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Absorption, Metabolism and Excretion of Droperidol by Human Subjects Folloiwing Intramuscular and Intravenous Administration

1973; Lippincott Williams & Wilkins; Volume: 38; Issue: 4 Linguagem: Inglês

10.1097/00000542-197304000-00010

1528-1175

William A. Cressman, Janis Plostnieks, P. C. Johnson,

Phosphodiesterase function and regulation

The absorption, metabolism and excretion of droperidol, a neuroleptic agent, was studied in human subjects following intramuscular and intravenous administration of droperido-3PH. Plasma, urinary and fecal levels of droperidol and total radioactivity were measured. Droperidol was rapidly absorbed following intramuscular administration. The plasma-level profiles of droperidol showed characteristic two-compartment open-model kinetics. The initial distribution phase was quite rapid, T1/3=10 minutes. In addition, droperidol was eliminated from the plasma at very similar rates in all subjects (T1/2=134 ± 13 minutes). Approximately 75 per cent of the radioactive dose of droperidol given intramuscularly was excreted in the urine; however, less than 1 per cent of the urinary radioactivity was accounted for by intact droperidol. Approximately 22 per cent of the dose of radioactivity given intramuscularly was recovered in the feces 50 per cent of the fecal radioactivity was intact droperidol), suggesting the possibility of biliary excretion of a portion of the dose.