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枸橼酸哌嗪与盐酸利多卡因的抗心律失常及局部麻醉作用比较

Comparative antiarrhythmic and local anaesthetic effects of piperazine citrate and lignocaine hydrochloride.

作者信息

Onuaguluchi G, Igbo I N

出版信息

Arch Int Pharmacodyn Ther. 1985 Apr;274(2):253-66.

PMID:4026459
Abstract

The effect of pretreatment with lignocaine hydrochloride (0.1 mg/g body weight) and piperazine citrate (1 mg/g body weight) on the number of deaths due to ouabain (0.02-0.12 mg/g body weight) was determined in the toad. Lignocaine was at least 10 times more potent than piperazine. Considering the doses that gave 50% protection from the 100% deaths due to ouabain (0.09 mg/g), lignocaine was 14.8 times more potent, but it was 56-60 times more toxic than piperazine as shown by the LD50s in the mouse and toad. Lignocaine was also about 10 times more potent than piperazine in preventing electrically-induced arrhythmia in the isolated guinea-pig atrium suspended in low potassium Ringer-Locke solution. With regard to infiltration anaesthesia, lignocaine was about 158 times more potent than piperazine. Therefore the relative potencies of the antiarrhythmic activities of piperazine and lignocaine do not correlate with the relative local anaesthetic potencies. It was concluded that, although lignocaine is 10-15 times more potent than piperazine as an antiarrhythmic agent, piperazine should be a much safer drug and could have potential utility as a substitute for lignocaine as an antiarrhythmic agent.

摘要

在蟾蜍身上测定了盐酸利多卡因(0.1毫克/克体重)和枸橼酸哌嗪(1毫克/克体重)预处理对因哇巴因(0.02 - 0.12毫克/克体重)导致的死亡数量的影响。利多卡因的效力至少是哌嗪的10倍。考虑到给予50%保护以避免因哇巴因导致100%死亡(0.09毫克/克)的剂量,利多卡因的效力高14.8倍,但如在小鼠和蟾蜍身上测定的半数致死量所示,其毒性比哌嗪高56 - 60倍。在防止悬浮于低钾林格 - 洛克溶液中的离体豚鼠心房发生电诱导心律失常方面,利多卡因的效力也比哌嗪高约10倍。关于浸润麻醉,利多卡因的效力比哌嗪高约158倍。因此,哌嗪和利多卡因抗心律失常活性的相对效力与相对局部麻醉效力不相关。得出的结论是,尽管利多卡因作为抗心律失常药物的效力比哌嗪高10 - 15倍,但哌嗪应该是一种更安全的药物,并且有可能作为利多卡因的替代抗心律失常药物具有潜在用途。

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