(For additional information see "Acebutolol: Patient drug information")
U.S. BRAND NAMES — Sectral®
PHARMACOLOGIC CATEGORY Antiarrhythmic Agent, Class IIBeta Blocker With Intrinsic Sympathomimetic Activity
DOSING: ADULTS Angina, ventricular arrhythmia: Oral: 400 mg/day in divided doses; maintenance: 600-1200 mg/day in divided doses; maximum: 1200 mg/day
Hypertension: Oral: 400-800 mg/day (larger doses may be divided); maximum: 1200 mg/day; usual dose range (JNC 7): 200-800 mg/day in 2 divided doses
DOSING: ELDERLY — Oral: Initial: 200-400 mg/day; dose reduction due to age-related decrease in Clcr will be necessary; do not exceed 800 mg/day.
DOSING: RENAL IMPAIRMENT Clcr 25-49 mL/minute/1.73 m2: Reduce dose by 50%.
Clcr <25 mL/minute/1.73 m2: Reduce dose by 75%.
DOSING: HEPATIC IMPAIRMENT — Use with caution.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, as hydrochloride: 200 mg, 400 mg Sectral®: 200 mg, 400 mg
DOSAGE FORMS: CONCISE Capsule, as hydrochloride: 200 mg, 400 mg Sectral®: 200 mg, 400 mg
GENERIC EQUIVALENT AVAILABLE — Yes
ADMINISTRATION — To discontinue therapy, taper dose gradually. May be administered without regard to meals.
USE — Treatment of hypertension, ventricular arrhythmias, angina
ADVERSE REACTIONS SIGNIFICANT >10%: Central nervous system: Fatigue (11%)
1% to 10%: Cardiovascular: Chest pain (2%), edema (2%), bradycardia, hypotension, CHF Central nervous system: Headache (6%), dizziness (6%), insomnia (3%), depression (2%), abnormal dreams (2%), anxiety, hyperesthesia, hypoesthesia, impotence Dermatologic: Rash (2%), pruritus Gastrointestinal: Constipation (4%), diarrhea (4%), dyspepsia (4%), nausea (4%), flatulence (3%), vomiting, abdominal pain Genitourinary: Micturition frequency (3%), dysuria, nocturia, impotence (2%) Neuromuscular & skeletal: Arthralgia (2%), myalgia (2%), back pain, joint pain Ocular: Abnormal vision (2%), conjunctivitis, dry eyes, eye pain Respiratory: Dyspnea (4%), rhinitis (2%), cough (1%), pharyngitis, wheezing
<1% (Limited to important or life-threatening): AV block, exacerbation of pre-existing renal insufficiency, hepatotoxic reaction, impotence, lichen planus, pleurisy, pneumonitis, pulmonary granulomas, systemic lupus erythematosus, urinary retention, ventricular arrhythmia
Potential adverse effects (based on experience with other beta-blocking agents) include reversible mental depression, disorientation, catatonia, short-term memory loss, emotional lability, slightly clouded sensorium, laryngospasm, respiratory distress, allergic reactions, erythematous rash, agranulocytosis, purpura, thrombocytopenia, mesenteric artery thrombosis, ischemic colitis, alopecia, Peyronie's disease, claudication
CONTRAINDICATIONS — Hypersensitivity to beta-blocking agents; uncompensated congestive heart failure; cardiogenic shock; bradycardia or second- and third-degree heart block (except in patients with a functioning artificial pacemaker); sinus node dysfunction; pregnancy (2nd and 3rd trimesters)
WARNINGS / PRECAUTIONS Disease-related concerns: Bronchospastic disease: In general, patients with bronchospastic disease should not receive beta-blockers; if used at all, should be used cautiously with close monitoring. CHF: Use with caution in patients with compensated heart failure and monitor for a worsening of the condition (beta-blockers with intrinsic sympathomimetic activity have not been demonstrated to be of value in CHF). Conduction ABNL: Consider pre-existing conditions such as sick sinus syndrome before initiating. Diabetes: Use with caution in patients with diabetes mellitus; may potentiate hypoglycemia and/or mask signs and symptoms. Hepatic impairment: Use with caution in patients with hepatic impairment. Myasthenia gravis: Use with caution in patients with myasthenia gravis. Peripheral vascular disease (PVD): Use with caution in patients with PVD (including Raynaud's). Pheochromocytoma (untreated): Adequate alpha-blockade is required prior to use of any beta-blocker. Psychiatric disease: Use with caution in patients with a history of psychiatric illness; may cause or exacerbate CNS depression. Renal impairment: Use with caution in patients with renal impairment, especially the elderly.
Special populations: Pediatrics: Safety and efficacy have not been established in children.
Other warnings/precautions: Abrupt withdrawal: Beta-blocker therapy should not be withdrawn abruptly (particularly in patients with CAD), but gradually tapered to avoid acute tachycardia, hypertension, and/or ischemia.
DRUG INTERACTIONS — Inhibits CYP2D6 (weak)
Alpha-blockers (prazosin, terazosin): Concurrent use of beta-blockers may increase risk of orthostasis.
Clonidine: Hypertensive crisis after or during withdrawal of either agent.
Drugs which slow AV conduction (digoxin): Effects may be additive with beta-blockers.
Glucagon: Acebutolol may blunt the hyperglycemic action of glucagon.
Insulin and oral hypoglycemics: Acebutolol masks the tachycardia from hypoglycemia.
NSAIDs (ibuprofen, indomethacin, naproxen, piroxicam) may reduce the antihypertensive effects of beta-blockers.
Salicylates may reduce the antihypertensive effects of beta-blockers.
Sulfonylureas: Beta-blockers may alter response to hypoglycemic agents.
Verapamil or diltiazem may have synergistic or additive pharmacological effects when taken concurrently with beta-blockers.
ETHANOL / NUTRITION / HERB INTERACTIONS Food: Peak serum acebutolol levels may be slightly decreased if taken with food.
Herb/Nutraceutical: Avoid dong quai if using for hypertension (has estrogenic activity). Avoid yohimbe, ginseng (may worsen hypertension).
PREGNANCY RISK FACTOR — B (show table) (manufacturer); D (2nd and 3rd trimesters - expert analysis)
PREGNANCY IMPLICATIONS — Acebutolol crosses the placenta. Beta-blockers have been associated with persistent bradycardia, hypotension, and IUGR; IUGR is probably related to maternal hypertension. Available evidence suggests beta-blockers are generally safe during pregnancy (JNC 7). Cases of neonatal hypoglycemia have been reported following maternal use of beta-blockers at parturition or during breast-feeding. Monitor breast-fed infant for symptoms of beta-blockade.
LACTATION — Enters breast milk/use caution
BREAST-FEEDING CONSIDERATIONS — Hypotension, bradycardia, and tachypnea have been reported in nursing infants.
DIETARY CONSIDERATIONS — May be taken without regard to meals.
PRICING — (data from drugstore.com)Capsules (Acebutolol HCl) 200 mg (60): $32.99 400 mg (30): $21.99
Capsules (Sectral) 200 mg (60): $169.99 400 mg (30): $124.99
MONITORING PARAMETERS — Blood pressure, orthostatic hypotension, heart rate, CNS effects, ECG
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms include cardiac disturbances, CNS toxicity, bronchospasm, hypoglycemia, and hyperkalemia. The most common cardiac symptoms include hypotension and bradycardia. Atrioventricular block, intraventricular conduction disturbances, cardiogenic shock, and asystole may occur with severe overdose, especially with membrane-depressant drugs (eg, propranolol). CNS effects include convulsions, coma, and respiratory arrest is commonly seen with propranolol and other membrane-depressant and lipid-soluble drugs. Treatment is symptomatic for seizures, hypotension, hyperkalemia, and hypoglycemia. Bradycardia and hypotension resistant to atropine, isoproterenol or pacing, may respond to glucagon. Wide QRS defects caused by membrane-depressant poisoning may respond to hypertonic sodium bicarbonate. Repeat-dose charcoal, hemoperfusion, or hemodialysis may be helpful.
CANADIAN BRAND NAMES — Apo-Acebutolol®; Gen-Acebutolol; Monitan®; Novo-Acebutolol; Nu-Acebutolol; Rhotral; Rhoxal-acebutolol; Sandoz-Acebutolol; Sectral®
INTERNATIONAL BRAND NAMES — Abutol (PL); ACB (NZ, SG); Acebutolol (PL); Acecor (PL); Apo-Acebutolol (CA); Beloc (CL); Cetolol (PL); Diasectral (DK, FI); Flebutol (VE); Gen-Acebutolol (CA); Grifobutol (CL); Monitan (CA); Novo-Acebutolol (CA); Nu-Acebutolol (CA); Prent (DE, IT, PT); Rhotral (CA); Rhoxal-acebutolol (CA); Sandoz-Acebutolol (CA); Sectral (AE, AN, BB, BE, BG, BH, BM, BS, BZ, CA, CH, CY, CZ, EG, ES, FR, GB, GY, HK, IE, IL, IQ, IR, IT, JM, JO, KW, LB, LY, MY, NL, OM, PL, QA, SA, SR, SY, TT, TW, YE, ZA); Sectral LP (FR)
MECHANISM OF ACTION — Competitively blocks beta1-adrenergic receptors with little or no effect on beta2-receptors except at high doses; exhibits membrane stabilizing and intrinsic sympathomimetic activity
PHARMACODYNAMICS / KINETICS Onset of action: 1-2 hours
Duration: 12-24 hours
Absorption: Oral: 40%
Protein binding: 5% to 15%
Metabolism: Extensive first-pass effect
Half-life elimination: 6-7 hours
Time to peak: 2-4 hours
Excretion: Feces (~55%); urine (35%)
PATIENT INFORMATION — Do not discontinue abruptly. Consult pharmacist or prescriber before taking with other adrenergic drugs (eg, cold medications). Take at the same time each day. May be taken without regard to meals. Use with caution while driving or performing tasks requiring alertness. Notify prescriber if CHF symptoms become worse or if other side effects occur. May mask signs of hypoglycemia in diabetics.
(For additional information see "Acebutolol: Patient drug information")
Wednesday, January 16, 2008
Acebutolol: Drug information
(For additional information see "Acebutolol: Patient drug information")
U.S. BRAND NAMES — Sectral®
PHARMACOLOGIC CATEGORY Antiarrhythmic Agent, Class IIBeta Blocker With Intrinsic Sympathomimetic Activity
DOSING: ADULTS Angina, ventricular arrhythmia: Oral: 400 mg/day in divided doses; maintenance: 600-1200 mg/day in divided doses; maximum: 1200 mg/day
Hypertension: Oral: 400-800 mg/day (larger doses may be divided); maximum: 1200 mg/day; usual dose range (JNC 7): 200-800 mg/day in 2 divided doses
DOSING: ELDERLY — Oral: Initial: 200-400 mg/day; dose reduction due to age-related decrease in Clcr will be necessary; do not exceed 800 mg/day.
DOSING: RENAL IMPAIRMENT Clcr 25-49 mL/minute/1.73 m2: Reduce dose by 50%.
Clcr <25 mL/minute/1.73 m2: Reduce dose by 75%.
DOSING: HEPATIC IMPAIRMENT — Use with caution.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, as hydrochloride: 200 mg, 400 mg Sectral®: 200 mg, 400 mg
DOSAGE FORMS: CONCISE Capsule, as hydrochloride: 200 mg, 400 mg Sectral®: 200 mg, 400 mg
GENERIC EQUIVALENT AVAILABLE — Yes
ADMINISTRATION — To discontinue therapy, taper dose gradually. May be administered without regard to meals.
