Dorandeu Frederic, Baille Valerie, Mikler John, Testylier Guy, Lallement Guy, Sawyer Thomas, Carpentier Pierre
Département de Toxicologie/CRSSA, 24 avenue des Maquis du Grésivaudan, La Tronche, France.
Toxicology. 2007 May 20;234(3):185-93. doi: 10.1016/j.tox.2007.02.012. Epub 2007 Feb 24.
Soman poisoning is known to induce full-blown tonic-clonic seizures, status epilepticus (SE), seizure-related brain damage (SRBD) and lethality. Previous studies in guinea-pigs have shown that racemic ketamine (KET), with atropine sulfate (AS), is very effective in preventing death, stopping seizures and protecting sensitive brain areas when given up to 1h after a supra-lethal challenge of soman. The active ketamine isomer, S(+) ketamine (S-KET), is more potent than the racemic mixture and it also induces less side-effects. To confirm the efficacy of KET and to evaluate the potential of S-KET for delayed medical treatment of soman-induced SE, we studied different S-KET dose regimens using the same paradigm used with KET. Guinea-pigs received pyridostigmine (26 microg/kg, IM) 30min before soman (62 microg/kg, 2 LD(50), IM), followed by therapy consisting of atropine methyl nitrate (AMN) (4 mg/kg, IM) 1min following soman exposure. S-KET, with AS (10mg/kg), was then administered IM at different times after the onset of seizures, starting at 1h post-soman exposure. The protective efficacy of S-KET proved to be comparable to KET against lethality and SRBD, but at doses two to three times lower. As with KET, delaying treatment by 2h post-poisoning greatly reduced efficacy. Conditions that may have led to an increased S-KET brain concentration (increased doses or number of injections, adjunct treatment with the oxime HI-6) did not prove to be beneficial. In summary, these observations confirm that ketamine, either racemic or S-KET, in association with AS and possibly other drugs, could be highly effective in the delayed treatment of severe soman intoxication.
已知梭曼中毒会引发全面的强直阵挛性癫痫发作、癫痫持续状态(SE)、癫痫相关脑损伤(SRBD)以及致死性。先前对豚鼠的研究表明,消旋氯胺酮(KET)与硫酸阿托品(AS)联合使用时,在梭曼超致死剂量攻击后1小时内给药,对于预防死亡、终止癫痫发作以及保护敏感脑区非常有效。氯胺酮的活性异构体S(+)氯胺酮(S-KET)比消旋混合物更有效,且副作用更少。为了证实KET的疗效并评估S-KET对梭曼诱导的SE进行延迟药物治疗的潜力,我们使用与KET相同的模式研究了不同的S-KET剂量方案。豚鼠在注射梭曼(62μg/kg,2倍半数致死剂量,肌肉注射)前30分钟接受吡啶斯的明(26μg/kg,肌肉注射),随后在接触梭曼1分钟后接受硝酸甲基阿托品(AMN)(4mg/kg,肌肉注射)治疗。然后在癫痫发作开始后的不同时间,即梭曼暴露后1小时开始,肌肉注射S-KET与AS(10mg/kg)。结果证明,S-KET在预防致死性和SRBD方面的保护效果与KET相当,但剂量低两到三倍。与KET一样,中毒后延迟2小时治疗会大大降低疗效。可能导致S-KET脑浓度增加的情况(增加剂量或注射次数、与肟HI-6联合治疗)并未证明有益。总之,这些观察结果证实,氯胺酮,无论是消旋体还是S-KET,与AS以及可能的其他药物联合使用,在严重梭曼中毒的延迟治疗中可能非常有效。