Reconstitution • For IV push, dilute each 50 mg with 20 ml 0.9% NaCl, D₅W. • For intermittent IV infusion (piggyback), dilute each 50 mg with 0.9% NaCl, D₅W to a maximum concentration of 0.5 mg/ml. • For IV infusion, dilute with 0.9% NaCl, D₅W to a maximum concentration of 2.5 mg/ml.

Rate of Administration • Administer IV push over minimum of 5 min (prevents arrhythmias, hypotension). • Infuse IV piggyback over 15–20 min. • Infuse IV infusion over 24 hrs.

Storage • IV solutions appear clear, colorless to yellow (slight darkening does not affect potency). • IV infusion (piggyback) is stable for 48 hrs at room temperature (discard if discolored or precipitate forms).

IV incompatibility

Amphotericin B complex (Abelcet, AmBisome, Amphotec).

IV compatibilities

Dexmedetomidine (Precedex), diltiazem (Cardizem), dobutamine (Dobutrex), dopamine (Intropin), heparin, hydromorphone (Dilaudid), insulin, lidocaine, lorazepam (Ativan), morphine, norepinephrine (Levophed), potassium chloride, propofol (Diprivan).

PO: ADULTS, ELDERLY: (Treatment): 150 mg twice daily or 300 mg once daily. (Maintenance): 150 mg once daily at bedtime. CHILDREN 1 MO TO 16 YRS: (Treatment): 4–8 mg/kg/day in 2 divided doses. Maximum: 300 mg. (Maintenance): 2–4 mg/kg/day once daily. Maximum: 150 mg.

Side effects

Occasional (2%): Diarrhea. Rare (1%): Constipation, headache (may be severe).

Adverse effects/toxic reactions

Reversible hepatitis, blood dyscrasias occur rarely.

Obtain history of epigastric/abdominal pain. Obtain baseline hepatic/renal function tests.

Patient/family teaching

• Smoking decreases effectiveness of medication. • Do not take medicine within 1 hr of magnesium- or aluminum-containing antacids. • Transient burning/pruritus may occur with IV administration. • Report headache. • Avoid alcohol, aspirin.

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