Acebutolol

Acebutolol

Acebutolol (Sectral) is a cardioselective β₁-adrenocep-tor blocking agent that also has some minor membrane stabilizing effects on the action potential.

Electrophysiological Actions

Acebutolol’s effects on the atria, sinoatrial and AV nodes, His-Purkinje system, and ventricular muscle are similar to those of propranolol.

Hemodynamic Effects

Acebutolol reduces blood pressure in patients with es-sential hypertension primarily through its negative ino-tropic and chronotropic effects.

Pharmacokinetics

The pharmacokinetic characteristics of acebutolol:

Oral bioavailability : 70%

Onset of action : 1–3 hours

Peak response : 3–8 hours

Duration of action : 12–24 hours

Plasma half-life : 3–4 hours

Primary route of metabolism: Hepatic

Primary route of excretion : Renal (30–40%); biliary/fecal (50–60%)

Therapeutic serum concentration: Not established

Clinical Uses

Acebutolol is effective in the management of the patient with essential hypertension, angina pectoris, and ventric-ular arrhythmias. Antiarrhythmic effects are observed with the patient both at rest and taking exercise.

Adverse Effects

Adverse effects include bradycardia, gastrointestinal upset, dizziness, and headache.

Contraindications

Acebutolol should not be administered in cardiogenic shock, uncontrolled heart failure, or severe bradycar-dia or to patients with known hypersensitivity to the drug.