PMID: 108382Apr 1, 1979

Plasma naltrexone kinetics after intravenous bolus administration in dogs and monkeys

Journal of Pharmaceutical Sciences
R H ReuningL Malspeis

Abstract

This investigation generated data characterize a specific electron-capture GLC assay reported previously for naltrexone and applied the method to a determination of naltrexone pharmacokinetics. Extraction efficiencies are reported for the assay, and mass spectral evidence indicates that naltrexone forms a triester when derivatized for electron-capture GLC with pentafluoropropionic anhydride and a base catalyst. Plasma level-time data for intravenous naltrexone at two dose levels in monkeys yielded no evidence of dose-dependent kinetics. A two-compartment open pharmacokinetic model was fitted to plasma level-time data for naltrexone in two dogs and yielded a total body clearance of 51-55 ml/min/kg. Urine collected for 0-24 hr contained 36% of the dose as naltrexone conjugates with less than 1% as unchanged naltrexone. Plasma level-time data for intravenous naltrexone in six monkeys yielded an average terminal half-life of 7.8 hr and a total body clearance of 64 ml/min/kg. The total body clearance for naltrexone was greater than the hepatic plasma or blood flow in both dogs and monkeys. This finding, together with the extremely low renal excretion of naltrexone, suggests the existence of elimination mechanisms besides liver metab...Continue Reading

Citations

Feb 27, 2007·Journal of Zoo and Wildlife Medicine : Official Publication of the American Association of Zoo Veterinarians·Alexander ColeBetsy L Dresser
Jan 18, 2005·Journal of Controlled Release : Official Journal of the Controlled Release Society·Satyanarayana ValivetiAudra L Stinchcomb
Aug 6, 2014·International Journal of Biological Macromolecules·Mohammad-Bagher GholivandVahid Nasirian
Aug 1, 1983·Journal of Pharmacokinetics and Biopharmaceutics·R H ReuningD L Wise

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