oripavine and Substance-Related-Disorders

The dependence potential of thebaine is at least partially attributed to oripavine which is one of the principal metabolites of thebaine. The analgesic potency of oripavine in mice is found to be much higher than that of thebaine and comparable to morphine. The reinforcing effect of this substance also appears to be more potent than thebaine. In rats the physical dependence potential of oripavine at a dose of 4 mg/kg is almost comparable to that of morphine at 0.5 mg/kg. Studies carried out on monkeys show that oripavine possesses weak morphine-antagonist properties. Further pharmacological studies of the metabolites of thebaine are recommended.

Topics: Animals; Humans; Macaca mulatta; Mice; Rats; Reinforcement, Psychology; Self Administration; Substance-Related Disorders; Thebaine

This report presents the recommendations of a WHO Expert Committee responsible for reviewing information on dependence-producing drugs to assess the need for their international control. The first part of the report contains a summary of the Committee's evaluations of seven substances (dronabinol, oripavine, buprenorphine, butorphanol, ketamine, khat and zopiclone). The report also discusses the substances that were pre-reviewed (gamma-hydroxybutyric acid and tramadol) and recommended gamma-hydroxybutyric acid for critical review at a future meeting. Two substances (gamma-butyrolactone and 1,4-butanediol) were identified for future pre-review). The second part of the report discusses the guidelines for the WHO review of dependence-producing psychoactive substances for international control. It includes sections on amending the current guidelines, interpretation of specific aspects of the guidelines and access to information necessary for the evaluation of substances. The final section considers other matters including activities of the EMCCDA, the use of pharmacovigilance data, promotion of education and information on the appropriate use of psychoactive drugs and the impact of international control on medical availability of substances.

Topics: 4-Butyrolactone; Advisory Committees; Azabicyclo Compounds; Buprenorphine; Butorphanol; Catha; Dronabinol; Drug and Narcotic Control; Drug Evaluation; Health Services Accessibility; Humans; Hydroxybutyrates; Ketamine; Piperazines; Psychotropic Drugs; Substance-Related Disorders; Thebaine; Tramadol; World Health Organization