Pickworth W B, Johnson R E, Holicky B A, Cone E J
National Institute on Drug Abuse, Addiction Research Center, Baltimore, MD 21224.
Clin Pharmacol Ther. 1993 May;53(5):570-6. doi: 10.1038/clpt.1993.72.
The pharmacologic profile of sublingual and subcutaneous buprenorphine, a partial opioid agonist, indicates it may be useful as a maintenance drug in the treatment of opioid dependence. However, illicit intravenous self-administration suggests that it may have a greater abuse potential by this route of administration. Physiologic and subjective effects of intravenous buprenorphine (0.0, 0.3, 0.6, and 1.2 mg) were determined in a dose-escalation study in six nondependent volunteers with histories of opioid use. Buprenorphine caused miosis and decreased respiratory rate, increased diastolic blood pressure, and transiently increased heart rate. Buprenorphine increased positive responses on a "feel drug" question and scores on scales of "liking," "good effects," euphoria, and apathetic sedation. Physiologic and subjective responses were not consistently dose related, a finding compatible with the pharmacologic profile of a partial agonist. The findings indicate that buprenorphine has substantial potential for abuse when administered intravenously.
舌下和皮下注射丁丙诺啡（一种阿片类部分激动剂）的药理学特征表明，它可能作为维持药物用于治疗阿片类药物依赖。然而，非法静脉自我给药表明，通过这种给药途径它可能具有更大的滥用潜力。在一项剂量递增研究中，对6名有阿片类药物使用史的非依赖志愿者测定了静脉注射丁丙诺啡（0.0、0.3、0.6和1.2毫克）的生理和主观效应。丁丙诺啡导致瞳孔缩小、呼吸频率降低、舒张压升高以及心率短暂加快。丁丙诺啡增加了关于“感觉药物”问题的阳性反应以及“喜欢”“良好效应”“欣快感”和“淡漠性镇静”量表的得分。生理和主观反应与剂量并非始终相关，这一发现与部分激动剂的药理学特征相符。这些发现表明，静脉注射丁丙诺啡时有很大的滥用潜力。
