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金刚乙胺在健康受试者和终末期肾衰竭患者中的药代动力学。

Rimantadine pharmacokinetics in healthy subjects and patients with end-stage renal failure.

作者信息

Capparelli E V, Stevens R C, Chow M S, Izard M, Wills R J

机构信息

Department of Pharmacy, Hartford Hospital, Conn.

出版信息

Clin Pharmacol Ther. 1988 May;43(5):536-41. doi: 10.1038/clpt.1988.69.

Abstract

The single-dose (two 100 mg doses) pharmacokinetics of rimantadine hydrochloride were compared in eight patients with end-stage renal disease who were on hemodialysis and seven age-matched healthy subjects. Plasma and urine rimantadine concentrations were determined by a GC/MS method. The plasma half-life (43.6 vs 27.5 hours) and AUC (9.9 +/- 2.1 vs 6.0 +/- 1.6 micrograms.hr/ml) were significantly (p less than 0.05) increased in the patient population. No significant differences were noted in the maximum rimantadine concentration, time of maximum concentration, or apparent volume of distribution. Urinary excretion of unchanged rimantadine accounted for 16% of the dose in the healthy subjects. Hemodialysis did not appreciably remove rimantadine. These findings suggest that rimantadine dosage may need to be reduced in patients with end-stage renal disease but supplemental doses on dialysis days are not required.

摘要

对8例接受血液透析的终末期肾病患者和7名年龄匹配的健康受试者的盐酸金刚乙胺单剂量(两剂100毫克)药代动力学进行了比较。采用气相色谱/质谱法测定血浆和尿液中的金刚乙胺浓度。患者组的血浆半衰期(43.6对27.5小时)和曲线下面积(9.9±2.1对6.0±1.6微克·小时/毫升)显著升高(p<0.05)。在金刚乙胺的最大浓度、达到最大浓度的时间或表观分布容积方面未观察到显著差异。在健康受试者中,未变化的金刚乙胺的尿排泄量占给药剂量的16%。血液透析并未明显清除金刚乙胺。这些发现表明,终末期肾病患者可能需要减少金刚乙胺的剂量,但透析日无需补充剂量。

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