Acebutolol

Pronunciation

(a se BYOO toe lole)

U.S. Brand Names

Sectral®

Synonyms

Acebutolol Hydrochloride

Generic Available

Yes

Canadian Brand Names

Apo-Acebutolol®; Gen-Acebutolol; Monitan®; Novo-Acebutolol; Nu-Acebutolol; Rhotral; Sectral®

Use

Treatment of hypertension, ventricular arrhythmias, angina

Pregnancy Risk Factor

B (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

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

Abrupt withdrawal of drug should be avoided. May result in an exaggerated cardiac responsiveness such as tachycardia, hypertension, ischemia, angina, myocardial infarction, and sudden death. It is recommended that patients be gradually tapered off beta-blockers (over a 2-week period) rather than via abrupt discontinuation. Although acebutolol primarily blocks beta1-receptors, high doses can result in beta2-receptor blockage. Use with caution in diabetic patients. Beta-blockers may impair glucose tolerance, potentiate hypoglycemia, and/or mask symptoms of hypoglycemia in a diabetic patient. Use with caution in bronchospastic lung disease and renal dysfunction (especially the elderly). Beta-blockers with intrinsic sympathomimetic activity do not appear to be of benefit in CHF and should be avoided. See Dosage - Renal/Hepatic Impairment.

Adverse Reactions

>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): Increased transaminases, increased bilirubin, increased alkaline phosphatase, hepatotoxic reaction, ventricular arrhythmia, AV block, facial edema, xerostomia, anorexia, impotence, urinary retention, cold extremities, systemic lupus erythematosus, palpitation, exacerbate pre-existing renal insufficiency

Postmarketing and/or case reports: Pleurisy, pulmonary granulomas, pneumonitis, lichen planus, lupus erythematosus, drug-induced lupus-like syndrome

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

Overdosage/Toxicology

Symptoms of intoxication 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 and coma. Respiratory arrest (commonly seen with propranolol and other membrane-depressant and lipid-soluble drugs). Treat symptomatically. Cardiac and hemodynamic monitoring may be necessary.

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).

Stability

Store at room temperature (~25°C/77°F); protect from light and dispense in a light-resistant, tight container

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%)

Dosage

Oral:

Adults:

Hypertension: 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

Ventricular arrhythmias: Initial: 400 mg/day; maintenance: 600-1200 mg/day in divided doses

Elderly: Initial: 200-400 mg/day; dose reduction due to age related decrease in Clcr will be necessary; do not exceed 800 mg/day

Dosing adjustment in 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 adjustment in hepatic impairment: Use with caution.

Administration

To discontinue therapy, taper dose gradually. May be administered without regard to meals.

Monitoring Parameters

Blood pressure, orthostatic hypotension, heart rate, CNS effects, ECG

Test Interactions

Increased triglycerides, potassium, uric acid, cholesterol (S), glucose; decreased HDL, increased thyroxine (S)

Dietary Considerations

May be taken without regard to meals.

Patient Education

Take exactly as directed; do not increase, decrease, or adjust dosage without consulting prescriber. May be taken without regard to meals. Take pulse daily, prior to medication, and follow prescriber's instruction about holding medication. Do not take with antacids. Do not use OTC medications such as cold remedies without consulting prescriber. If you have diabetes, monitor serum sugar closely (drug may alter glucose tolerance or mask signs of hypoglycemia). May cause fatigue, dizziness (use caution when driving or engaging in tasks that require alertness until response to drug is known); postural hypotension (use caution when changing position from lying or sitting to standing or when climbing stairs); or alteration in sexual performance (reversible). Report chest pain or palpitations, unresolved swelling of extremities or unusual weight gain, respiratory difficulty or new cough, skin rash, unresolved fatigue, unresolved constipation or diarrhea, unusual muscle weakness, or CNS disturbances. Pregnancy/breast-feeding precautions: Inform prescriber if you are pregnant. Consult prescriber if breast-feeding.

Cardiovascular Considerations

This drug possesses intrinsic sympathomimetic activity. While beta-blockers with intrinsic sympathomimetic activity induce fewer side effects, the cardiovascular benefits listed below are less clear than for beta-blockers without intrinsic sympathomimetic activity.

Hypertension: Beta-blocker therapy in the treatment of hypertension has been associated with improved cardiovascular outcomes. This class of drug is beneficial for elderly patients with hypertension. A recent UKPDS study showed that beta-blocker therapy (atenolol) was as effective as an ACE inhibitor in reducing cardiovascular events and that the benefits of therapy were related more to the degree of antihypertensive efficacy rather than the class of drug used.

Myocardial infarction: Beta-blockers, in general without intrinsic sympathomimetic activity (ISA), have been shown to decrease morbidity and mortality when initiated in the acute treatment of myocardial infarction and continued long-term. In this setting, therapy should be avoided in patients with hypotension, cardiogenic shock, or heart block.

