Description
Mechanism of Action
Propranolol is a non-cardioselective β-blocker that competitively blocks β1- and β2-receptors resulting in decreased heart rate, myocardial contractility, BP and myocardial oxygen demand. It has membrane-stabilising properties.
Onset: 1-2 hr (oral).
Absorption: Almost completely absorbed from the GI tract. Bioavailability: Approx 25%. Time to peak plasma concentration: Approx 1-2 hr (oral).
Distribution: Widely distributed, enters breast milk, crosses blood brain barrier and placenta. Volume of distribution: 4 L/kg. Plasma protein binding: Approx 90%.
Metabolism: Undergoes hepatic metabolism via CYP2D6 isoenzyme, and CYP1A2 to 4-hydroxypropranolol (biologically active).
Excretion: Via urine (96-99% as metabolites and <1% as unchanged drug). Elimination half-life: Approx 3-6 hr.
MIMS Class
Beta-Blockers / Antimigraine Preparations
ATC Classification
C07AA05 – propranolol; Belongs to the class of non-selective beta-blocking agents. Used in the treatment of cardiovascular diseases.