Aptine: Full Drug Profile

Aptine - General Information

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

Pharmacology of Aptine

Aptine is a non-selective beta-blocker used in the treatment of hypertension, edema, ventricular tachycardias, and atrial fibrillation. Aptine impairs AV node conduction and decreases sinus rate and may also increase plasma triglycerides and decrease HDL-cholesterol levels. Aptine is nonpolar and hydrophobic, with low to moderate lipid solubility. Aptine 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.

Additional information about Aptine

Aptine Indication

For the treatment of hypertension, angina, and arrhythmia

Mechanism Of Action

Aptine non-selectively blocks beta-1 adrenergic receptors mainly in the heart, inhibiting the effects of epinephrine and norepinephrine resulting in a decrease in heart rate and blood pressure. By binding beta-2 receptors in the juxtaglomerular apparatus, alprenolol inhibits the production of renin, thereby inhibiting angiotensin II and aldosterone production and therefore inhibits the vasoconstriction and water retention due to angiotensin II and aldosterone, respectively.

Generic Name

Alprenolol

Synonyms

Alprenololum [Inn-Latin]; Alfeprol [Russian]; Alpheprol

Drug Category

Sympatholytics; Antihypertensive Agents; Antiarrhythmic Agents

Drug Type

Small Molecule; Approved

Other Brand Names containing Alprenolol

Apllobal; Aptine; Aptol Duriles; Gubernal; Regletin; Yobir;

Toxicity (Overdose)

LD₅₀=597.0 mg/kg (Orally in rats)

Protein Binding

80-90%

Biotransformation

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

Half Life

2-3 hours

Chemical IUPAC Name

1-(propan-2-ylamino)-3-(2-prop-2-enylphenoxy)propan-2-ol

Chemical Formula

C15H23NO2

Organisms Affected

Humans and other mammals