Surgery: Atenolol has also been shown to improve cardiovascular outcomes when used in the perioperative period in patients with underlying cardiovascular disease who are undergoing noncardiac surgery. Bisoprolol in high-risk patients undergoing vascular surgery reduced the perioperative incidence of death from cardiac causes and nonfatal myocardial infarction.

Atrial fibrillation: Beta-blocker therapy provides effective rate control in patients with atrial fibrillation.

Angina: Beta-blockers are effective in the treatment of angina as monotherapy or when combined with nitrates and/or calcium channel blockers.

Unstable angina/non-ST-segment elevation MI: In the treatment of unstable angina/non-ST-segment elevation MI, a beta-blocker, with the first dose administered intravenously if there is ongoing chest pain, followed by oral administration, is recommended (in the absence of contraindications).

Withdrawal: Beta-blocker therapy should not be withdrawn abruptly, but gradually tapered to avoid acute tachycardia and hypertension.

Heart failure: There is emerging evidence that beta-blocker therapy, without intrinsic sympathomimetic activity (ISA), should be initiated in select patients with stable congestive heart failure (NYHA Class II-III). Acebutolol exhibits ISA. To date, carvedilol, sustained release metoprolol, and bisoprolol have demonstrated a beneficial effect on morbidity and mortality. It is important that beta-blocker therapy be instituted initially at very low doses with gradual and very careful titration.

Dental Health: Effects on Dental Treatment

Acebutolol is a cardioselective beta-blocker. Local anesthetic with vasoconstrictor can be safely used in patients medicated with acebutolol. Nonselective beta-blockers (ie, propranolol, nadolol) enhance the pressor response to epinephrine, resulting in hypertension and bradycardia; this has not been reported for acebutolol. Many nonsteroidal anti-inflammatory drugs, such as ibuprofen and indomethacin, can reduce the hypotensive effect of beta-blockers after 3 or more weeks of therapy with the NSAID. Short-term NSAID use (ie, 3 days) requires no special precautions in patients taking beta-blockers.

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Mental Health: Effects on Mental Status

Drowsiness/fatigue is common; may cause insomnia, depression, abnormal dreams, and polyuria

Mental Health: Effects on Psychiatric Treatment

Additive hypotensive and/or sedative effects may be seen with concurrent use of antipsychotics, antidepressants, or benzodiazepines

Dosage Forms

Capsule, as hydrochloride: 200 mg, 400 mg

References

"American Academy of Pediatrics Committee on Drugs. The Transfer of Drugs and Other Chemicals Into Human Milk," Pediatrics , 2001, 108(3):776-89.

Braunwald E, Antman EM, Beasley JW, et al, "ACC/AHA Guidelines for the Management of Patients With Unstable Angina and Non-ST-Segment Elevation Myocardial Infarction. A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines (Committee on the Management of Patients With Unstable Angina)," J Am Coll Cardiol , 2000, 36(3):970-1062.

Chobanian AV, Bakris GL, Black HR, et al, "The Seventh Report of the Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure: The JNC 7 Report," JAMA , 2003, 289(19):2560-71.

"Consensus Recommendations for the Management of Chronic Heart Failure. On Behalf of the Membership of the Advisory Council to Improve Outcomes Nationwide in Heart Failure," Am J Cardiol , 1999, 83(2A):1A-38A.

Gibbons RJ, Chatterjee K, Daley J, et al, "ACC/AHA/ACP-ASIM Guidelines for the Management of Patients With Chronic Stable Angina: A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines," J Am Coll Cardiol , 1999, 33(7):2092-197.

Mokhlesi B, Leikin JB, Murray P, et al, "Adult Toxicology in Critical Care: Part II: Specific Poisonings," Chest , 2003, 123(3):897-922.

Ryan TJ, Anderson JL, Antman EM, et al, "ACC/AHA Guidelines for the Management of Patients With Acute Myocardial Infarction. A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines (Committee on Management of Acute Myocardial Infarction)," J Am Coll Cardiol , 1996, 28(5):1328-428.

International Brand Names

Abutol® (PL); ACB® (NZ, SG); Acebutol-400 von CT® (RO); Acebutolol Heumann® (DE); Acebutolol® (PL); Acecor® (CZ, PL, RO); Acetanol® (JP); Apo-Acebutolol® (CA, SG); Beloc® (CL); Cetolol® (PL); Diasectral® (DK, FI); Espesil® (FI); Gen-Acebutolol (CA); Grifobutol® (CL); Monitan® (CA); Novo-Acebutolol (CA); Nu-Acebutolol (CA); Prent® (DE, IT, TR); Rhodiasectral® (AR); Rhotral (CA); Sectral® (BE, BG, CA, CH, CZ, ES, FR, GB, HK, ID, IE, IL, IN, IT, JP, LU, NL, PL, SG, ZA); Spectral® (RO); Wesfalin® (AR)

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