USE — Treatment of hypertension, ventricular arrhythmias, angina
ADVERSE REACTIONS SIGNIFICANT >10%: Central nervous system: Fatigue (11%)
1% to 10%: Cardiovascular: Chest pain (2%), edema (2%), bradycardia, hypotension, CHF Central nervous system: Headache (6%), dizziness (6%), insomnia (3%), depression (2%), abnormal dreams (2%), anxiety, hyperesthesia, hypoesthesia, impotence Dermatologic: Rash (2%), pruritus Gastrointestinal: Constipation (4%), diarrhea (4%), dyspepsia (4%), nausea (4%), flatulence (3%), vomiting, abdominal pain Genitourinary: Micturition frequency (3%), dysuria, nocturia, impotence (2%) Neuromuscular & skeletal: Arthralgia (2%), myalgia (2%), back pain, joint pain Ocular: Abnormal vision (2%), conjunctivitis, dry eyes, eye pain Respiratory: Dyspnea (4%), rhinitis (2%), cough (1%), pharyngitis, wheezing
<1% (Limited to important or life-threatening): AV block, exacerbation of pre-existing renal insufficiency, hepatotoxic reaction, impotence, lichen planus, pleurisy, pneumonitis, pulmonary granulomas, systemic lupus erythematosus, urinary retention, ventricular arrhythmia
Potential adverse effects (based on experience with other beta-blocking agents) include reversible mental depression, disorientation, catatonia, short-term memory loss, emotional lability, slightly clouded sensorium, laryngospasm, respiratory distress, allergic reactions, erythematous rash, agranulocytosis, purpura, thrombocytopenia, mesenteric artery thrombosis, ischemic colitis, alopecia, Peyronie's disease, claudication
CONTRAINDICATIONS — Hypersensitivity to beta-blocking agents; uncompensated congestive heart failure; cardiogenic shock; bradycardia or second- and third-degree heart block (except in patients with a functioning artificial pacemaker); sinus node dysfunction; pregnancy (2nd and 3rd trimesters)
WARNINGS / PRECAUTIONS Disease-related concerns: Bronchospastic disease: In general, patients with bronchospastic disease should not receive beta-blockers; if used at all, should be used cautiously with close monitoring. CHF: Use with caution in patients with compensated heart failure and monitor for a worsening of the condition (beta-blockers with intrinsic sympathomimetic activity have not been demonstrated to be of value in CHF). Conduction ABNL: Consider pre-existing conditions such as sick sinus syndrome before initiating. Diabetes: Use with caution in patients with diabetes mellitus; may potentiate hypoglycemia and/or mask signs and symptoms. Hepatic impairment: Use with caution in patients with hepatic impairment. Myasthenia gravis: Use with caution in patients with myasthenia gravis. Peripheral vascular disease (PVD): Use with caution in patients with PVD (including Raynaud's). Pheochromocytoma (untreated): Adequate alpha-blockade is required prior to use of any beta-blocker. Psychiatric disease: Use with caution in patients with a history of psychiatric illness; may cause or exacerbate CNS depression. Renal impairment: Use with caution in patients with renal impairment, especially the elderly.
Special populations: Pediatrics: Safety and efficacy have not been established in children.
Other warnings/precautions: Abrupt withdrawal: Beta-blocker therapy should not be withdrawn abruptly (particularly in patients with CAD), but gradually tapered to avoid acute tachycardia, hypertension, and/or ischemia.
DRUG INTERACTIONS — Inhibits CYP2D6 (weak)
Alpha-blockers (prazosin, terazosin): Concurrent use of beta-blockers may increase risk of orthostasis.
Clonidine: Hypertensive crisis after or during withdrawal of either agent.
Drugs which slow AV conduction (digoxin): Effects may be additive with beta-blockers.
Glucagon: Acebutolol may blunt the hyperglycemic action of glucagon.
Insulin and oral hypoglycemics: Acebutolol masks the tachycardia from hypoglycemia.
NSAIDs (ibuprofen, indomethacin, naproxen, piroxicam) may reduce the antihypertensive effects of beta-blockers.
Salicylates may reduce the antihypertensive effects of beta-blockers.
Sulfonylureas: Beta-blockers may alter response to hypoglycemic agents.
Verapamil or diltiazem may have synergistic or additive pharmacological effects when taken concurrently with beta-blockers.
ETHANOL / NUTRITION / HERB INTERACTIONS Food: Peak serum acebutolol levels may be slightly decreased if taken with food.
Herb/Nutraceutical: Avoid dong quai if using for hypertension (has estrogenic activity). Avoid yohimbe, ginseng (may worsen hypertension).
PREGNANCY RISK FACTOR — B (show table) (manufacturer); D (2nd and 3rd trimesters - expert analysis)
PREGNANCY IMPLICATIONS — Acebutolol crosses the placenta. Beta-blockers have been associated with persistent bradycardia, hypotension, and IUGR; IUGR is probably related to maternal hypertension. Available evidence suggests beta-blockers are generally safe during pregnancy (JNC 7). Cases of neonatal hypoglycemia have been reported following maternal use of beta-blockers at parturition or during breast-feeding. Monitor breast-fed infant for symptoms of beta-blockade.
LACTATION — Enters breast milk/use caution
BREAST-FEEDING CONSIDERATIONS — Hypotension, bradycardia, and tachypnea have been reported in nursing infants.
DIETARY CONSIDERATIONS — May be taken without regard to meals.
PRICING — (data from drugstore.com)Capsules (Acebutolol HCl) 200 mg (60): $32.99 400 mg (30): $21.99
Capsules (Sectral) 200 mg (60): $169.99 400 mg (30): $124.99
MONITORING PARAMETERS — Blood pressure, orthostatic hypotension, heart rate, CNS effects, ECG
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms include cardiac disturbances, CNS toxicity, bronchospasm, hypoglycemia, and hyperkalemia. The most common cardiac symptoms include hypotension and bradycardia. Atrioventricular block, intraventricular conduction disturbances, cardiogenic shock, and asystole may occur with severe overdose, especially with membrane-depressant drugs (eg, propranolol). CNS effects include convulsions, coma, and respiratory arrest is commonly seen with propranolol and other membrane-depressant and lipid-soluble drugs. Treatment is symptomatic for seizures, hypotension, hyperkalemia, and hypoglycemia. Bradycardia and hypotension resistant to atropine, isoproterenol or pacing, may respond to glucagon. Wide QRS defects caused by membrane-depressant poisoning may respond to hypertonic sodium bicarbonate. Repeat-dose charcoal, hemoperfusion, or hemodialysis may be helpful.
CANADIAN BRAND NAMES — Apo-Acebutolol®; Gen-Acebutolol; Monitan®; Novo-Acebutolol; Nu-Acebutolol; Rhotral; Rhoxal-acebutolol; Sandoz-Acebutolol; Sectral®
INTERNATIONAL BRAND NAMES — Abutol (PL); ACB (NZ, SG); Acebutolol (PL); Acecor (PL); Apo-Acebutolol (CA); Beloc (CL); Cetolol (PL); Diasectral (DK, FI); Flebutol (VE); Gen-Acebutolol (CA); Grifobutol (CL); Monitan (CA); Novo-Acebutolol (CA); Nu-Acebutolol (CA); Prent (DE, IT, PT); Rhotral (CA); Rhoxal-acebutolol (CA); Sandoz-Acebutolol (CA); Sectral (AE, AN, BB, BE, BG, BH, BM, BS, BZ, CA, CH, CY, CZ, EG, ES, FR, GB, GY, HK, IE, IL, IQ, IR, IT, JM, JO, KW, LB, LY, MY, NL, OM, PL, QA, SA, SR, SY, TT, TW, YE, ZA); Sectral LP (FR)
MECHANISM OF ACTION — Competitively blocks beta1-adrenergic receptors with little or no effect on beta2-receptors except at high doses; exhibits membrane stabilizing and intrinsic sympathomimetic activity
PHARMACODYNAMICS / KINETICS Onset of action: 1-2 hours
Duration: 12-24 hours
Absorption: Oral: 40%
Protein binding: 5% to 15%
Metabolism: Extensive first-pass effect
Half-life elimination: 6-7 hours
Time to peak: 2-4 hours
Excretion: Feces (~55%); urine (35%)
PATIENT INFORMATION — Do not discontinue abruptly. Consult pharmacist or prescriber before taking with other adrenergic drugs (eg, cold medications). Take at the same time each day. May be taken without regard to meals. Use with caution while driving or performing tasks requiring alertness. Notify prescriber if CHF symptoms become worse or if other side effects occur. May mask signs of hypoglycemia in diabetics.
(For additional information see "Acebutolol: Patient drug information")
U.S. BRAND NAMES — Sectral®
PHARMACOLOGIC CATEGORY Antiarrhythmic Agent, Class IIBeta Blocker With Intrinsic Sympathomimetic Activity
DOSING: ADULTS Angina, ventricular arrhythmia: Oral: 400 mg/day in divided doses; maintenance: 600-1200 mg/day in divided doses; maximum: 1200 mg/day
Hypertension: Oral: 400-800 mg/day (larger doses may be divided); maximum: 1200 mg/day; usual dose range (JNC 7): 200-800 mg/day in 2 divided doses
DOSING: ELDERLY — Oral: Initial: 200-400 mg/day; dose reduction due to age-related decrease in Clcr will be necessary; do not exceed 800 mg/day.
DOSING: RENAL IMPAIRMENT Clcr 25-49 mL/minute/1.73 m2: Reduce dose by 50%.
Clcr <25 mL/minute/1.73 m2: Reduce dose by 75%.
DOSING: HEPATIC IMPAIRMENT — Use with caution.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, as hydrochloride: 200 mg, 400 mg Sectral®: 200 mg, 400 mg
DOSAGE FORMS: CONCISE Capsule, as hydrochloride: 200 mg, 400 mg Sectral®: 200 mg, 400 mg
GENERIC EQUIVALENT AVAILABLE — Yes
ADMINISTRATION — To discontinue therapy, taper dose gradually. May be administered without regard to meals.
