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伏立康唑单次口服剂量在腹膜透析患者中的药代动力学

Pharmacokinetics of single, oral-dose voriconazole in peritoneal dialysis patients.

作者信息

Peng Luon W, Lien Yeong-Hau H

机构信息

Department of Medicine, University of Arizona Health Sciences Center, Tucson, AZ 85724, USA.

出版信息

Am J Kidney Dis. 2005 Jan;45(1):162-6. doi: 10.1053/j.ajkd.2004.09.017.

DOI:10.1053/j.ajkd.2004.09.017
PMID:15696456
Abstract

BACKGROUND

Voriconazole is a new triazole antifungal drug. Its pharmacokinetics and transfer to peritoneal dialysate in peritoneal dialysis (PD) patients have not been studied.

METHODS

Five patients with end-stage renal disease requiring support by PD were administered a single dose of 200 mg of voriconazole orally. Plasma and peritoneal dialysate were collected for measurement of voriconazole concentrations at times 1, 2, 4, and 24 hours.

RESULTS

Voriconazole was absorbed and achieved maximum concentration (Cmax) in plasma at mean time 2.4 +/- 0.7 (SE) hours. Time to Cmax in dialysate was 2.8 +/- 0.5 hours. Mean Cmax for plasma was 0.55 +/- 0.20 microg/mL, and for dialysate, approximately half that of plasma (0.25 +/- 0.09 mug/mL). The dialysate to plasma ratio of voriconazole was 0.66 +/- 0.11. Less than 1% of the administered voriconazole dose (1.3 +/- 0.2 mg) was recovered in dialysate 24 hours after dosing.

CONCLUSION

Voriconazole penetrates well into peritoneal fluid. There is minimal peritoneal clearance of voriconazole; therefore, no dosage adjustment is needed for patients on PD therapy.

摘要

背景

伏立康唑是一种新型三唑类抗真菌药物。尚未对其在腹膜透析(PD)患者中的药代动力学及向腹膜透析液中的转运情况进行研究。

方法

对5例需要PD支持的终末期肾病患者口服单剂量200mg伏立康唑。在1、2、4和24小时采集血浆和腹膜透析液以测定伏立康唑浓度。

结果

伏立康唑被吸收,血浆中平均在2.4±0.7(SE)小时达到最大浓度(Cmax)。透析液中达到Cmax的时间为2.8±0.5小时。血浆的平均Cmax为0.55±0.20μg/mL,而透析液中的约为血浆的一半(0.25±0.09μg/mL)。伏立康唑的透析液与血浆浓度比为0.66±0.11。给药24小时后,透析液中回收的伏立康唑剂量不到给药剂量的1%(1.3±0.2mg)。

结论

伏立康唑能很好地渗透到腹膜液中。伏立康唑的腹膜清除率极低;因此,接受PD治疗的患者无需调整剂量。

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