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肾功能受损患者中磺胺甲恶唑及其代谢产物N4-乙酰磺胺甲恶唑的肾脏排泄情况。

Renal excretion of sulphamethoxazole and its metabolite N4-acetylsulphamethoxazole in patients with impaired kidney function.

作者信息

Vree T B, Hekster Y A, Damsma J E, van Dalen R, Hafkenscheid J C, Friesen W T

出版信息

Ther Drug Monit. 1981;3(2):129-35. doi: 10.1097/00007691-198102000-00003.

Abstract

Plasma and urine concentrations of creatinine, sulphamethoxazole and its metabolite N4-acetylsulphamethoxazole were measured in patients with varying degrees of kidney impairment. The plasma elimination half-life of sulphamethoxazole is not influenced by the kidney function, while the half-life of the metabolite is fully dependent on the kidney function. The renal clearances of the metabolites and that of the parent compound under alkaline urine conditions are linearly related to the creatinine clearance. Kidney impairment affects only the renal clearance of the metabolite, whereas sulphamethoxazole is metabolized (acetylated) independently of kidney function.

摘要

对不同程度肾功能损害患者的血浆和尿液中的肌酐、磺胺甲恶唑及其代谢产物N4-乙酰磺胺甲恶唑浓度进行了测定。磺胺甲恶唑的血浆消除半衰期不受肾功能影响,而其代谢产物的半衰期则完全取决于肾功能。在碱性尿液条件下,代谢产物和母体化合物的肾清除率与肌酐清除率呈线性相关。肾功能损害仅影响代谢产物的肾清除率,而磺胺甲恶唑的代谢(乙酰化)与肾功能无关。

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