USE — Treatment of hypertension, ventricular arrhythmias, angina
ADVERSE REACTIONS SIGNIFICANT >10%: Central nervous system: Fatigue (11%)
1% to 10%: Cardiovascular: Chest pain (2%), edema (2%), bradycardia, hypotension, CHF Central nervous system: Headache (6%), dizziness (6%), insomnia (3%), depression (2%), abnormal dreams (2%), anxiety, hyperesthesia, hypoesthesia, impotence Dermatologic: Rash (2%), pruritus Gastrointestinal: Constipation (4%), diarrhea (4%), dyspepsia (4%), nausea (4%), flatulence (3%), vomiting, abdominal pain Genitourinary: Micturition frequency (3%), dysuria, nocturia, impotence (2%) Neuromuscular & skeletal: Arthralgia (2%), myalgia (2%), back pain, joint pain Ocular: Abnormal vision (2%), conjunctivitis, dry eyes, eye pain Respiratory: Dyspnea (4%), rhinitis (2%), cough (1%), pharyngitis, wheezing
<1% (Limited to important or life-threatening): AV block, exacerbation of pre-existing renal insufficiency, hepatotoxic reaction, impotence, lichen planus, pleurisy, pneumonitis, pulmonary granulomas, systemic lupus erythematosus, urinary retention, ventricular arrhythmia
Potential adverse effects (based on experience with other beta-blocking agents) include reversible mental depression, disorientation, catatonia, short-term memory loss, emotional lability, slightly clouded sensorium, laryngospasm, respiratory distress, allergic reactions, erythematous rash, agranulocytosis, purpura, thrombocytopenia, mesenteric artery thrombosis, ischemic colitis, alopecia, Peyronie's disease, claudication
CONTRAINDICATIONS — Hypersensitivity to beta-blocking agents; uncompensated congestive heart failure; cardiogenic shock; bradycardia or second- and third-degree heart block (except in patients with a functioning artificial pacemaker); sinus node dysfunction; pregnancy (2nd and 3rd trimesters)
WARNINGS / PRECAUTIONS Disease-related concerns: Bronchospastic disease: In general, patients with bronchospastic disease should not receive beta-blockers; if used at all, should be used cautiously with close monitoring. CHF: Use with caution in patients with compensated heart failure and monitor for a worsening of the condition (beta-blockers with intrinsic sympathomimetic activity have not been demonstrated to be of value in CHF). Conduction ABNL: Consider pre-existing conditions such as sick sinus syndrome before initiating. Diabetes: Use with caution in patients with diabetes mellitus; may potentiate hypoglycemia and/or mask signs and symptoms. Hepatic impairment: Use with caution in patients with hepatic impairment. Myasthenia gravis: Use with caution in patients with myasthenia gravis. Peripheral vascular disease (PVD): Use with caution in patients with PVD (including Raynaud's). Pheochromocytoma (untreated): Adequate alpha-blockade is required prior to use of any beta-blocker. Psychiatric disease: Use with caution in patients with a history of psychiatric illness; may cause or exacerbate CNS depression. Renal impairment: Use with caution in patients with renal impairment, especially the elderly.
Special populations: Pediatrics: Safety and efficacy have not been established in children.
Other warnings/precautions: Abrupt withdrawal: Beta-blocker therapy should not be withdrawn abruptly (particularly in patients with CAD), but gradually tapered to avoid acute tachycardia, hypertension, and/or ischemia.
DRUG INTERACTIONS — Inhibits CYP2D6 (weak)
Alpha-blockers (prazosin, terazosin): Concurrent use of beta-blockers may increase risk of orthostasis.
Clonidine: Hypertensive crisis after or during withdrawal of either agent.
Drugs which slow AV conduction (digoxin): Effects may be additive with beta-blockers.
Glucagon: Acebutolol may blunt the hyperglycemic action of glucagon.
Insulin and oral hypoglycemics: Acebutolol masks the tachycardia from hypoglycemia.
NSAIDs (ibuprofen, indomethacin, naproxen, piroxicam) may reduce the antihypertensive effects of beta-blockers.
Salicylates may reduce the antihypertensive effects of beta-blockers.
Sulfonylureas: Beta-blockers may alter response to hypoglycemic agents.
Verapamil or diltiazem may have synergistic or additive pharmacological effects when taken concurrently with beta-blockers.
ETHANOL / NUTRITION / HERB INTERACTIONS Food: Peak serum acebutolol levels may be slightly decreased if taken with food.
Herb/Nutraceutical: Avoid dong quai if using for hypertension (has estrogenic activity). Avoid yohimbe, ginseng (may worsen hypertension).
PREGNANCY RISK FACTOR — B (show table) (manufacturer); D (2nd and 3rd trimesters - expert analysis)
PREGNANCY IMPLICATIONS — Acebutolol crosses the placenta. Beta-blockers have been associated with persistent bradycardia, hypotension, and IUGR; IUGR is probably related to maternal hypertension. Available evidence suggests beta-blockers are generally safe during pregnancy (JNC 7). Cases of neonatal hypoglycemia have been reported following maternal use of beta-blockers at parturition or during breast-feeding. Monitor breast-fed infant for symptoms of beta-blockade.
LACTATION — Enters breast milk/use caution
BREAST-FEEDING CONSIDERATIONS — Hypotension, bradycardia, and tachypnea have been reported in nursing infants.
DIETARY CONSIDERATIONS — May be taken without regard to meals.
PRICING — (data from drugstore.com)Capsules (Acebutolol HCl) 200 mg (60): $32.99 400 mg (30): $21.99
Capsules (Sectral) 200 mg (60): $169.99 400 mg (30): $124.99
MONITORING PARAMETERS — Blood pressure, orthostatic hypotension, heart rate, CNS effects, ECG
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms include cardiac disturbances, CNS toxicity, bronchospasm, hypoglycemia, and hyperkalemia. The most common cardiac symptoms include hypotension and bradycardia. Atrioventricular block, intraventricular conduction disturbances, cardiogenic shock, and asystole may occur with severe overdose, especially with membrane-depressant drugs (eg, propranolol). CNS effects include convulsions, coma, and respiratory arrest is commonly seen with propranolol and other membrane-depressant and lipid-soluble drugs. Treatment is symptomatic for seizures, hypotension, hyperkalemia, and hypoglycemia. Bradycardia and hypotension resistant to atropine, isoproterenol or pacing, may respond to glucagon. Wide QRS defects caused by membrane-depressant poisoning may respond to hypertonic sodium bicarbonate. Repeat-dose charcoal, hemoperfusion, or hemodialysis may be helpful.
CANADIAN BRAND NAMES — Apo-Acebutolol®; Gen-Acebutolol; Monitan®; Novo-Acebutolol; Nu-Acebutolol; Rhotral; Rhoxal-acebutolol; Sandoz-Acebutolol; Sectral®
INTERNATIONAL BRAND NAMES — Abutol (PL); ACB (NZ, SG); Acebutolol (PL); Acecor (PL); Apo-Acebutolol (CA); Beloc (CL); Cetolol (PL); Diasectral (DK, FI); Flebutol (VE); Gen-Acebutolol (CA); Grifobutol (CL); Monitan (CA); Novo-Acebutolol (CA); Nu-Acebutolol (CA); Prent (DE, IT, PT); Rhotral (CA); Rhoxal-acebutolol (CA); Sandoz-Acebutolol (CA); Sectral (AE, AN, BB, BE, BG, BH, BM, BS, BZ, CA, CH, CY, CZ, EG, ES, FR, GB, GY, HK, IE, IL, IQ, IR, IT, JM, JO, KW, LB, LY, MY, NL, OM, PL, QA, SA, SR, SY, TT, TW, YE, ZA); Sectral LP (FR)
MECHANISM OF ACTION — Competitively blocks beta1-adrenergic receptors with little or no effect on beta2-receptors except at high doses; exhibits membrane stabilizing and intrinsic sympathomimetic activity
PHARMACODYNAMICS / KINETICS Onset of action: 1-2 hours
Duration: 12-24 hours
Absorption: Oral: 40%
Protein binding: 5% to 15%
Metabolism: Extensive first-pass effect
Half-life elimination: 6-7 hours
Time to peak: 2-4 hours
Excretion: Feces (~55%); urine (35%)
PATIENT INFORMATION — Do not discontinue abruptly. Consult pharmacist or prescriber before taking with other adrenergic drugs (eg, cold medications). Take at the same time each day. May be taken without regard to meals. Use with caution while driving or performing tasks requiring alertness. Notify prescriber if CHF symptoms become worse or if other side effects occur. May mask signs of hypoglycemia in diabetics.
(For additional information see "Acebutolol: Patient drug information")
Acarbose: Drug information
(For additional information see "Acarbose: Patient drug information" and see "Acarbose: Pediatric drug information")
U.S. BRAND NAMES — Precose®
PHARMACOLOGIC CATEGORY Antidiabetic Agent, Alpha-Glucosidase Inhibitor
DOSING: ADULTS — Type 2 diabetes: Oral:
Initial: 25 mg 3 times/day
Maintenance dose: Should be adjusted at 4- to 8-week intervals based on 1-hour postprandial glucose levels and tolerance until maintenance dose is reached; maintenance dose: 50-100 mg 3 times/day. Dosage must be individualized on the basis of effectiveness and tolerance while not exceeding the maximum recommended dose.
Maximum: 60 kg: 50 mg 3 times/day >60 kg: 100 mg 3 times/day
Patients receiving sulfonylureas: Acarbose given in combination with a sulfonylurea will cause a further lowering of blood glucose and may increase the hypoglycemic potential of the sulfonylurea. If hypoglycemia occurs, appropriate adjustments in the dosage of these agents should be made.
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — Clcr <25 mL/minute: Peak plasma concentrations were 5 times higher and AUCs were 6 times larger than in volunteers with normal renal function; however, long-term clinical trials in diabetic patients with significant renal dysfunction have not been conducted and treatment of these patients with acarbose is not recommended
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet: 25 mg, 50 mg, 100 mg
DOSAGE FORMS: CONCISE Tablet: Precose®: 25 mg, 50 mg, 100 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Should be administered with the first bite of each main meal.
USE Monotherapy, as indicated as an adjunct to diet to lower blood glucose in patients with type 2 diabetes mellitus (noninsulin dependent, NIDDM) whose hyperglycemia cannot be managed on diet alone
Combination with a sulfonylurea, metformin, or insulin in patients with type 2 diabetes mellitus (noninsulin dependent, NIDDM) when diet plus acarbose do not result in adequate glycemic control. The effect of acarbose to enhance glycemic control is additive to that of other hypoglycemic agents when used in combination.
ADVERSE REACTIONS SIGNIFICANT >10%: Gastrointestinal: Abdominal pain (21%) and diarrhea (33%) tend to return to pretreatment levels over time, and the frequency and intensity of flatulence (77%) tend to abate with time Hepatic: Transaminases increased
<1% (Limited to important or life-threatening): Severe gastrointestinal distress
CONTRAINDICATIONS — Hypersensitivity to acarbose or any component of the formulation; patients with diabetic ketoacidosis or cirrhosis; patients with inflammatory bowel disease, colonic ulceration, partial intestinal obstruction, or in patients predisposed to intestinal obstruction; patients who have chronic intestinal diseases associated with marked disorders of digestion or absorption, and in patients who have conditions that may deteriorate as a result of increased gas formation in the intestine
WARNINGS / PRECAUTIONS Concerns related to adverse effects: Elevated serum transaminases: Treatment-emergent elevations of serum transaminases (AST and/or ALT) occurred in 15% of acarbose-treated patients in long-term studies. These serum transaminase elevations appear to be dose related. At doses >100 mg 3 times/day, the incidence of serum transaminase elevations greater than 3 times the upper limit of normal was 2-3 times higher in the acarbose group than in the placebo group. These elevations were asymptomatic, reversible, more common in females, and, in general, were not associated with other evidence of liver dysfunction.
Disease-related concerns: Stress-related states: It may be necessary to discontinue acarbose and administer insulin if the patient is exposed to stress (ie, fever, trauma, infection, surgery).
Concurrent drug therapy issues: Sulfonylureas: In combination with a sulfonylurea will cause a further lowering of blood glucose and may increase the hypoglycemic potential of the sulfonylurea.
Special populations: Pediatrics: Safety and efficacy have not been established in children.
DRUG INTERACTIONS Calcium channel blocking agents: May decrease the efficacy of acarbose due to hyperglycemic effects.
Corticosteroids: May decrease the efficacy of acarbose due to hyperglycemic effects.
Digoxin: Acarbose decreases the bioavailability of digoxin, resulting in lower serum concentrations.
Diuretics (including thiazides): May decrease the efficacy of acarbose due to hyperglycemic effects.
Enzyme replacement (pancrelipase, amylase): May decrease the efficacy of acarbose due to effects on carbohydrate metabolism.
