Drug Groups

approved

Description

One of the adrenergic beta-antagonists used as an antihypertensive, anti-anginal, and anti-arrhythmic agent. [PubChem]

Indication

For the treatment of hypertension, angina, and arrhythmia

Pharmacology

Alprenolol is a non-selective beta-blocker used in the treatment of hypertension, edema, ventricular tachycardias, and atrial fibrillation. Alprenolol impairs AV node conduction and decreases sinus rate and may also increase plasma triglycerides and decrease HDL-cholesterol levels. Alprenolol is nonpolar and hydrophobic, with low to moderate lipid solubility. Alprenolol has little to no intrinsic sympathomimetic activity and, unlike some other beta-adrenergic blocking agents, alprenolol has little direct myocardial depressant activity and does not have an anesthetic-like membrane-stabilizing action.

Toxicity

LD₅₀=597.0 mg/kg (Orally in rats)

Affected Organisms

Biotransformation

Hepatic. One of the active metabolites, 4-OH-alprenolol, is an active beta-blocker.

Half Life

2-3 hours

Protein Binding

80-90%