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卧床老年患者中阿米卡星和头孢噻吩的药代动力学

Pharmacokinetics of amikacin and cephalothin in bedridden elderly patients.

作者信息

Yasuhara H, Kobayashi S, Sakamoto K, Kamijo K

出版信息

J Clin Pharmacol. 1982 Aug-Sep;22(8-9):403-9. doi: 10.1002/j.1552-4604.1982.tb02693.x.

Abstract

The pharmacokinetics of amikacin (5.5 mg/kg intramuscularly) and cephalothin (1000 mg/body intravenously) in bedridden elderly patients were studied in comparison with those in healthy volunteers. The eliminations of amikacin and cephalothin from the plasma followed the course of a one-compartment open model. For amikacin, five healthy volunteers, elimination rate constant Kel was 0.396 hr-1, biologic half-life t1/2 was 1.80 hour, volume of distribution Vd was 0.201 l./kg; in five bedridden elderly patients, Kel was 0.208 hr-1, t1/2 was 3.55 hours, Vd was 0.376 l./kg. Cumulative renal excretion of amikacin in 8 hours was 44 per cent of the total dose in bedridden elderly patients and 69 per cent in healthy volunteers. For cephalothin, in seven healthy volunteers, Kel was 0.0353 min-1, t1/2 was 19.7 min, Vd was 0.176 l./kg; in four bedridden elderly patients, Kel was 0.0127 min-1, t1/2 was 56.4 min, Vd was 0.283 l./kg. Cumulative renal excretion of cephalothin reached a plateau by 4 hours of 40.8 per cent of the total dose in bedridden elderly patients and of 56.7 per cent in healthy volunteers. These results suggest that in bedridden elderly patients decreased renal excretion of amikacin and cephalothin is related to decreased renal function and an increased Vd.

摘要

对卧床老年患者和健康志愿者肌注阿米卡星(5.5毫克/千克)及静注头孢噻吩(1000毫克/人)后的药代动力学进行了研究比较。血浆中阿米卡星和头孢噻吩的消除符合一室开放模型。对于阿米卡星,5名健康志愿者的消除速率常数Kel为0.396小时-1,生物半衰期t1/2为1.80小时,分布容积Vd为0.201升/千克;5名卧床老年患者的Kel为0.208小时-1,t1/2为3.55小时,Vd为0.376升/千克。卧床老年患者8小时内阿米卡星的累积肾排泄量占总剂量的44%,健康志愿者为69%。对于头孢噻吩,7名健康志愿者的Kel为0.0353分钟-1,t1/2为19.7分钟,Vd为0.176升/千克;4名卧床老年患者的Kel为0.0127分钟-1,t1/2为56.4分钟,Vd为0.283升/千克。卧床老年患者头孢噻吩的累积肾排泄量在4小时时达到平台期,占总剂量的40.8%,健康志愿者为56.7%。这些结果表明,卧床老年患者中阿米卡星和头孢噻吩的肾排泄减少与肾功能下降及分布容积增加有关。

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