Viotte G, Leroy A, Godin M, Fillastre J P
Nouv Presse Med. 1982 Nov 18;11(46):3414-8.
The pharmacokinetics of dibekacin were studied in 23 patients with varying degrees of renal insufficiency. Creatinine clearance was between 4 and 51 ml/min. Chronic renal insufficiency did not affect maximum serum concentrations, nor the time required to reach a peak level after an intramuscular injection of 1 mg/kg of dibekacin. The maximum concentration was 4 to 5 mcg/ml and the peak obtained within the first hour. Renal insufficiency caused a very marked prolongation in the serum half-life of elimination. This rose from 6 hours in moderate renal insufficiency to 50 hours in a patient with a clearance of a few millilitres. Whatever the degree of renal insufficiency, it should be noted that urinary concentrations remained markedly higher than the MIC of organisms sensitive to the aminoglycoside. Dibekacin is highly dialysable, being virtually totally extracted during a 6 hours dialysis session using a membrane of 1 m2 surface area. An outline of dose adaptations in relation to the degree of renal insufficiency is suggested on the basis of these pharmacokinetic data.
对23例不同程度肾功能不全患者进行了地贝卡星的药代动力学研究。肌酐清除率在4至51毫升/分钟之间。慢性肾功能不全不影响血清最高浓度,也不影响肌肉注射1毫克/千克地贝卡星后达到峰值水平所需的时间。最高浓度为4至5微克/毫升,在第一小时内达到峰值。肾功能不全会导致血清消除半衰期显著延长。这一数值从中度肾功能不全患者的6小时升至肌酐清除率仅为几毫升的患者的50小时。无论肾功能不全程度如何,都应注意尿药浓度仍显著高于对氨基糖苷类敏感的微生物的最低抑菌浓度。地贝卡星具有高度透析性,在使用1平方米表面积的透析膜进行6小时透析过程中几乎可被完全清除。基于这些药代动力学数据,建议了根据肾功能不全程度调整剂量的概要。