PHARMACOKINETICS OF CEFTAZIDIME IN NORMAL AND UREMIC SUBJECTS

PHARMACOKINETICS OF CEFTAZIDIME IN NORMAL AND UREMIC SUBJECTS
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DOI:
10.1128/aac.25.5.638
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发表时间:
1984-01-01
影响因子:
4.9
通讯作者:
HUMBERT, G
HUMBERT, G
中科院分区:
医学2区
文献类型:
--
作者:
LEROY, A;LEGUY, F;HUMBERT, G

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单次静脉注射头孢他啶(抗菌剂)的药代动力学在 5 名正常受试者和 19 名尿毒症患者中进行了研究,以 15 mg/kg 的剂量在 3 分钟内推注。根据内源性肌酐清除率(CLCR)值将研究对象分为 5 组:第 1 组,5 名 CLCR > 80 ml/min 的受试者;第 1 组,5 名 CLCR > 80 ml/min 的受试者;第2组,5名患者CLCR=30-80ml/min;第3组,6例CLCR=10-30ml/min;第4组,4名患者CLCR=2-10ml/min;第5组有4名无尿患者进行血液透析。使用二室开放模型计算药代动力学参数。在正常受试者中,平均表观消除半衰期为 1.57±。 0.13小时。中心分布容积和表观分布容积为0.127±。 0.023 和 0.230.+-。分别为 0.015 升/千克。注射剂量中,83.6±。 3.6%在24小时内以母药形式从尿中消除。终末半衰期随着肾功能损害而增加至.apprx。严重尿毒症患者25小时。功能损伤并未显着改变α半衰期。相、中心分布体积或表观分布体积。 6-8小时的血液透析程序将血浆中头孢他啶的浓度降低了约. 88%;消除半衰期为2.8.+-。 0.2小时。 4 名患有严重和慢性功能障碍的患者接受每 24 小时 0.5-1.0 g 剂量,连续 10 天,没有发现头孢他啶蓄积的证据。
The pharmacokinetics of ceftazidime [an antibacterial agent], administered as a single i.v. dose of 15 mg/kg given in a bolus injection over 3 min, were investigated in 5 normal subjects and in 19 uremic patients. The subjects studied were divided into 5 groups according to values for endogenous creatinine clearance (CLCR): group 1, 5 subjects with CLCR > 80 ml/min; group 2, 5 patients with CLCR = 30-80 ml/min; group 3, 6 patients with CLCR = 10-30 ml/min; group 4, 4 patients with CLCR = 2-10 ml/min; and group 5, 4 anuric patients on hemodialysis. A 2-compartment open model was used to calculate the pharmacokinetic parameters. In normal subjects, the mean apparent elimination half-life was 1.57 .+-. 0.13 h. The central distribution volume and the apparent volume of distribution were 0.127 .+-. 0.023 and 0.230 .+-. 0.015 l/kg, respectively. Of the injected dose, 83.6 .+-. 3.6% was eliminated in the urine as parent drug within 24 h. The terminal half-life increased with impairment of renal function to .apprx. 25 h in severely uremic patients. Impairment of function did not significantly modify the half-life at .alpha. phase, central distribution volume or apparent distribution volume. A 6-8 h hemodialysis procedure reduced concentrations of ceftazidime in plasma by .apprx. 88%; the elimination half-life was 2.8 .+-. 0.2 h. There was no evidence of accumulation of ceftazidime in 4 patients with severe and chronic impariment of function who received doses of 0.5-1.0 g every 24 h for 10 days.