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利多卡因及其活性代谢物在犬体内的药代动力学

Pharmacokinetics of lidocaine and its active metabolites in dogs.

作者信息

Wilcke J R, Davis L E, Neff-Davis C A, Koritz G D

出版信息

J Vet Pharmacol Ther. 1983 Mar;6(1):49-57. doi: 10.1111/j.1365-2885.1983.tb00454.x.

DOI:10.1111/j.1365-2885.1983.tb00454.x
PMID:6854732
Abstract

The pharmacokinetics of lidocaine in dogs were investigated following the intravenous and intramuscular administration of single doses of lidocaine hydrochloride. The mean elimination rate constant and the mean specific clearance determined for the intravenous portion of the study were 0.786 h-1 and 2.40 1/kg/h, respectively. Following intramuscular administration the mean absorption rate constant was 7.74 h-1. Absorption was nearly complete as the percentage of an intramuscular dose absorbed averaged 91.9%. Concentrations of two N-deethylated metabolites, determined following the administration of lidocaine suggest that monoethylglycinexylidide is eliminated rapidly while glycinexylidide is more slowly eliminated. The relative contribution of these metabolites to the therapeutic and toxic effects of lidocaine and the potential for glycinexylidide accumulation during lidocaine administration remain to be investigated.

摘要

在犬单次静脉注射和肌肉注射盐酸利多卡因后,对其药代动力学进行了研究。该研究静脉给药部分测得的平均消除速率常数和平均比清除率分别为0.786 h⁻¹和2.40 l/kg/h。肌肉注射后,平均吸收速率常数为7.74 h⁻¹。肌肉注射剂量的平均吸收百分比为91.9%,吸收几乎完全。利多卡因给药后测定的两种N-去乙基代谢物的浓度表明,单乙基甘氨酰二甲苯酰胺消除迅速,而甘氨酰二甲苯酰胺消除较慢。这些代谢物对利多卡因治疗和毒性作用的相对贡献以及利多卡因给药期间甘氨酰二甲苯酰胺蓄积的可能性仍有待研究。

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