U.S. BRAND NAMES — Alamag Plus [OTC]; Aldroxicon I [OTC]; Aldroxicon II [OTC]; Almacone Double Strength® [OTC]; Almacone® [OTC]; Gelusil® [OTC]; Maalox® Max [OTC]; Maalox® [OTC]; Mi-Acid Maximum Strength [OTC]; Mi-Acid [OTC]; Mintox Extra Strength [OTC]; Mintox Plus [OTC]; Mylanta® Liquid [OTC]; Mylanta® Maximum Strength Liquid [OTC]
PHARMACOLOGIC CATEGORY
Antacid
Antiflatulent
DOSING: ADULTS — Dyspepsia, abdominal bloating: Oral: 10-20 mL or 2-4 tablets 4-6 times/day between meals and at bedtime; may be used every hour for severe symptoms
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — Aluminum and/or magnesium may accumulate in renal impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Liquid: Aluminum hydroxide 200 mg, magnesium hydroxide 200 mg, and simethicone 20 mg per 5 mL (360 mL); aluminum hydroxide 400 mg, magnesium hydroxide 400 mg, and simethicone 40 mg per 5 mL (360 mL)
Aldroxicon I: Aluminum hydroxide 200 mg, magnesium hydroxide 200 mg, and simethicone 20 mg per 5 mL (30 mL)
Aldroxicon II: Aluminum hydroxide 400 mg, magnesium hydroxide 400 mg, and simethicone 40 mg per 5 mL (30 mL)
Almacone®: Aluminum hydroxide 200 mg, magnesium hydroxide 200 mg, and simethicone 20 mg per 5 mL (360 mL)
Almacone Double Strength®: Aluminum hydroxide 400 mg, magnesium hydroxide 400 mg, and simethicone 40 mg per 5 mL (360 mL)
Maalox®: Aluminum hydroxide 200 mg, magnesium hydroxide 200 mg, and simethicone 20 mg per 5 mL (360 mL, 770 mL) [lemon and mint flavors]
Maalox® Max: Aluminum hydroxide 400 mg, magnesium hydroxide 400 mg, and simethicone 40 mg per 5 mL (360 mL, 770 mL) [cherry, vanilla creme, and wild berry flavors]
Mi-Acid: Aluminum hydroxide 200 mg, magnesium hydroxide 200 mg, and simethicone 20 mg per 5 mL (360 mL)
Mi-Acid Maximum Strength: Aluminum hydroxide 400 mg, magnesium hydroxide 400 mg, and simethicone 40 mg per 5 mL (360 mL)
Mintox Extra Strength: Aluminum hydroxide 500 mg, magnesium hydroxide 450 mg, and simethicone 40 mg per 5 mL (360 mL) [lemon creme flavor]
Mylanta®: Aluminum hydroxide 200 mg, magnesium hydroxide 200 mg, and simethicone 20 mg per 5 mL (180 mL, 360 mL, 720 mL) [original, cherry, and mint flavors]
Mylanta® Maximum Strength: Aluminum hydroxide 400 mg, magnesium hydroxide 400 mg, and simethicone 40 mg per 5 mL (180 mL, 360 mL, 720 mL) [original, cherry, orange creme, and mint flavors]
Suspension (Alamag Plus): Aluminum hydroxide 225 mg, magnesium hydroxide 200 mg, and simethicone 25 mg per 5 mL (360 mL)
Tablet, chewable: Aluminum hydroxide 200 mg, magnesium hydroxide 200 mg, and simethicone 25 mg
Alamag Plus: Aluminum hydroxide 200 mg, magnesium hydroxide 200 mg, and simethicone 25 mg [cherry flavor]
Almacone®: Aluminum hydroxide 200 mg, magnesium hydroxide 200 mg, and simethicone 20 mg [peppermint flavor]
Gelusil®: Aluminum hydroxide 200 mg, magnesium hydroxide 200 mg, and simethicone 25 mg [peppermint flavor]
Mintox Plus: Aluminum hydroxide 200 mg, magnesium hydroxide 200 mg, and simethicone 25 mg
DOSAGE FORMS: CONCISE
Liquid: Aluminum hydroxide 200 mg, magnesium hydroxide 200 mg, and simethicone 20 mg per 5 mL; aluminum hydroxide 400 mg, magnesium hydroxide 400 mg, and simethicone 40 mg per 5 mL
Aldroxicon I [OTC], Almacone® [OTC], Maalox® [OTC], Mi-Acid [OTC], Mylanta® [OTC]: Aluminum hydroxide 200 mg, magnesium hydroxide 200 mg, and simethicone 20 mg per 5 mL
Aldroxicon II [OTC], Almacone Double Strength [OTC], Maalox® Max® [OTC], Mi-Acid Maximum Strength [OTC], Mylanta® Maximum Strength [OTC]: Aluminum hydroxide 400 mg, magnesium hydroxide 400 mg, and simethicone 40 mg per 5 mL
Mintox Extra Strength [OTC]: Aluminum hydroxide 500 mg, magnesium hydroxide 450 mg, and simethicone 40 mg per 5 mL
Suspension:
Alamag Plus [OTC]: Aluminum hydroxide 225 mg, magnesium hydroxide 200 mg, and simethicone 25 mg per 5 mL
Tablet, chewable: Aluminum hydroxide 200 mg, magnesium hydroxide 200 mg, and simethicone 25 mg
Alamag Plus [OTC], Gelusil® [OTC], Mintox Plus [OTC]: Aluminum hydroxide 200 mg, magnesium hydroxide 200 mg, and simethicone 25 mg
Almacone® [OTC]: Aluminum hydroxide 200 mg, magnesium hydroxide 200 mg, and simethicone 20 mg
GENERIC EQUIVALENT AVAILABLE — Yes
ADMINISTRATION — Administer 1-2 hours apart from oral drugs.
USE — Temporary relief of hyperacidity associated with gas; may also be used for indications associated with other antacids
ADVERSE REACTIONS SIGNIFICANT
>10%: Gastrointestinal: Chalky taste, stomach cramps, constipation, bowel motility decreased, fecal impaction, hemorrhoids
1% to 10%: Gastrointestinal: Nausea, vomiting, discoloration of feces (white speckles)
<1% (Limited to important or life-threatening): Dehydration or fluid restriction, hypomagnesemia, hypophosphatemia
DRUG INTERACTIONS — Decreased effect: Tetracyclines, digoxin, indomethacin, iron salts, isoniazid, allopurinol, benzodiazepines, corticosteroids, penicillamine, phenothiazines, ranitidine, ketoconazole, itraconazole
PREGNANCY RISK FACTOR — C (show table)
DIETARY CONSIDERATIONS — Should be taken 1-3 hours after meals.
PRICING — (data from drugstore.com)
Suspension (Mylanta)
200-200-20 mg/5 mL (355): $7.99
200-200-20 mg/5 mL (355): $7.99
200-200-20 mg/5 mL (710): $8.80
Suspension (Mylanta Double-Strength)
400-400-40 mg/5 mL (355): $7.99
400-400-40 mg/5 mL (710): $9.51
CANADIAN BRAND NAMES — Diovol Plus®; Gelusil®; Mylanta® Double Strength; Mylanta® Extra Strength; Mylanta® Regular Strength
INTERNATIONAL BRAND NAMES — Diovol Plus (CA); Gelusil (CA); Mylanta Double Strength (CA); Mylanta Extra Strength (CA); Mylanta Regular Strength (CA)
Saturday, April 26, 2008
Aluminum hydroxide and magnesium trisilicate
U.S. BRAND NAMES — Alenic Alka Tablet [OTC]; Gaviscon® Tablet [OTC]; Genaton Tablet [OTC]
PHARMACOLOGIC CATEGORY
Antacid
DOSING: ADULTS — Dyspepsia, gastric acidity: Oral: Chew 2-4 tablets 4 times/day or as directed by healthcare provider
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — Aluminum and/or magnesium may accumulate in renal impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, chewable: Aluminum hydroxide 80 mg and magnesium trisilicate 20 mg
Alenic Alka: Aluminum hydroxide 80 mg and magnesium trisilicate 20 mg [butterscotch flavor]
Gaviscon®: Aluminum hydroxide 80 mg and magnesium trisilicate 20 mg [contains sodium 0.8 mEq/tablet; butterscotch flavor]
Genaton: Aluminum hydroxide 80 mg and magnesium trisilicate 20 mg
DOSAGE FORMS: CONCISE
Tablet, chewable: Aluminum hydroxide 80 mg and magnesium trisilicate 20 mg
Alenic Alka [OTC], Gaviscon® [OTC], Genaton [OTC]: Aluminum hydroxide 80 mg and magnesium trisilicate 20 mg
GENERIC EQUIVALENT AVAILABLE — Yes
ADMINISTRATION — Tablets should be chewed and not swallowed whole.
USE — Temporary relief of hyperacidity
DRUG INTERACTIONS — Decreased effect: Tetracyclines, digoxin, indomethacin, iron salts, isoniazid, allopurinol, benzodiazepines, corticosteroids, penicillamine, phenothiazines, ranitidine, ketoconazole, itraconazole
PREGNANCY RISK FACTOR — C (show table)
DIETARY CONSIDERATIONS — Should be taken 1-3 hours after meals with water, milk, or juice. Gaviscon® chewable tablet contains sodium 0.8 mEq/tablet.
PHARMACOLOGIC CATEGORY
Antacid
DOSING: ADULTS — Dyspepsia, gastric acidity: Oral: Chew 2-4 tablets 4 times/day or as directed by healthcare provider
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — Aluminum and/or magnesium may accumulate in renal impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, chewable: Aluminum hydroxide 80 mg and magnesium trisilicate 20 mg
Alenic Alka: Aluminum hydroxide 80 mg and magnesium trisilicate 20 mg [butterscotch flavor]
Gaviscon®: Aluminum hydroxide 80 mg and magnesium trisilicate 20 mg [contains sodium 0.8 mEq/tablet; butterscotch flavor]
Genaton: Aluminum hydroxide 80 mg and magnesium trisilicate 20 mg
DOSAGE FORMS: CONCISE
Tablet, chewable: Aluminum hydroxide 80 mg and magnesium trisilicate 20 mg
Alenic Alka [OTC], Gaviscon® [OTC], Genaton [OTC]: Aluminum hydroxide 80 mg and magnesium trisilicate 20 mg
GENERIC EQUIVALENT AVAILABLE — Yes
ADMINISTRATION — Tablets should be chewed and not swallowed whole.
USE — Temporary relief of hyperacidity
DRUG INTERACTIONS — Decreased effect: Tetracyclines, digoxin, indomethacin, iron salts, isoniazid, allopurinol, benzodiazepines, corticosteroids, penicillamine, phenothiazines, ranitidine, ketoconazole, itraconazole
PREGNANCY RISK FACTOR — C (show table)
DIETARY CONSIDERATIONS — Should be taken 1-3 hours after meals with water, milk, or juice. Gaviscon® chewable tablet contains sodium 0.8 mEq/tablet.
Aluminum hydroxide and magnesium hydroxide
U.S. BRAND NAMES — Alamag [OTC]; Rulox No. 1 [DSC]; Rulox [OTC]
PHARMACOLOGIC CATEGORY
Antacid
DOSING: ADULTS — Dyspepsia: Oral: 5-10 mL 4-6 times/day, between meals and at bedtime; may be used every hour for severe symptoms
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — Aluminum and/or magnesium may accumulate in renal impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Suspension: Aluminum hydroxide 225 mg and magnesium hydroxide 200 mg per 5 mL (360 mL)
Alamag, Rulox: Aluminum hydroxide 225 mg and magnesium hydroxide 200 mg per 5 mL (360 mL)
Tablet, chewable:
Alamag: Aluminum hydroxide 300 mg and magnesium hydroxide 150 mg
Rulox No. 1: Aluminum hydroxide 200 mg and magnesium hydroxide 200 mg [DSC]
DOSAGE FORMS: CONCISE
Suspension: Aluminum hydroxide 225 mg and magnesium hydroxide 200 mg per 5 mL
Alamag [OTC], Rulox [OTC]: Aluminum hydroxide 225 mg and magnesium hydroxide 200 mg per 5 mL
Tablet, chewable:
Alamag [OTC]: Aluminum hydroxide 300 mg and magnesium hydroxide 150 mg
GENERIC EQUIVALENT AVAILABLE — Yes
USE — Antacid, hyperphosphatemia in renal failure
ADVERSE REACTIONS SIGNIFICANT
>10%: Gastrointestinal: Constipation, chalky taste, stomach cramps, fecal impaction
1% to 10%: Gastrointestinal: Nausea, vomiting, discoloration of feces (white speckles)
<1% (Limited to important or life-threatening): Hypomagnesemia, hypophosphatemia
DRUG INTERACTIONS — Decreased effect: Tetracyclines, digoxin, indomethacin, iron salts, isoniazid, allopurinol, benzodiazepines, corticosteroids, penicillamine, phenothiazines, ranitidine, ketoconazole, itraconazole
PREGNANCY RISK FACTOR — C (show table)
DIETARY CONSIDERATIONS — Should be taken 1-3 hours after meals.
CANADIAN BRAND NAMES — Diovol® Ex; Diovol®; Gelusil® Extra Strength; Mylanta™
INTERNATIONAL BRAND NAMES — Diovol (CA); Diovol Ex (CA); Gelusil Extra Strength (CA); Mylanta® (CA)
PHARMACOLOGIC CATEGORY
Antacid
DOSING: ADULTS — Dyspepsia: Oral: 5-10 mL 4-6 times/day, between meals and at bedtime; may be used every hour for severe symptoms
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — Aluminum and/or magnesium may accumulate in renal impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Suspension: Aluminum hydroxide 225 mg and magnesium hydroxide 200 mg per 5 mL (360 mL)
Alamag, Rulox: Aluminum hydroxide 225 mg and magnesium hydroxide 200 mg per 5 mL (360 mL)
Tablet, chewable:
Alamag: Aluminum hydroxide 300 mg and magnesium hydroxide 150 mg
Rulox No. 1: Aluminum hydroxide 200 mg and magnesium hydroxide 200 mg [DSC]
DOSAGE FORMS: CONCISE
Suspension: Aluminum hydroxide 225 mg and magnesium hydroxide 200 mg per 5 mL
Alamag [OTC], Rulox [OTC]: Aluminum hydroxide 225 mg and magnesium hydroxide 200 mg per 5 mL
Tablet, chewable:
Alamag [OTC]: Aluminum hydroxide 300 mg and magnesium hydroxide 150 mg
GENERIC EQUIVALENT AVAILABLE — Yes
USE — Antacid, hyperphosphatemia in renal failure
ADVERSE REACTIONS SIGNIFICANT
>10%: Gastrointestinal: Constipation, chalky taste, stomach cramps, fecal impaction
1% to 10%: Gastrointestinal: Nausea, vomiting, discoloration of feces (white speckles)
<1% (Limited to important or life-threatening): Hypomagnesemia, hypophosphatemia
DRUG INTERACTIONS — Decreased effect: Tetracyclines, digoxin, indomethacin, iron salts, isoniazid, allopurinol, benzodiazepines, corticosteroids, penicillamine, phenothiazines, ranitidine, ketoconazole, itraconazole
PREGNANCY RISK FACTOR — C (show table)
DIETARY CONSIDERATIONS — Should be taken 1-3 hours after meals.
