Buprenorphine sublingual tablets: effects on IV heroin self-administration by humans. 2001

S D Comer, and E D Collins, and M W Fischman
New York State Psychiatric Institute and Department of Psychiatry, College of Physicians and Surgeons of Columbia University, NY 10032, USA. sdc10@columbia.edu

BACKGROUND Studies have shown that buprenorphine, a partial mu opioid agonist, effectively reduces heroin taking. While previous research with buprenorphine utilized a liquid formulation, a tablet formulation is proposed for clinical use. However, because recent research suggests that the liquid and tablet differ in bio-availability, it is unclear what dose of the buprenorphine tablet effectively antagonizes the reinforcing effects of heroin. OBJECTIVE The present study was designed to compare the effects of two sublingual doses of buprenorphine maintenance on heroin self-administration. METHODS Eight heroin-dependent men participated in a 6-week, double-blind, placebo-controlled inpatient study to evaluate the reinforcing effects of intravenous heroin (0, 6.25, 12.5, 25 mg) during maintenance on 8 or 16 mg sublingual buprenorphine. Participants first sampled the available dose of heroin, and then were allowed to respond under a progressive ratio schedule for either heroin or $20. For each heroin dose, one sample session and three choice sessions occurred. Two sessions per day were conducted. A sample session was followed by the first choice session on one day, and the second and third choice sessions occurred on the following day. These sessions were conducted while participants were maintained on daily doses of 8 or 16 mg buprenorphine (3 weeks each). RESULTS Relative to placebo, 12.5 and 25 mg heroin produced significant increases in break point values under both maintenance dose conditions. The mean break point value for 12.5 mg heroin was significantly lower under 16 mg buprenorphine, compared to 8 mg. CONCLUSIONS These results demonstrate that the reinforcing effects of heroin were not fully antagonized by these doses of the tablet formulation of buprenorphine, and that 16 mg buprenorphine reduced heroin self-administration relative to 8 mg.

UI MeSH Term Description Entries
D008297 Male Males
D009292 Narcotic Antagonists Agents inhibiting the effect of narcotics on the central nervous system. Competitive Opioid Antagonist,Narcotic Antagonist,Opioid Antagonist,Opioid Antagonists,Opioid Receptor Antagonist,Opioid Reversal Agent,Competitive Opioid Antagonists,Opioid Receptor Antagonists,Opioid Reversal Agents,Agent, Opioid Reversal,Agents, Opioid Reversal,Antagonist, Competitive Opioid,Antagonist, Narcotic,Antagonist, Opioid,Antagonist, Opioid Receptor,Antagonists, Competitive Opioid,Antagonists, Narcotic,Antagonists, Opioid,Antagonists, Opioid Receptor,Opioid Antagonist, Competitive,Opioid Antagonists, Competitive,Receptor Antagonist, Opioid,Receptor Antagonists, Opioid,Reversal Agent, Opioid,Reversal Agents, Opioid
D009294 Narcotics Agents that induce NARCOSIS. Narcotics include agents that cause somnolence or induced sleep (STUPOR); natural or synthetic derivatives of OPIUM or MORPHINE or any substance that has such effects. They are potent inducers of ANALGESIA and OPIOID-RELATED DISORDERS. Analgesics, Narcotic,Narcotic Analgesics,Narcotic,Narcotic Effect,Narcotic Effects,Effect, Narcotic,Effects, Narcotic
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
D011680 Pupil The aperture in the iris through which light passes. Pupils
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
D003932 Heroin A narcotic analgesic that may be habit-forming. It is a controlled substance (opium derivative) listed in the U.S. Code of Federal Regulations, Title 21 Parts 329.1, 1308.11 (1987). Sale is forbidden in the United States by Federal statute. (Merck Index, 11th ed) Diacetylmorphine,Diamorphine,Diacetylmorphine Hydrochloride,Diagesil,Diamorf,Heroin Hydrochloride,Min-I-Jet Morphine Sulphate,Hydrochloride, Diacetylmorphine,Hydrochloride, Heroin,Min I Jet Morphine Sulphate
D005260 Female Females
D006556 Heroin Dependence Strong dependence or addiction, both physiological and emotional, upon HEROIN. Heroin Abuse,Heroin Addiction,Heroin Smoking,Abuse, Heroin,Addiction, Heroin,Dependence, Heroin,Heroin Smokings,Smoking, Heroin
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man

Related Publications

S D Comer, and E D Collins, and M W Fischman
October 1982, The Journal of pharmacology and experimental therapeutics,
S D Comer, and E D Collins, and M W Fischman
February 1994, Behavioural pharmacology,
S D Comer, and E D Collins, and M W Fischman
May 1998, The Journal of pharmacology and experimental therapeutics,
S D Comer, and E D Collins, and M W Fischman
September 2007, Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology,
S D Comer, and E D Collins, and M W Fischman
April 2002, Psychopharmacology,
S D Comer, and E D Collins, and M W Fischman
July 2001, Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology,
S D Comer, and E D Collins, and M W Fischman
February 1993, The Journal of pharmacology and experimental therapeutics,
S D Comer, and E D Collins, and M W Fischman
November 1993, Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology,
S D Comer, and E D Collins, and M W Fischman
September 1990, The Journal of pharmacology and experimental therapeutics,
S D Comer, and E D Collins, and M W Fischman
January 1980, Psychopharmacology,
Copied contents to your clipboard!