Harris D S, Jones R T, Welm S, Upton R A, Lin E, Mendelson J
Drug Dependence Research Center, Langley Porter Psychiatric Institute, and Department of Biopharmaceutical Sciences, University of California, San Francisco, 401 Parnassus Avenue, 94143-0984, San Francisco, CA 94143-0984, USA.
Drug Alcohol Depend. 2000 Dec 22;61(1):85-94. doi: 10.1016/s0376-8716(00)00126-5.
Buprenorphine and naloxone sublingual (s.l.) dose formulations may decrease parenteral buprenorphine abuse. We evaluated pharmacologic interactions between 8 mg s.l. buprenorphine combined with 0, 4, or 8 mg of naloxone in nine opiate-dependent volunteers stabilized on 8 mg s.l. buprenorphine for 7 days. Combined naloxone and buprenorphine did not diminish buprenorphine's effects on opiate withdrawal nor alter buprenorphine bioavailability. Opiate addicts stabilized on buprenorphine showed no evidence of precipitated opiate withdrawal after s.l. buprenorphine-naloxone combinations. Buprenorphine and naloxone bioavailability was approximately 40 and 10%, respectively. Intravenous buprenorphine and naloxone produced subjective effects similar to those of s.l. buprenorphine and did not precipitate opiate withdrawal.
丁丙诺啡和纳洛酮舌下给药剂量配方可能会减少丁丙诺啡注射剂的滥用情况。我们评估了在9名依赖阿片类药物的志愿者中,8毫克舌下丁丙诺啡与0、4或8毫克纳洛酮联合使用的药理相互作用,这些志愿者已服用8毫克舌下丁丙诺啡稳定剂量7天。纳洛酮与丁丙诺啡联合使用既没有减弱丁丙诺啡对阿片类药物戒断的作用,也没有改变丁丙诺啡的生物利用度。服用丁丙诺啡稳定剂量的阿片类药物成瘾者在舌下含服丁丙诺啡 - 纳洛酮组合后,没有出现阿片类药物戒断症状加剧的迹象。丁丙诺啡和纳洛酮的生物利用度分别约为40%和10%。静脉注射丁丙诺啡和纳洛酮产生的主观效果与舌下含服丁丙诺啡相似,且不会引发阿片类药物戒断症状。