CANADIAN BRAND NAMES — Diovol® Ex; Diovol®; Gelusil® Extra Strength; Mylanta™
INTERNATIONAL BRAND NAMES — Diovol (CA); Diovol Ex (CA); Gelusil Extra Strength (CA); Mylanta® (CA)
Aluminum hydroxide and magnesium carbonate
U.S. BRAND NAMES — Acid Gone Extra Strength [OTC]; Acid Gone [OTC]; Alenic Alka [OTC]; Gaviscon® Extra Strength [OTC]; Gaviscon® Liquid [OTC]; Genaton™ [OTC]
PHARMACOLOGIC CATEGORY
Antacid
DOSING: ADULTS — Dyspepsia, gastric acidity: Oral:
Liquid:
Gaviscon® Regular Strength: 15-30 mL 4 times/day after meals and at bedtime
Gaviscon® Extra Strength Relief: 15-30 mL 4 times/day after meals
Tablet (Gaviscon® Extra Strength Relief): Chew 2-4 tablets 4 times/day
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — Aluminum and/or magnesium may accumulate in renal impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Liquid:
Acid Gone: Aluminum hydroxide 31.7 mg and magnesium carbonate 119.3 mg per 5 mL (360 mL)
Alenic Alka: Aluminum hydroxide 31.7 mg and magnesium carbonate 119.3 mg per 5 mL (355 mL) [contains magnesium 35 mg/5 mL, sodium 13 mg/5 mL, and benzyl alcohol; cool mint flavor]
Gaviscon®: Aluminum hydroxide 31.7 mg and magnesium carbonate 119.3 mg per 5 mL (355 mL) [contains sodium 0.57 mEq/5 mL and benzyl alcohol; cool mint flavor]
Gaviscon® Extra Strength: Aluminum hydroxide 84.6 mg and magnesium carbonate 79.1 mg per 5 mL (355 mL) [contains sodium 0.9 mEq/5 mL and benzyl alcohol; cool mint flavor]
Genaton™: Aluminum hydroxide 31.7 mg and magnesium carbonate 119.3 mg per 5 mL (360 mL)
Tablet, chewable:
Acid Gone Extra Strength: Aluminum hydroxide 160 mg and magnesium carbonate 105 mg
Gaviscon® Extra Strength: Aluminum hydroxide 160 mg and magnesium carbonate 105 mg [contains sodium 19 mg/tablet (1.3 mEq/tablet); cherry and original flavors]
DOSAGE FORMS: CONCISE
Liquid: Aluminum hydroxide 31.7 mg and magnesium carbonate 119.3 mg per 5 mL; aluminum hydroxide 84.6 mg and magnesium carbonate 79.1 mg per 5 mL
Acid Gone [OTC], Alenic Alka [OTC], Gaviscon® [OTC], Genaton™ [OTC]: Aluminum hydroxide 31.7 mg and magnesium carbonate 119.3 mg per 5 mL
Gaviscon® Extra Strength [OTC]: Aluminum hydroxide 84.6 mg and magnesium carbonate 79.1 mg per 5 mL
Tablet, chewable: Aluminum hydroxide 160 mg and magnesium carbonate 105 mg
Acid Gone Extra Strength [OTC], Gaviscon® Extra Strength [OTC]: Aluminum hydroxide 160 mg and magnesium carbonate 105 mg
GENERIC EQUIVALENT AVAILABLE — Yes
USE — Temporary relief of symptoms associated with gastric acidity
ADVERSE REACTIONS SIGNIFICANT — 1% to 10%:
Endocrine & metabolic: Hypermagnesemia, aluminum intoxication (prolonged use and concomitant renal failure), hypophosphatemia
Gastrointestinal: Constipation, diarrhea
Neuromuscular & skeletal: Osteomalacia
DRUG INTERACTIONS — Decreased effect: Tetracyclines, digoxin, indomethacin, iron salts, isoniazid, allopurinol, benzodiazepines, corticosteroids, penicillamine, phenothiazines, ranitidine, ketoconazole, itraconazole
DIETARY CONSIDERATIONS — Should be taken 1-3 hours after meals with water, milk or juice. Some products contain sodium; Gaviscon® regular strength liquid: 0.57 mEq/5 mL, Gaviscon® Extra Strength liquid: 0.9 mEq/5 mL extra strength liquid, Gaviscon® Extra Strength tablet 19 mg [1.3 mEq], Alenic Alka liquid: 13 mg/5 mL
PHARMACOLOGIC CATEGORY
Antacid
DOSING: ADULTS — Dyspepsia, gastric acidity: Oral:
Liquid:
Gaviscon® Regular Strength: 15-30 mL 4 times/day after meals and at bedtime
Gaviscon® Extra Strength Relief: 15-30 mL 4 times/day after meals
Tablet (Gaviscon® Extra Strength Relief): Chew 2-4 tablets 4 times/day
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — Aluminum and/or magnesium may accumulate in renal impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Liquid:
Acid Gone: Aluminum hydroxide 31.7 mg and magnesium carbonate 119.3 mg per 5 mL (360 mL)
Alenic Alka: Aluminum hydroxide 31.7 mg and magnesium carbonate 119.3 mg per 5 mL (355 mL) [contains magnesium 35 mg/5 mL, sodium 13 mg/5 mL, and benzyl alcohol; cool mint flavor]
Gaviscon®: Aluminum hydroxide 31.7 mg and magnesium carbonate 119.3 mg per 5 mL (355 mL) [contains sodium 0.57 mEq/5 mL and benzyl alcohol; cool mint flavor]
Gaviscon® Extra Strength: Aluminum hydroxide 84.6 mg and magnesium carbonate 79.1 mg per 5 mL (355 mL) [contains sodium 0.9 mEq/5 mL and benzyl alcohol; cool mint flavor]
Genaton™: Aluminum hydroxide 31.7 mg and magnesium carbonate 119.3 mg per 5 mL (360 mL)
Tablet, chewable:
Acid Gone Extra Strength: Aluminum hydroxide 160 mg and magnesium carbonate 105 mg
Gaviscon® Extra Strength: Aluminum hydroxide 160 mg and magnesium carbonate 105 mg [contains sodium 19 mg/tablet (1.3 mEq/tablet); cherry and original flavors]
DOSAGE FORMS: CONCISE
Liquid: Aluminum hydroxide 31.7 mg and magnesium carbonate 119.3 mg per 5 mL; aluminum hydroxide 84.6 mg and magnesium carbonate 79.1 mg per 5 mL
Acid Gone [OTC], Alenic Alka [OTC], Gaviscon® [OTC], Genaton™ [OTC]: Aluminum hydroxide 31.7 mg and magnesium carbonate 119.3 mg per 5 mL
Gaviscon® Extra Strength [OTC]: Aluminum hydroxide 84.6 mg and magnesium carbonate 79.1 mg per 5 mL
Tablet, chewable: Aluminum hydroxide 160 mg and magnesium carbonate 105 mg
Acid Gone Extra Strength [OTC], Gaviscon® Extra Strength [OTC]: Aluminum hydroxide 160 mg and magnesium carbonate 105 mg
GENERIC EQUIVALENT AVAILABLE — Yes
USE — Temporary relief of symptoms associated with gastric acidity
ADVERSE REACTIONS SIGNIFICANT — 1% to 10%:
Endocrine & metabolic: Hypermagnesemia, aluminum intoxication (prolonged use and concomitant renal failure), hypophosphatemia
Gastrointestinal: Constipation, diarrhea
Neuromuscular & skeletal: Osteomalacia
DRUG INTERACTIONS — Decreased effect: Tetracyclines, digoxin, indomethacin, iron salts, isoniazid, allopurinol, benzodiazepines, corticosteroids, penicillamine, phenothiazines, ranitidine, ketoconazole, itraconazole
DIETARY CONSIDERATIONS — Should be taken 1-3 hours after meals with water, milk or juice. Some products contain sodium; Gaviscon® regular strength liquid: 0.57 mEq/5 mL, Gaviscon® Extra Strength liquid: 0.9 mEq/5 mL extra strength liquid, Gaviscon® Extra Strength tablet 19 mg [1.3 mEq], Alenic Alka liquid: 13 mg/5 mL
Aluminum hydroxide
U.S. BRAND NAMES — ALternaGel® [OTC]; Dermagran® [OTC]
PHARMACOLOGIC CATEGORY
Antacid
Antidote
Protectant, Topical
DOSING: ADULTS
Hyperphosphatemia: Oral: Initial: 300-600 mg 3 times/day with meals
Hyperacidity: Oral: 600-1200 mg between meals and at bedtime
Skin protectant: Topical: Apply to affected area as needed; reapply at least every 12 hours
DOSING: PEDIATRIC
Hyperphosphatemia: Oral: 50-150 mg/kg/24 hours in divided doses every 4-6 hours, titrate dosage to maintain serum phosphorus within normal range
Skin protectant: Topical: Refer to adult dosing.
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — Aluminum may accumulate in renal impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Ointment:
Dermagran®: 0.275% (120 g)
Suspension, oral: 320 mg/5 mL (473 mL)
ALternaGel®: 600 mg/5 mL (360 mL)
DOSAGE FORMS: CONCISE
Ointment:
Dermagran® [OTC]: 0.275% (120 g)
Suspension, oral: 320 mg/5 mL
ALternaGel® [OTC]: 600 mg/5 mL
GENERIC EQUIVALENT AVAILABLE — Yes: Suspension
ADMINISTRATION
Oral: Dose should be followed with water.
Topical: Apply as needed to affected area; reapply at least every 12 hours.
USE — Treatment of hyperacidity; hyperphosphatemia; temporary protection of minor cuts, scrapes, and burns
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Gastrointestinal: Constipation, stomach cramps, fecal impaction, nausea, vomiting, discoloration of feces (white speckles)
Endocrine & metabolic: Hypophosphatemia, hypomagnesemia
CONTRAINDICATIONS — Hypersensitivity to aluminum salts or any component of the formulation
WARNINGS / PRECAUTIONS — Oral: Hypophosphatemia may occur with prolonged administration or large doses; aluminum intoxication and osteomalacia may occur in patients with uremia. Use with caution in patients with CHF, renal failure, edema, cirrhosis, and low sodium diets, and patients who have recently suffered gastrointestinal hemorrhage; uremic patients not receiving dialysis may develop osteomalacia and osteoporosis due to phosphate depletion.
Elderly may be predisposed to constipation and fecal impaction. Careful evaluation of possible drug interactions must be done. When used as an antacid in ulcer treatment, consider buffer capacity (mEq/mL) to calculate dose.
Topical: Not for application over deep wounds, puncture wounds, infected areas, or lacerations. When used for self medication (OTC use), consult with healthcare provider if needed for >7 days or for use in children <6 months of age.
DRUG INTERACTIONS
Decreased effect: Aluminum hydroxide may decrease the absorption of allopurinol, antibiotics (tetracyclines, quinolones, some cephalosporins), bisphosphonate derivatives, corticosteroids, cyclosporine, delavirdine, iron salts, imidazole antifungals, isoniazid, mycophenolate, penicillamine, phosphate supplements, phenytoin, phenothiazines, trientine.
Absorption of aluminum hydroxide may be decreased by citric acid derivatives.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — No data available on clinical effects on the fetus; available evidence suggests safe use during pregnancy and breast-feeding.
LACTATION — Excretion in breast milk unknown
DIETARY CONSIDERATIONS — Should be taken 1-3 hours after meals when used as an antacid. When used to decrease phosphorus, should be taken within 20 minutes of a meal.
MONITORING PARAMETERS — Monitor phosphorus levels periodically when patient is on chronic therapy.
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Aluminum antacids may cause constipation, phosphate depletion, and bezoar or fecalith formation. In patients with renal failure, aluminum may accumulate to toxic levels. Deferoxamine, traditionally used as an iron chelator, has been shown to increase urinary aluminum output. Deferoxamine chelation of aluminum has resulted in improvements of clinical symptoms and bone histology; however, remains an experimental treatment for aluminum poisoning and has a significant potential for adverse effects.
CANADIAN BRAND NAMES — Amphojel®; Basaljel®
INTERNATIONAL BRAND NAMES — Acidex (ZA); Aldrox (BE); Algeldraat (NL); Alu-Cap (AE, BF, BH, BJ, CI, CY, EG, ET, GH, GM, GN, IQ, IR, JO, KE, KW, LB, LR, LY, MA, ML, MR, MU, MW, NE, NG, OM, QA, SA, SC, SD, SL, SN, SY, TZ, UG, YE, ZM, ZW); Alu-Tab (HK, PH); Alucol (IT); Aludrox (DE, IE); Alugel (DE, TW); Alugelibys (ES); Alumigel (JP); Alutab (MY, NZ); Alzinox (PH); Amphogel (AU); Amphojel (CA, NZ, ZA); Basaljel (CA); Gastracol (CH); Pepsamar (BF, BJ, BR, CI, CL, CO, ES, ET, GH, GM, GN, GR, KE, LR, MA, ML, MR, MU, MW, NE, NG, PE, PT, SC, SD, SL, SN, TZ, UG, VE, ZM, ZW); Rocgel (FR); Ulcerin-P (TW)
MECHANISM OF ACTION — Neutralizes hydrochloride in stomach to form Al (Cl)3 salt + H2O
PATIENT INFORMATION — Do not take oral drugs within 1-2 hours of administration; notify prescriber if relief is not obtained or if there are any signs to suggest bleeding from the GI tract
(For additional information see "Aluminum hydroxide: Patient drug information")
Use of UpToDate is subject to the Subscription and License Agreement. REFERENCES 1. Bohannon, AD, Lyles, KW. Drug-Induced Bone Disease. Clin Geriatr Med 1994; 10:611.
2. Cumming, RG, Klineberg, RJ. Aluminum in Antacids and Cooking Pots and the Risk of Hip Fractures in Elderly People. Age Ageing 1994; 23:468.
3. Gupta, S, Ahlawat, SK. Aluminum Phosphide Poisoning - A Review. J Toxicol Clin Toxicol 1995; 33:19.
4. Maher, ER, Brown, EA, Curtis, JR, et al. Accumulation of Aluminum in Chronic Renal Failure Due to Administration of Albumin Replacement Solutions. Br Med J (Clin Res Ed) 1986; 292:306.
5. Monteagudo, FS, Cassidy, MJ, Folb, PI. Recent Developments in Aluminum Toxicity. Med Toxicol Adverse Drug Exp 1989; 4:1.
6. Robertson, JA, Salusky, IB, Goodman, WG, et al. Sucralfate, Intestinal Aluminum Absorption, and Aluminum Toxicity in a Patient on Dialysis. Ann Intern Med 1989; 111:179.
7. U.S. Department of, Health, Human, Services. Toxicological Profile for Aluminum TP-91/01. Agency for Toxic Substances and Diseases Registry, July 1992.
PHARMACOLOGIC CATEGORY
Antacid
Antidote
Protectant, Topical
DOSING: ADULTS
Hyperphosphatemia: Oral: Initial: 300-600 mg 3 times/day with meals
Hyperacidity: Oral: 600-1200 mg between meals and at bedtime
Skin protectant: Topical: Apply to affected area as needed; reapply at least every 12 hours
DOSING: PEDIATRIC
Hyperphosphatemia: Oral: 50-150 mg/kg/24 hours in divided doses every 4-6 hours, titrate dosage to maintain serum phosphorus within normal range
Skin protectant: Topical: Refer to adult dosing.
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — Aluminum may accumulate in renal impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Ointment:
Dermagran®: 0.275% (120 g)
Suspension, oral: 320 mg/5 mL (473 mL)
ALternaGel®: 600 mg/5 mL (360 mL)
DOSAGE FORMS: CONCISE
Ointment:
Dermagran® [OTC]: 0.275% (120 g)
Suspension, oral: 320 mg/5 mL
ALternaGel® [OTC]: 600 mg/5 mL
GENERIC EQUIVALENT AVAILABLE — Yes: Suspension
ADMINISTRATION
Oral: Dose should be followed with water.
Topical: Apply as needed to affected area; reapply at least every 12 hours.
USE — Treatment of hyperacidity; hyperphosphatemia; temporary protection of minor cuts, scrapes, and burns
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Gastrointestinal: Constipation, stomach cramps, fecal impaction, nausea, vomiting, discoloration of feces (white speckles)
Endocrine & metabolic: Hypophosphatemia, hypomagnesemia
CONTRAINDICATIONS — Hypersensitivity to aluminum salts or any component of the formulation
WARNINGS / PRECAUTIONS — Oral: Hypophosphatemia may occur with prolonged administration or large doses; aluminum intoxication and osteomalacia may occur in patients with uremia. Use with caution in patients with CHF, renal failure, edema, cirrhosis, and low sodium diets, and patients who have recently suffered gastrointestinal hemorrhage; uremic patients not receiving dialysis may develop osteomalacia and osteoporosis due to phosphate depletion.
Elderly may be predisposed to constipation and fecal impaction. Careful evaluation of possible drug interactions must be done. When used as an antacid in ulcer treatment, consider buffer capacity (mEq/mL) to calculate dose.
Topical: Not for application over deep wounds, puncture wounds, infected areas, or lacerations. When used for self medication (OTC use), consult with healthcare provider if needed for >7 days or for use in children <6 months of age.
DRUG INTERACTIONS
Decreased effect: Aluminum hydroxide may decrease the absorption of allopurinol, antibiotics (tetracyclines, quinolones, some cephalosporins), bisphosphonate derivatives, corticosteroids, cyclosporine, delavirdine, iron salts, imidazole antifungals, isoniazid, mycophenolate, penicillamine, phosphate supplements, phenytoin, phenothiazines, trientine.
Absorption of aluminum hydroxide may be decreased by citric acid derivatives.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — No data available on clinical effects on the fetus; available evidence suggests safe use during pregnancy and breast-feeding.
LACTATION — Excretion in breast milk unknown
DIETARY CONSIDERATIONS — Should be taken 1-3 hours after meals when used as an antacid. When used to decrease phosphorus, should be taken within 20 minutes of a meal.
MONITORING PARAMETERS — Monitor phosphorus levels periodically when patient is on chronic therapy.
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Aluminum antacids may cause constipation, phosphate depletion, and bezoar or fecalith formation. In patients with renal failure, aluminum may accumulate to toxic levels. Deferoxamine, traditionally used as an iron chelator, has been shown to increase urinary aluminum output. Deferoxamine chelation of aluminum has resulted in improvements of clinical symptoms and bone histology; however, remains an experimental treatment for aluminum poisoning and has a significant potential for adverse effects.
