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