Drug discrimination assessment of agonist-antagonist opioids in humans: a three-choice saline-hydromorphone-butorphanol procedure. 1994

K L Preston, and G E Bigelow
Department of Psychiatry and Behavioral Sciences, Johns Hopkins University School of Medicine, Baltimore, Maryland.

To assess the discriminative stimulus properties of mixed agonist-antagonist opioids in humans, postaddict volunteers were trained in a three-choice drug discrimination procedure to discriminate among the effects of saline (4 ml i.m.), hydromorphone (3 mg i.m.) and butorphanol (6 mg i.m.). Subjects earned monetary reinforcement by correctly identifying the training drugs by letter code. Other subjective, behavioral and physiological measures were concurrently collected. After training, generalization curves for hydromorphone, butorphanol, pentazocine, nalbuphine and buprenorphine were determined. In generalization testing, both hydromorphone and butorphanol produced dose-related increases in hydromorphone-appropriate and butorphanol-appropriate responses, respectively, and other characteristic subjective effect measures. Nalbuphine produced dose-related increases in discrimination as butorphanol and in those subjective effect measures increased by butorphanol. Buprenorphine produced dose-related increases in discrimination as hydromorphone and in those subjective effect measures increased by hydromorphone. Pentazocine was not consistently discriminated as either butorphanol or hydromorphone. These results differ from those of previous discrimination studies using similar methods but different training drugs. Compared to a previous study in which pentazocine served as the kappa-like training drug, the use as a training drug of the more pharmacologically specific kappa-like drug butorphanol permitted greater differentiation among test drugs and yielded discrimination results more consistent with other pharmacological evidence (buprenorphine being mu-like and nalbuphine being kappa-like). There was a close relationship between results of the discrimination measures and the subjective effect measures.

UI MeSH Term Description Entries
D008297 Male Males
D009266 Nalbuphine A narcotic used as a pain medication. It appears to be an agonist at KAPPA RECEPTORS and an antagonist or partial agonist at MU RECEPTORS. EN-2234A,Nalbuphine Hydrochloride,Nalbuphine Serb,Nubain,EN 2234A,EN2234A
D010423 Pentazocine The first mixed agonist-antagonist analgesic to be marketed. It is an agonist at the kappa and sigma opioid receptors and has a weak antagonist action at the mu receptor. (From AMA Drug Evaluations Annual, 1991, p97) Fortral,Lexir,Pentazocine Hydrochloride,Pentazocine Lactate,Talwin,Hydrochloride, Pentazocine,Lactate, Pentazocine
D011597 Psychomotor Performance The coordination of a sensory or ideational (cognitive) process and a motor activity. Perceptual Motor Performance,Sensory Motor Performance,Visual Motor Coordination,Coordination, Visual Motor,Coordinations, Visual Motor,Motor Coordination, Visual,Motor Coordinations, Visual,Motor Performance, Perceptual,Motor Performance, Sensory,Motor Performances, Perceptual,Motor Performances, Sensory,Perceptual Motor Performances,Performance, Perceptual Motor,Performance, Psychomotor,Performance, Sensory Motor,Performances, Perceptual Motor,Performances, Psychomotor,Performances, Sensory Motor,Psychomotor Performances,Sensory Motor Performances,Visual Motor Coordinations
D002047 Buprenorphine A derivative of the opioid alkaloid THEBAINE that is a more potent and longer lasting analgesic than MORPHINE. It appears to act as a partial agonist at mu and kappa opioid receptors and as an antagonist at delta receptors. The lack of delta-agonist activity has been suggested to account for the observation that buprenorphine tolerance may not develop with chronic use. 6029-M,Buprenex,Buprenorphine Hydrochloride,Buprex,Prefin,RX-6029-M,Subutex,Temgesic,Temgésic,6029 M,6029M,Hydrochloride, Buprenorphine,RX 6029 M,RX6029M
D002077 Butorphanol A synthetic morphinan analgesic with narcotic antagonist action. It is used in the management of severe pain. 17-(Cyclobutylmethyl)morphinan-3,14-diol,Apo-Butorphanol,BC-2627,Beforal,Butorphanol Tartrate,Dolorex,Moradol,Stadol,Stadol NS,Torbugesic,BC 2627,BC2627
D004091 Hydromorphone An opioid analgesic made from MORPHINE and used mainly as an analgesic. It has a shorter duration of action than morphine. Dihydromorphinone,Hydromorphon,Dilaudid,Hydromorphone Hydrochloride,Laudacon,Palladone
D004193 Discrimination Learning Learning that is manifested in the ability to respond differentially to various stimuli. Discriminative Learning,Discrimination Learnings,Discriminative Learnings,Learning, Discrimination,Learning, Discriminative
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D005793 Generalization, Psychological The phenomenon of an organism's responding to all situations similar to one in which it has been conditioned. Generalization (Psychology),Generalization, Psychology,Generalizations (Psychology),Generalizations, Psychological,Generalizations, Psychology,Psychological Generalization,Psychological Generalizations,Psychology Generalization,Psychology Generalizations

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