CANADIAN BRAND NAMES — Amphojel®; Basaljel®
INTERNATIONAL BRAND NAMES — Acidex (ZA); Aldrox (BE); Algeldraat (NL); Alu-Cap (AE, BF, BH, BJ, CI, CY, EG, ET, GH, GM, GN, IQ, IR, JO, KE, KW, LB, LR, LY, MA, ML, MR, MU, MW, NE, NG, OM, QA, SA, SC, SD, SL, SN, SY, TZ, UG, YE, ZM, ZW); Alu-Tab (HK, PH); Alucol (IT); Aludrox (DE, IE); Alugel (DE, TW); Alugelibys (ES); Alumigel (JP); Alutab (MY, NZ); Alzinox (PH); Amphogel (AU); Amphojel (CA, NZ, ZA); Basaljel (CA); Gastracol (CH); Pepsamar (BF, BJ, BR, CI, CL, CO, ES, ET, GH, GM, GN, GR, KE, LR, MA, ML, MR, MU, MW, NE, NG, PE, PT, SC, SD, SL, SN, TZ, UG, VE, ZM, ZW); Rocgel (FR); Ulcerin-P (TW)
MECHANISM OF ACTION — Neutralizes hydrochloride in stomach to form Al (Cl)3 salt + H2O
PATIENT INFORMATION — Do not take oral drugs within 1-2 hours of administration; notify prescriber if relief is not obtained or if there are any signs to suggest bleeding from the GI tract
(For additional information see "Aluminum hydroxide: Patient drug information")
Use of UpToDate is subject to the Subscription and License Agreement. REFERENCES 1. Bohannon, AD, Lyles, KW. Drug-Induced Bone Disease. Clin Geriatr Med 1994; 10:611.
2. Cumming, RG, Klineberg, RJ. Aluminum in Antacids and Cooking Pots and the Risk of Hip Fractures in Elderly People. Age Ageing 1994; 23:468.
3. Gupta, S, Ahlawat, SK. Aluminum Phosphide Poisoning - A Review. J Toxicol Clin Toxicol 1995; 33:19.
4. Maher, ER, Brown, EA, Curtis, JR, et al. Accumulation of Aluminum in Chronic Renal Failure Due to Administration of Albumin Replacement Solutions. Br Med J (Clin Res Ed) 1986; 292:306.
5. Monteagudo, FS, Cassidy, MJ, Folb, PI. Recent Developments in Aluminum Toxicity. Med Toxicol Adverse Drug Exp 1989; 4:1.
6. Robertson, JA, Salusky, IB, Goodman, WG, et al. Sucralfate, Intestinal Aluminum Absorption, and Aluminum Toxicity in a Patient on Dialysis. Ann Intern Med 1989; 111:179.
7. U.S. Department of, Health, Human, Services. Toxicological Profile for Aluminum TP-91/01. Agency for Toxic Substances and Diseases Registry, July 1992.
Aluminum chloride hexahydrate
U.S. BRAND NAMES — Certain Dri® [OTC]; Drysol™; Xerac AC™
PHARMACOLOGIC CATEGORY
Topical Skin Product
DOSING: ADULTS — Hyperhidrosis: Topical: Apply once daily at bedtime; once excessive sweating has stopped, may decrease to once or twice weekly, or as needed. Wash treated area in the morning.
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, topical:
Certain Dri®: 12% (36 mL)
Drysol™: 20% (35 mL, 37.5 mL, 60 mL) [contains ethyl alcohol 93%]
Xerac AC™: 6.25% (35 mL, 60 mL) [contains ethyl alcohol 95%]
DOSAGE FORMS: CONCISE
Solution, topical:
Certain Dri® [OTC]: 12% (36 mL)
Drysol™: 20% (35 mL, 37.5 mL, 60 mL)
Xerac AC™: 6.25% (35 mL, 60 mL)
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Topical: Apply to dry skin. Area may be covered with plastic wrap held in place with snug-fitting T-shirt. Do not hold in place with tape.
USE — Astringent in the management of hyperhidrosis
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Dermatologic: Skin irritation
Local: Burning sensation, prickling sensation, transient itching or stinging
CONTRAINDICATIONS — Hypersensitivity to any component of the formulation
WARNINGS / PRECAUTIONS — Do not apply to broken or recently shaved skin. For external use only; avoid contact with eyes. May be harmful to certain metals or fabrics. Discontinue if skin irritation occurs.
PRICING — (data from drugstore.com)
Solution (Drysol)
20% (35): $10.88
20% (37.5): $10.32
20% (60): $13.54
Solution (Hypercare)
20% (35): $8.99
20% (60): $8.99
Solution (Xerac AC)
6.25% (35): $9.94
6.25% (60): $12.05
PATIENT INFORMATION — For external use only. Product may discolor clothing if not completely dry. Discontinue if rash develops.
PHARMACOLOGIC CATEGORY
Topical Skin Product
DOSING: ADULTS — Hyperhidrosis: Topical: Apply once daily at bedtime; once excessive sweating has stopped, may decrease to once or twice weekly, or as needed. Wash treated area in the morning.
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, topical:
Certain Dri®: 12% (36 mL)
Drysol™: 20% (35 mL, 37.5 mL, 60 mL) [contains ethyl alcohol 93%]
Xerac AC™: 6.25% (35 mL, 60 mL) [contains ethyl alcohol 95%]
DOSAGE FORMS: CONCISE
Solution, topical:
Certain Dri® [OTC]: 12% (36 mL)
Drysol™: 20% (35 mL, 37.5 mL, 60 mL)
Xerac AC™: 6.25% (35 mL, 60 mL)
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Topical: Apply to dry skin. Area may be covered with plastic wrap held in place with snug-fitting T-shirt. Do not hold in place with tape.
USE — Astringent in the management of hyperhidrosis
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Dermatologic: Skin irritation
Local: Burning sensation, prickling sensation, transient itching or stinging
CONTRAINDICATIONS — Hypersensitivity to any component of the formulation
WARNINGS / PRECAUTIONS — Do not apply to broken or recently shaved skin. For external use only; avoid contact with eyes. May be harmful to certain metals or fabrics. Discontinue if skin irritation occurs.
PRICING — (data from drugstore.com)
Solution (Drysol)
20% (35): $10.88
20% (37.5): $10.32
20% (60): $13.54
Solution (Hypercare)
20% (35): $8.99
20% (60): $8.99
Solution (Xerac AC)
6.25% (35): $9.94
6.25% (60): $12.05
PATIENT INFORMATION — For external use only. Product may discolor clothing if not completely dry. Discontinue if rash develops.
Aluminum chloride (dental)
U.S. BRAND NAMES — Hemodent™
PHARMACOLOGIC CATEGORY
Astringent
Hemostatic Agent
DOSING: ADULTS — Control of bleeding: Apply retraction cord as directed
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Liquid:
Hemodent™: 21% (10 mL, 20 mL, 40 mL)
Retraction cord [impregnated with 21% solution]:
Hemodent™: Braided cord, thin (7 ft); braided cord medium thin (7 ft); twisted cord #3 (7 ft); twisted cord #9 (7ft)
DOSAGE FORMS: CONCISE
Liquid:
Hemodent™: 21% (10 mL, 20 mL, 40 mL)
Retraction cord [impregnated with 21% solution]:
Hemodent™: Braided cord, thin (7 ft); braided cord medium thin (7 ft); twisted cord #3 (7 ft); twisted cord #9 (7ft)
GENERIC EQUIVALENT AVAILABLE — No
USE — Hemostatic
ADVERSE REACTIONS SIGNIFICANT — No data reported.
CONTRAINDICATIONS — No data reported
WARNINGS / PRECAUTIONS — Since large amounts of astringents may cause tissue irritation and possible damage, only small amounts should be applied.
DRUG INTERACTIONS — No data reported
MECHANISM OF ACTION — Precipitates tissue and blood proteins causing a mechanical obstruction to hemorrhage from injured blood vessels
PHARMACOLOGIC CATEGORY
Astringent
Hemostatic Agent
DOSING: ADULTS — Control of bleeding: Apply retraction cord as directed
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Liquid:
Hemodent™: 21% (10 mL, 20 mL, 40 mL)
Retraction cord [impregnated with 21% solution]:
Hemodent™: Braided cord, thin (7 ft); braided cord medium thin (7 ft); twisted cord #3 (7 ft); twisted cord #9 (7ft)
DOSAGE FORMS: CONCISE
Liquid:
Hemodent™: 21% (10 mL, 20 mL, 40 mL)
Retraction cord [impregnated with 21% solution]:
Hemodent™: Braided cord, thin (7 ft); braided cord medium thin (7 ft); twisted cord #3 (7 ft); twisted cord #9 (7ft)
GENERIC EQUIVALENT AVAILABLE — No
USE — Hemostatic
ADVERSE REACTIONS SIGNIFICANT — No data reported.
CONTRAINDICATIONS — No data reported
WARNINGS / PRECAUTIONS — Since large amounts of astringents may cause tissue irritation and possible damage, only small amounts should be applied.
DRUG INTERACTIONS — No data reported
MECHANISM OF ACTION — Precipitates tissue and blood proteins causing a mechanical obstruction to hemorrhage from injured blood vessels
Aluminum acetate
U.S. BRAND NAMES — Domeboro® [OTC]; Gordon Boro-Packs [OTC]; Pedi-Boro® [OTC]
PHARMACOLOGIC CATEGORY
Topical Skin Product
DOSING: ADULTS — Dermal inflammation, dermatitis: Topical: Soak affected area in the solution 2-4 times/day for 15-30 minutes or apply wet dressing soaked in the solution for more extended periods; rewet dressing with solution 2-4 times/day every 15-30 minutes
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Powder, for topical solution:
Domeboro®: Aluminum sulfate 1191 mg and calcium acetate 938 mg per packet (12s, 100s)
Gordon Boro-Packs: Aluminum sulfate 49% and calcium acetate 51% per packet (100s)
Pedi-Boro®: Aluminum sulfate 49% and calcium acetate 51% per packet (12s, 100s)
DOSAGE FORMS: CONCISE
Powder, for topical solution:
Domeboro® [OTC]: Aluminum sulfate 1191 mg and calcium acetate 938 mg per packet (12s, 100s)
Gordon Boro-Packs: Aluminum sulfate 49% and calcium acetate 51% per packet (100s)
Pedi-Boro® [OTC]: Aluminum sulfate 49% and calcium acetate 51% per packet (12s, 100s)
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — For external use only. Do not occlude dressing to prevent evaporation.
USE — Astringent wet dressing for relief of inflammatory conditions of the skin; reduce weeping that may occur in dermatitis
WARNINGS / PRECAUTIONS — For external use only; avoid contact with eyes. Not for OTC use >7 days.
PHARMACOLOGIC CATEGORY
Topical Skin Product
DOSING: ADULTS — Dermal inflammation, dermatitis: Topical: Soak affected area in the solution 2-4 times/day for 15-30 minutes or apply wet dressing soaked in the solution for more extended periods; rewet dressing with solution 2-4 times/day every 15-30 minutes
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Powder, for topical solution:
Domeboro®: Aluminum sulfate 1191 mg and calcium acetate 938 mg per packet (12s, 100s)
Gordon Boro-Packs: Aluminum sulfate 49% and calcium acetate 51% per packet (100s)
Pedi-Boro®: Aluminum sulfate 49% and calcium acetate 51% per packet (12s, 100s)
DOSAGE FORMS: CONCISE
Powder, for topical solution:
Domeboro® [OTC]: Aluminum sulfate 1191 mg and calcium acetate 938 mg per packet (12s, 100s)
Gordon Boro-Packs: Aluminum sulfate 49% and calcium acetate 51% per packet (100s)
Pedi-Boro® [OTC]: Aluminum sulfate 49% and calcium acetate 51% per packet (12s, 100s)
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — For external use only. Do not occlude dressing to prevent evaporation.
USE — Astringent wet dressing for relief of inflammatory conditions of the skin; reduce weeping that may occur in dermatitis
WARNINGS / PRECAUTIONS — For external use only; avoid contact with eyes. Not for OTC use >7 days.
Altretamine
U.S. BRAND NAMES — Hexalen®
PHARMACOLOGIC CATEGORY
Antineoplastic Agent, Miscellaneous
DOSING: ADULTS — Refer to individual protocols.
Ovarian cancer: Oral: 260 mg/m2/day in 4 divided doses for 14 or 21 days of a 28-day cycle
Alternatively (unlabeled use): 4-12 mg/kg/day in 3-4 divided doses for 21-90 days
Alternatively (unlabeled use): 240-320 mg/m2/day in 3-4 divided doses for 21 days, repeated every 6 weeks
Alternatively (unlabeled use): 150 mg/m2/day in 3-4 divided doses for 14 days of a 28-day cycle
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Gelcap:
Hexalen®: 50 mg
DOSAGE FORMS: CONCISE
Gelcap:
Hexalen®: 50 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Administer total daily dose as 3-4 divided doses after meals and at bedtime.
USE — Palliative treatment of persistent or recurrent ovarian cancer
ADVERSE REACTIONS SIGNIFICANT
>10%:
Central nervous system: Peripheral sensory neuropathy (31%; moderate-to-severe 9%), neurotoxicity (21%; may be progressive and dose-limiting)
Gastrointestinal: Nausea/vomiting (33% to 70%; severe 1%), diarrhea (48%)
Hematologic: Anemia (33%), leukopenia (5% to 15%; grade 4: 1%), neutropenia
1% to 10%:
Central nervous system: Fatigue (1%), seizure (1%)
Gastrointestinal: Stomach cramps, anorexia (1%)
Hematologic: Thrombocytopenia (9%)
Hepatic: Alkaline phosphatase increased (9%)
<1% (Limited to important or life-threatening): Alopecia, ataxia, depression, dizziness, hepatotoxicity, mood disorders, pruritus, rash, tremor, vertigo
CONTRAINDICATIONS — Hypersensitivity to altretamine or any component of the formulation; pre-existing severe bone marrow suppression or severe neurologic toxicity; pregnancy
WARNINGS / PRECAUTIONS
Box warnings: Bone marrow suppression: See "Concerns related to adverse effects" below. Experienced physician: See "Other warnings/precautions" below. Neurotoxicity: See "Concerns related to adverse effects" below.
Special handling: Hazardous agent: Use appropriate precautions for handling and disposal.
Concerns related to adverse effects: Bone marrow suppression: [U.S. Boxed Warning]: Peripheral blood counts should be done routinely before and after drug therapy; bone marrow suppression is common. Use with caution in patients previously treated with other myelosuppressive drugs. Neurotoxicity: [U.S. Boxed Warning]: Neurologic examinations should be done routinely before and after drug therapy; neurotoxicity is common. USe with caution in patients with pre-existing neurotoxicity.
Disease-related concerns: Hepatic impairment: Use with caution in patients with hepatic impairment. Renal impairment: Use with caution in patients with renal impairment.
Special populations: Pediatrics: Safety and efficacy have not been established in children.
Other warnings/precautions: Experienced physician: [U.S. Boxed Warning]: Should be administered under the supervision of an experienced cancer chemotherapy physician.
DRUG INTERACTIONS
MAO inhibitors: Altretamine may enhance the orthostatic effect of MAO inhibitors.
Pyridoxine: May diminish the therapeutic effect of altretamine; concurrent use not recommended.
Tricyclic antidepressants: Altretamine may enhance the orthostatic effect of tricyclic antidepressants.
PREGNANCY RISK FACTOR — D (show table)
PREGNANCY IMPLICATIONS — Teratogenic effects were noted in animal studies. There are no adequate and well-controlled studies in pregnant women. Women of childbearing potential should avoid becoming pregnant while on therapy.
LACTATION — Excretion in breast milk unknown/not recommended
BREAST-FEEDING CONSIDERATIONS — Due to the potential toxicity in the nursing infant, breast-feeding is not recommended.
DIETARY CONSIDERATIONS — Should be taken after meals at bedtime.
MONITORING PARAMETERS — CBC with differential, liver function tests; neurologic examination
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms include nausea, vomiting, peripheral neuropathy, and severe bone marrow suppression. Treatment is symptom-directed and supportive.
CANADIAN BRAND NAMES — Hexalen®
INTERNATIONAL BRAND NAMES — Hexalen (AU, BG, CA, CN, GB, IE, IL, JP, NZ, SE, TH); Hexastat (DK, FR, NO, PT); Hexinawas (ES)
MECHANISM OF ACTION — Although altretamine's clinical antitumor spectrum resembles that of alkylating agents, the drug has demonstrated activity in alkylator-resistant patients. The drug selectively inhibits the incorporation of radioactive thymidine and uridine into DNA and RNA, inhibiting DNA and RNA synthesis; reactive intermediates covalently bind to microsomal proteins and DNA; can spontaneously degrade to demethylated melamines and formaldehyde which are also cytotoxic.
