Self-administration of intravenous buprenorphine and the buprenorphine/naloxone combination by recently detoxified heroin abusers
Self-administration of intravenous buprenorphine and the buprenorphine/naloxone combination by recently detoxified heroin abusers
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DOI：
10.1124/jpet.102.038141
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发表时间：
2002-11-01
影响因子：
3.5
通讯作者：
Collins, ED
中科院分区：
文献类型：
--
作者：
Comer, SD;Collins, ED
丁丙诺啡是一种部分μ-阿片类激动剂和κ-阿片类拮抗剂，目前正在开发作为海洛因依赖的维持药物。由于担心丁丙诺啡的非法转移，已开发出含有丁丙诺啡和纳洛酮的复方片剂。本研究在一项为期6周的住院研究中评价了安慰剂、丁丙诺啡单药（BUP; 2和8 mg）和丁丙诺啡/纳洛酮联合给药（BUP/NX; 2 mg丁丙诺啡+0. 5 mg纳洛酮，8 mg丁丙诺啡+2 mg纳洛酮）对近期脱毒的海洛因滥用者的强化作用。参与者（n = 6）在入院后立即戒毒约1周。在接下来的5周内，评价了安慰剂、BUP和BUP/NX的强化作用。参与者首先接受一剂药物和20美元，然后有机会在选择期间自我管理剂量或20美元。与安慰剂相比，活性药物治疗后的进展比率断点值显著更高，但作为剂量或药物的函数，它们没有显著差异。相比之下，与BUP/NX相比，BUP给药后的积极主观评分更高，并且这些评分以剂量依赖性方式增加。BUP和组合对性能几乎没有影响。与安慰剂相比，BUP和BUP/NX均降低了瞳孔直径，但瞳孔直径作为药物或剂量的函数无显著差异。这些结果表明，无论是BUP和BUP/NX在这些条件下作为兴奋剂，他们可能有类似的滥用倾向，在最近戒毒的个人滥用海洛因。
Buprenorphine is a partial mu-opioid agonist and kappa-opioid antagonist currently under development as a maintenance medication for heroin dependence. Because of concerns about illicit diversion of buprenorphine, a combination tablet containing buprenorphine and naloxone has been developed. The present study evaluated the reinforcing effects of intravenously administered placebo, buprenorphine alone (BUP; 2 and 8 mg), and the buprenorphine/naloxone combination (BUP/NX; 2 mg of buprenorphine plus 0.5 mg of naloxone, and 8 mg of buprenorphine plus 2 mg of naloxone) in recently detoxified heroin abusers during a 6-week inpatient study. Participants (n = 6) were detoxified from heroin over approximately 1 week immediately after admission. During the next 5 weeks, the reinforcing effects of placebo, BUP, and BUP/NX were evaluated. Participants first received a dose of drug and $20 and then were given the opportunity to self-administer either the dose or $20 during choice sessions. Progressive ratio break point values were significantly higher after active drug, compared with placebo, but they did not significantly differ as a function of dose or drug. In contrast, positive subjective ratings were higher after administration of BUP compared with BUP/NX, and these ratings increased in a dose-dependent manner. BUP and the combination had few effects on performance. Relative to placebo, both BUP and BUP/NX decreased pupil diameter, but there were no significant differences in pupil diameter as a function of drug or dose. These results demonstrate that both BUP and BUP/NX served as reinforcers under these conditions and that they may have similar abuse liability in recently detoxified individuals who abuse heroin.