The effect of different sulfonamides on phenytoin metabolism in man.
The effect of different sulfonamides on phenytoin metabolism in man.
复制标题
不同磺胺类药物对人体苯妥英代谢的影响。
DOI：
10.1111/j.0954-6820.1979.tb00729.x
复制
发表时间：
2009
期刊：
影响因子：
--
通讯作者：
L. Skovsted
中科院分区：
文献类型：
--
作者：
J. Hansen;J. Kampmann;K. Siersbaek;I. B. Lumholtz;M. Arrøé;U. Abildgaard;L. Skovsted
本文研究了常用临床剂量的磺胺类药物对苯妥英代谢的影响。在单次给药实验中，磺胺苯吡唑使苯妥英半衰期（T/2）延长237%，使苯妥英代谢清除率（MCR）降低67%。磺胺嘧啶、磺胺甲噻唑、磺胺甲恶唑+甲氧苄啶和甲氧苄啶分别使苯妥英T/2增加80、66、39和51%，使苯妥英MCR分别降低45、36、27和30%。磺胺甲恶唑导致苯妥英T/2小幅但显著增加，但苯妥英MCR未相应下降。用磺胺甲氧哒嗪、磺胺二甲氧嘧啶和磺胺甲氧嘧啶治疗后，苯妥英T/2和MCR无变化。稳态实验证实了单次给药实验的结果。提示磺胺苯吡唑、磺胺嘧啶、磺胺甲唑、磺胺甲恶唑+甲氧苄啶和甲氧苄啶抑制苯妥英的肝代谢。
The influence on the metabolism of phenytoin of some sulfonamides given in common clinical doses has been studied. In single dose experiments sulfaphenazole increased phenytoin half-life (T/2) by 237% and decreased phenytoin metabolic clearance rate (MCR) by 67%. Sulfadiazine, sulfamethiazole, sulfamethoxazole + trimethoprim and trimethoprim increased phenytoin T/2 by 80, 66, 39 and 51% respectively, and decreased phenytoin MCR by 45, 36, 27 and 30% respectively. Sulfamethoxazole gave a small but significant increase in phenytoin T/2 but not a corresponding fall in phenytoin MCR. No changes were found in phenytoin T/2 and MCR after treatment with sulfamethoxypyridazine, sulfadimethoxine and sulfamethoxydiazine. Steady state experiments confirmed the findings of the single dose experiments. It is suggested that sulfaphenazole, sulfadiazine, sulfamethizole, sulfamethoxazole + trimethoprim and trimethoprim inhibit hepatic metabolism of phenytoin.