Pharmacokinetics of bretylium in man after intravenous administration.
The pharmacokinetic profile of bretylium was studied in four normal male volunteers using a new sensitive EC-GC procedure for its quantitative in biological fluids. The plasma concentrations and urinary excretion rates following the constant i.v. infusion of a single 4 mg/kg dose of bretylium tosylate declined biexponentially and the data were fitted to a two-compartment model with a renal and a nonrenal route of elimination. The drug had a mean half-life (t1/2 beta) of 7.8 hr and apparent volume of distribution (Vd, beta) of 8.18 liters/kg. The renal clearance, which was 6 times that of the glomerular filtration rate, accounted for almost 84% of the total body clearance and correlated linearly with the subjects' creatinine clearance. The observed side effects of bretylium were mild and similar to those of other adrenergic blocking agents.
D000328:Adult; D001949:Bretylium Compounds / Q000378:metabolism*; D001950:Bretylium Tosylate / Q000008:administration & dosage / Q000009:adverse effects / Q000378:metabolism*; D006801:Humans; D007263:Infusions, Parenteral; D007668:Kidney / Q000378:metabolism; D007700:Kinetics; D008297:Male; D008657:Metabolic Clearance Rate; D008954:Models, Biological
D001949:Bretylium Compounds; D001950:Bretylium Tosylate