Acebutolol

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")