Estrogens: May decrease the efficacy of acarbose due to hyperglycemic effects.
Insulin: Acarbose may increase the hypoglycemic potential of insulin. Oral glucose (dextrose) should be used in the treatment of mild-to-moderate hypoglycemia; severe hypoglycemia may require the use of either intravenous glucose infusion or glucagon injection.
Isoniazid: May decrease the efficacy of acarbose due to hyperglycemic effects.
Nicotinic acid: May decrease the efficacy of acarbose due to hyperglycemic effects.
Oral contraceptives: May decrease the efficacy of acarbose due to hyperglycemic effects.
Phenothiazines: May decrease the efficacy of acarbose due to hyperglycemic effects.
Sulfonylureas: Acarbose may increase the hypoglycemic potential of sulfonylureas. Oral glucose (dextrose) should be used in the treatment of mild-to-moderate hypoglycemia; severe hypoglycemia may require the use of either intravenous glucose infusion or glucagon injection.
Thyroid hormones: May decrease the efficacy of acarbose due to hyperglycemic effects.
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Limit ethanol.
PREGNANCY RISK FACTOR — B (show table)
PREGNANCY IMPLICATIONS — Abnormal blood glucose levels are associated with a higher incidence of congenital abnormalities. Insulin is the drug of choice for the control of diabetes mellitus during pregnancy.
LACTATION — Excretion in breast milk unknown/use caution
PRICING — (data from drugstore.com)Tablets (Precose) 25 mg (90): $79.17 50 mg (90): $81.95 100 mg (90): $94.45
MONITORING PARAMETERS — Postprandial glucose, glycosylated hemoglobin levels, serum transaminase levels should be checked every 3 months during the first year of treatment and periodically thereafter.
TOXICOLOGY / OVERDOSE COMPREHENSIVE — An overdose of acarbose will not result in hypoglycemia. An overdose may result in transient increases in flatulence, diarrhea, and abdominal discomfort which shortly subside. However, acarbose may complicate the treatment of hypoglycemia from other causes, since it will inhibit the absorption of oral disaccharides (sucrose). Oral glucose (dextrose) should be used in mild-to-moderate hypoglycemia; severe hypoglycemia should be treated with I.V. glucose. In cases of overdosage, the patient should not be given fluids or food containing carbohydrates (polysaccharides, oligosaccharides, or disaccharides) for 4-6 hours following overdose.
CANADIAN BRAND NAMES — Prandase®
INTERNATIONAL BRAND NAMES — Deglu (TW); Glibose (TW); Glicobase (IT); Glucobay (AE, AN, AR, AT, AU, BB, BE, BF, BG, BH, BJ, BM, BR, BS, BZ, CH, CI, CL, CN, CO, CR, CY, CZ, DE, DK, DO, EC, EG, ES, ET, FI, GB, GH, GM, GN, GT, GY, HK, HN, HR, HU, ID, IN, IQ, IR, IT, JM, JO, JP, KE, KR, KW, LB, LR, LY, MA, ML, MR, MU, MW, MX, MY, NE, NG, NI, NL, NO, NZ, OM, PA, PE, PH, PK, PL, PT, PY, QA, SA, SC, SD, SE, SG, SL, SN, SR, SV, SY, TH, TT, TW, TZ, UG, UY, VE, YE, ZA, ZM, ZW); Gluconase (PH); Glucor (FR); Glumida (ES); Prandase (CA, IL); Rebose (IN)
MECHANISM OF ACTION — Competitive inhibitor of pancreatic alpha-amylase and intestinal brush border alpha-glucosidases, resulting in delayed hydrolysis of ingested complex carbohydrates and disaccharides and absorption of glucose; dose-dependent reduction in postprandial serum insulin and glucose peaks; inhibits the metabolism of sucrose to glucose and fructose
PHARMACODYNAMICS / KINETICS Absorption: <2% as active drug
Metabolism: Exclusively via GI tract, principally by intestinal bacteria and digestive enzymes; 13 metabolites identified
Bioavailability: Low systemic bioavailability of parent compound; acts locally in GI tract
Excretion: Urine (~34%)
PATIENT INFORMATION — Take this medication exactly as directed, with the first bite of each main meal. It is important to continue to adhere to dietary instructions, a regular exercise program, and regular testing of urine and/or blood glucose. The risk of hypoglycemia, its symptoms and treatment, and conditions that predispose to its development should be well understood by patients and responsible family members. A source of glucose (dextrose) should be readily available to treat symptoms of low blood glucose when taking acarbose in combination with a sulfonylurea or insulin. If side effects occur, they usually develop during the first few weeks of therapy and are most often mild-to-moderate gastrointestinal effects, such as flatulence, diarrhea, or abdominal discomfort and generally diminish in frequency and intensity with time.
(For additional information see "Acarbose: Patient drug information")
U.S. BRAND NAMES — Precose®
PHARMACOLOGIC CATEGORY Antidiabetic Agent, Alpha-Glucosidase Inhibitor
DOSING: ADULTS — Type 2 diabetes: Oral:
Initial: 25 mg 3 times/day
Maintenance dose: Should be adjusted at 4- to 8-week intervals based on 1-hour postprandial glucose levels and tolerance until maintenance dose is reached; maintenance dose: 50-100 mg 3 times/day. Dosage must be individualized on the basis of effectiveness and tolerance while not exceeding the maximum recommended dose.
Maximum: 60 kg: 50 mg 3 times/day >60 kg: 100 mg 3 times/day
Patients receiving sulfonylureas: Acarbose given in combination with a sulfonylurea will cause a further lowering of blood glucose and may increase the hypoglycemic potential of the sulfonylurea. If hypoglycemia occurs, appropriate adjustments in the dosage of these agents should be made.
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — Clcr <25 mL/minute: Peak plasma concentrations were 5 times higher and AUCs were 6 times larger than in volunteers with normal renal function; however, long-term clinical trials in diabetic patients with significant renal dysfunction have not been conducted and treatment of these patients with acarbose is not recommended
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet: 25 mg, 50 mg, 100 mg
DOSAGE FORMS: CONCISE Tablet: Precose®: 25 mg, 50 mg, 100 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Should be administered with the first bite of each main meal.
USE Monotherapy, as indicated as an adjunct to diet to lower blood glucose in patients with type 2 diabetes mellitus (noninsulin dependent, NIDDM) whose hyperglycemia cannot be managed on diet alone
Combination with a sulfonylurea, metformin, or insulin in patients with type 2 diabetes mellitus (noninsulin dependent, NIDDM) when diet plus acarbose do not result in adequate glycemic control. The effect of acarbose to enhance glycemic control is additive to that of other hypoglycemic agents when used in combination.
ADVERSE REACTIONS SIGNIFICANT >10%: Gastrointestinal: Abdominal pain (21%) and diarrhea (33%) tend to return to pretreatment levels over time, and the frequency and intensity of flatulence (77%) tend to abate with time Hepatic: Transaminases increased
<1% (Limited to important or life-threatening): Severe gastrointestinal distress
CONTRAINDICATIONS — Hypersensitivity to acarbose or any component of the formulation; patients with diabetic ketoacidosis or cirrhosis; patients with inflammatory bowel disease, colonic ulceration, partial intestinal obstruction, or in patients predisposed to intestinal obstruction; patients who have chronic intestinal diseases associated with marked disorders of digestion or absorption, and in patients who have conditions that may deteriorate as a result of increased gas formation in the intestine
WARNINGS / PRECAUTIONS Concerns related to adverse effects: Elevated serum transaminases: Treatment-emergent elevations of serum transaminases (AST and/or ALT) occurred in 15% of acarbose-treated patients in long-term studies. These serum transaminase elevations appear to be dose related. At doses >100 mg 3 times/day, the incidence of serum transaminase elevations greater than 3 times the upper limit of normal was 2-3 times higher in the acarbose group than in the placebo group. These elevations were asymptomatic, reversible, more common in females, and, in general, were not associated with other evidence of liver dysfunction.
Disease-related concerns: Stress-related states: It may be necessary to discontinue acarbose and administer insulin if the patient is exposed to stress (ie, fever, trauma, infection, surgery).
Concurrent drug therapy issues: Sulfonylureas: In combination with a sulfonylurea will cause a further lowering of blood glucose and may increase the hypoglycemic potential of the sulfonylurea.
Special populations: Pediatrics: Safety and efficacy have not been established in children.
DRUG INTERACTIONS Calcium channel blocking agents: May decrease the efficacy of acarbose due to hyperglycemic effects.
Corticosteroids: May decrease the efficacy of acarbose due to hyperglycemic effects.
Digoxin: Acarbose decreases the bioavailability of digoxin, resulting in lower serum concentrations.
Diuretics (including thiazides): May decrease the efficacy of acarbose due to hyperglycemic effects.
Enzyme replacement (pancrelipase, amylase): May decrease the efficacy of acarbose due to effects on carbohydrate metabolism.
Estrogens: May decrease the efficacy of acarbose due to hyperglycemic effects.
Insulin: Acarbose may increase the hypoglycemic potential of insulin. Oral glucose (dextrose) should be used in the treatment of mild-to-moderate hypoglycemia; severe hypoglycemia may require the use of either intravenous glucose infusion or glucagon injection.
Isoniazid: May decrease the efficacy of acarbose due to hyperglycemic effects.
Nicotinic acid: May decrease the efficacy of acarbose due to hyperglycemic effects.
Oral contraceptives: May decrease the efficacy of acarbose due to hyperglycemic effects.
Phenothiazines: May decrease the efficacy of acarbose due to hyperglycemic effects.
Sulfonylureas: Acarbose may increase the hypoglycemic potential of sulfonylureas. Oral glucose (dextrose) should be used in the treatment of mild-to-moderate hypoglycemia; severe hypoglycemia may require the use of either intravenous glucose infusion or glucagon injection.
Thyroid hormones: May decrease the efficacy of acarbose due to hyperglycemic effects.
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Limit ethanol.
PREGNANCY RISK FACTOR — B (show table)
PREGNANCY IMPLICATIONS — Abnormal blood glucose levels are associated with a higher incidence of congenital abnormalities. Insulin is the drug of choice for the control of diabetes mellitus during pregnancy.
LACTATION — Excretion in breast milk unknown/use caution
PRICING — (data from drugstore.com)Tablets (Precose) 25 mg (90): $79.17 50 mg (90): $81.95 100 mg (90): $94.45
MONITORING PARAMETERS — Postprandial glucose, glycosylated hemoglobin levels, serum transaminase levels should be checked every 3 months during the first year of treatment and periodically thereafter.
TOXICOLOGY / OVERDOSE COMPREHENSIVE — An overdose of acarbose will not result in hypoglycemia. An overdose may result in transient increases in flatulence, diarrhea, and abdominal discomfort which shortly subside. However, acarbose may complicate the treatment of hypoglycemia from other causes, since it will inhibit the absorption of oral disaccharides (sucrose). Oral glucose (dextrose) should be used in mild-to-moderate hypoglycemia; severe hypoglycemia should be treated with I.V. glucose. In cases of overdosage, the patient should not be given fluids or food containing carbohydrates (polysaccharides, oligosaccharides, or disaccharides) for 4-6 hours following overdose.
