Acute effects of intramuscular and sublingual buprenorphine and buprenorphine/naloxone in non-dependent opioid abusers.
Acute effects of intramuscular and sublingual buprenorphine and buprenorphine/naloxone in non-dependent opioid abusers.
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DOI：
10.1007/s00213-010-1898-4
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发表时间：
2010-08
影响因子：
3.4
通讯作者：
Strain, Eric C.
中科院分区：
文献类型：
--
作者：
Duke, Angela N.;Correia, Christopher J.;Walsh, Sharon L.;Bigelow, George E.;Strain, Eric C.
丁丙诺啡是一种部分MU阿片受体激动剂，作为阿片依赖的药物治疗具有临床疗效。开发了一种含有丁丙诺啡和纳洛酮的舌下联合制剂，目的是减少阿片类药物依赖个人的滥用倾向。然而，当没有阿片类药物身体依赖的个人服用时，添加纳洛酮可能不会限制该药物的滥用潜力。本研究调查了丁丙诺啡单独和联合纳洛酮肌肉注射和舌下注射对非依赖阿片类药物滥用者的影响。在受试者内交叉设计中，非依赖阿片类药物经验的志愿者(N=8)通过肌肉和舌下途径给予急性剂量的丁丙诺啡(4，8，16 mg)和丁丙诺啡/纳洛酮(4/1，8/2，16/4 mg)，肌肉注射氢吗啡(2，4 mg作为阿片类激动剂对照)和安慰剂，总共15种药物条件。实验采用双盲、双假人设计，每周进行两次。丁丙诺啡和丁丙诺啡/纳洛酮产生类似于氢吗啡的作用。与舌下注射中剂量丁丙诺啡以及丁丙诺啡/纳洛酮低剂量和高剂量联合给药相比，肌肉注射产生的效果更大。添加纳洛酮并未显著改变丁丙诺啡的作用。这些结果表明，丁丙诺啡和丁丙诺啡/纳洛酮在非依赖性阿片类药物滥用者中具有类似的滥用潜力，在这些剂量和这种剂量比例下添加纳洛酮对于减少该人群肌肉内或舌下丁丙诺啡的滥用潜力没有明显优势。
Buprenorphine is a partial mu opioid receptor agonist with clinical efficacy as a pharmacotherapy for opioid dependence. A sublingual combination formulation was developed containing buprenorphine and naloxone with the intent of decreasing abuse liability in opioid dependent individuals. However, the addition of naloxone may not limit abuse potential of this medication when taken by individuals without opioid physical dependence. The present study investigated the effects of buprenorphine alone and in combination with naloxone administered intramuscularly and sublingually to non-dependent opioid abusers. In a within-subject crossover design, non-dependent opioid-experienced volunteers (N=8) were administered acute doses of buprenorphine (4, 8, 16 mg) and buprenorphine/naloxone (4/1, 8/2, 16/4 mg) via both intramuscular and sublingual routes, intramuscular hydromorphone (2, 4 mg as an opioid agonist control), and placebo, for a total of 15 drug conditions. Laboratory sessions were conducted twice per week using a double blind, double-dummy design. Buprenorphine and buprenorphine/naloxone engendered effects similar to hydromorphone. Intramuscular administration produced a greater magnitude of effects compared to the sublingual route at the intermediate dose of buprenorphine and at both the low and high doses of the buprenorphine/naloxone combination. The addition of naloxone did not significantly alter the effects of buprenorphine. These results suggest that buprenorphine and buprenorphine/naloxone have similar abuse potential in non-dependent opioid abusers, and that the addition of naloxone at these doses and in this dose ratio confers no evident advantage for decreasing the abuse potential of intramuscular or sublingual buprenorphine in this population.
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影响因子：
7.3
作者：
DUM, JE;HERZ, A
通讯作者：
HERZ, A
DOI：
10.1124/jpet.102.038141
发表时间：
2002-11-01
影响因子：
3.5
作者：
Comer, SD;Collins, ED
通讯作者：
Collins, ED
影响因子：
4.2
作者：
LEWIS, JW
通讯作者：
LEWIS, JW
影响因子：
2.9
作者：
Mendelson, J;Upton, RA;Jones, RT
通讯作者：
Jones, RT
影响因子：
4.2
作者：
Rosado, James;Walsh, Sharon L.;Strain, Eric C.
通讯作者：
Strain, Eric C.