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首页> 外文期刊>Journal of Analytical Toxicology >Procainamide and quinidine inhibition of the human hepatic degradation of meperidine in vitro.
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Procainamide and quinidine inhibition of the human hepatic degradation of meperidine in vitro.

机译:普鲁卡因酰胺和奎尼丁在体外抑制人肝素对哌替啶的降解。

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摘要

Procainamide and quinidine inhibition of the degradation of meperidine in human liver was investigated by incubation of two concentrations of either drug with meperidine in homogenates of human liver over 24 and 36 h. Meperidine concentrations declined by 26% after incubation for 24 h and by 42% after incubation for 36 h. In the presence of procainamide, however, they decreased by only 15% to 18% at 24 h and by only 26% to 28% at 36 h. In the presence of quinidine, they declined by only 18% to 19% at 24 h and by only 27% to 28% at 36 h. Procainamide and quinidine may inhibit human hepatic carboxylesterase hCE-1, which is responsible for catalyzing the hydrolysis of meperidine. This inhibition may prolong the biological half-life of meperidine in patients receiving the drug together with either procainamide or quinidine.
机译:通过在人肝匀浆中将两种浓度的两种药物与哌啶一起温育在人肝的匀浆中24小时和36小时,研究了普鲁卡因酰胺和奎尼丁对人肝素中哌替啶降解的抑制作用。孵育24小时后,哌替啶浓度降低26%,孵育36小时后降低42%。但是,在普鲁卡因酰胺存在下,它们在24小时内仅降低15%至18%,在36小时时仅降低26%至28%。在奎尼丁存在下,它们在24 h时仅下降18%至19%,在36 h时仅下降27%至28%。普鲁卡因酰胺和奎尼丁可能抑制人肝羧酸酯酶hCE-1,后者负责催化哌替啶的水解。这种抑制作用可以延长与普鲁卡因胺或奎尼丁同时接受药物治疗的患者的哌替啶的生物半衰期。

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