CANADIAN BRAND NAMES — Prandase®
INTERNATIONAL BRAND NAMES — Deglu (TW); Glibose (TW); Glicobase (IT); Glucobay (AE, AN, AR, AT, AU, BB, BE, BF, BG, BH, BJ, BM, BR, BS, BZ, CH, CI, CL, CN, CO, CR, CY, CZ, DE, DK, DO, EC, EG, ES, ET, FI, GB, GH, GM, GN, GT, GY, HK, HN, HR, HU, ID, IN, IQ, IR, IT, JM, JO, JP, KE, KR, KW, LB, LR, LY, MA, ML, MR, MU, MW, MX, MY, NE, NG, NI, NL, NO, NZ, OM, PA, PE, PH, PK, PL, PT, PY, QA, SA, SC, SD, SE, SG, SL, SN, SR, SV, SY, TH, TT, TW, TZ, UG, UY, VE, YE, ZA, ZM, ZW); Gluconase (PH); Glucor (FR); Glumida (ES); Prandase (CA, IL); Rebose (IN)
MECHANISM OF ACTION — Competitive inhibitor of pancreatic alpha-amylase and intestinal brush border alpha-glucosidases, resulting in delayed hydrolysis of ingested complex carbohydrates and disaccharides and absorption of glucose; dose-dependent reduction in postprandial serum insulin and glucose peaks; inhibits the metabolism of sucrose to glucose and fructose
PHARMACODYNAMICS / KINETICS Absorption: <2% as active drug
Metabolism: Exclusively via GI tract, principally by intestinal bacteria and digestive enzymes; 13 metabolites identified
Bioavailability: Low systemic bioavailability of parent compound; acts locally in GI tract
Excretion: Urine (~34%)
PATIENT INFORMATION — Take this medication exactly as directed, with the first bite of each main meal. It is important to continue to adhere to dietary instructions, a regular exercise program, and regular testing of urine and/or blood glucose. The risk of hypoglycemia, its symptoms and treatment, and conditions that predispose to its development should be well understood by patients and responsible family members. A source of glucose (dextrose) should be readily available to treat symptoms of low blood glucose when taking acarbose in combination with a sulfonylurea or insulin. If side effects occur, they usually develop during the first few weeks of therapy and are most often mild-to-moderate gastrointestinal effects, such as flatulence, diarrhea, or abdominal discomfort and generally diminish in frequency and intensity with time.
(For additional information see "Acarbose: Patient drug information")
Acarbose: Drug information
(For additional information see "Acarbose: Patient drug information" and see "Acarbose: Pediatric drug information")
U.S. BRAND NAMES — Precose®
PHARMACOLOGIC CATEGORY Antidiabetic Agent, Alpha-Glucosidase Inhibitor
DOSING: ADULTS — Type 2 diabetes: Oral:
Initial: 25 mg 3 times/day
Maintenance dose: Should be adjusted at 4- to 8-week intervals based on 1-hour postprandial glucose levels and tolerance until maintenance dose is reached; maintenance dose: 50-100 mg 3 times/day. Dosage must be individualized on the basis of effectiveness and tolerance while not exceeding the maximum recommended dose.
Maximum: 60 kg: 50 mg 3 times/day >60 kg: 100 mg 3 times/day
Patients receiving sulfonylureas: Acarbose given in combination with a sulfonylurea will cause a further lowering of blood glucose and may increase the hypoglycemic potential of the sulfonylurea. If hypoglycemia occurs, appropriate adjustments in the dosage of these agents should be made.
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — Clcr <25 mL/minute: Peak plasma concentrations were 5 times higher and AUCs were 6 times larger than in volunteers with normal renal function; however, long-term clinical trials in diabetic patients with significant renal dysfunction have not been conducted and treatment of these patients with acarbose is not recommended
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet: 25 mg, 50 mg, 100 mg
DOSAGE FORMS: CONCISE Tablet: Precose®: 25 mg, 50 mg, 100 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Should be administered with the first bite of each main meal.
USE Monotherapy, as indicated as an adjunct to diet to lower blood glucose in patients with type 2 diabetes mellitus (noninsulin dependent, NIDDM) whose hyperglycemia cannot be managed on diet alone
Combination with a sulfonylurea, metformin, or insulin in patients with type 2 diabetes mellitus (noninsulin dependent, NIDDM) when diet plus acarbose do not result in adequate glycemic control. The effect of acarbose to enhance glycemic control is additive to that of other hypoglycemic agents when used in combination.
ADVERSE REACTIONS SIGNIFICANT >10%: Gastrointestinal: Abdominal pain (21%) and diarrhea (33%) tend to return to pretreatment levels over time, and the frequency and intensity of flatulence (77%) tend to abate with time Hepatic: Transaminases increased
<1% (Limited to important or life-threatening): Severe gastrointestinal distress
CONTRAINDICATIONS — Hypersensitivity to acarbose or any component of the formulation; patients with diabetic ketoacidosis or cirrhosis; patients with inflammatory bowel disease, colonic ulceration, partial intestinal obstruction, or in patients predisposed to intestinal obstruction; patients who have chronic intestinal diseases associated with marked disorders of digestion or absorption, and in patients who have conditions that may deteriorate as a result of increased gas formation in the intestine
WARNINGS / PRECAUTIONS Concerns related to adverse effects: Elevated serum transaminases: Treatment-emergent elevations of serum transaminases (AST and/or ALT) occurred in 15% of acarbose-treated patients in long-term studies. These serum transaminase elevations appear to be dose related. At doses >100 mg 3 times/day, the incidence of serum transaminase elevations greater than 3 times the upper limit of normal was 2-3 times higher in the acarbose group than in the placebo group. These elevations were asymptomatic, reversible, more common in females, and, in general, were not associated with other evidence of liver dysfunction.
Disease-related concerns: Stress-related states: It may be necessary to discontinue acarbose and administer insulin if the patient is exposed to stress (ie, fever, trauma, infection, surgery).
Concurrent drug therapy issues: Sulfonylureas: In combination with a sulfonylurea will cause a further lowering of blood glucose and may increase the hypoglycemic potential of the sulfonylurea.
Special populations: Pediatrics: Safety and efficacy have not been established in children.
DRUG INTERACTIONS Calcium channel blocking agents: May decrease the efficacy of acarbose due to hyperglycemic effects.
Corticosteroids: May decrease the efficacy of acarbose due to hyperglycemic effects.
Digoxin: Acarbose decreases the bioavailability of digoxin, resulting in lower serum concentrations.
Diuretics (including thiazides): May decrease the efficacy of acarbose due to hyperglycemic effects.
Enzyme replacement (pancrelipase, amylase): May decrease the efficacy of acarbose due to effects on carbohydrate metabolism.
Estrogens: May decrease the efficacy of acarbose due to hyperglycemic effects.
Insulin: Acarbose may increase the hypoglycemic potential of insulin. Oral glucose (dextrose) should be used in the treatment of mild-to-moderate hypoglycemia; severe hypoglycemia may require the use of either intravenous glucose infusion or glucagon injection.
Isoniazid: May decrease the efficacy of acarbose due to hyperglycemic effects.
Nicotinic acid: May decrease the efficacy of acarbose due to hyperglycemic effects.
Oral contraceptives: May decrease the efficacy of acarbose due to hyperglycemic effects.
Phenothiazines: May decrease the efficacy of acarbose due to hyperglycemic effects.
Sulfonylureas: Acarbose may increase the hypoglycemic potential of sulfonylureas. Oral glucose (dextrose) should be used in the treatment of mild-to-moderate hypoglycemia; severe hypoglycemia may require the use of either intravenous glucose infusion or glucagon injection.
Thyroid hormones: May decrease the efficacy of acarbose due to hyperglycemic effects.
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Limit ethanol.
PREGNANCY RISK FACTOR — B (show table)
PREGNANCY IMPLICATIONS — Abnormal blood glucose levels are associated with a higher incidence of congenital abnormalities. Insulin is the drug of choice for the control of diabetes mellitus during pregnancy.
LACTATION — Excretion in breast milk unknown/use caution
PRICING — (data from drugstore.com)Tablets (Precose) 25 mg (90): $79.17 50 mg (90): $81.95 100 mg (90): $94.45
MONITORING PARAMETERS — Postprandial glucose, glycosylated hemoglobin levels, serum transaminase levels should be checked every 3 months during the first year of treatment and periodically thereafter.
TOXICOLOGY / OVERDOSE COMPREHENSIVE — An overdose of acarbose will not result in hypoglycemia. An overdose may result in transient increases in flatulence, diarrhea, and abdominal discomfort which shortly subside. However, acarbose may complicate the treatment of hypoglycemia from other causes, since it will inhibit the absorption of oral disaccharides (sucrose). Oral glucose (dextrose) should be used in mild-to-moderate hypoglycemia; severe hypoglycemia should be treated with I.V. glucose. In cases of overdosage, the patient should not be given fluids or food containing carbohydrates (polysaccharides, oligosaccharides, or disaccharides) for 4-6 hours following overdose.
CANADIAN BRAND NAMES — Prandase®
INTERNATIONAL BRAND NAMES — Deglu (TW); Glibose (TW); Glicobase (IT); Glucobay (AE, AN, AR, AT, AU, BB, BE, BF, BG, BH, BJ, BM, BR, BS, BZ, CH, CI, CL, CN, CO, CR, CY, CZ, DE, DK, DO, EC, EG, ES, ET, FI, GB, GH, GM, GN, GT, GY, HK, HN, HR, HU, ID, IN, IQ, IR, IT, JM, JO, JP, KE, KR, KW, LB, LR, LY, MA, ML, MR, MU, MW, MX, MY, NE, NG, NI, NL, NO, NZ, OM, PA, PE, PH, PK, PL, PT, PY, QA, SA, SC, SD, SE, SG, SL, SN, SR, SV, SY, TH, TT, TW, TZ, UG, UY, VE, YE, ZA, ZM, ZW); Gluconase (PH); Glucor (FR); Glumida (ES); Prandase (CA, IL); Rebose (IN)
MECHANISM OF ACTION — Competitive inhibitor of pancreatic alpha-amylase and intestinal brush border alpha-glucosidases, resulting in delayed hydrolysis of ingested complex carbohydrates and disaccharides and absorption of glucose; dose-dependent reduction in postprandial serum insulin and glucose peaks; inhibits the metabolism of sucrose to glucose and fructose
PHARMACODYNAMICS / KINETICS Absorption: <2% as active drug
Metabolism: Exclusively via GI tract, principally by intestinal bacteria and digestive enzymes; 13 metabolites identified
Bioavailability: Low systemic bioavailability of parent compound; acts locally in GI tract
Excretion: Urine (~34%)
PATIENT INFORMATION — Take this medication exactly as directed, with the first bite of each main meal. It is important to continue to adhere to dietary instructions, a regular exercise program, and regular testing of urine and/or blood glucose. The risk of hypoglycemia, its symptoms and treatment, and conditions that predispose to its development should be well understood by patients and responsible family members. A source of glucose (dextrose) should be readily available to treat symptoms of low blood glucose when taking acarbose in combination with a sulfonylurea or insulin. If side effects occur, they usually develop during the first few weeks of therapy and are most often mild-to-moderate gastrointestinal effects, such as flatulence, diarrhea, or abdominal discomfort and generally diminish in frequency and intensity with time.
(For additional information see "Acarbose: Patient drug information")
U.S. BRAND NAMES — Precose®
PHARMACOLOGIC CATEGORY Antidiabetic Agent, Alpha-Glucosidase Inhibitor
DOSING: ADULTS — Type 2 diabetes: Oral:
Initial: 25 mg 3 times/day
Maintenance dose: Should be adjusted at 4- to 8-week intervals based on 1-hour postprandial glucose levels and tolerance until maintenance dose is reached; maintenance dose: 50-100 mg 3 times/day. Dosage must be individualized on the basis of effectiveness and tolerance while not exceeding the maximum recommended dose.
