Ceiling respiratory depression by dezocine.
Dezocine in equianalgesic intravenous doses depressed respiratory response to CO2 breathing of six healthy subjects to approximately the same degree as morphine but with a more rapid onset and higher peak depression. The depression was dose related up to 30 mg/70 kg but was not increased by an additional 10 mg/70 kg dose. Its duration of effect was approximately the same as that of morphine. Respiratory depression by dezocine was promptly and almost completely antagonized by 0.4 mg naloxone, but antagonism lasted less than 1 hr. Healthy subjects found dezocine less pleasant than morphine and after large doses reported sensations suggestive of psychotomimetic effects. A ceiling effect for respiratory depression has now been demonstrated for three agonist-antagonist analgesics: nalorphine, nalbuphine, and dezocine. It is not yet clear to what extent this is a general characteristic of agonist-antagonist analgesics.
D000328:Adult; D019086:Bridged Bicyclo Compounds, Heterocyclic; D002245:Carbon Dioxide / Q000378:metabolism; D003516:Cycloparaffins / Q000037:antagonists & inhibitors / Q000506:poisoning*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D007275:Injections, Intravenous; D008297:Male; D009020:Morphine / Q000037:antagonists & inhibitors / Q000506:poisoning; D009266:Nalbuphine / Q000494:pharmacology; D009270:Naloxone / Q000494:pharmacology; D012120:Respiration Disorders / Q000139:chemically induced*; D013764:Tetrahydronaphthalenes
D019086:Bridged Bicyclo Compounds, Heterocyclic; D003516:Cycloparaffins; D013764:Tetrahydronaphthalenes; D002245:Carbon Dioxide; D009270:Naloxone; D009020:Morphine; D009266:Nalbuphine; C010827:dezocine