Resnick R B, Kestenbaum R S, Washton A, Poole D
Clin Pharmacol Ther. 1977 Apr;21(4):409-13. doi: 10.1002/cpt1977214409.
We examined naloxone-precipitated withdrawal as a means for rapid opiate detoxification and induction onto naltrexone. In 29 patients dependent on methadone (5 to 20 mg/day), abstinence was precipitated by an injection of naloxone. Repeated injections of naloxone were given subsequently until symptoms of abstinence were no longer induced. Successive injections induced less intense withdrawal assessed by vital signs and ratings on abstinence scales. The most rapid procedure consisted of 1.2 mg naxolone every 30 min for 3 to 6 hr, for 3 to 6 hr, followed by hourly increasing doses of naltrexone. This procedure allowed transition from opiate dependence to naltrexone maintenance (50 to 100 mg/day) within 48 hr. The results are consistent with assumptions that antagonists actively displace opiates from receptor sites.
我们研究了纳洛酮诱发戒断反应作为快速阿片类药物脱毒及诱导使用纳曲酮的一种方法。对29例依赖美沙酮(每日5至20毫克)的患者,通过注射纳洛酮诱发戒断反应。随后重复注射纳洛酮,直至不再诱发戒断症状。连续注射诱发的戒断反应强度通过生命体征及戒断量表评分评估逐渐减轻。最快速的方法是每30分钟注射1.2毫克纳洛酮,持续3至6小时,之后每小时增加纳曲酮剂量。该方法可使患者在48小时内从阿片类药物依赖过渡到纳曲酮维持治疗(每日50至100毫克)。这些结果与拮抗剂能主动将阿片类药物从受体部位置换出来的假设相符。