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Active ingredient: Acebutolol - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Adrenergic beta-Antagonists
  • Anti-Arrhythmia Agents
  • Antihypertensive Agents

Dosage Forms

  • Tablet
  • Capsule (200 mg and 400 mg)

Brands / Synonyms

Acebrutololum [INN-Latin]; Acebutolol; Acebutolol HCL; Acebutolol [USAN:BAN:INN]; Acebutololo; Acebutololum [INN-Latin]; Acetobutolol; Acetobutolol [INN-Spanish]; dl-Acebutolol ; Monitan; Neptal; Prent; Sectral

Indications

For the management of hypertension and ventricular premature beats in adults.

Pharmacology

Acebutolol is a cardioselective, beta-adrenoreceptor blocking agent, which possesses mild intrinsic sympathomimetic activity (ISA) in its therapeutically effective dose range. In general, beta-blockers reduce the work the heart has to do and allow it to beat more regularly. Acebutolol has less antagonistic effects on peripheral vascular ß2-receptors at rest and after epinephrine stimulation than nonselective beta-antagonists. Low doses of acebutolol produce less evidence of bronchoconstriction than nonselective agents like propranolol but more than atenolol.

Mechanism of Action

Acebutolol is a selective β1-receptor antagonist. Activation of β1-receptors by epinephrine increases the heart rate and the blood pressure, and the heart consumes more oxygen. Acebutolol blocks these receptors which reverses the effects of epinephrine, lowering the heart rate and blood pressure. In addition, beta blockers prevent the release of renin, which is a hormone produced by the kidneys which leads to constriction of blood vessels.

Absorption

Well absorbed from the Gl tract with an absolute bioavailability of approximately 40% for the parent compound. In

Toxicity

Symptoms of overdose include extreme bradycardia, advanced atrioventricular block, intraventricular conduction defects, hypotension, severe congestive heart failure, seizures, and in susceptible patients, bronchospasm, and hypoglycemia.

Biotrnasformation / Drug Metabolism

Subject to extensive first-pass hepatic biotransformation (primarily to diacetolol).

Contraindications

Acebutolol hydrochloride capsules are contraindicated in: 1) persistently severe bradycardia; 2) second- and third-degree heart block; 3) overt cardiac failure; and 4) cardiogenic shock.

Drug Interactions

Catecholamine-depleting drugs, such as reserpine, may have an additive effect when given with beta-blocking agents. Patients treated with acebutolol plus catecholamine depletors should, therefore, be observed closely for evidence of marked bradycardia or hypotension which may present as vertigo, syncope/presyncope, or orthostatic changes in blood pressure without compensatory tachycardia. Exaggerated hypertensive responses have been reported from the combined use of beta-adrenergic antagonists and alpha-adrenergic stimulants, including those contained in proprietary cold remedies and vasoconstrictive nasal drops. Patients receiving beta-blockers should be warned of this potential hazard.

Blunting of the antihypertensive effect of beta-adrenoceptor blocking agents by nonsteroidal anti-inflammatory drugs has been reported.

No significant interactions with digoxin, hydrochlorothiazide, hydralazine, sulfinpyrazone, oral contraceptives, tolbutamide, or warfarin have been observed.

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