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Name: bretylium
PubChem Compound ID: 18499
Molecular formula: C11H17Br2N
Molecular weight: 323.067 g/mol
AMMONIUM, (o-BROMOBENZYL)ETHYLDIMETHYL-, BROMIDE; Ornido; 3170-72-7; Bretyllium; N-o-Bromobenzyl-N-ethyl-N,N-dimethylammonium bromide; Bretylium bromide; Ordil; Benzenemethanaminium, 2-bromo-N-ethyl-N,N-dimethyl-, bromide (9CI); 59-41-6
Name: bretylium
Name (isomeric): DB01158
Drug Type: small molecule
Bretylum; Bretylium tosylate; Bretylium p-toluenesulfonate; Bretylate; Bretylium tolsylate
Brand: Bretylan, Ornid, Darenthin, Bretylol, Darentin
Category: Adrenergic Antagonists, Anti-Arrhythmia Agents, Antihypertensive Agents
CAS number: 59-41-6
Indication: For use in the prophylaxis and therapy of ventricular fibrillation. Also used in the treatment of life-threatening ventricular arrhythmias, such as ventricular tachycardia, that have failed to respond to adequate doses of a first-line antiarrhythmic agent, such as lidocaine.
Pharmacology: Bretylium is a bromobenzyl quaternary ammonium compound which selectively accumulates in sympathetic ganglia and their postganglionic adrenergic neurons where it inhibits norepinephrine release by depressing adrenergic nerve terminal excitability. Bretylium also suppresses ventricular fibrillation and ventricular arrhythmias.
Mechanism of Action:
Bretylium inhibits norepinephrine release by depressing adrenergic nerve terminal excitability. The mechanisms of the antifibrillatory and antiarrhythmic actions of bretylium are not established. In efforts to define these mechanisms, the following electrophysiologic actions of bretylium have been demonstrated in animal experiments: increase in ven...
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Biotransformation: No metabolites have been identified following administration in man and laboratory animals.
Half Life: The terminal half-life in four normal volunteers averaged 7.8±0.6 hours (range 6.9-8.1). During hemodialysis, this patient's arterial and venous bretylium concentrations declined rapidly, resulting in a half-life of 13 hours.
Toxicity: Oral, mouse: LD50 = 400 mg/kg. In the presence of life-threatening arrhythmias, underdosing with bretylium probably presents a greater risk to the patient than potential overdosage. However, one case of accidental overdose has been reported in which a rapidly injected intravenous bolus of 30 mg/kg was given instead of an intended 10 mg/kg dose during an episode of ventricular tachycardia. Marked hypertension resulted, followed by protracted refractory hypotension. The patient expired 18 hours later in asystole, complicated by renal failure and aspiration pneumonitis. Bretylium serum levels were 8000 ng/mL.
Affected organisms: Humans and other mammals
Drug interaction:
GrepafloxacinIncreased risk of cardiotoxicity and arrhythmias
ClarithromycinIncreased risk of cardiotoxicity and arrhythmias
LevofloxacinIncreased risk of cardiotoxicity and arrhythmias
ThioridazineIncreased risk of cardiotoxicity and arrhythmias
TelithromycinIncreased risk of cardiotoxicity and arrhythmias
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