PHARMACODYNAMICS / KINETICS
Absorption: Well absorbed (75% to 89%)
Distribution: Highly concentrated hepatically and renally; low in other organs
Protein binding: 50% to 94%
Metabolism: Hepatic; rapid and extensive demethylation to active metabolites (pentamethylmelamine and tetramethylmelamine)
Half-life elimination: 13 hours
Time to peak, plasma: 0.5-3 hours
Excretion: Urine (90%, <1% as unchanged drug)
PATIENT INFORMATION — Report any numbness or tingling in extremities. Nausea and vomiting may occur.
(For additional information see "Altretamine: Patient drug information")
Use of UpToDate is subject to the Subscription and License Agreement. REFERENCES 1. Ames, MM. Hexamethylmelamine: Pharmacology and Mechanism of Action. Cancer Treat Rev 1991; 18(Suppl A):3.
2. Bruckner, HW, Schleifer, SJ. Orthostatic Hypotension as a Complication of Hexamethylmelamine Antidepressant Interaction. Cancer Treat Rep 1983; 67:516.
3. Damia, G, D'Incalci, M. Clinical Pharmacokinetics of Altretamine. Clin Pharmacokinet 1995; 28:439.
4. Hahn, DA, Black, C. Hexamethylamine: A Review. Drug Intell Clin Pharm 1980; 14:541.
5. Hansen, LA, Hughes, TE. Altretamine. DICP 1991; 25:146.
6. Lee, CR, Faulds, D. Altretamine. A Review of Its Pharmacodynamic and Pharmacokinetic Properties, and Therapeutic Potential in Cancer Chemotherapy. Drugs 1995; 49:932.
7. Manetta, A, Mac Neill, C, Lyter, JA, et al. Hexamethylmelamine as a Single Second-Line Agent in Ovarian Cancer. Gynecol Oncol 1990; 36:93.
8. Sutton, GP. Secondary Therapy for Epithelial Ovarian Cancer - 1994. Semin Oncol 1994; 21(4 Suppl 7):32.
9. Thigpen, JT, Vance, RB, Khansur, T. Second-Line Chemotherapy for Recurrent Carcinoma of the Ovary. Cancer 1993; 71(4 Suppl):1559.
PHARMACOLOGIC CATEGORY
Antineoplastic Agent, Miscellaneous
DOSING: ADULTS — Refer to individual protocols.
Ovarian cancer: Oral: 260 mg/m2/day in 4 divided doses for 14 or 21 days of a 28-day cycle
Alternatively (unlabeled use): 4-12 mg/kg/day in 3-4 divided doses for 21-90 days
Alternatively (unlabeled use): 240-320 mg/m2/day in 3-4 divided doses for 21 days, repeated every 6 weeks
Alternatively (unlabeled use): 150 mg/m2/day in 3-4 divided doses for 14 days of a 28-day cycle
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Gelcap:
Hexalen®: 50 mg
DOSAGE FORMS: CONCISE
Gelcap:
Hexalen®: 50 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Administer total daily dose as 3-4 divided doses after meals and at bedtime.
USE — Palliative treatment of persistent or recurrent ovarian cancer
ADVERSE REACTIONS SIGNIFICANT
>10%:
Central nervous system: Peripheral sensory neuropathy (31%; moderate-to-severe 9%), neurotoxicity (21%; may be progressive and dose-limiting)
Gastrointestinal: Nausea/vomiting (33% to 70%; severe 1%), diarrhea (48%)
Hematologic: Anemia (33%), leukopenia (5% to 15%; grade 4: 1%), neutropenia
1% to 10%:
Central nervous system: Fatigue (1%), seizure (1%)
Gastrointestinal: Stomach cramps, anorexia (1%)
Hematologic: Thrombocytopenia (9%)
Hepatic: Alkaline phosphatase increased (9%)
<1% (Limited to important or life-threatening): Alopecia, ataxia, depression, dizziness, hepatotoxicity, mood disorders, pruritus, rash, tremor, vertigo
CONTRAINDICATIONS — Hypersensitivity to altretamine or any component of the formulation; pre-existing severe bone marrow suppression or severe neurologic toxicity; pregnancy
WARNINGS / PRECAUTIONS
Box warnings: Bone marrow suppression: See "Concerns related to adverse effects" below. Experienced physician: See "Other warnings/precautions" below. Neurotoxicity: See "Concerns related to adverse effects" below.
Special handling: Hazardous agent: Use appropriate precautions for handling and disposal.
Concerns related to adverse effects: Bone marrow suppression: [U.S. Boxed Warning]: Peripheral blood counts should be done routinely before and after drug therapy; bone marrow suppression is common. Use with caution in patients previously treated with other myelosuppressive drugs. Neurotoxicity: [U.S. Boxed Warning]: Neurologic examinations should be done routinely before and after drug therapy; neurotoxicity is common. USe with caution in patients with pre-existing neurotoxicity.
Disease-related concerns: Hepatic impairment: Use with caution in patients with hepatic impairment. Renal impairment: Use with caution in patients with renal impairment.
Special populations: Pediatrics: Safety and efficacy have not been established in children.
Other warnings/precautions: Experienced physician: [U.S. Boxed Warning]: Should be administered under the supervision of an experienced cancer chemotherapy physician.
DRUG INTERACTIONS
MAO inhibitors: Altretamine may enhance the orthostatic effect of MAO inhibitors.
Pyridoxine: May diminish the therapeutic effect of altretamine; concurrent use not recommended.
Tricyclic antidepressants: Altretamine may enhance the orthostatic effect of tricyclic antidepressants.
PREGNANCY RISK FACTOR — D (show table)
PREGNANCY IMPLICATIONS — Teratogenic effects were noted in animal studies. There are no adequate and well-controlled studies in pregnant women. Women of childbearing potential should avoid becoming pregnant while on therapy.
LACTATION — Excretion in breast milk unknown/not recommended
BREAST-FEEDING CONSIDERATIONS — Due to the potential toxicity in the nursing infant, breast-feeding is not recommended.
DIETARY CONSIDERATIONS — Should be taken after meals at bedtime.
MONITORING PARAMETERS — CBC with differential, liver function tests; neurologic examination
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms include nausea, vomiting, peripheral neuropathy, and severe bone marrow suppression. Treatment is symptom-directed and supportive.
CANADIAN BRAND NAMES — Hexalen®
INTERNATIONAL BRAND NAMES — Hexalen (AU, BG, CA, CN, GB, IE, IL, JP, NZ, SE, TH); Hexastat (DK, FR, NO, PT); Hexinawas (ES)
MECHANISM OF ACTION — Although altretamine's clinical antitumor spectrum resembles that of alkylating agents, the drug has demonstrated activity in alkylator-resistant patients. The drug selectively inhibits the incorporation of radioactive thymidine and uridine into DNA and RNA, inhibiting DNA and RNA synthesis; reactive intermediates covalently bind to microsomal proteins and DNA; can spontaneously degrade to demethylated melamines and formaldehyde which are also cytotoxic.
PHARMACODYNAMICS / KINETICS
Absorption: Well absorbed (75% to 89%)
Distribution: Highly concentrated hepatically and renally; low in other organs
Protein binding: 50% to 94%
Metabolism: Hepatic; rapid and extensive demethylation to active metabolites (pentamethylmelamine and tetramethylmelamine)
Half-life elimination: 13 hours
Time to peak, plasma: 0.5-3 hours
Excretion: Urine (90%, <1% as unchanged drug)
PATIENT INFORMATION — Report any numbness or tingling in extremities. Nausea and vomiting may occur.
(For additional information see "Altretamine: Patient drug information")
Use of UpToDate is subject to the Subscription and License Agreement. REFERENCES 1. Ames, MM. Hexamethylmelamine: Pharmacology and Mechanism of Action. Cancer Treat Rev 1991; 18(Suppl A):3.
2. Bruckner, HW, Schleifer, SJ. Orthostatic Hypotension as a Complication of Hexamethylmelamine Antidepressant Interaction. Cancer Treat Rep 1983; 67:516.
3. Damia, G, D'Incalci, M. Clinical Pharmacokinetics of Altretamine. Clin Pharmacokinet 1995; 28:439.
4. Hahn, DA, Black, C. Hexamethylamine: A Review. Drug Intell Clin Pharm 1980; 14:541.
5. Hansen, LA, Hughes, TE. Altretamine. DICP 1991; 25:146.
6. Lee, CR, Faulds, D. Altretamine. A Review of Its Pharmacodynamic and Pharmacokinetic Properties, and Therapeutic Potential in Cancer Chemotherapy. Drugs 1995; 49:932.
7. Manetta, A, Mac Neill, C, Lyter, JA, et al. Hexamethylmelamine as a Single Second-Line Agent in Ovarian Cancer. Gynecol Oncol 1990; 36:93.
8. Sutton, GP. Secondary Therapy for Epithelial Ovarian Cancer - 1994. Semin Oncol 1994; 21(4 Suppl 7):32.
9. Thigpen, JT, Vance, RB, Khansur, T. Second-Line Chemotherapy for Recurrent Carcinoma of the Ovary. Cancer 1993; 71(4 Suppl):1559.
Alteplase
U.S. BRAND NAMES — Activase®; Cathflo® Activase®
PHARMACOLOGIC CATEGORY
Thrombolytic Agent
DOSING: ADULTS
Coronary artery thrombi: I.V. Front loading dose (weight-based):
Patients >67 kg: Total dose: 100 mg over 1.5 hours; infuse 15 mg over 1-2 minutes. Infuse 50 mg over 30 minutes. Infuse remaining 35 mg of alteplase over the next hour. See "Note."
Patients 67 kg: Infuse 15 mg I.V. bolus over 1-2 minutes, then infuse 0.75 mg/kg (not to exceed 50 mg) over next 30 minutes, followed by 0.5 mg/kg over next 60 minutes (not to exceed 35 mg). See "Note."
Note: Concurrently, begin heparin 60 units/kg bolus (maximum: 4000 units) followed by continuous infusion of 12 units/kg/hour (maximum: 1000 units/hour) and adjust to aPTT target of 1.5-2 times the upper limit of control.
Acute pulmonary embolism: I.V.: 100 mg over 2 hours.
Acute ischemic stroke: I.V.: Doses should be given within the first 3 hours of the onset of symptoms; recommended total dose: 0.9 mg/kg (maximum dose should not exceed 90 mg) infused over 60 minutes.
Load with 0.09 mg/kg (10% of the 0.9 mg/kg dose) as an I.V. bolus over 1 minute, followed by 0.81 mg/kg (90% of the 0.9 mg/kg dose) as a continuous infusion over 60 minutes. Heparin should not be started for 24 hours or more after starting alteplase for stroke.
Central venous catheter clearance: Intracatheter (Cathflo® Activase® 1 mg/mL):
Patients <30>185 mm Hg systolic or >110 mm Hg diastolic); seizure at the onset of stroke; active internal bleeding; intracranial neoplasm; arteriovenous malformation or aneurysm; known bleeding diathesis including but not limited to: current use of anticoagulants or an INR >1.7, administration of heparin within 48 hours preceding the onset of stroke and an elevated aPTT at presentation, platelet count <100,000/mm3.>400 mg/dL, arterial puncture at a noncompressible site or lumbar puncture within 1 week, clinical presentation suggesting post-MI pericarditis, pregnancy, breast-feeding.
WARNINGS / PRECAUTIONS
Concerns related to adverse effects: Arrhythmias: Coronary thrombolysis may result in reperfusion arrhythmias. Bleeding: Doses >150 mg are associated with increased risk of intracranial hemorrhage; monitor all potential bleeding sites. If serious bleeding occurs, the infusion of alteplase and heparin should be stopped.
Disease-related concerns: Conditions that increase bleeding risk: For the following conditions, the risk of bleeding is higher with use of thrombolytics and should be weighed against the benefits of therapy: Recent (within 10 days) major surgery (eg, CABG, obstetrical delivery, organ biopsy, previous puncture of noncompressible vessels), cerebrovascular disease, recent gastrointestinal or genitourinary bleeding, recent trauma, hypertension (systolic BP >175 mm Hg and/or diastolic BP >110 mm Hg), high likelihood of left heart thrombus (eg, mitral stenosis with atrial fibrillation), acute pericarditis, subacute bacterial endocarditis, hemostatic defects including ones caused by severe renal or hepatic dysfunction, significant hepatic dysfunction, diabetic hemorrhagic retinopathy or other hemorrhagic ophthalmic conditions, septic thrombophlebitis or occluded AV cannula at seriously infected site and/or any other condition in which bleeding constitutes a significant hazard or would be particularly difficult to manage because of location. Myocardial infarct (MI): Appropriate use: Follow standard management for MI while infusing alteplase. Stroke: Appropriate use: Treatment of patients with acute ischemic stroke more than 3 hours after symptom onset is not recommended. Treatment of patients with minor neurological deficit or with rapidly improving symptoms is not recommended.
Concurrent drug therapy issues: Anticoagulants: Use with caution in patients receiving oral anticoagulants; increased risk of bleeding. Heparin: Concurrent heparin anticoagulation may contribute to bleeding.
Special populations: Elderly: Use with caution in patients with advanced age (eg, >75 years); increased risk of bleeding. Pregnancy: Use with caution in pregnancy; increased risk of bleeding.
Dosage form specific issues: Cathflo® Activase®: When used to restore catheter function, use Cathflo® cautiously in those patients with known or suspected catheter infections. Evaluate catheter for other causes of dysfunction before use. Avoid excessive pressure when instilling into catheter.
Other warnings/precautions: Administration: Intramuscular injections and nonessential handling of the patient should be avoided. Venipunctures should be performed carefully and only when necessary. If arterial puncture is necessary, use an upper extremity vessel that can be manually compressed.
DRUG INTERACTIONS
Aminocaproic acid (antifibrinolytic agent) may decrease effectiveness.
Drugs which affect platelet function (eg, NSAIDs, dipyridamole, ticlopidine, clopidogrel, IIb/IIIa antagonists) may potentiate the risk of hemorrhage; use with caution.
Heparin and aspirin: Use with aspirin and heparin may increase the risk of bleeding. However, aspirin and heparin were used concomitantly with alteplase in many patients in myocardial infarction or pulmonary embolism trials. This combination was prohibited in the NINDS tPA stroke trial.
Nitroglycerin may increase the hepatic clearance of alteplase, potentially reducing lytic activity (limited clinical information).
Warfarin or oral anticoagulants: Risk of bleeding may be increased during concurrent therapy.
ETHANOL / NUTRITION / HERB INTERACTIONS — Herb/Nutraceutical: Avoid cat's claw, dong quai, evening primrose, feverfew, red clover, horse chestnut, garlic, green tea, ginseng, ginkgo (all have additional antiplatelet activity).
PREGNANCY RISK FACTOR — C (show table)
LACTATION — Excretion in breast milk unknown/use caution
MONITORING PARAMETERS
When using for central venous catheter clearance: Assess catheter function by attempting to aspirate blood.
When using for management of acute myocardial infarction: Assess for evidence of cardiac reperfusion through resolution of chest pain, resolution of baseline ECG changes, preserved left ventricular function, cardiac enzyme washout phenomenon, and/or the appearance of reperfusion arrhythmias; assess for bleeding potential through clinical evidence of GI bleeding, hematuria, gingival bleeding, fibrinogen levels, fibrinogen degradation products, prothrombin times, and partial thromboplastin times.
REFERENCE RANGE
Not routinely measured; literature supports therapeutic levels of 0.52-1.8 mcg/mL
Fibrinogen: 200-400 mg/dL
Activated partial thromboplastin time (aPTT): 22.5-38.7 seconds
Prothrombin time (PT): 10.9-12.2 seconds
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms include increased incidence of intracranial bleeding.
CANADIAN BRAND NAMES — Activase® rt-PA; Cathflo® Activase®
INTERNATIONAL BRAND NAMES — Actilyse (AE, AR, AT, AU, BE, BF, BG, BH, BJ, BR, CH, CI, CL, CN, CO, CY, CZ, DE, DK, EE, EG, ES, ET, FI, FR, GB, GH, GM, GN, GR, HK, HU, ID, IN, IQ, IR, IT, JO, KE, KR, KW, LB, LR, LY, MA, ML, MR, MU, MW, MX, MY, NE, NG, NL, NO, NZ, OM, PH, PL, PT, PY, QA, SA, SC, SD, SE, SG, SL, SN, SY, TH, TW, TZ, UG, UY, YE, ZA, ZM, ZW); Activacin (JP); Activase rt-PA (CA); Cathflo Activase (CA)
MECHANISM OF ACTION — Initiates local fibrinolysis by binding to fibrin in a thrombus (clot) and converts entrapped plasminogen to plasmin
PHARMACODYNAMICS / KINETICS
Duration: >50% present in plasma cleared ~5 minutes after infusion terminated, ~80% cleared within 10 minutes
Excretion: Clearance: Rapidly from circulating plasma (550-650 mL/minute), primarily hepatic; >50% present in plasma is cleared within 5 minutes after the infusion is terminated, ~80% cleared within 10 minutes
PHARMACOLOGIC CATEGORY
Thrombolytic Agent
DOSING: ADULTS
Coronary artery thrombi: I.V. Front loading dose (weight-based):
Patients >67 kg: Total dose: 100 mg over 1.5 hours; infuse 15 mg over 1-2 minutes. Infuse 50 mg over 30 minutes. Infuse remaining 35 mg of alteplase over the next hour. See "Note."
