摘要
为证实氯硝基安定(clonazepam,CZP)经直肠给药的有效性,按每公斤体重1.5和0.1mgCZP溶液分别进行Wistar大鼠及儿童单剂直肠给药的药动学及药效研究。结果表明,CZP溶液能被直肠迅速吸收,分别于5及10~20分钟达到有效血浓度及峰浓度,比肌内、皮下注射和口服吸收迅速。给药5分钟后,大鼠及儿童脑电背景活动均明显改变,癫痫放电波抑制,并能有效抑制美解眠诱发的大鼠惊厥发作和死亡。未发现局部或全身副作用。说明直肠注入CZP溶液是一种简便安全,快速有效的急救用药途径,对惊厥的现场抢救有重要价值。
To study the efficacy of rectal administration of clonazepam (CNP), the authors administrated CNP rectally to Wistar rats in a dose of 1.5 mg/kg and to children in a dose of 0.1 mg/kg. The pharmacokinetics demonstrated that in both rats and children CNP was rapidly absorbed from rectum with a therapeutic and peak blood level at 5 and 10~20 minutes, respectively. At 5 min after CNP administration, EEG patterns were significantly changed with complete disappearance of epileptic discharges. CNP also effectively prevented severe seizures induced by megimide. There were no obviously pathological changes of rectal mucosa or any side effect in children. The results suggest that CNP administrated rectally is a safe, quick and effective way to control seizures, which can be used easily and conveniently for outpatients.
出处
《中华儿科杂志》
CAS
CSCD
北大核心
1997年第4期202-205,共4页
Chinese Journal of Pediatrics
关键词
氯硝西泮
惊厥
直肠给药
药代动力学
儿童
Clonazepam Administration, rectum Pharmacokinetics Pharmacology