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甲哌卡因和丙胺卡因的药代动力学及临床药理学研究。

Pharmacokinetic and clinical pharmacological studies with mepivacaine and prilocaine.

作者信息

Arthur G R, Scott D H, Boyes R N, Scott D B

出版信息

Br J Anaesth. 1979 Jun;51(6):481-5. doi: 10.1093/bja/51.6.481.

DOI:10.1093/bja/51.6.481
PMID:380609
Abstract

The tolerance and pharmacokinetic properties of mepivacaine and prilocaine were compared following i.v. infusion of 250 mg (0.88 and 0.97 mmol respectively) of each drug in five healthy volunteers. Side-effects were minor and occurred in only two subjects during the infusion of mepivacaine. Plasma concentrations of mepivacaine were greater in each subject than the corresponding values for prilocaine. The elimination half-life of mepivacaine was generally longer than that for prilocaine, whereas the total body clearance of prilocaine was consistently greater than the corresponding value for mepivacaine. For each subject the clearance of prilocaine substantially exceeded normal heptic blood flow and therefore an extra-hepatic site of metabolism of prilocaine has been postulated.

摘要

在五名健康志愿者中静脉输注250毫克(分别为0.88和0.97毫摩尔)的甲哌卡因和丙胺卡因后,比较了它们的耐受性和药代动力学特性。副作用较小,仅在输注甲哌卡因时有两名受试者出现。甲哌卡因在每个受试者中的血浆浓度均高于丙胺卡因的相应值。甲哌卡因的消除半衰期通常比丙胺卡因长,而丙胺卡因的全身清除率始终高于甲哌卡因的相应值。对于每个受试者,丙胺卡因的清除率大大超过正常肝血流量,因此推测丙胺卡因存在肝外代谢部位。

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