Simon C, Maleryzk V, Ahlendorf W
Int J Clin Pharmacol Biopharm. 1978 Apr;16(4):145-9.
In vitro activity of sisomicin and gentamicin was compared in serial dilution tests for 619 bacterial strains (Staphylococcus aureus, E. coli, Proteus mirabilis, Proteus vulgaris, Enterobacter, Klebsiella, Pseudomonas aeruginosa, Salmonella, Serratia marcescens). Mean MIC of sisomicin was lower by one geometrical dilution step compared with gentamicin for Pseudomonas, Proteus vulgaris, Klebsiella, and Serratia, while it was almost identical with the other species. Resistance (MIC greater than 5 microgram/ml) against sisomicin was observed in 2% of Pseudomonas strains, resistance against gentamicin in 8%. Ten healthy adult volunteers had serum peak levels (after i,m. injection of 40 mg and 80 mg sisomicin) of 2.7 and 3.2 microgram/ml. Urine recovery (in 24 hrs) was 76%. Continuous i.v. infusion of sisomicin or gentamicin (6.6 mg/hour in 7 healthy adult volunteers) yielded in serum levels of 0.64 and 1.03 microgram/ml respectively. Biological half-life (90 minutes), urine recovery (60% in the fourth hour), renal clearance and skin blister levels at the end of infusion were almost identical for both antibiotics; total clearance was somewhat higher with sisomicin than with gentamicin.
在对619株细菌(金黄色葡萄球菌、大肠杆菌、奇异变形杆菌、普通变形杆菌、肠杆菌属、克雷伯菌属、铜绿假单胞菌、沙门氏菌、粘质沙雷氏菌)进行的系列稀释试验中,比较了西索米星和庆大霉素的体外活性。对于铜绿假单胞菌、普通变形杆菌、克雷伯菌属和粘质沙雷氏菌,西索米星的平均最低抑菌浓度(MIC)比庆大霉素低一个几何稀释级,而与其他菌种的MIC几乎相同。在2%的铜绿假单胞菌菌株中观察到对西索米星的耐药性(MIC大于5微克/毫升),对庆大霉素的耐药性为8%。10名健康成年志愿者(肌肉注射40毫克和80毫克西索米星后)的血清峰值水平分别为2.7微克/毫升和3.2微克/毫升。尿液回收率(24小时内)为76%。对7名健康成年志愿者持续静脉输注西索米星或庆大霉素(6.6毫克/小时),血清水平分别为0.64微克/毫升和1.03微克/毫升。两种抗生素的生物半衰期(90分钟)、尿液回收率(第4小时为60%)、肾脏清除率以及输注结束时的皮肤水疱水平几乎相同;西索米星的总清除率略高于庆大霉素。