Yamazaki M, Suzuki T, Narita M, Lipkowski A W
Intensive Care Unit, Toyama Medical and Pharmaceutical University Hospital, Sugitani, Toyama, Japan.
Life Sci. 2001 Jul 20;69(9):1023-8. doi: 10.1016/s0024-3205(01)01194-8.
We compared the physical dependence liability of biphalin, a dimeric enkephalin analogue that possesses high antinociceptive activity, with that of morphine in equipotent intravenous doses. Naloxone challenge produced severe withdrawal signs after a 5-day infusion of morphine but only minor withdrawal signs after a 5-day biphalin infusion. In a cross-dependence study, biphalin did not suppress body weight loss after morphine withdrawal, but successfully suppressed weight loss after pentazocine withdrawal. These data support consideration of biphalin as a new analgesic with a novel pharmacological profile and minimum dependence liability.
我们比较了双丙戊酸（一种具有高抗伤害感受活性的二聚脑啡肽类似物）与吗啡在等效静脉剂量下的身体依赖性倾向。在吗啡进行5天输注后，纳洛酮激发试验产生了严重的戒断症状，但在双丙戊酸进行5天输注后仅产生了轻微的戒断症状。在一项交叉依赖性研究中，双丙戊酸不能抑制吗啡戒断后的体重减轻，但能成功抑制喷他佐辛戒断后的体重减轻。这些数据支持将双丙戊酸视为一种具有新型药理学特征和最小依赖性倾向的新型镇痛药。
