Comer Sandra D, Collins Eric D, Fischman Marian W
Division on Substance Abuse, New York State Psychiatric Institute and Department of Psychiatry, College of Physicians and Surgeons of Columbia University, New York, New York 10032, USA.
J Pharmacol Exp Ther. 2002 Apr;301(1):266-76. doi: 10.1124/jpet.301.1.266.
Several sources indicate that intravenously administered buprenorphine may have significant abuse liability in humans. The present study evaluated the reinforcing effects of intravenously administered buprenorphine (0, 2, and 8 mg) in detoxified heroin-dependent participants during a 7.5-week inpatient study. Participants (n = 6) were detoxified from heroin over a 1.5-week period immediately after admission. Testing subsequently occurred in three 2-week blocks. During the first week of each 2-week block, the reinforcing effects of buprenorphine were evaluated. Participants first received a dose of buprenorphine and $20 and then were given either the opportunity to self-administer the dose or $20 during choice sessions. During the second week of each 2-week block, the direct effects of heroin were measured to evaluate potential long-lasting antagonist effects of buprenorphine. Progressive ratio break-point values were significantly higher after 2 and 8 mg of buprenorphine compared with placebo. Correspondingly, several positive subjective ratings increased after administration of active buprenorphine relative to placebo. Although there were few differences in peak effects produced by 2 versus 8 mg of buprenorphine, the higher buprenorphine dose generally produced longer-lasting effects. Heroin also produced dose-related increases in several subjective effects. Peak ratings produced by heroin were generally higher than peak ratings produced by buprenorphine. There was little evidence of residual antagonism produced by buprenorphine. These results demonstrate that buprenorphine served as a reinforcer under these conditions, and that it may have abuse liability in nonopioid-dependent individuals who abuse heroin.
有多个来源表明，静脉注射丁丙诺啡在人体中可能具有显著的滥用可能性。本研究在一项为期7.5周的住院研究中，评估了静脉注射丁丙诺啡（0、2和8毫克）对已戒毒的海洛因依赖参与者的强化作用。参与者（n = 6）入院后立即在1.5周内完成海洛因脱毒。随后的测试分三个为期2周的阶段进行。在每个2周阶段的第一周，评估丁丙诺啡的强化作用。参与者首先接受一剂丁丙诺啡和20美元，然后在选择环节中，他们有机会自行注射该剂量或获得20美元。在每个2周阶段的第二周，测量海洛因的直接作用，以评估丁丙诺啡潜在的持久拮抗作用。与安慰剂相比，2毫克和8毫克丁丙诺啡后的渐进比率断点值显著更高。相应地，与安慰剂相比，注射活性丁丙诺啡后，几项积极的主观评分有所增加。虽然2毫克和8毫克丁丙诺啡产生的峰值效应差异不大，但较高剂量的丁丙诺啡通常产生更持久的效应。海洛因也产生了与剂量相关的几种主观效应增加。海洛因产生的峰值评分通常高于丁丙诺啡产生的峰值评分。几乎没有证据表明丁丙诺啡产生了残留拮抗作用。这些结果表明，在这些条件下丁丙诺啡起到了强化物的作用，并且它可能对滥用海洛因的非阿片类药物依赖个体具有滥用可能性。
