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肾功能正常和受损患者静脉注射美洛西林的药代动力学(作者译)

[Pharmacokinetics of intravenous mezlocillin in patients with normal and impaired renal function (author's transl)].

作者信息

Cano J P, Rigault J P, Gevaudan M J, Saingra S, Murisasco A, Charpin J

出版信息

Nouv Presse Med. 1982 Feb 4;11(5 Pt 2):335-9.

PMID:6460972
Abstract

The pharmacokinetics of mezlocillin after intravenous infusion of 5 g over 30 minutes was compared in 15 patients divided into 3 groups. Group I patients had normal renal function, group II patients had moderate chronic renal impairment and group III patients were under haemodialysis. Plasma mezlocillin levels were measured by the microbiological method. Plasma kinetic values were calculated from a linear two-compartment model, using global estimation of macroconstants by the non-linear least square method. The elimination half-life was 1.19 +/- 0.107 h in group I patients 1.98 +/- 0.19 h in group II patients and 2.34 +/- 0.11 h in group III patients. Renal impairment did not significantly alter the apparent volume of distribution but influenced the total plasma clearance which was 139 +/- 9 ml/min, 87 +/- 9 ml/min and 61 +/- 8 ml/min in groups I, II and III patients respectively. There was a slight decrease of V1 (central compartment) and a noticeable increase of V2 (peripheral compartment), depending on the degree of renal impairment. The total volume of distribution (V1 + V2) remained relatively constant between 12 and 14 litres. Homogeneous results were obtained in each group of patients, thus confirming the regularity of the mezlocillin kinetic model at the dose administered. This should enable dosage adjustment according to renal function, as assessed by laboratory criteria.

摘要

将15名患者分为3组,比较了在30分钟内静脉输注5克美洛西林后的药代动力学。第一组患者肾功能正常,第二组患者有中度慢性肾功能损害,第三组患者接受血液透析。采用微生物学方法测定血浆美洛西林水平。血浆动力学值由线性二室模型计算得出,采用非线性最小二乘法对宏观常数进行整体估计。第一组患者的消除半衰期为1.19±0.107小时,第二组患者为1.98±0.19小时,第三组患者为2.34±0.11小时。肾功能损害并未显著改变表观分布容积,但影响了血浆总清除率,第一组、第二组和第三组患者的血浆总清除率分别为139±9毫升/分钟、87±9毫升/分钟和61±8毫升/分钟。根据肾功能损害程度,V1(中央室)略有下降,V2(外周室)显著增加。分布总体积(V1+V2)在12至14升之间保持相对恒定。每组患者均获得了一致的结果,从而证实了在所给药剂量下美洛西林动力学模型的规律性。这应该能够根据实验室标准评估的肾功能进行剂量调整。

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