Vree T B, Martea M, Hekster Y A, Termond E F, Van Klaveren R, Lammers J W, Berden J H
Pharm Weekbl Sci. 1987 Apr 24;9(2):117-24. doi: 10.1007/BF01960746.
High doses of co-trimoxazole in a patient with Pneumocystis carinii and impaired kidney function (creatinine clearance 10 ml/min) resulted in a declining renal clearance of the drug but did not affect the average creatinine clearance. The renal clearance of sulfamethoxazole and its metabolites 5-hydroxy-, N4-acetyl-, N4-acetyl-5-hydroxysulfamethoxazole decreased 80%, while the renal clearance of trimethoprim decreased 60%. The renal clearance of all compounds was evidently dependent on urine flow. The observed phenomena may be explained by the assumption that crystalluria occurred, obstructing kidney tubules. The crystalluria effect can be reversed by cessation of the drug or by lowering its dosage.
对一名患有卡氏肺孢子虫且肾功能受损(肌酐清除率为10毫升/分钟)的患者使用高剂量复方新诺明,结果导致该药物的肾清除率下降,但未影响平均肌酐清除率。磺胺甲恶唑及其代谢产物5-羟基-、N4-乙酰-、N4-乙酰-5-羟基磺胺甲恶唑的肾清除率下降了80%,而甲氧苄啶的肾清除率下降了60%。所有化合物的肾清除率显然取决于尿流。观察到的现象可以通过存在结晶尿阻塞肾小管这一假设来解释。停药或降低药物剂量可逆转结晶尿效应。