Pharmacokinetics of parenteral dezocine in rhesus monkeys and dogs.
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.
D000700:Analgesics / Q000378:metabolism*; D000818:Animals; D019086:Bridged Bicyclo Compounds, Heterocyclic; D002849:Chromatography, Gas; D003516:Cycloparaffins / Q000378:metabolism*; D004285:Dogs / Q000378:metabolism*; D005260:Female; D005965:Glucuronates / Q000378:metabolism; D007700:Kinetics; D008251:Macaca / Q000378:metabolism*; D008253:Macaca mulatta / Q000378:metabolism*; D008297:Male; D013045:Species Specificity; D013764:Tetrahydronaphthalenes
D000700:Analgesics; D019086:Bridged Bicyclo Compounds, Heterocyclic; D003516:Cycloparaffins; D005965:Glucuronates; D013764:Tetrahydronaphthalenes; C010827:dezocine