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Abstract

Buprenorphine effects in methadone-maintained volunteers: effects at two hours after methadone.

E C Strain, K L Preston, I A Liebson and G E Bigelow
Journal of Pharmacology and Experimental Therapeutics February 1995, 272 (2) 628-638;
E C Strain
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K L Preston
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I A Liebson
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G E Bigelow
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Abstract

Buprenorphine is an opioid partial agonist being developed for possible use in the treatment of opioid dependence. In a previous study up to 8 mg of buprenorphine administered 20 hr after a daily dose of methadone in methadone-maintained volunteers produced neither agonist-like nor antagonist-like effects. The purpose of this study was to examine the effects of buprenorphine challenges given 2 hr after a daily methadone dose in maintained volunteers. Seven male volunteers maintained on 30 mg of methadone daily underwent pharmacologic challenges two to three times per week. Medication challenges consisted of double-blind i.m. injections of buprenorphine (0.5-8.0 mg), the opioid antagonist naloxone (0.1 and 0.2 mg), the prototypic opioid mu agonist hydromorphone (5 and 10 mg) or saline. Assessments of physiologic measures, volunteers' self-reports and observer ratings of drug effects were collected in a laboratory session for 2 hr after drug administration, and then for 8 additional hr postsession. Results from the laboratory session showed that on subject and observer ratings naloxone produced typical antagonist-like effects, hydromorphone produced mild agonist-like effects and buprenorphine produced antagonist-like effects. Interestingly, buprenorphine's antagonist activity was not directly dose-related; its most prominent antagonist effects occurred at the 1- and 2-mg doses. These results are consistent with buprenorphine's action as a partial mu opioid agonist and demonstrate that antagonist-like effects can occur under some conditions suggesting buprenorphine should have a low abuse liability in methadone-maintained patients.

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Journal of Pharmacology and Experimental Therapeutics
Vol. 272, Issue 2
1 Feb 1995
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Abstract

Buprenorphine effects in methadone-maintained volunteers: effects at two hours after methadone.

E C Strain, K L Preston, I A Liebson and G E Bigelow
Journal of Pharmacology and Experimental Therapeutics February 1, 1995, 272 (2) 628-638;

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Abstract

Buprenorphine effects in methadone-maintained volunteers: effects at two hours after methadone.

E C Strain, K L Preston, I A Liebson and G E Bigelow
Journal of Pharmacology and Experimental Therapeutics February 1, 1995, 272 (2) 628-638;
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