Patients 67 kg: Infuse 15 mg I.V. bolus over 1-2 minutes, then infuse 0.75 mg/kg (not to exceed 50 mg) over next 30 minutes, followed by 0.5 mg/kg over next 60 minutes (not to exceed 35 mg). See "Note."
Note: Concurrently, begin heparin 60 units/kg bolus (maximum: 4000 units) followed by continuous infusion of 12 units/kg/hour (maximum: 1000 units/hour) and adjust to aPTT target of 1.5-2 times the upper limit of control.
Acute pulmonary embolism: I.V.: 100 mg over 2 hours.
Acute ischemic stroke: I.V.: Doses should be given within the first 3 hours of the onset of symptoms; recommended total dose: 0.9 mg/kg (maximum dose should not exceed 90 mg) infused over 60 minutes.
Load with 0.09 mg/kg (10% of the 0.9 mg/kg dose) as an I.V. bolus over 1 minute, followed by 0.81 mg/kg (90% of the 0.9 mg/kg dose) as a continuous infusion over 60 minutes. Heparin should not be started for 24 hours or more after starting alteplase for stroke.
Central venous catheter clearance: Intracatheter (Cathflo® Activase® 1 mg/mL):
Patients <30>185 mm Hg systolic or >110 mm Hg diastolic); seizure at the onset of stroke; active internal bleeding; intracranial neoplasm; arteriovenous malformation or aneurysm; known bleeding diathesis including but not limited to: current use of anticoagulants or an INR >1.7, administration of heparin within 48 hours preceding the onset of stroke and an elevated aPTT at presentation, platelet count <100,000/mm3.>400 mg/dL, arterial puncture at a noncompressible site or lumbar puncture within 1 week, clinical presentation suggesting post-MI pericarditis, pregnancy, breast-feeding.
WARNINGS / PRECAUTIONS
Concerns related to adverse effects: Arrhythmias: Coronary thrombolysis may result in reperfusion arrhythmias. Bleeding: Doses >150 mg are associated with increased risk of intracranial hemorrhage; monitor all potential bleeding sites. If serious bleeding occurs, the infusion of alteplase and heparin should be stopped.
Disease-related concerns: Conditions that increase bleeding risk: For the following conditions, the risk of bleeding is higher with use of thrombolytics and should be weighed against the benefits of therapy: Recent (within 10 days) major surgery (eg, CABG, obstetrical delivery, organ biopsy, previous puncture of noncompressible vessels), cerebrovascular disease, recent gastrointestinal or genitourinary bleeding, recent trauma, hypertension (systolic BP >175 mm Hg and/or diastolic BP >110 mm Hg), high likelihood of left heart thrombus (eg, mitral stenosis with atrial fibrillation), acute pericarditis, subacute bacterial endocarditis, hemostatic defects including ones caused by severe renal or hepatic dysfunction, significant hepatic dysfunction, diabetic hemorrhagic retinopathy or other hemorrhagic ophthalmic conditions, septic thrombophlebitis or occluded AV cannula at seriously infected site and/or any other condition in which bleeding constitutes a significant hazard or would be particularly difficult to manage because of location. Myocardial infarct (MI): Appropriate use: Follow standard management for MI while infusing alteplase. Stroke: Appropriate use: Treatment of patients with acute ischemic stroke more than 3 hours after symptom onset is not recommended. Treatment of patients with minor neurological deficit or with rapidly improving symptoms is not recommended.
Concurrent drug therapy issues: Anticoagulants: Use with caution in patients receiving oral anticoagulants; increased risk of bleeding. Heparin: Concurrent heparin anticoagulation may contribute to bleeding.
Special populations: Elderly: Use with caution in patients with advanced age (eg, >75 years); increased risk of bleeding. Pregnancy: Use with caution in pregnancy; increased risk of bleeding.
Dosage form specific issues: Cathflo® Activase®: When used to restore catheter function, use Cathflo® cautiously in those patients with known or suspected catheter infections. Evaluate catheter for other causes of dysfunction before use. Avoid excessive pressure when instilling into catheter.
Other warnings/precautions: Administration: Intramuscular injections and nonessential handling of the patient should be avoided. Venipunctures should be performed carefully and only when necessary. If arterial puncture is necessary, use an upper extremity vessel that can be manually compressed.
DRUG INTERACTIONS
Aminocaproic acid (antifibrinolytic agent) may decrease effectiveness.
Drugs which affect platelet function (eg, NSAIDs, dipyridamole, ticlopidine, clopidogrel, IIb/IIIa antagonists) may potentiate the risk of hemorrhage; use with caution.
Heparin and aspirin: Use with aspirin and heparin may increase the risk of bleeding. However, aspirin and heparin were used concomitantly with alteplase in many patients in myocardial infarction or pulmonary embolism trials. This combination was prohibited in the NINDS tPA stroke trial.
Nitroglycerin may increase the hepatic clearance of alteplase, potentially reducing lytic activity (limited clinical information).
Warfarin or oral anticoagulants: Risk of bleeding may be increased during concurrent therapy.
ETHANOL / NUTRITION / HERB INTERACTIONS — Herb/Nutraceutical: Avoid cat's claw, dong quai, evening primrose, feverfew, red clover, horse chestnut, garlic, green tea, ginseng, ginkgo (all have additional antiplatelet activity).
PREGNANCY RISK FACTOR — C (show table)
LACTATION — Excretion in breast milk unknown/use caution
MONITORING PARAMETERS
When using for central venous catheter clearance: Assess catheter function by attempting to aspirate blood.
When using for management of acute myocardial infarction: Assess for evidence of cardiac reperfusion through resolution of chest pain, resolution of baseline ECG changes, preserved left ventricular function, cardiac enzyme washout phenomenon, and/or the appearance of reperfusion arrhythmias; assess for bleeding potential through clinical evidence of GI bleeding, hematuria, gingival bleeding, fibrinogen levels, fibrinogen degradation products, prothrombin times, and partial thromboplastin times.
REFERENCE RANGE
Not routinely measured; literature supports therapeutic levels of 0.52-1.8 mcg/mL
Fibrinogen: 200-400 mg/dL
Activated partial thromboplastin time (aPTT): 22.5-38.7 seconds
Prothrombin time (PT): 10.9-12.2 seconds
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms include increased incidence of intracranial bleeding.
CANADIAN BRAND NAMES — Activase® rt-PA; Cathflo® Activase®
INTERNATIONAL BRAND NAMES — Actilyse (AE, AR, AT, AU, BE, BF, BG, BH, BJ, BR, CH, CI, CL, CN, CO, CY, CZ, DE, DK, EE, EG, ES, ET, FI, FR, GB, GH, GM, GN, GR, HK, HU, ID, IN, IQ, IR, IT, JO, KE, KR, KW, LB, LR, LY, MA, ML, MR, MU, MW, MX, MY, NE, NG, NL, NO, NZ, OM, PH, PL, PT, PY, QA, SA, SC, SD, SE, SG, SL, SN, SY, TH, TW, TZ, UG, UY, YE, ZA, ZM, ZW); Activacin (JP); Activase rt-PA (CA); Cathflo Activase (CA)
MECHANISM OF ACTION — Initiates local fibrinolysis by binding to fibrin in a thrombus (clot) and converts entrapped plasminogen to plasmin
PHARMACODYNAMICS / KINETICS
Duration: >50% present in plasma cleared ~5 minutes after infusion terminated, ~80% cleared within 10 minutes
Excretion: Clearance: Rapidly from circulating plasma (550-650 mL/minute), primarily hepatic; >50% present in plasma is cleared within 5 minutes after the infusion is terminated, ~80% cleared within 10 minutes
Alprostadil
U.S. BRAND NAMES — Caverject Impulse®; Caverject®; Edex®; Muse®; Prostin VR Pediatric®
PHARMACOLOGIC CATEGORY
Prostaglandin
DOSING: ADULTS
Erectile dysfunction:
Intracavernous (Caverject®, Edex®): Individualize dose by careful titration; doses >40 mcg (Edex®) or >60 mcg (Caverject®) are not recommended: Initial dose must be titrated in physician's office. Patient must stay in the physician's office until complete detumescence occurs; if there is no response, then the next higher dose may be given within 1 hour; if there is still no response, a 1-day interval before giving the next dose is recommended; increasing the dose or concentration in the treatment of impotence results in increasing pain and discomfort.
Vasculogenic, psychogenic, or mixed etiology: Initiate dosage titration at 2.5 mcg, increasing by 2.5 mcg to a dose of 5 mcg and then in increments of 5-10 mcg depending on the erectile response until the dose produces an erection suitable for intercourse, not lasting >1 hour; if there is absolutely no response to initial 2.5 mcg dose, the second dose may be increased to 7.5 mcg, followed by increments of 5-10 mcg
Neurogenic etiology (eg, spinal cord injury): Initiate dosage titration at 1.25 mcg, increasing to a dose of 2.5 mcg and then 5 mcg; increase further in increments 5 mcg until the dose is reached that produces an erection suitable for intercourse, not lasting >1 hour
Maintenance: Once appropriate dose has been determined, patient may self-administer injections at a frequency of no more than 3 times/week with at least 24 hours between doses
Intraurethral (Muse® Pellet):
Initial: 125-250 mcg
Maintenance: Administer as needed to achieve an erection; duration of action is about 30-60 minutes; use only two systems per 24-hour period
DOSING: PEDIATRIC
(For additional information see "Alprostadil: Pediatric drug information")
Patent ductus arteriosus I.V.:
Prostin VR Pediatric®: I.V. continuous infusion into a large vein, or alternatively through an umbilical artery catheter placed at the ductal opening: 0.05-0.1 mcg/kg/minute with therapeutic response, rate is reduced to lowest effective dosage. With unsatisfactory response, rate is increased gradually; maintenance: 0.01-0.4 mcg/kg/minute.
Note: PGE1 is usually given at an infusion rate of 0.1 mcg/kg/minute, but it is often possible to reduce the dosage to 1/2 or even 1/10 without losing the therapeutic effect. The mixing schedule is shown in the table.
Mixing Schedule
Note: 500 mcg equals 1 ampul. For a concentration of 2 mcg/mL, add 500 mcg to 250 mL; infuse at 0.05 mL/kg/minute (72 mL/kg/24 hours) For a concentration of 5 mcg/mL, add 500 mcg to 100 mL; infuse at 0.02 mL/kg/minute (28.8 mL/kg/24 hours) For a concentration of 10 mcg/mL, add 500 mcg to 50 mL; infuse at 0.01 mL/kg/minute (14.4 mL/kg/24 hours) For a concentration of 20 mcg/mL, add 500 mcg to 25 mL; infuse at 0.005 mL/kg/minute (7.2 mL/kg/24 hours)
Note: Therapeutic response is indicated by increased pH in those with acidosis or by an increase in oxygenation (PO2) usually evident within 30 minutes.
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution:
Caverject®: 20 mcg, 40 mcg [contains lactose; diluent contains benzyl alcohol]
Caverject Impulse®: 10 mcg, 20 mcg [prefilled injection system; contains lactose; diluent contains benzyl alcohol]
Edex®: 10 mcg, 20 mcg, 40 mcg [contains lactose; packaged in kits containing diluent, syringe, and alcohol swab]
Injection, solution: 500 mcg/mL (1 mL)
Prostin VR Pediatric®: 500 mcg/mL (1 mL) [contains dehydrated alcohol]
Pellet, urethral (Muse®): 125 mcg (6s), 250 mcg (6s), 500 mcg (6s), 1000 mcg (6s)
DOSAGE FORMS: CONCISE
Injection, powder for reconstitution: 10 mcg, 20 mcg, 40 mcg
Caverject®: 20 mcg, 40 mcg
Caverject Impulse®: 10 mcg, 20 mcg
Edex®: 10 mcg, 20 mcg, 40 mcg
Injection, solution: 500 mcg/mL (1 mL)
Prostin VR Pediatric®: 500 mcg/mL (1 mL)
Pellet, urethral: 125 mcg, 250 mcg, 500 mcg, 1000 mcg
Muse®: 125 mcg (6s), 250 mcg (6s), 500 mcg (6s), 1000 mcg (6s)
GENERIC EQUIVALENT AVAILABLE — Yes: Solution for injection
ADMINISTRATION — Erectile dysfunction: Use a 1/2 inch, 27- to 30-gauge needle. Inject into the dorsolateral aspect of the proximal third of the penis, avoiding visible veins; alternate side of the penis for injections.
USE
Prostin VR Pediatric®: Temporary maintenance of patency of ductus arteriosus in neonates with ductal-dependent congenital heart disease until surgery can be performed. These defects include cyanotic (eg, pulmonary atresia, pulmonary stenosis, tricuspid atresia, Fallot's tetralogy, transposition of the great vessels) and acyanotic (eg, interruption of aortic arch, coarctation of aorta, hypoplastic left ventricle) heart disease.
Caverject®: Treatment of erectile dysfunction of vasculogenic, psychogenic, or neurogenic etiology; adjunct in the diagnosis of erectile dysfunction
Edex®, Muse®: Treatment of erectile dysfunction of vasculogenic, psychogenic, or neurogenic etiology
USE - UNLABELED / INVESTIGATIONAL — Investigational: Treatment of pulmonary hypertension in infants and children with congenital heart defects with left-to-right shunts
ADVERSE REACTIONS SIGNIFICANT
Intraurethral:
>10%: Genitourinary: Penile pain, urethral burning
2% to 10%:
Central nervous system: Headache, dizziness, pain
Genitourinary: Vaginal itching (female partner), testicular pain, urethral bleeding (minor)
<2%>10%: Genitourinary: Penile pain
1% to 10%:
Cardiovascular: Hypertension
Central nervous system: Headache, dizziness
Genitourinary: Prolonged erection (>4 hours, 4%), penile fibrosis, penis disorder, penile rash, penile edema
Local: Injection site hematoma and/or bruising
<1%>10%:
Cardiovascular: Flushing
Central nervous system: Fever
Respiratory: Apnea
1% to 10%:
Cardiovascular: Bradycardia, hyper-/hypotension, tachycardia, cardiac arrest, edema
Central nervous system: Seizures, headache, dizziness
Endocrine & metabolic: Hypokalemia
Gastrointestinal: Diarrhea
Hematologic: Disseminated intravascular coagulation
Neuromuscular & skeletal: Back pain
Respiratory: Upper respiratory infection, flu syndrome, sinusitis, nasal congestion, cough
Miscellaneous: Sepsis, localized pain in structures other than the injection site
<1%>120 hours has been associated with antral hyperplasia and gastric outlet obstruction.
Special populations: Neonates: Use with caution in neonates with bleeding tendencies.
Dosage form specific issues: Muse®: When used in erectile dysfunction, syncope occurring within 1 hour of administration has been reported. The potential for drug-drug interactions may occur when prescribed concomitantly with antihypertensives. Some lowering of blood pressure may occur without symptoms, and swelling of leg veins, leg pain, perineal pain, and rapid pulse have been reported in <2%>4 hours to a prescriber immediately; inform a prescriber as soon as possible if any new penile pain, nodules, hard tissue, or signs of infection develop; the risk of transmission of blood-borne diseases is increased with use of alprostadil injections since a small amount of bleeding at the injection site is possible. Do not drive or operate heavy machinery within 1 hour of administration.
(For additional information see "Alprostadil: Patient drug information")
Erectile dysfunction: If the patient is going to be self-injecting at home, carefully assess his aseptic technique for injection and knowledge of proper disposal of the syringe, needle, and vial. Observe for signs of infection, penile fibrosis, and significant pain or priapism
PHARMACOLOGIC CATEGORY
Prostaglandin
DOSING: ADULTS
Erectile dysfunction:
Intracavernous (Caverject®, Edex®): Individualize dose by careful titration; doses >40 mcg (Edex®) or >60 mcg (Caverject®) are not recommended: Initial dose must be titrated in physician's office. Patient must stay in the physician's office until complete detumescence occurs; if there is no response, then the next higher dose may be given within 1 hour; if there is still no response, a 1-day interval before giving the next dose is recommended; increasing the dose or concentration in the treatment of impotence results in increasing pain and discomfort.
