Bickenbach R, Peitsch W, Ansorg R
Arzneimittelforschung. 1977;27(10):2023-7.
In 24 patients with normal renal function the serum concentration of gentamicin was checked during a period of 3--5 days. The biological test is simple and rapid to perform. The patients were given doses of 80--240 mg gentamicin per day. Even at doses of 240 mg/day no accumulation of the drug occurred. Intramuscular application of an 80 mg maximum dose of gentamicin did not result in any toxic serum concentrations. The measurement of peak concentrations--1 h after application--is therefore jus aimed at correcting too low dosages. The median values of the serum peak concentrations are 4--6 microgram/ml in the case of single dose application of 80 mg and 3 microgram/ml in the case of single dose application of 40 mg. Consequently serum concentrations effective against moderately susceptible bacteria (MIC = 1--4 microgram/ml) do not act for a sufficiently long time, since the half-life for elimination is 2 h. Daily dosages of up to 240 mg (3X80 mg) gentamicin are only effective in infections caused by very susceptible bacteria with a MIC up to 1 microgram/ml.
对24名肾功能正常的患者在3至5天的时间内检测了庆大霉素的血清浓度。生物学检测操作简单且快速。患者每天接受80至240毫克庆大霉素的剂量。即使在每天240毫克的剂量下,药物也未出现蓄积。肌肉注射最大剂量80毫克的庆大霉素未导致任何毒性血清浓度。因此,在用药1小时后测量峰值浓度只是为了纠正过低的剂量。单次应用80毫克时血清峰值浓度的中位数为4至6微克/毫升,单次应用40毫克时为3微克/毫升。因此,对中度敏感细菌(MIC = 1至4微克/毫升)有效的血清浓度作用时间不够长,因为消除半衰期为2小时。每天高达240毫克(3×80毫克)的庆大霉素剂量仅对MIC高达1微克/毫升的极敏感细菌引起的感染有效。