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左非他明类阿片样活性的临床及实验证据。

Clinical and experimental evidence of an opiate-like activity of lefetamine.

作者信息

Paroli E, Nencini P, Moscucci M

出版信息

Pharmacol Res Commun. 1984 Sep;16(9):915-22. doi: 10.1016/s0031-6989(84)80028-4.

DOI:10.1016/s0031-6989(84)80028-4
PMID:6095332
Abstract

A case of lefetamine abuse (0.9-1.8 g/day in 15-30 i.m. divided doses) is reported. In this patient, the administration of naloxone precipitated a mild opiate-like withdrawal syndrome, characterized by mydriasis, piloerection, yawning and a slight increase of blood pressure. The complete withdrawal of lefetamine, substituted by a placebo regimen, aggravated these symptoms. Furthermore, experimental results showed that lefetamine induced a naloxone-reversible inhibition of the guinea-pig ileum contractile response to electric field stimulation, and that naloxone pretreatment of mice prevented lefetamine antinociceptive activity in the hot-plate test. The clinical and experimental findings suggest that lefetamine has an opiate-like activity.

摘要

报告了一例左非他明滥用病例(每天0.9 - 1.8克,分15 - 30次肌肉注射)。在该患者中,给予纳洛酮引发了轻度阿片样戒断综合征,其特征为瞳孔散大、竖毛、打哈欠以及血压略有升高。用安慰剂方案替代左非他明完全停药后,这些症状加重。此外,实验结果表明,左非他明可诱导豚鼠回肠对电场刺激的收缩反应出现纳洛酮可逆性抑制,并且对小鼠进行纳洛酮预处理可在热板试验中阻止左非他明的镇痛活性。临床和实验结果提示左非他明具有阿片样活性。

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