Vasculogenic, psychogenic, or mixed etiology: Initiate dosage titration at 2.5 mcg, increasing by 2.5 mcg to a dose of 5 mcg and then in increments of 5-10 mcg depending on the erectile response until the dose produces an erection suitable for intercourse, not lasting >1 hour; if there is absolutely no response to initial 2.5 mcg dose, the second dose may be increased to 7.5 mcg, followed by increments of 5-10 mcg
Neurogenic etiology (eg, spinal cord injury): Initiate dosage titration at 1.25 mcg, increasing to a dose of 2.5 mcg and then 5 mcg; increase further in increments 5 mcg until the dose is reached that produces an erection suitable for intercourse, not lasting >1 hour
Maintenance: Once appropriate dose has been determined, patient may self-administer injections at a frequency of no more than 3 times/week with at least 24 hours between doses
Intraurethral (Muse® Pellet):
Initial: 125-250 mcg
Maintenance: Administer as needed to achieve an erection; duration of action is about 30-60 minutes; use only two systems per 24-hour period
DOSING: PEDIATRIC
(For additional information see "Alprostadil: Pediatric drug information")
Patent ductus arteriosus I.V.:
Prostin VR Pediatric®: I.V. continuous infusion into a large vein, or alternatively through an umbilical artery catheter placed at the ductal opening: 0.05-0.1 mcg/kg/minute with therapeutic response, rate is reduced to lowest effective dosage. With unsatisfactory response, rate is increased gradually; maintenance: 0.01-0.4 mcg/kg/minute.
Note: PGE1 is usually given at an infusion rate of 0.1 mcg/kg/minute, but it is often possible to reduce the dosage to 1/2 or even 1/10 without losing the therapeutic effect. The mixing schedule is shown in the table.
Mixing Schedule
Note: 500 mcg equals 1 ampul. For a concentration of 2 mcg/mL, add 500 mcg to 250 mL; infuse at 0.05 mL/kg/minute (72 mL/kg/24 hours) For a concentration of 5 mcg/mL, add 500 mcg to 100 mL; infuse at 0.02 mL/kg/minute (28.8 mL/kg/24 hours) For a concentration of 10 mcg/mL, add 500 mcg to 50 mL; infuse at 0.01 mL/kg/minute (14.4 mL/kg/24 hours) For a concentration of 20 mcg/mL, add 500 mcg to 25 mL; infuse at 0.005 mL/kg/minute (7.2 mL/kg/24 hours)
Note: Therapeutic response is indicated by increased pH in those with acidosis or by an increase in oxygenation (PO2) usually evident within 30 minutes.
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution:
Caverject®: 20 mcg, 40 mcg [contains lactose; diluent contains benzyl alcohol]
Caverject Impulse®: 10 mcg, 20 mcg [prefilled injection system; contains lactose; diluent contains benzyl alcohol]
Edex®: 10 mcg, 20 mcg, 40 mcg [contains lactose; packaged in kits containing diluent, syringe, and alcohol swab]
Injection, solution: 500 mcg/mL (1 mL)
Prostin VR Pediatric®: 500 mcg/mL (1 mL) [contains dehydrated alcohol]
Pellet, urethral (Muse®): 125 mcg (6s), 250 mcg (6s), 500 mcg (6s), 1000 mcg (6s)
DOSAGE FORMS: CONCISE
Injection, powder for reconstitution: 10 mcg, 20 mcg, 40 mcg
Caverject®: 20 mcg, 40 mcg
Caverject Impulse®: 10 mcg, 20 mcg
Edex®: 10 mcg, 20 mcg, 40 mcg
Injection, solution: 500 mcg/mL (1 mL)
Prostin VR Pediatric®: 500 mcg/mL (1 mL)
Pellet, urethral: 125 mcg, 250 mcg, 500 mcg, 1000 mcg
Muse®: 125 mcg (6s), 250 mcg (6s), 500 mcg (6s), 1000 mcg (6s)
GENERIC EQUIVALENT AVAILABLE — Yes: Solution for injection
ADMINISTRATION — Erectile dysfunction: Use a 1/2 inch, 27- to 30-gauge needle. Inject into the dorsolateral aspect of the proximal third of the penis, avoiding visible veins; alternate side of the penis for injections.
USE
Prostin VR Pediatric®: Temporary maintenance of patency of ductus arteriosus in neonates with ductal-dependent congenital heart disease until surgery can be performed. These defects include cyanotic (eg, pulmonary atresia, pulmonary stenosis, tricuspid atresia, Fallot's tetralogy, transposition of the great vessels) and acyanotic (eg, interruption of aortic arch, coarctation of aorta, hypoplastic left ventricle) heart disease.
Caverject®: Treatment of erectile dysfunction of vasculogenic, psychogenic, or neurogenic etiology; adjunct in the diagnosis of erectile dysfunction
Edex®, Muse®: Treatment of erectile dysfunction of vasculogenic, psychogenic, or neurogenic etiology
USE - UNLABELED / INVESTIGATIONAL — Investigational: Treatment of pulmonary hypertension in infants and children with congenital heart defects with left-to-right shunts
ADVERSE REACTIONS SIGNIFICANT
Intraurethral:
>10%: Genitourinary: Penile pain, urethral burning
2% to 10%:
Central nervous system: Headache, dizziness, pain
Genitourinary: Vaginal itching (female partner), testicular pain, urethral bleeding (minor)
<2%>10%: Genitourinary: Penile pain
1% to 10%:
Cardiovascular: Hypertension
Central nervous system: Headache, dizziness
Genitourinary: Prolonged erection (>4 hours, 4%), penile fibrosis, penis disorder, penile rash, penile edema
Local: Injection site hematoma and/or bruising
<1%>10%:
Cardiovascular: Flushing
Central nervous system: Fever
Respiratory: Apnea
1% to 10%:
Cardiovascular: Bradycardia, hyper-/hypotension, tachycardia, cardiac arrest, edema
Central nervous system: Seizures, headache, dizziness
Endocrine & metabolic: Hypokalemia
Gastrointestinal: Diarrhea
Hematologic: Disseminated intravascular coagulation
Neuromuscular & skeletal: Back pain
Respiratory: Upper respiratory infection, flu syndrome, sinusitis, nasal congestion, cough
Miscellaneous: Sepsis, localized pain in structures other than the injection site
<1%>120 hours has been associated with antral hyperplasia and gastric outlet obstruction.
Special populations: Neonates: Use with caution in neonates with bleeding tendencies.
Dosage form specific issues: Muse®: When used in erectile dysfunction, syncope occurring within 1 hour of administration has been reported. The potential for drug-drug interactions may occur when prescribed concomitantly with antihypertensives. Some lowering of blood pressure may occur without symptoms, and swelling of leg veins, leg pain, perineal pain, and rapid pulse have been reported in <2%>4 hours to a prescriber immediately; inform a prescriber as soon as possible if any new penile pain, nodules, hard tissue, or signs of infection develop; the risk of transmission of blood-borne diseases is increased with use of alprostadil injections since a small amount of bleeding at the injection site is possible. Do not drive or operate heavy machinery within 1 hour of administration.
(For additional information see "Alprostadil: Patient drug information")
Erectile dysfunction: If the patient is going to be self-injecting at home, carefully assess his aseptic technique for injection and knowledge of proper disposal of the syringe, needle, and vial. Observe for signs of infection, penile fibrosis, and significant pain or priapism
Alprazolam
U.S. BRAND NAMES — Alprazolam Intensol®; Niravam™; Xanax XR®; Xanax®
PHARMACOLOGIC CATEGORY
Benzodiazepine
DOSING: ADULTS — Note: Treatment >4 months should be re-evaluated to determine the patient's continued need for the drug
Anxiety: Oral: Immediate release: Effective doses are 0.5-4 mg/day in divided doses; the manufacturer recommends starting at 0.25-0.5 mg 3 times/day; titrate dose upward; usual maximum: 4 mg/day. Patients requiring doses >4 mg/day should be increased cautiously. Periodic reassessment and consideration of dosage reduction is recommended.
Anxiety associated with depression: Oral: Immediate release: Average dose required: 2.5-3 mg/day in divided doses
Ethanol withdrawal (unlabeled use): Oral: Immediate release: Usual dose: 2-2.5 mg/day in divided doses
Panic disorder: Oral:
Immediate release: Initial: 0.5 mg 3 times/day; dose may be increased every 3-4 days in increments 1 mg/day. Mean effective dosage: 5-6 mg/day; many patients obtain relief at 2 mg/day, as much as 10 mg/day may be required
Extended release: 0.5-1 mg once daily; may increase dose every 3-4 days in increments 1 mg/day (range: 3-6 mg/day)
Switching from immediate release to extended release: Patients may be switched to extended release tablets by taking the total daily dose of the immediate release tablets and giving it once daily using the extended release preparation.
Preoperative sedation: Oral: 0.5 mg in evening at bedtime and 0.5 mg 1 hour before procedure
Dose reduction: Abrupt discontinuation should be avoided. Daily dose may be decreased by 0.5 mg every 3 days, however, some patients may require a slower reduction. If withdrawal symptoms occur, resume previous dose and discontinue on a less rapid schedule.
DOSING: PEDIATRIC
(For additional information see "Alprazolam: Pediatric drug information")
Anxiety (unlabeled use): Oral: Immediate release: Initial: 0.005 mg/kg/dose or 0.125 mg/dose 3 times/day; increase in increments of 0.125-0.25 mg, up to a maximum of 0.02 mg/kg/dose or 0.06 mg/kg/day (0.375-3 mg/day). See "Dose Reduction" comment in adult dosing.
Note: Treatment >4 months should be re-evaluated to determine the patient's continued need for the drug.
DOSING: ELDERLY — Initial: 0.125-0.25 mg twice daily; increase by 0.125 mg/day as needed. The smallest effective dose should be used.
Immediate release: Initial 0.25 mg 2-3 times/day
Extended release: Initial: 0.5 mg once daily
DOSING: RENAL IMPAIRMENT — No guidelines for adjustment; use caution.
DOSING: HEPATIC IMPAIRMENT — Oral: Reduce dose by 50% to 60% or avoid in cirrhosis.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, oral [concentrate]:
Alprazolam Intensol®: 1 mg/mL (30 mL)
Tablet: 0.25 mg, 0.5 mg, 1 mg, 2 mg
Xanax®: 0.25 mg, 0.5 mg, 1 mg, 2 mg
Tablet, extended release: 0.5 mg, 1 mg, 2 mg, 3 mg
Xanax XR®: 0.5 mg, 1 mg, 2 mg, 3 mg
Tablet, orally disintegrating [scored]:
Niravam™: 0.25 mg, 0.5 mg, 1 mg, 2 mg [orange flavor]
DOSAGE FORMS: CONCISE
Solution, oral [concentrate]:
Alprazolam Intensol®: 1 mg/mL
Tablet: 0.25 mg, 0.5 mg, 1 mg, 2 mg
Xanax®: 0.25 mg, 0.5 mg, 1 mg, 2 mg
Tablet, extended release: 0.5 mg, 1 mg, 2 mg, 3 mg
Xanax XR®: 0.5 mg, 1 mg, 2 mg, 3 mg
Tablet, orally disintegrating [scored]:
Niravam™: 0.25 mg, 0.5 mg, 1 mg, 2 mg
GENERIC EQUIVALENT AVAILABLE — Yes: Extended release tablet, immediate release tablet
ADMINISTRATION
Immediate release preparations: Can be administered sublingually with comparable onset and completeness of absorption.
Extended release tablet: Should be taken once daily in the morning; do not crush, break, or chew.
Orally-disintegrating tablets: Using dry hands, place tablet on top of tongue. If using one-half of tablet, immediately discard remaining half (may not remain stable). Administration with water is not necessary.
USE — Treatment of anxiety disorder (GAD); panic disorder, with or without agoraphobia; anxiety associated with depression
USE - UNLABELED / INVESTIGATIONAL — Anxiety in children
ADVERSE REACTIONS SIGNIFICANT
>10%:
Central nervous system: Abnormal coordination, cognitive disorder, depression, drowsiness, fatigue, irritability, lightheadedness, memory impairment, sedation, somnolence
Gastrointestinal: Appetite increased/decreased, constipation, salivation decreased, weight gain/loss, xerostomia
Genitourinary: Micturition difficulty
Neuromuscular & skeletal: Dysarthria
1% to 10%:
Cardiovascular: Hypotension
Central nervous system: Agitation, attention disturbance, confusion, depersonalization, derealization, disorientation, disinhibition, dizziness, dream abnormalities, fear, hallucinations, hypersomnia, nightmares, seizure, talkativeness
Dermatologic: Dermatitis, pruritus, rash
Endocrine & metabolic: Libido decreased/increased, menstrual disorders
Gastrointestinal: Salivation increased
Genitourinary: Incontinence
Hepatic: Bilirubin increased, jaundice, liver enzymes increased
Neuromuscular & skeletal: Arthralgia, ataxia, myalgia, paresthesia
Ocular: Diplopia
Respiratory: Allergic rhinitis, dyspnea
<1%>10 days). Hepatic impairment: Use with caution in patients with hepatic impairment. Impaired gag reflux: Use with caution in patients with an impaired gag reflux. Renal impairment: Use with caution in patients with renal impairment or predisposition to urate nephropathy; has weak uricosuric properties. Respiratory disease: Use with caution in patients with respiratory disease.
Concurrent drug therapy issues: CNS depressants/psychoactive medications: Use with caution in patients receiving other CNS depressants or psychoactive medication; effects with other sedative drugs or ethanol may be potentiated. High potential for interactions: Use with caution in patients taking strong CYP3A4 inhibitors, moderate or strong CYP3A4 inducers and major CYP3A4 substrates (see Drug Interactions); consider alternative agents that avoid or lessen the potential for CYP-mediated interactions.
Special populations: Debilitated patients: Use with caution in debilitated patients. Elderly: Use with caution in the elderly; benzodiazepines have been associated with falls and traumatic injury. Fall risk: Use with extreme caution in patients who are at risk of falls; benzodiazepines have been associated with falls and traumatic injury. Obese patients: Use with caution in obese patients; may have prolonged action when discontinued.
Other warnings/precautions: Appropriate use: Does not have analgesic, antidepressant, or antipsychotic properties. Breakthrough anxiety: At the end of dosing interval, breakthrough anxiety may occur. Withdrawal: Rebound or withdrawal symptoms, including seizures, may occur 18 hours to 3 days following abrupt discontinuation or large decreases in dose (more common in patients receiving >4 mg/day or prolonged treatment). Use caution when reducing dose or withdrawing therapy; decrease slowly and monitor for withdrawal symptoms. Flumazenil may cause withdrawal in patients receiving long-term benzodiazepine therapy.
RESTRICTIONS — C-IV
DRUG INTERACTIONS — Substrate of CYP3A4 (major)
CNS depressants: Sedative effects and/or respiratory depression may be additive with CNS depressants. Includes ethanol, barbiturates, opioid analgesics, and other sedative agents; monitor for increased effect.
CYP3A4 inducers: CYP3A4 inducers may decrease the levels/effects of alprazolam. Example inducers include aminoglutethimide, carbamazepine, nafcillin, nevirapine, phenobarbital, phenytoin, and rifamycins.
CYP3A4 inhibitors: May increase the levels/effects of alprazolam. Example inhibitors include azole antifungals, clarithromycin, diclofenac, doxycycline, erythromycin, imatinib, isoniazid, nefazodone, nicardipine, propofol, protease inhibitors, quinidine, telithromycin, and verapamil. Contraindicated with itraconazole and ketoconazole.
Fluoxetine: May increase plasma concentrations/effects of alprazolam.
Oral contraceptives: May increase serum levels/effects of alprazolam.
Theophylline: May partially antagonize some of the effects of benzodiazepines; monitor for decreased response; may require higher doses for sedation.
Tricyclic antidepressants: Plasma concentrations of imipramine and desipramine have been reported to be increased 31% and 20%, respectively, by concomitant administration; monitor.
ETHANOL / NUTRITION / HERB INTERACTIONS
Cigarette smoking: May decrease alprazolam concentrations up to 50%.
Ethanol: Avoid ethanol (may increase CNS depression).
Food: Alprazolam serum concentration is unlikely to be increased by grapefruit juice because of alprazolam's high oral bioavailability. The Cmax of the extended release formulation is increased by 25% when a high-fat meal is given 2 hours before dosing. Tmax is decreased 30% when food is given immediately prior to dose. Tmax is increased by 30% when food is given 1 hour after dose.
Herb/Nutraceutical: St John's wort may decrease alprazolam levels. Avoid valerian, St John's wort, kava kava, gotu kola (may increase CNS depression).
PREGNANCY RISK FACTOR — D (show table)
PREGNANCY IMPLICATIONS — Benzodiazepines have the potential to cause harm to the fetus, particularly when administered during the first trimester. In addition, withdrawal symptoms may occur in the neonate following in utero exposure. Use during pregnancy should be avoided.
LACTATION — Enters breast milk/not recommended (AAP rates "of concern")
BREAST-FEEDING CONSIDERATIONS — Symptoms of withdrawal, lethargy, and loss of body weight have been reported in infants exposed to alprazolam and/or benzodiazepines while nursing. Breast-feeding is not recommended.