Maximum: 60 kg: 50 mg 3 times/day >60 kg: 100 mg 3 times/day
Patients receiving sulfonylureas: Acarbose given in combination with a sulfonylurea will cause a further lowering of blood glucose and may increase the hypoglycemic potential of the sulfonylurea. If hypoglycemia occurs, appropriate adjustments in the dosage of these agents should be made.
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — Clcr <25 mL/minute: Peak plasma concentrations were 5 times higher and AUCs were 6 times larger than in volunteers with normal renal function; however, long-term clinical trials in diabetic patients with significant renal dysfunction have not been conducted and treatment of these patients with acarbose is not recommended
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet: 25 mg, 50 mg, 100 mg
DOSAGE FORMS: CONCISE Tablet: Precose®: 25 mg, 50 mg, 100 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Should be administered with the first bite of each main meal.
USE Monotherapy, as indicated as an adjunct to diet to lower blood glucose in patients with type 2 diabetes mellitus (noninsulin dependent, NIDDM) whose hyperglycemia cannot be managed on diet alone
Combination with a sulfonylurea, metformin, or insulin in patients with type 2 diabetes mellitus (noninsulin dependent, NIDDM) when diet plus acarbose do not result in adequate glycemic control. The effect of acarbose to enhance glycemic control is additive to that of other hypoglycemic agents when used in combination.
ADVERSE REACTIONS SIGNIFICANT >10%: Gastrointestinal: Abdominal pain (21%) and diarrhea (33%) tend to return to pretreatment levels over time, and the frequency and intensity of flatulence (77%) tend to abate with time Hepatic: Transaminases increased
<1% (Limited to important or life-threatening): Severe gastrointestinal distress
CONTRAINDICATIONS — Hypersensitivity to acarbose or any component of the formulation; patients with diabetic ketoacidosis or cirrhosis; patients with inflammatory bowel disease, colonic ulceration, partial intestinal obstruction, or in patients predisposed to intestinal obstruction; patients who have chronic intestinal diseases associated with marked disorders of digestion or absorption, and in patients who have conditions that may deteriorate as a result of increased gas formation in the intestine
WARNINGS / PRECAUTIONS Concerns related to adverse effects: Elevated serum transaminases: Treatment-emergent elevations of serum transaminases (AST and/or ALT) occurred in 15% of acarbose-treated patients in long-term studies. These serum transaminase elevations appear to be dose related. At doses >100 mg 3 times/day, the incidence of serum transaminase elevations greater than 3 times the upper limit of normal was 2-3 times higher in the acarbose group than in the placebo group. These elevations were asymptomatic, reversible, more common in females, and, in general, were not associated with other evidence of liver dysfunction.
Disease-related concerns: Stress-related states: It may be necessary to discontinue acarbose and administer insulin if the patient is exposed to stress (ie, fever, trauma, infection, surgery).
Concurrent drug therapy issues: Sulfonylureas: In combination with a sulfonylurea will cause a further lowering of blood glucose and may increase the hypoglycemic potential of the sulfonylurea.
Special populations: Pediatrics: Safety and efficacy have not been established in children.
DRUG INTERACTIONS Calcium channel blocking agents: May decrease the efficacy of acarbose due to hyperglycemic effects.
Corticosteroids: May decrease the efficacy of acarbose due to hyperglycemic effects.
Digoxin: Acarbose decreases the bioavailability of digoxin, resulting in lower serum concentrations.
Diuretics (including thiazides): May decrease the efficacy of acarbose due to hyperglycemic effects.
Enzyme replacement (pancrelipase, amylase): May decrease the efficacy of acarbose due to effects on carbohydrate metabolism.
Estrogens: May decrease the efficacy of acarbose due to hyperglycemic effects.
Insulin: Acarbose may increase the hypoglycemic potential of insulin. Oral glucose (dextrose) should be used in the treatment of mild-to-moderate hypoglycemia; severe hypoglycemia may require the use of either intravenous glucose infusion or glucagon injection.
Isoniazid: May decrease the efficacy of acarbose due to hyperglycemic effects.
Nicotinic acid: May decrease the efficacy of acarbose due to hyperglycemic effects.
Oral contraceptives: May decrease the efficacy of acarbose due to hyperglycemic effects.
Phenothiazines: May decrease the efficacy of acarbose due to hyperglycemic effects.
Sulfonylureas: Acarbose may increase the hypoglycemic potential of sulfonylureas. Oral glucose (dextrose) should be used in the treatment of mild-to-moderate hypoglycemia; severe hypoglycemia may require the use of either intravenous glucose infusion or glucagon injection.
Thyroid hormones: May decrease the efficacy of acarbose due to hyperglycemic effects.
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Limit ethanol.
PREGNANCY RISK FACTOR — B (show table)
PREGNANCY IMPLICATIONS — Abnormal blood glucose levels are associated with a higher incidence of congenital abnormalities. Insulin is the drug of choice for the control of diabetes mellitus during pregnancy.
LACTATION — Excretion in breast milk unknown/use caution
PRICING — (data from drugstore.com)Tablets (Precose) 25 mg (90): $79.17 50 mg (90): $81.95 100 mg (90): $94.45
MONITORING PARAMETERS — Postprandial glucose, glycosylated hemoglobin levels, serum transaminase levels should be checked every 3 months during the first year of treatment and periodically thereafter.
TOXICOLOGY / OVERDOSE COMPREHENSIVE — An overdose of acarbose will not result in hypoglycemia. An overdose may result in transient increases in flatulence, diarrhea, and abdominal discomfort which shortly subside. However, acarbose may complicate the treatment of hypoglycemia from other causes, since it will inhibit the absorption of oral disaccharides (sucrose). Oral glucose (dextrose) should be used in mild-to-moderate hypoglycemia; severe hypoglycemia should be treated with I.V. glucose. In cases of overdosage, the patient should not be given fluids or food containing carbohydrates (polysaccharides, oligosaccharides, or disaccharides) for 4-6 hours following overdose.
CANADIAN BRAND NAMES — Prandase®
INTERNATIONAL BRAND NAMES — Deglu (TW); Glibose (TW); Glicobase (IT); Glucobay (AE, AN, AR, AT, AU, BB, BE, BF, BG, BH, BJ, BM, BR, BS, BZ, CH, CI, CL, CN, CO, CR, CY, CZ, DE, DK, DO, EC, EG, ES, ET, FI, GB, GH, GM, GN, GT, GY, HK, HN, HR, HU, ID, IN, IQ, IR, IT, JM, JO, JP, KE, KR, KW, LB, LR, LY, MA, ML, MR, MU, MW, MX, MY, NE, NG, NI, NL, NO, NZ, OM, PA, PE, PH, PK, PL, PT, PY, QA, SA, SC, SD, SE, SG, SL, SN, SR, SV, SY, TH, TT, TW, TZ, UG, UY, VE, YE, ZA, ZM, ZW); Gluconase (PH); Glucor (FR); Glumida (ES); Prandase (CA, IL); Rebose (IN)
MECHANISM OF ACTION — Competitive inhibitor of pancreatic alpha-amylase and intestinal brush border alpha-glucosidases, resulting in delayed hydrolysis of ingested complex carbohydrates and disaccharides and absorption of glucose; dose-dependent reduction in postprandial serum insulin and glucose peaks; inhibits the metabolism of sucrose to glucose and fructose
PHARMACODYNAMICS / KINETICS Absorption: <2% as active drug
Metabolism: Exclusively via GI tract, principally by intestinal bacteria and digestive enzymes; 13 metabolites identified
Bioavailability: Low systemic bioavailability of parent compound; acts locally in GI tract
Excretion: Urine (~34%)
PATIENT INFORMATION — Take this medication exactly as directed, with the first bite of each main meal. It is important to continue to adhere to dietary instructions, a regular exercise program, and regular testing of urine and/or blood glucose. The risk of hypoglycemia, its symptoms and treatment, and conditions that predispose to its development should be well understood by patients and responsible family members. A source of glucose (dextrose) should be readily available to treat symptoms of low blood glucose when taking acarbose in combination with a sulfonylurea or insulin. If side effects occur, they usually develop during the first few weeks of therapy and are most often mild-to-moderate gastrointestinal effects, such as flatulence, diarrhea, or abdominal discomfort and generally diminish in frequency and intensity with time.
(For additional information see "Acarbose: Patient drug information")
Acamprosate: Drug information
(For additional information see "Acamprosate: Patient drug information")
U.S. BRAND NAMES — Campral®
PHARMACOLOGIC CATEGORY GABA Agonist/Glutamate Antagonist
DOSING: ADULTS — Alcohol abstinence: Oral: 666 mg 3 times/day (a lower dose may be effective in some patients). Adjustment in patients with low body weight (unlabeled): A lower dose (4 tablets/day) may be considered in patients with low body weight (eg, <60 kg).
Note: Treatment should be initiated as soon as possible following the period of alcohol withdrawal, when the patient has achieved abstinence.
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT Clcr 30-50 mL/minute: Initial dose should be reduced to 333 mg 3 times/day.
Clcr <30 mL/minute: Contraindicated in severe renal impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, enteric coated, delayed release, as calcium: 333 mg [contains calcium 33 mg and sulfites]
DOSAGE FORMS: CONCISE Tablet, enteric coated, delayed release: Campral®: 333 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — May be administered without regard to meals. Tablet should be swallowed whole; do not crush or chew.
USE — Maintenance of alcohol abstinence
ADVERSE REACTIONS SIGNIFICANT Note: Many adverse effects associated with treatment may be related to alcohol abstinence; reported frequency range may overlap with placebo.
>10%: Gastrointestinal: Diarrhea (10% to 17%)
1% to 10%: Cardiovascular: Syncope, palpitation, edema (peripheral) Central nervous system: Insomnia (6% to 9%), anxiety (5% to 8%), depression (4% to 8%), dizziness (3% to 4%), pain (2% to 4%), paresthesia (2% to 3%), headache, somnolence, amnesia, tremor, chills Dermatologic: Pruritus (3% to 4%), rash Endocrine and metabolic: Weight gain, libido decreased Gastrointestinal: Anorexia (2% to 5%), flatulence (1% to 3%), nausea (3% to 4%), abdominal pain, dry mouth (1% to 3%), vomiting, dyspepsia, constipation, appetite increased, taste perversion Genitourinary: Impotence Neuromuscular & skeletal: Weakness (5% to 7%), back pain, myalgia, arthralgia Ocular: Abnormal vision Respiratory: Rhinitis, dyspnea, pharyngitis, bronchitis Miscellaneous: Diaphoresis (2% to 3%), suicide attempt
<1%, postmarketing, and/or case reports (limited to important or life-threatening): Angina, asthma, exfoliative dermatitis, gastrointestinal hemorrhage, hallucinations, hypothyroidism, MI, ophthalmitis, pancreatitis, photosensitivity, psychosis, pulmonary embolus, renal calculus, renal failure, seizure, suicidal ideation, suicide attempts, suicide completion
CONTRAINDICATIONS — Hypersensitivity to acamprosate or any component of the formulation; severe renal impairment (Clcr <30 mL/minute)
WARNINGS / PRECAUTIONS Concerns related to adverse effects: Suicidal ideation/attempt: Attempted and completed suicides have occurred in acamprosate-treated patients; use with caution in suicidal ideation. Monitor for depression and/or suicidal thinking.
