PT  - JOURNAL ARTICLE
AU  - S F Sisenwine
AU  - C O Tio
AU  - A L Liu
AU  - H W Ruelius
TI  - Pharmacokinetics of parenteral dezocine in rhesus monkeys and dogs.
DP  - 1982 Jul 01
TA  - Drug Metabolism and Disposition
PG  - 366--370
VI  - 10
IP  - 4
4099  - http://dmd.aspetjournals.org/content/10/4/366.short
4100  - http://dmd.aspetjournals.org/content/10/4/366.full
SO  - Drug Metab Dispos1982 Jul 01; 10
AB  - Pharmacokinetic parameters of the analgesic, dezocine, were determined after intravenous and intramuscular injection (1 mg/kg) to rhesus monkeys and dogs. In both species, the drug was rapidly distributed after intravenous administration and then eliminated with a mean half-life of 2.4 hr. Systemic clearance was 54.8 +/- 8.6(SD) and 65.8 +/- 14.0(SD) ml/min/kg in the rhesus monkey and dog, respectively. Glucuronidation was recognized as a major metabolic pathway in both species, and sulfate conjugation was indicated in the dog. Renal elimination of dezocine was minimal. Less than 4% of the dose was eliminated as unchanged dezocine in urine of rhesus monkeys and 1% of the dose in dog urine. After im administration, release from the injection site was rapid and no metabolism at the injection site was indicated. Multiple-dose experiments in dogs did not reveal accumulation. The acquisition of data was made possible by the development of a sensitive, specific assay, which depends on gas-liquid (electron capture) chromatography of a pentafluorobenzoylated derivative of dezocine.