PRICING — (data from drugstore.com)
Tablet, 24-hour (Alprazolam)
0.5 mg (30): $31.99
1 mg (30): $69.99
2 mg (30): $106.45
Tablet, 24-hour (Xanax XR)
0.5 mg (30): $70.04
1 mg (30): $89.89
2 mg (30): $116.75
3 mg (30): $175.13
Tablet, orally-disintegrating (Niravam)
0.5 mg (30): $41.99
0.25 mg (30): $33.99
1 mg (30): $56.99
2 mg (30): $94.99
Tablets (Alprazolam)
0.5 mg (30): $7.99
0.25 mg (30): $9.99
1 mg (30): $7.99
2 mg (30): $8.99
Tablets (Xanax)
0.5 mg (30): $40.85
0.25 mg (30): $34.09
1 mg (30): $54.86
2 mg (30): $86.39
MONITORING PARAMETERS — Respiratory and cardiovascular status
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms include somnolence, confusion, coma, and diminished reflexes. Treatment for benzodiazepine overdose is supportive. Mechanical ventilation is rarely required. Flumazenil has been shown to selectively block the binding of benzodiazepines to CNS receptors, resulting in a reversal of benzodiazepine-induced sedation; however, its use may not alter the course of overdose.
CANADIAN BRAND NAMES — Alti-Alprazolam; Apo-Alpraz® TS; Apo-Alpraz®; Gen-Alprazolam; Novo-Alprazol; Nu-Alprax; Xanax TS™; Xanax®
INTERNATIONAL BRAND NAMES — Aceprax (PY, UY); Afobam (PL); Alcelam (TH); Alganax (ID); Alnax (TH); Alpaz (PE); Alplax (AR); Alpralid (IL); Alpram (KR); Alprax (AU, HK, IN, TH); Alprazomerck (PL); Alprocontin (IN); Alprox (IL, PL, TW); Alti-Alprazolam (CA); Alviz (ID); Alzam (ZA); Alzax (KR); Alzolam (IN); Anax (TH); Anpress (TH); Ansiopax (CL); Anxirid (ZA); Apo-Alpraz (CA, SG); Apo-Alpraz TS (CA); Apraz (BR); Azor (ZA); Calmlet (ID); Cassadan (DE); Constan (JP); Daclor (DO); Dixin (CO); Drimpam (ZA); Feprax (ID); Frontal (BR); Frontin (PL); Gen-Alprazolam (CA); Helex (HR); Kalma (AU, TW); Kinax (TW); Marzolam (TH); Nalion (HK); Neupax (MX); Neurol (PL); Nirvan (CO); Novo-Alprazol (CA); Nu-Alprax (CA); Pacyl (IN); Panix (ZA); Pharnax (TH); Prazol (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Prinox (AR); Renax (HK); Solanax (JP); Tafil (CR, DE, DK, GT, HN, MX, NI, PA, SV, VE); Tafil D (MU); Tensivan (CO); Trankimazin (ES); Tranquinal (BR, EC, PE, PY, UY); Tricalma (CL, PE); Valeans (IT); Xanacine (TH); Xanagis (IL); Xanax (AE, AN, AR, AU, BB, BE, BF, BG, BH, BJ, BM, BS, BZ, CA, CH, CI, CO, CY, CZ, DE, EC, EE, EG, ET, FR, GB, GH, GM, GN, GR, GY, HK, HR, HU, IE, IQ, IR, IT, JM, JO, KE, KW, LB, LR, LY, MA, ML, MR, MU, MW, MY, NE, NG, NL, NZ, OM, PE, PK, PL, PT, QA, SA, SC, SD, SL, SN, SR, SY, TH, TT, TW, TZ, UG, YE, ZM, ZW); Xanax SR (SG); Xanax TS® (CA); Xanax XR (TW); Xanolam (ZA); Xanor (AT, FI, NO, PH, SE, ZA); Xanor XR (PH); Zacetin (KR); Zanapam (AE, BH, CY, EG, IL, IQ, IR, JO, KR, KW, LB, LY, OM, QA, SA, SY, YE); Zolam (IN); Zolarem (AE, BF, BH, BJ, CI, CY, EG, ET, GH, GM, GN, IQ, IR, JO, KE, KW, LB, LR, LY, MA, ML, MR, MU, MW, NE, NG, OM, QA, SA, SC, SD, SL, SN, SY, TZ, UG, YE, ZA, ZM, ZW); Zoldac (BF, BJ, CI, ET, GH, GM, GN, KE, LR, MA, ML, MR, MU, MW, NE, NG, SC, SD, SL, SN, TZ, UG, ZM, ZW); Zomiren (PL); Zopax (ZA); Zotran (CL); Zypraz (ID)
MECHANISM OF ACTION — Binds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron at several sites within the central nervous system, including the limbic system, reticular formation. Enhancement of the inhibitory effect of GABA on neuronal excitability results by increased neuronal membrane permeability to chloride ions. This shift in chloride ions results in hyperpolarization (a less excitable state) and stabilization.
PHARMACODYNAMICS / KINETICS
Distribution: Vd: 0.9-1.2 L/kg; enters breast milk
Protein binding: 80%
Metabolism: Hepatic via CYP3A4; forms two active metabolites (4-hydroxyalprazolam and alpha-hydroxyalprazolam)
Bioavailability: 90%
Half-life elimination:
Adults: 11.2 hours (range: 6.3-26.9)
Elderly: 16.3 hours (range: 9-26.9 hours)
Alcoholic liver disease: 19.7 hours (range: 5.8-65.3 hours)
Obesity: 21.8 hours (range: 9.9-40.4 hours)
Time to peak, serum: 1-2 hours
Excretion: Urine (as unchanged drug and metabolites)
PATIENT INFORMATION — Avoid alcohol and other CNS depressants; avoid activities needing good psychomotor coordination until CNS effects are known; drug may cause physical or psychological dependence; avoid abrupt discontinuation after prolonged use; do not crush, break, or chew extended release tablets
PHARMACOLOGIC CATEGORY
Benzodiazepine
DOSING: ADULTS — Note: Treatment >4 months should be re-evaluated to determine the patient's continued need for the drug
Anxiety: Oral: Immediate release: Effective doses are 0.5-4 mg/day in divided doses; the manufacturer recommends starting at 0.25-0.5 mg 3 times/day; titrate dose upward; usual maximum: 4 mg/day. Patients requiring doses >4 mg/day should be increased cautiously. Periodic reassessment and consideration of dosage reduction is recommended.
Anxiety associated with depression: Oral: Immediate release: Average dose required: 2.5-3 mg/day in divided doses
Ethanol withdrawal (unlabeled use): Oral: Immediate release: Usual dose: 2-2.5 mg/day in divided doses
Panic disorder: Oral:
Immediate release: Initial: 0.5 mg 3 times/day; dose may be increased every 3-4 days in increments 1 mg/day. Mean effective dosage: 5-6 mg/day; many patients obtain relief at 2 mg/day, as much as 10 mg/day may be required
Extended release: 0.5-1 mg once daily; may increase dose every 3-4 days in increments 1 mg/day (range: 3-6 mg/day)
Switching from immediate release to extended release: Patients may be switched to extended release tablets by taking the total daily dose of the immediate release tablets and giving it once daily using the extended release preparation.
Preoperative sedation: Oral: 0.5 mg in evening at bedtime and 0.5 mg 1 hour before procedure
Dose reduction: Abrupt discontinuation should be avoided. Daily dose may be decreased by 0.5 mg every 3 days, however, some patients may require a slower reduction. If withdrawal symptoms occur, resume previous dose and discontinue on a less rapid schedule.
DOSING: PEDIATRIC
(For additional information see "Alprazolam: Pediatric drug information")
Anxiety (unlabeled use): Oral: Immediate release: Initial: 0.005 mg/kg/dose or 0.125 mg/dose 3 times/day; increase in increments of 0.125-0.25 mg, up to a maximum of 0.02 mg/kg/dose or 0.06 mg/kg/day (0.375-3 mg/day). See "Dose Reduction" comment in adult dosing.
Note: Treatment >4 months should be re-evaluated to determine the patient's continued need for the drug.
DOSING: ELDERLY — Initial: 0.125-0.25 mg twice daily; increase by 0.125 mg/day as needed. The smallest effective dose should be used.
Immediate release: Initial 0.25 mg 2-3 times/day
Extended release: Initial: 0.5 mg once daily
DOSING: RENAL IMPAIRMENT — No guidelines for adjustment; use caution.
DOSING: HEPATIC IMPAIRMENT — Oral: Reduce dose by 50% to 60% or avoid in cirrhosis.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, oral [concentrate]:
Alprazolam Intensol®: 1 mg/mL (30 mL)
Tablet: 0.25 mg, 0.5 mg, 1 mg, 2 mg
Xanax®: 0.25 mg, 0.5 mg, 1 mg, 2 mg
Tablet, extended release: 0.5 mg, 1 mg, 2 mg, 3 mg
Xanax XR®: 0.5 mg, 1 mg, 2 mg, 3 mg
Tablet, orally disintegrating [scored]:
Niravam™: 0.25 mg, 0.5 mg, 1 mg, 2 mg [orange flavor]
DOSAGE FORMS: CONCISE
Solution, oral [concentrate]:
Alprazolam Intensol®: 1 mg/mL
Tablet: 0.25 mg, 0.5 mg, 1 mg, 2 mg
Xanax®: 0.25 mg, 0.5 mg, 1 mg, 2 mg
Tablet, extended release: 0.5 mg, 1 mg, 2 mg, 3 mg
Xanax XR®: 0.5 mg, 1 mg, 2 mg, 3 mg
Tablet, orally disintegrating [scored]:
Niravam™: 0.25 mg, 0.5 mg, 1 mg, 2 mg
GENERIC EQUIVALENT AVAILABLE — Yes: Extended release tablet, immediate release tablet
ADMINISTRATION
Immediate release preparations: Can be administered sublingually with comparable onset and completeness of absorption.
Extended release tablet: Should be taken once daily in the morning; do not crush, break, or chew.
Orally-disintegrating tablets: Using dry hands, place tablet on top of tongue. If using one-half of tablet, immediately discard remaining half (may not remain stable). Administration with water is not necessary.
USE — Treatment of anxiety disorder (GAD); panic disorder, with or without agoraphobia; anxiety associated with depression
USE - UNLABELED / INVESTIGATIONAL — Anxiety in children
ADVERSE REACTIONS SIGNIFICANT
>10%:
Central nervous system: Abnormal coordination, cognitive disorder, depression, drowsiness, fatigue, irritability, lightheadedness, memory impairment, sedation, somnolence
Gastrointestinal: Appetite increased/decreased, constipation, salivation decreased, weight gain/loss, xerostomia
Genitourinary: Micturition difficulty
Neuromuscular & skeletal: Dysarthria
1% to 10%:
Cardiovascular: Hypotension
Central nervous system: Agitation, attention disturbance, confusion, depersonalization, derealization, disorientation, disinhibition, dizziness, dream abnormalities, fear, hallucinations, hypersomnia, nightmares, seizure, talkativeness
Dermatologic: Dermatitis, pruritus, rash
Endocrine & metabolic: Libido decreased/increased, menstrual disorders
Gastrointestinal: Salivation increased
Genitourinary: Incontinence
Hepatic: Bilirubin increased, jaundice, liver enzymes increased
Neuromuscular & skeletal: Arthralgia, ataxia, myalgia, paresthesia
Ocular: Diplopia
Respiratory: Allergic rhinitis, dyspnea
<1%>10 days). Hepatic impairment: Use with caution in patients with hepatic impairment. Impaired gag reflux: Use with caution in patients with an impaired gag reflux. Renal impairment: Use with caution in patients with renal impairment or predisposition to urate nephropathy; has weak uricosuric properties. Respiratory disease: Use with caution in patients with respiratory disease.
Concurrent drug therapy issues: CNS depressants/psychoactive medications: Use with caution in patients receiving other CNS depressants or psychoactive medication; effects with other sedative drugs or ethanol may be potentiated. High potential for interactions: Use with caution in patients taking strong CYP3A4 inhibitors, moderate or strong CYP3A4 inducers and major CYP3A4 substrates (see Drug Interactions); consider alternative agents that avoid or lessen the potential for CYP-mediated interactions.
Special populations: Debilitated patients: Use with caution in debilitated patients. Elderly: Use with caution in the elderly; benzodiazepines have been associated with falls and traumatic injury. Fall risk: Use with extreme caution in patients who are at risk of falls; benzodiazepines have been associated with falls and traumatic injury. Obese patients: Use with caution in obese patients; may have prolonged action when discontinued.
Other warnings/precautions: Appropriate use: Does not have analgesic, antidepressant, or antipsychotic properties. Breakthrough anxiety: At the end of dosing interval, breakthrough anxiety may occur. Withdrawal: Rebound or withdrawal symptoms, including seizures, may occur 18 hours to 3 days following abrupt discontinuation or large decreases in dose (more common in patients receiving >4 mg/day or prolonged treatment). Use caution when reducing dose or withdrawing therapy; decrease slowly and monitor for withdrawal symptoms. Flumazenil may cause withdrawal in patients receiving long-term benzodiazepine therapy.
RESTRICTIONS — C-IV
DRUG INTERACTIONS — Substrate of CYP3A4 (major)
CNS depressants: Sedative effects and/or respiratory depression may be additive with CNS depressants. Includes ethanol, barbiturates, opioid analgesics, and other sedative agents; monitor for increased effect.
CYP3A4 inducers: CYP3A4 inducers may decrease the levels/effects of alprazolam. Example inducers include aminoglutethimide, carbamazepine, nafcillin, nevirapine, phenobarbital, phenytoin, and rifamycins.
CYP3A4 inhibitors: May increase the levels/effects of alprazolam. Example inhibitors include azole antifungals, clarithromycin, diclofenac, doxycycline, erythromycin, imatinib, isoniazid, nefazodone, nicardipine, propofol, protease inhibitors, quinidine, telithromycin, and verapamil. Contraindicated with itraconazole and ketoconazole.
Fluoxetine: May increase plasma concentrations/effects of alprazolam.
Oral contraceptives: May increase serum levels/effects of alprazolam.
Theophylline: May partially antagonize some of the effects of benzodiazepines; monitor for decreased response; may require higher doses for sedation.
Tricyclic antidepressants: Plasma concentrations of imipramine and desipramine have been reported to be increased 31% and 20%, respectively, by concomitant administration; monitor.
ETHANOL / NUTRITION / HERB INTERACTIONS
Cigarette smoking: May decrease alprazolam concentrations up to 50%.
Ethanol: Avoid ethanol (may increase CNS depression).
Food: Alprazolam serum concentration is unlikely to be increased by grapefruit juice because of alprazolam's high oral bioavailability. The Cmax of the extended release formulation is increased by 25% when a high-fat meal is given 2 hours before dosing. Tmax is decreased 30% when food is given immediately prior to dose. Tmax is increased by 30% when food is given 1 hour after dose.
Herb/Nutraceutical: St John's wort may decrease alprazolam levels. Avoid valerian, St John's wort, kava kava, gotu kola (may increase CNS depression).
PREGNANCY RISK FACTOR — D (show table)
PREGNANCY IMPLICATIONS — Benzodiazepines have the potential to cause harm to the fetus, particularly when administered during the first trimester. In addition, withdrawal symptoms may occur in the neonate following in utero exposure. Use during pregnancy should be avoided.
LACTATION — Enters breast milk/not recommended (AAP rates "of concern")
BREAST-FEEDING CONSIDERATIONS — Symptoms of withdrawal, lethargy, and loss of body weight have been reported in infants exposed to alprazolam and/or benzodiazepines while nursing. Breast-feeding is not recommended.
PRICING — (data from drugstore.com)
Tablet, 24-hour (Alprazolam)
0.5 mg (30): $31.99
1 mg (30): $69.99
2 mg (30): $106.45
Tablet, 24-hour (Xanax XR)
0.5 mg (30): $70.04
1 mg (30): $89.89
2 mg (30): $116.75
3 mg (30): $175.13
Tablet, orally-disintegrating (Niravam)
0.5 mg (30): $41.99
0.25 mg (30): $33.99
1 mg (30): $56.99
2 mg (30): $94.99
Tablets (Alprazolam)
0.5 mg (30): $7.99
0.25 mg (30): $9.99
1 mg (30): $7.99
2 mg (30): $8.99
Tablets (Xanax)
0.5 mg (30): $40.85
0.25 mg (30): $34.09
1 mg (30): $54.86
2 mg (30): $86.39
MONITORING PARAMETERS — Respiratory and cardiovascular status
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms include somnolence, confusion, coma, and diminished reflexes. Treatment for benzodiazepine overdose is supportive. Mechanical ventilation is rarely required. Flumazenil has been shown to selectively block the binding of benzodiazepines to CNS receptors, resulting in a reversal of benzodiazepine-induced sedation; however, its use may not alter the course of overdose.