Disease-related concerns: Alcohol dependence: Appropriate use: Should be used as part of a comprehensive program to treat alcohol dependence. Treatment should be initiated as soon as possible following the period of alcohol withdrawal, when the patient has achieved abstinence. Acamprosate does not eliminate or diminish the symptoms of alcohol withdrawal. Renal impairment: Use with caution in patients with moderate renal impairment (Clcr 30-50 mL/minute).
Special populations: Pediatrics: Safety and efficacy have not been established in children.
Dosage form specific issues: Sulfites: Traces of sulfites may be present in the formulation.
DRUG INTERACTIONS — No clinically-significant drug-to-drug interactions have been identified.
ETHANOL / NUTRITION / HERB INTERACTIONS Ethanol: Abstinence is required during treatment. Ethanol does not affect the pharmacokinetics of acamprosate; however, the continued use of ethanol will decrease desired efficacy of acamprosate.
Food: Food decreases absorption of acamprosate (not clinically significant).
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Teratogenic in animal studies. No adequate or well-controlled studies in pregnant women; use only if potential benefit outweighs possible risk to the fetus.
LACTATION — Excretion in breast milk unknown/use caution
DIETARY CONSIDERATIONS — May be taken without regard to meals. Each 333 mg tablet contains 33 mg of elemental calcium.
PRICING — (data from drugstore.com)Tablet, EC (Campral) 333 mg (180): $121.36
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms may include diarrhea and (in chronic overdose) hypercalcemia. Treatment is symptom-directed and supportive.
INTERNATIONAL BRAND NAMES — Acampral (KR); Aotal (FR); Campral (AR, AT, AU, BE, BR, CH, CL, DE, DK, ES, GB, HU, IE, NL, PL, RU, SE); Sobrial (ZA)
MECHANISM OF ACTION — Mechanism not fully defined. Structurally similar to gamma-amino butyric acid (GABA), acamprosate appears to increase the activity of the GABA-ergic system, and decreases activity of glutamate within the CNS, including a decrease in activity at N-methyl D-aspartate (NMDA) receptors; may also affect CNS calcium channels. Restores balance to GABA and glutamate activities which appear to be disrupted in alcohol dependence. During therapeutic use, reduces alcohol intake, but does not cause a disulfiram-like reaction following alcohol ingestion.
PHARMACODYNAMICS / KINETICS Distribution: Vd: 1 L/kg
Protein binding: Negligible
Metabolism: Not metabolized
Bioavailability: 11%
Half-life elimination: 20-33 hours
Excretion: Urine (as unchanged drug)
U.S. BRAND NAMES — Campral®
PHARMACOLOGIC CATEGORY GABA Agonist/Glutamate Antagonist
DOSING: ADULTS — Alcohol abstinence: Oral: 666 mg 3 times/day (a lower dose may be effective in some patients). Adjustment in patients with low body weight (unlabeled): A lower dose (4 tablets/day) may be considered in patients with low body weight (eg, <60 kg).
Note: Treatment should be initiated as soon as possible following the period of alcohol withdrawal, when the patient has achieved abstinence.
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT Clcr 30-50 mL/minute: Initial dose should be reduced to 333 mg 3 times/day.
Clcr <30 mL/minute: Contraindicated in severe renal impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, enteric coated, delayed release, as calcium: 333 mg [contains calcium 33 mg and sulfites]
DOSAGE FORMS: CONCISE Tablet, enteric coated, delayed release: Campral®: 333 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — May be administered without regard to meals. Tablet should be swallowed whole; do not crush or chew.
USE — Maintenance of alcohol abstinence
ADVERSE REACTIONS SIGNIFICANT Note: Many adverse effects associated with treatment may be related to alcohol abstinence; reported frequency range may overlap with placebo.
>10%: Gastrointestinal: Diarrhea (10% to 17%)
1% to 10%: Cardiovascular: Syncope, palpitation, edema (peripheral) Central nervous system: Insomnia (6% to 9%), anxiety (5% to 8%), depression (4% to 8%), dizziness (3% to 4%), pain (2% to 4%), paresthesia (2% to 3%), headache, somnolence, amnesia, tremor, chills Dermatologic: Pruritus (3% to 4%), rash Endocrine and metabolic: Weight gain, libido decreased Gastrointestinal: Anorexia (2% to 5%), flatulence (1% to 3%), nausea (3% to 4%), abdominal pain, dry mouth (1% to 3%), vomiting, dyspepsia, constipation, appetite increased, taste perversion Genitourinary: Impotence Neuromuscular & skeletal: Weakness (5% to 7%), back pain, myalgia, arthralgia Ocular: Abnormal vision Respiratory: Rhinitis, dyspnea, pharyngitis, bronchitis Miscellaneous: Diaphoresis (2% to 3%), suicide attempt
<1%, postmarketing, and/or case reports (limited to important or life-threatening): Angina, asthma, exfoliative dermatitis, gastrointestinal hemorrhage, hallucinations, hypothyroidism, MI, ophthalmitis, pancreatitis, photosensitivity, psychosis, pulmonary embolus, renal calculus, renal failure, seizure, suicidal ideation, suicide attempts, suicide completion
CONTRAINDICATIONS — Hypersensitivity to acamprosate or any component of the formulation; severe renal impairment (Clcr <30 mL/minute)
WARNINGS / PRECAUTIONS Concerns related to adverse effects: Suicidal ideation/attempt: Attempted and completed suicides have occurred in acamprosate-treated patients; use with caution in suicidal ideation. Monitor for depression and/or suicidal thinking.
Disease-related concerns: Alcohol dependence: Appropriate use: Should be used as part of a comprehensive program to treat alcohol dependence. Treatment should be initiated as soon as possible following the period of alcohol withdrawal, when the patient has achieved abstinence. Acamprosate does not eliminate or diminish the symptoms of alcohol withdrawal. Renal impairment: Use with caution in patients with moderate renal impairment (Clcr 30-50 mL/minute).
Special populations: Pediatrics: Safety and efficacy have not been established in children.
Dosage form specific issues: Sulfites: Traces of sulfites may be present in the formulation.
DRUG INTERACTIONS — No clinically-significant drug-to-drug interactions have been identified.
ETHANOL / NUTRITION / HERB INTERACTIONS Ethanol: Abstinence is required during treatment. Ethanol does not affect the pharmacokinetics of acamprosate; however, the continued use of ethanol will decrease desired efficacy of acamprosate.
Food: Food decreases absorption of acamprosate (not clinically significant).
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Teratogenic in animal studies. No adequate or well-controlled studies in pregnant women; use only if potential benefit outweighs possible risk to the fetus.
LACTATION — Excretion in breast milk unknown/use caution
DIETARY CONSIDERATIONS — May be taken without regard to meals. Each 333 mg tablet contains 33 mg of elemental calcium.
PRICING — (data from drugstore.com)Tablet, EC (Campral) 333 mg (180): $121.36
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms may include diarrhea and (in chronic overdose) hypercalcemia. Treatment is symptom-directed and supportive.
INTERNATIONAL BRAND NAMES — Acampral (KR); Aotal (FR); Campral (AR, AT, AU, BE, BR, CH, CL, DE, DK, ES, GB, HU, IE, NL, PL, RU, SE); Sobrial (ZA)
MECHANISM OF ACTION — Mechanism not fully defined. Structurally similar to gamma-amino butyric acid (GABA), acamprosate appears to increase the activity of the GABA-ergic system, and decreases activity of glutamate within the CNS, including a decrease in activity at N-methyl D-aspartate (NMDA) receptors; may also affect CNS calcium channels. Restores balance to GABA and glutamate activities which appear to be disrupted in alcohol dependence. During therapeutic use, reduces alcohol intake, but does not cause a disulfiram-like reaction following alcohol ingestion.
PHARMACODYNAMICS / KINETICS Distribution: Vd: 1 L/kg
Protein binding: Negligible
Metabolism: Not metabolized
Bioavailability: 11%
Half-life elimination: 20-33 hours
Excretion: Urine (as unchanged drug)
Acamprosate: Drug information
(For additional information see "Acamprosate: Patient drug information")
U.S. BRAND NAMES — Campral®
PHARMACOLOGIC CATEGORY GABA Agonist/Glutamate Antagonist
DOSING: ADULTS — Alcohol abstinence: Oral: 666 mg 3 times/day (a lower dose may be effective in some patients). Adjustment in patients with low body weight (unlabeled): A lower dose (4 tablets/day) may be considered in patients with low body weight (eg, <60 kg).
Note: Treatment should be initiated as soon as possible following the period of alcohol withdrawal, when the patient has achieved abstinence.
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT Clcr 30-50 mL/minute: Initial dose should be reduced to 333 mg 3 times/day.
Clcr <30 mL/minute: Contraindicated in severe renal impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, enteric coated, delayed release, as calcium: 333 mg [contains calcium 33 mg and sulfites]
DOSAGE FORMS: CONCISE Tablet, enteric coated, delayed release: Campral®: 333 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — May be administered without regard to meals. Tablet should be swallowed whole; do not crush or chew.
USE — Maintenance of alcohol abstinence
ADVERSE REACTIONS SIGNIFICANT Note: Many adverse effects associated with treatment may be related to alcohol abstinence; reported frequency range may overlap with placebo.
>10%: Gastrointestinal: Diarrhea (10% to 17%)
1% to 10%: Cardiovascular: Syncope, palpitation, edema (peripheral) Central nervous system: Insomnia (6% to 9%), anxiety (5% to 8%), depression (4% to 8%), dizziness (3% to 4%), pain (2% to 4%), paresthesia (2% to 3%), headache, somnolence, amnesia, tremor, chills Dermatologic: Pruritus (3% to 4%), rash Endocrine and metabolic: Weight gain, libido decreased Gastrointestinal: Anorexia (2% to 5%), flatulence (1% to 3%), nausea (3% to 4%), abdominal pain, dry mouth (1% to 3%), vomiting, dyspepsia, constipation, appetite increased, taste perversion Genitourinary: Impotence Neuromuscular & skeletal: Weakness (5% to 7%), back pain, myalgia, arthralgia Ocular: Abnormal vision Respiratory: Rhinitis, dyspnea, pharyngitis, bronchitis Miscellaneous: Diaphoresis (2% to 3%), suicide attempt
<1%, postmarketing, and/or case reports (limited to important or life-threatening): Angina, asthma, exfoliative dermatitis, gastrointestinal hemorrhage, hallucinations, hypothyroidism, MI, ophthalmitis, pancreatitis, photosensitivity, psychosis, pulmonary embolus, renal calculus, renal failure, seizure, suicidal ideation, suicide attempts, suicide completion
CONTRAINDICATIONS — Hypersensitivity to acamprosate or any component of the formulation; severe renal impairment (Clcr <30 mL/minute)
WARNINGS / PRECAUTIONS Concerns related to adverse effects: Suicidal ideation/attempt: Attempted and completed suicides have occurred in acamprosate-treated patients; use with caution in suicidal ideation. Monitor for depression and/or suicidal thinking.
Disease-related concerns: Alcohol dependence: Appropriate use: Should be used as part of a comprehensive program to treat alcohol dependence. Treatment should be initiated as soon as possible following the period of alcohol withdrawal, when the patient has achieved abstinence. Acamprosate does not eliminate or diminish the symptoms of alcohol withdrawal. Renal impairment: Use with caution in patients with moderate renal impairment (Clcr 30-50 mL/minute).
Special populations: Pediatrics: Safety and efficacy have not been established in children.
