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新型强效促胃肠动力药多潘立酮的止吐作用。

The antiemetic effects of domperidone, a novel potent gastrokinetic.

作者信息

Niemegeers C J, Schellekens K H, Janssen P A

出版信息

Arch Int Pharmacodyn Ther. 1980 Mar;244(1):130-40.

PMID:7416883
Abstract

Domperidone is the prototype of a new chemical class of compounds with potent gastrokinetic properties. The present study reports on the antiemetic activity and safety of domperidone in dogs. The lowest ED50-values protecting from apomorphine (0.31 mg/kg s.c.) induced emesis are 0.003 mg/kg intravenously, 0.007 mg/kg subcutaneously, 0.03 mg/kg orally and 0.10 mg/kg rectally. Emesis induced by i.v. hydergine, s.c. morphine and oral levodopa is also prevented by low doses of intravenous domperidone, whereas oral copper sulphate-induced emesis is not antagonized. The doses of domperidone needed to induce central depressant effects in dogs (inhibition of conditioned reactions) are at least 300 times higher than the antiemetic doses (apomorphine-induced emesis). Domperidone is also devoid of sedative, adrenolytic and cardiovascular side-effects. The LD50-values in dogs are 42.7 mg/kg intravenously, and more than 160 mg/kg subcutaneously and orally.

摘要

多潘立酮是一类具有强大胃肠动力特性的新型化合物的原型。本研究报告了多潘立酮在犬类中的止吐活性和安全性。预防阿扑吗啡(0.31mg/kg皮下注射)诱发呕吐的最低半数有效剂量(ED50值)分别为:静脉注射0.003mg/kg、皮下注射0.007mg/kg、口服0.03mg/kg和直肠给药0.10mg/kg。静脉注射海得琴、皮下注射吗啡和口服左旋多巴诱发的呕吐也可被低剂量静脉注射的多潘立酮预防,而口服硫酸铜诱发的呕吐则不能被拮抗。在犬类中诱导中枢抑制作用(抑制条件反应)所需的多潘立酮剂量至少比止吐剂量(阿扑吗啡诱发的呕吐)高300倍。多潘立酮也没有镇静、抗肾上腺素能和心血管副作用。犬类的半数致死量(LD50值)分别为:静脉注射42.7mg/kg,皮下注射和口服超过160mg/kg。

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