CANADIAN BRAND NAMES — Alti-Alprazolam; Apo-Alpraz® TS; Apo-Alpraz®; Gen-Alprazolam; Novo-Alprazol; Nu-Alprax; Xanax TS™; Xanax®
INTERNATIONAL BRAND NAMES — Aceprax (PY, UY); Afobam (PL); Alcelam (TH); Alganax (ID); Alnax (TH); Alpaz (PE); Alplax (AR); Alpralid (IL); Alpram (KR); Alprax (AU, HK, IN, TH); Alprazomerck (PL); Alprocontin (IN); Alprox (IL, PL, TW); Alti-Alprazolam (CA); Alviz (ID); Alzam (ZA); Alzax (KR); Alzolam (IN); Anax (TH); Anpress (TH); Ansiopax (CL); Anxirid (ZA); Apo-Alpraz (CA, SG); Apo-Alpraz TS (CA); Apraz (BR); Azor (ZA); Calmlet (ID); Cassadan (DE); Constan (JP); Daclor (DO); Dixin (CO); Drimpam (ZA); Feprax (ID); Frontal (BR); Frontin (PL); Gen-Alprazolam (CA); Helex (HR); Kalma (AU, TW); Kinax (TW); Marzolam (TH); Nalion (HK); Neupax (MX); Neurol (PL); Nirvan (CO); Novo-Alprazol (CA); Nu-Alprax (CA); Pacyl (IN); Panix (ZA); Pharnax (TH); Prazol (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Prinox (AR); Renax (HK); Solanax (JP); Tafil (CR, DE, DK, GT, HN, MX, NI, PA, SV, VE); Tafil D (MU); Tensivan (CO); Trankimazin (ES); Tranquinal (BR, EC, PE, PY, UY); Tricalma (CL, PE); Valeans (IT); Xanacine (TH); Xanagis (IL); Xanax (AE, AN, AR, AU, BB, BE, BF, BG, BH, BJ, BM, BS, BZ, CA, CH, CI, CO, CY, CZ, DE, EC, EE, EG, ET, FR, GB, GH, GM, GN, GR, GY, HK, HR, HU, IE, IQ, IR, IT, JM, JO, KE, KW, LB, LR, LY, MA, ML, MR, MU, MW, MY, NE, NG, NL, NZ, OM, PE, PK, PL, PT, QA, SA, SC, SD, SL, SN, SR, SY, TH, TT, TW, TZ, UG, YE, ZM, ZW); Xanax SR (SG); Xanax TS® (CA); Xanax XR (TW); Xanolam (ZA); Xanor (AT, FI, NO, PH, SE, ZA); Xanor XR (PH); Zacetin (KR); Zanapam (AE, BH, CY, EG, IL, IQ, IR, JO, KR, KW, LB, LY, OM, QA, SA, SY, YE); Zolam (IN); Zolarem (AE, BF, BH, BJ, CI, CY, EG, ET, GH, GM, GN, IQ, IR, JO, KE, KW, LB, LR, LY, MA, ML, MR, MU, MW, NE, NG, OM, QA, SA, SC, SD, SL, SN, SY, TZ, UG, YE, ZA, ZM, ZW); Zoldac (BF, BJ, CI, ET, GH, GM, GN, KE, LR, MA, ML, MR, MU, MW, NE, NG, SC, SD, SL, SN, TZ, UG, ZM, ZW); Zomiren (PL); Zopax (ZA); Zotran (CL); Zypraz (ID)
MECHANISM OF ACTION — Binds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron at several sites within the central nervous system, including the limbic system, reticular formation. Enhancement of the inhibitory effect of GABA on neuronal excitability results by increased neuronal membrane permeability to chloride ions. This shift in chloride ions results in hyperpolarization (a less excitable state) and stabilization.
PHARMACODYNAMICS / KINETICS
Distribution: Vd: 0.9-1.2 L/kg; enters breast milk
Protein binding: 80%
Metabolism: Hepatic via CYP3A4; forms two active metabolites (4-hydroxyalprazolam and alpha-hydroxyalprazolam)
Bioavailability: 90%
Half-life elimination:
Adults: 11.2 hours (range: 6.3-26.9)
Elderly: 16.3 hours (range: 9-26.9 hours)
Alcoholic liver disease: 19.7 hours (range: 5.8-65.3 hours)
Obesity: 21.8 hours (range: 9.9-40.4 hours)
Time to peak, serum: 1-2 hours
Excretion: Urine (as unchanged drug and metabolites)
PATIENT INFORMATION — Avoid alcohol and other CNS depressants; avoid activities needing good psychomotor coordination until CNS effects are known; drug may cause physical or psychological dependence; avoid abrupt discontinuation after prolonged use; do not crush, break, or chew extended release tablets
Thursday, April 17, 2008
Alpha-1 proteinase inhibitor
U.S. BRAND NAMES — Aralast; Prolastin®; Zemaira®
PHARMACOLOGIC CATEGORY Antitrypsin Deficiency Agent
DOSING: ADULTS — Alpha1-antitrypsin deficiency: I.V.: 60 mg/kg once weekly
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution [preservative free]:
Aralast, Prolastin®: 500 mg, 1000 mg [packaged with diluent]
Zemaira®: 1000 mg [packaged with diluent]
DOSAGE FORMS: CONCISE Injection, powder for reconstitution[preservative free]: Aralast, Prolastin®: 500 mg, 1000 mg Zemaira®: 1000 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — For I.V. infusion only; reduce rate or temporarily discontinue infusion if adverse effects occur. Infuse at ~0.08 mL/kg/minute; actual rate may be increased or decreased based on patient response. Emergency equipment (including epinephrine) should be available during infusion. Do not mix with other agents or solutions.
USE — Replacement therapy in congenital alpha1-antitrypsin deficiency with clinical emphysema
ADVERSE REACTIONS SIGNIFICANT >10%: Hepatic: ALT/AST increased (11%; ~4 times ULN)
1% to 10%: Respiratory: Pharyngitis (2%)
<1% (Limited to important or life-threatening): Allergic reactions, bilateral pulmonary infiltrates, bronchitis, chest pain, chills, cough increased, dizziness, dyspnea, fever <102ºF (delayed up to 12 hours after treatment), flu-like syndrome, headache, hypotension, leukocytosis, lightheadedness, pain, pruritus, rash, sinusitis, somnolence, tachycardia, vasodilation, vision abnormal. Severe reactions (anaphylaxis) may occur in patients with anti-IgA antibody.
CONTRAINDICATIONS — Hypersensitivity to any component of the formulation or other A1-PI products; selective IgA deficiency with known anti-IgA antibody
WARNINGS / PRECAUTIONS — Use caution in patients at risk for fluid overload. Products are made from pooled human plasma; risk of infection is theoretical, however, any infections thought to be transmitted by these products should be reported to the manufacturer. Hepatitis B immunization may be considered. Safety and efficacy in pediatric patients have not been established.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Reproduction studies have not been conducted.
LACTATION — Excretion in breast milk unknown/use caution
DIETARY CONSIDERATIONS — Sodium content of 1 L after reconstitution:
Aralast™: 230 mEq/L
Prolastin®: 100-210 mEq/L
MONITORING PARAMETERS — Alpha1-PI serum levels; vital signs during infusion
CANADIAN BRAND NAMES — Prolastin®
INTERNATIONAL BRAND NAMES — Prolastin (CA)
MECHANISM OF ACTION — Alpha1-antitrypsin (AAT) is the principle protease inhibitor in serum. Its major physiologic role is to render proteolytic enzymes (secreted during inflammation) inactive. A decrease in AAT, as seen in congenital AAT deficiency, leads to increased elastic damage in the lung, causing emphysema.
PHARMACODYNAMICS / KINETICS Half-life elimination: Metabolic: 5.9 days (Aralast™)
Time to peak, serum: Threshold levels achieved after 3 weeks
PATIENT INFORMATION — This medication is given by injection only.
PHARMACOLOGIC CATEGORY Antitrypsin Deficiency Agent
DOSING: ADULTS — Alpha1-antitrypsin deficiency: I.V.: 60 mg/kg once weekly
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution [preservative free]:
Aralast, Prolastin®: 500 mg, 1000 mg [packaged with diluent]
Zemaira®: 1000 mg [packaged with diluent]
DOSAGE FORMS: CONCISE Injection, powder for reconstitution[preservative free]: Aralast, Prolastin®: 500 mg, 1000 mg Zemaira®: 1000 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — For I.V. infusion only; reduce rate or temporarily discontinue infusion if adverse effects occur. Infuse at ~0.08 mL/kg/minute; actual rate may be increased or decreased based on patient response. Emergency equipment (including epinephrine) should be available during infusion. Do not mix with other agents or solutions.
USE — Replacement therapy in congenital alpha1-antitrypsin deficiency with clinical emphysema
ADVERSE REACTIONS SIGNIFICANT >10%: Hepatic: ALT/AST increased (11%; ~4 times ULN)
1% to 10%: Respiratory: Pharyngitis (2%)
<1% (Limited to important or life-threatening): Allergic reactions, bilateral pulmonary infiltrates, bronchitis, chest pain, chills, cough increased, dizziness, dyspnea, fever <102ºF (delayed up to 12 hours after treatment), flu-like syndrome, headache, hypotension, leukocytosis, lightheadedness, pain, pruritus, rash, sinusitis, somnolence, tachycardia, vasodilation, vision abnormal. Severe reactions (anaphylaxis) may occur in patients with anti-IgA antibody.
CONTRAINDICATIONS — Hypersensitivity to any component of the formulation or other A1-PI products; selective IgA deficiency with known anti-IgA antibody
WARNINGS / PRECAUTIONS — Use caution in patients at risk for fluid overload. Products are made from pooled human plasma; risk of infection is theoretical, however, any infections thought to be transmitted by these products should be reported to the manufacturer. Hepatitis B immunization may be considered. Safety and efficacy in pediatric patients have not been established.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Reproduction studies have not been conducted.
LACTATION — Excretion in breast milk unknown/use caution
DIETARY CONSIDERATIONS — Sodium content of 1 L after reconstitution:
Aralast™: 230 mEq/L
Prolastin®: 100-210 mEq/L
MONITORING PARAMETERS — Alpha1-PI serum levels; vital signs during infusion
CANADIAN BRAND NAMES — Prolastin®
INTERNATIONAL BRAND NAMES — Prolastin (CA)
MECHANISM OF ACTION — Alpha1-antitrypsin (AAT) is the principle protease inhibitor in serum. Its major physiologic role is to render proteolytic enzymes (secreted during inflammation) inactive. A decrease in AAT, as seen in congenital AAT deficiency, leads to increased elastic damage in the lung, causing emphysema.
PHARMACODYNAMICS / KINETICS Half-life elimination: Metabolic: 5.9 days (Aralast™)
Time to peak, serum: Threshold levels achieved after 3 weeks
PATIENT INFORMATION — This medication is given by injection only.
Alpha-1 proteinase inhibitor
U.S. BRAND NAMES — Aralast; Prolastin®; Zemaira®
PHARMACOLOGIC CATEGORY Antitrypsin Deficiency Agent
DOSING: ADULTS — Alpha1-antitrypsin deficiency: I.V.: 60 mg/kg once weekly
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution [preservative free]:
Aralast, Prolastin®: 500 mg, 1000 mg [packaged with diluent]
Zemaira®: 1000 mg [packaged with diluent]
DOSAGE FORMS: CONCISE Injection, powder for reconstitution[preservative free]: Aralast, Prolastin®: 500 mg, 1000 mg Zemaira®: 1000 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — For I.V. infusion only; reduce rate or temporarily discontinue infusion if adverse effects occur. Infuse at ~0.08 mL/kg/minute; actual rate may be increased or decreased based on patient response. Emergency equipment (including epinephrine) should be available during infusion. Do not mix with other agents or solutions.
USE — Replacement therapy in congenital alpha1-antitrypsin deficiency with clinical emphysema
ADVERSE REACTIONS SIGNIFICANT >10%: Hepatic: ALT/AST increased (11%; ~4 times ULN)
1% to 10%: Respiratory: Pharyngitis (2%)
<1% (Limited to important or life-threatening): Allergic reactions, bilateral pulmonary infiltrates, bronchitis, chest pain, chills, cough increased, dizziness, dyspnea, fever <102ºF (delayed up to 12 hours after treatment), flu-like syndrome, headache, hypotension, leukocytosis, lightheadedness, pain, pruritus, rash, sinusitis, somnolence, tachycardia, vasodilation, vision abnormal. Severe reactions (anaphylaxis) may occur in patients with anti-IgA antibody.
CONTRAINDICATIONS — Hypersensitivity to any component of the formulation or other A1-PI products; selective IgA deficiency with known anti-IgA antibody
WARNINGS / PRECAUTIONS — Use caution in patients at risk for fluid overload. Products are made from pooled human plasma; risk of infection is theoretical, however, any infections thought to be transmitted by these products should be reported to the manufacturer. Hepatitis B immunization may be considered. Safety and efficacy in pediatric patients have not been established.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Reproduction studies have not been conducted.
LACTATION — Excretion in breast milk unknown/use caution
DIETARY CONSIDERATIONS — Sodium content of 1 L after reconstitution:
Aralast™: 230 mEq/L
Prolastin®: 100-210 mEq/L
MONITORING PARAMETERS — Alpha1-PI serum levels; vital signs during infusion
CANADIAN BRAND NAMES — Prolastin®
INTERNATIONAL BRAND NAMES — Prolastin (CA)
MECHANISM OF ACTION — Alpha1-antitrypsin (AAT) is the principle protease inhibitor in serum. Its major physiologic role is to render proteolytic enzymes (secreted during inflammation) inactive. A decrease in AAT, as seen in congenital AAT deficiency, leads to increased elastic damage in the lung, causing emphysema.
PHARMACODYNAMICS / KINETICS Half-life elimination: Metabolic: 5.9 days (Aralast™)
Time to peak, serum: Threshold levels achieved after 3 weeks
PATIENT INFORMATION — This medication is given by injection only.
PHARMACOLOGIC CATEGORY Antitrypsin Deficiency Agent
DOSING: ADULTS — Alpha1-antitrypsin deficiency: I.V.: 60 mg/kg once weekly
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution [preservative free]:
Aralast, Prolastin®: 500 mg, 1000 mg [packaged with diluent]
Zemaira®: 1000 mg [packaged with diluent]
DOSAGE FORMS: CONCISE Injection, powder for reconstitution[preservative free]: Aralast, Prolastin®: 500 mg, 1000 mg Zemaira®: 1000 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — For I.V. infusion only; reduce rate or temporarily discontinue infusion if adverse effects occur. Infuse at ~0.08 mL/kg/minute; actual rate may be increased or decreased based on patient response. Emergency equipment (including epinephrine) should be available during infusion. Do not mix with other agents or solutions.
USE — Replacement therapy in congenital alpha1-antitrypsin deficiency with clinical emphysema
ADVERSE REACTIONS SIGNIFICANT >10%: Hepatic: ALT/AST increased (11%; ~4 times ULN)
1% to 10%: Respiratory: Pharyngitis (2%)
<1% (Limited to important or life-threatening): Allergic reactions, bilateral pulmonary infiltrates, bronchitis, chest pain, chills, cough increased, dizziness, dyspnea, fever <102ºF (delayed up to 12 hours after treatment), flu-like syndrome, headache, hypotension, leukocytosis, lightheadedness, pain, pruritus, rash, sinusitis, somnolence, tachycardia, vasodilation, vision abnormal. Severe reactions (anaphylaxis) may occur in patients with anti-IgA antibody.
CONTRAINDICATIONS — Hypersensitivity to any component of the formulation or other A1-PI products; selective IgA deficiency with known anti-IgA antibody
WARNINGS / PRECAUTIONS — Use caution in patients at risk for fluid overload. Products are made from pooled human plasma; risk of infection is theoretical, however, any infections thought to be transmitted by these products should be reported to the manufacturer. Hepatitis B immunization may be considered. Safety and efficacy in pediatric patients have not been established.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Reproduction studies have not been conducted.
LACTATION — Excretion in breast milk unknown/use caution
DIETARY CONSIDERATIONS — Sodium content of 1 L after reconstitution:
Aralast™: 230 mEq/L
Prolastin®: 100-210 mEq/L
MONITORING PARAMETERS — Alpha1-PI serum levels; vital signs during infusion
CANADIAN BRAND NAMES — Prolastin®
INTERNATIONAL BRAND NAMES — Prolastin (CA)
MECHANISM OF ACTION — Alpha1-antitrypsin (AAT) is the principle protease inhibitor in serum. Its major physiologic role is to render proteolytic enzymes (secreted during inflammation) inactive. A decrease in AAT, as seen in congenital AAT deficiency, leads to increased elastic damage in the lung, causing emphysema.
PHARMACODYNAMICS / KINETICS Half-life elimination: Metabolic: 5.9 days (Aralast™)
Time to peak, serum: Threshold levels achieved after 3 weeks
PATIENT INFORMATION — This medication is given by injection only.
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