Dosage form specific issues: Sulfites: Traces of sulfites may be present in the formulation.
DRUG INTERACTIONS — No clinically-significant drug-to-drug interactions have been identified.
ETHANOL / NUTRITION / HERB INTERACTIONS Ethanol: Abstinence is required during treatment. Ethanol does not affect the pharmacokinetics of acamprosate; however, the continued use of ethanol will decrease desired efficacy of acamprosate.
Food: Food decreases absorption of acamprosate (not clinically significant).
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Teratogenic in animal studies. No adequate or well-controlled studies in pregnant women; use only if potential benefit outweighs possible risk to the fetus.
LACTATION — Excretion in breast milk unknown/use caution
DIETARY CONSIDERATIONS — May be taken without regard to meals. Each 333 mg tablet contains 33 mg of elemental calcium.
PRICING — (data from drugstore.com)Tablet, EC (Campral) 333 mg (180): $121.36
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms may include diarrhea and (in chronic overdose) hypercalcemia. Treatment is symptom-directed and supportive.
INTERNATIONAL BRAND NAMES — Acampral (KR); Aotal (FR); Campral (AR, AT, AU, BE, BR, CH, CL, DE, DK, ES, GB, HU, IE, NL, PL, RU, SE); Sobrial (ZA)
MECHANISM OF ACTION — Mechanism not fully defined. Structurally similar to gamma-amino butyric acid (GABA), acamprosate appears to increase the activity of the GABA-ergic system, and decreases activity of glutamate within the CNS, including a decrease in activity at N-methyl D-aspartate (NMDA) receptors; may also affect CNS calcium channels. Restores balance to GABA and glutamate activities which appear to be disrupted in alcohol dependence. During therapeutic use, reduces alcohol intake, but does not cause a disulfiram-like reaction following alcohol ingestion.
PHARMACODYNAMICS / KINETICS Distribution: Vd: 1 L/kg
Protein binding: Negligible
Metabolism: Not metabolized
Bioavailability: 11%
Half-life elimination: 20-33 hours
Excretion: Urine (as unchanged drug)
U.S. BRAND NAMES — Campral®
PHARMACOLOGIC CATEGORY GABA Agonist/Glutamate Antagonist
DOSING: ADULTS — Alcohol abstinence: Oral: 666 mg 3 times/day (a lower dose may be effective in some patients). Adjustment in patients with low body weight (unlabeled): A lower dose (4 tablets/day) may be considered in patients with low body weight (eg, <60 kg).
Note: Treatment should be initiated as soon as possible following the period of alcohol withdrawal, when the patient has achieved abstinence.
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT Clcr 30-50 mL/minute: Initial dose should be reduced to 333 mg 3 times/day.
Clcr <30 mL/minute: Contraindicated in severe renal impairment.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, enteric coated, delayed release, as calcium: 333 mg [contains calcium 33 mg and sulfites]
DOSAGE FORMS: CONCISE Tablet, enteric coated, delayed release: Campral®: 333 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — May be administered without regard to meals. Tablet should be swallowed whole; do not crush or chew.
USE — Maintenance of alcohol abstinence
ADVERSE REACTIONS SIGNIFICANT Note: Many adverse effects associated with treatment may be related to alcohol abstinence; reported frequency range may overlap with placebo.
>10%: Gastrointestinal: Diarrhea (10% to 17%)
1% to 10%: Cardiovascular: Syncope, palpitation, edema (peripheral) Central nervous system: Insomnia (6% to 9%), anxiety (5% to 8%), depression (4% to 8%), dizziness (3% to 4%), pain (2% to 4%), paresthesia (2% to 3%), headache, somnolence, amnesia, tremor, chills Dermatologic: Pruritus (3% to 4%), rash Endocrine and metabolic: Weight gain, libido decreased Gastrointestinal: Anorexia (2% to 5%), flatulence (1% to 3%), nausea (3% to 4%), abdominal pain, dry mouth (1% to 3%), vomiting, dyspepsia, constipation, appetite increased, taste perversion Genitourinary: Impotence Neuromuscular & skeletal: Weakness (5% to 7%), back pain, myalgia, arthralgia Ocular: Abnormal vision Respiratory: Rhinitis, dyspnea, pharyngitis, bronchitis Miscellaneous: Diaphoresis (2% to 3%), suicide attempt
<1%, postmarketing, and/or case reports (limited to important or life-threatening): Angina, asthma, exfoliative dermatitis, gastrointestinal hemorrhage, hallucinations, hypothyroidism, MI, ophthalmitis, pancreatitis, photosensitivity, psychosis, pulmonary embolus, renal calculus, renal failure, seizure, suicidal ideation, suicide attempts, suicide completion
CONTRAINDICATIONS — Hypersensitivity to acamprosate or any component of the formulation; severe renal impairment (Clcr <30 mL/minute)
WARNINGS / PRECAUTIONS Concerns related to adverse effects: Suicidal ideation/attempt: Attempted and completed suicides have occurred in acamprosate-treated patients; use with caution in suicidal ideation. Monitor for depression and/or suicidal thinking.
Disease-related concerns: Alcohol dependence: Appropriate use: Should be used as part of a comprehensive program to treat alcohol dependence. Treatment should be initiated as soon as possible following the period of alcohol withdrawal, when the patient has achieved abstinence. Acamprosate does not eliminate or diminish the symptoms of alcohol withdrawal. Renal impairment: Use with caution in patients with moderate renal impairment (Clcr 30-50 mL/minute).
Special populations: Pediatrics: Safety and efficacy have not been established in children.
Dosage form specific issues: Sulfites: Traces of sulfites may be present in the formulation.
DRUG INTERACTIONS — No clinically-significant drug-to-drug interactions have been identified.
ETHANOL / NUTRITION / HERB INTERACTIONS Ethanol: Abstinence is required during treatment. Ethanol does not affect the pharmacokinetics of acamprosate; however, the continued use of ethanol will decrease desired efficacy of acamprosate.
Food: Food decreases absorption of acamprosate (not clinically significant).
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Teratogenic in animal studies. No adequate or well-controlled studies in pregnant women; use only if potential benefit outweighs possible risk to the fetus.
LACTATION — Excretion in breast milk unknown/use caution
DIETARY CONSIDERATIONS — May be taken without regard to meals. Each 333 mg tablet contains 33 mg of elemental calcium.
PRICING — (data from drugstore.com)Tablet, EC (Campral) 333 mg (180): $121.36
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms may include diarrhea and (in chronic overdose) hypercalcemia. Treatment is symptom-directed and supportive.
INTERNATIONAL BRAND NAMES — Acampral (KR); Aotal (FR); Campral (AR, AT, AU, BE, BR, CH, CL, DE, DK, ES, GB, HU, IE, NL, PL, RU, SE); Sobrial (ZA)
MECHANISM OF ACTION — Mechanism not fully defined. Structurally similar to gamma-amino butyric acid (GABA), acamprosate appears to increase the activity of the GABA-ergic system, and decreases activity of glutamate within the CNS, including a decrease in activity at N-methyl D-aspartate (NMDA) receptors; may also affect CNS calcium channels. Restores balance to GABA and glutamate activities which appear to be disrupted in alcohol dependence. During therapeutic use, reduces alcohol intake, but does not cause a disulfiram-like reaction following alcohol ingestion.
PHARMACODYNAMICS / KINETICS Distribution: Vd: 1 L/kg
Protein binding: Negligible
Metabolism: Not metabolized
Bioavailability: 11%
Half-life elimination: 20-33 hours
Excretion: Urine (as unchanged drug)
Absorbable gelatin: Drug information
U.S. BRAND NAMES — Gelfilm®; Gelfoam®
PHARMACOLOGIC CATEGORY Hemostatic Agent
DOSING: ADULTS — Hemostasis: Local: Apply packs or sponges dry or saturated with sodium chloride. When applied dry, hold in place with moderate pressure. When applied wet, squeeze to remove air bubbles. The powder is applied as a paste prepared by adding approximately 4 mL of sterile saline solution to the powder.
DOSING: PEDIATRIC — Refer to adult dosing.
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Film, ophthalmic (Gelfilm®): 25 mm x 50 mm (6s)
Film, topical (Gelfilm®): 100 mm x 125 mm (1s)
Powder, topical (Gelfoam®): 1 g
Sponge, dental (Gelfoam®): Size 4 (12s)
Sponge, topical (Gelfoam®): Size 50 (4s) Size 100 (6s) Size 200 (6s) Size 2 cm (1s) Size 6 cm (6s) Size 12-7 mm (12s)
DOSAGE FORMS: CONCISE Film, ophthalmic: Gelfilm®: 25 mm x 50 mm (6s)
Film, topical: Gelfilm®: 100 mm x 125 mm (1s)
Powder, topical: Gelfoam®: 1 g
Sponge, dental: Gelfoam®: Size 4 (12s)
Sponge, topical: Gelfoam®: Size 50 (4s) Size 100 (6s) Size 200 (6s) Size 2 cm (1s) Size 6 cm (6s) Size 12-7 mm (12s)
GENERIC EQUIVALENT AVAILABLE — No
USE — Adjunct to provide hemostasis in surgery; open prostatic surgery
ADVERSE REACTIONS SIGNIFICANT — 1% to 10%: Local: Infection and abscess formation
CONTRAINDICATIONS — Should not be used in closure of skin incisions since they may interfere with the healing of skin edges
WARNINGS / PRECAUTIONS — Do not sterilize by heat; do not use in the presence of infection
DRUG INTERACTIONS — No data reported
PREGNANCY RISK FACTOR — No (show table) data reported
PHARMACOLOGIC CATEGORY Hemostatic Agent
DOSING: ADULTS — Hemostasis: Local: Apply packs or sponges dry or saturated with sodium chloride. When applied dry, hold in place with moderate pressure. When applied wet, squeeze to remove air bubbles. The powder is applied as a paste prepared by adding approximately 4 mL of sterile saline solution to the powder.
DOSING: PEDIATRIC — Refer to adult dosing.
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Film, ophthalmic (Gelfilm®): 25 mm x 50 mm (6s)
Film, topical (Gelfilm®): 100 mm x 125 mm (1s)
Powder, topical (Gelfoam®): 1 g
Sponge, dental (Gelfoam®): Size 4 (12s)
Sponge, topical (Gelfoam®): Size 50 (4s) Size 100 (6s) Size 200 (6s) Size 2 cm (1s) Size 6 cm (6s) Size 12-7 mm (12s)
DOSAGE FORMS: CONCISE Film, ophthalmic: Gelfilm®: 25 mm x 50 mm (6s)
Film, topical: Gelfilm®: 100 mm x 125 mm (1s)
Powder, topical: Gelfoam®: 1 g
Sponge, dental: Gelfoam®: Size 4 (12s)
Sponge, topical: Gelfoam®: Size 50 (4s) Size 100 (6s) Size 200 (6s) Size 2 cm (1s) Size 6 cm (6s) Size 12-7 mm (12s)
GENERIC EQUIVALENT AVAILABLE — No
USE — Adjunct to provide hemostasis in surgery; open prostatic surgery
ADVERSE REACTIONS SIGNIFICANT — 1% to 10%: Local: Infection and abscess formation
CONTRAINDICATIONS — Should not be used in closure of skin incisions since they may interfere with the healing of skin edges
WARNINGS / PRECAUTIONS — Do not sterilize by heat; do not use in the presence of infection
DRUG INTERACTIONS — No data reported
PREGNANCY RISK FACTOR — No (show table) data reported
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