Drug intelligence / Profile preview

bretylium

Development stage
Unknown
Lead developer
University of Minnesota
Modality
Small Molecules
Administration
Intravenous, Intramuscular
01

Overview

Bretylium is a small molecule antiarrhythmic agent, primarily used for the prophylaxis and treatment of life-threatening ventricular arrhythmias such as ventricular fibrillation and ventricular tachycardia. It acts mainly by inhibiting the release of norepinephrine from sympathetic nerve terminals, leading to adrenergic neuronal blockade. Additionally, it blocks voltage-gated potassium channels (class III antiarrhythmic action) and may inhibit Na,K-ATPase by binding to the extracellular K-site. These actions increase the ventricular fibrillation threshold, prolong action potential duration and effective refractory period in cardiac tissue without significantly depressing conduction velocity or automaticity. Bretylium was originally introduced for hypertension but found its main use in emergency cardiology settings for arrhythmia management[1][2][4][5][7][8].

Brand names
Bretylol
Other names
bretylium tosylate
02

Targets

ATP1A1 (Sodium/potassium-transporting ATPase subunit alpha-1)ADRB1 (β1)Kir (Inward-rectifier potassium channels)mAChR (Muscarinic acetylcholine receptors)

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