Fadda F, Mosca E, Meloni R, Gessa G L
Eur J Pharmacol. 1985 Mar 12;109(3):321-5. doi: 10.1016/0014-2999(85)90391-7.
Progabide, a specific and clinically used GABA receptor agonist, was tested for its ability to suppress ethanol withdrawal syndrome. Male rats were rendered physically dependent on ethanol by feeding for 12 days on a liquid diet in which ethanol isocalorically replaced dextrose. Progabide (100-400 mg/kg i.p.), administered 8 h after ethanol was withdrawn, produced a dose-related inhibition of both tremors and audiogenically induced seizures. A single dose of 400 mg/kg of progabide completely suppressed all ethanol withdrawal reactions. Seizures were more sensitive to the drug than tremors. The results support the view that a decrease in GABA transmission plays a role in ethanol withdrawal symptoms and suggest that progabide may be tested as a possible treatment of ethanol withdrawal syndrome in man.
普罗加比是一种特效且临床常用的γ-氨基丁酸(GABA)受体激动剂,对其抑制乙醇戒断综合征的能力进行了测试。通过给雄性大鼠喂食12天液体饲料(其中乙醇等热量替代葡萄糖)使其对乙醇产生身体依赖。在撤掉乙醇8小时后腹腔注射普罗加比(100 - 400毫克/千克),对震颤和听源性惊厥均产生剂量相关的抑制作用。单次给予400毫克/千克的普罗加比可完全抑制所有乙醇戒断反应。惊厥对该药物比震颤更敏感。结果支持γ-氨基丁酸传递减少在乙醇戒断症状中起作用这一观点,并表明普罗加比可作为人类乙醇戒断综合征可能的治疗方法进行测试。