Scully B E, Swabb E A, Neu H C
Antimicrob Agents Chemother. 1983 Jul;24(1):18-22. doi: 10.1128/AAC.24.1.18.
The pharmacokinetics of aztreonam, a monocyclic beta-lactam which inhibits most members of the family Enterobacteriaceae at concentrations of less than 1 microgram/ml and most Pseudomonas aeruginosa isolates at concentrations of less than 16 micrograms/ml, were examined in healthy male volunteers after 30-min intravenous infusions of 0.5, 1, and 2 g of the drug. Mean peak levels of the drug in serum at the end of infusion were 65.5, 164, 255 micrograms/ml after 0.5 1, and 2 g, respectively, with levels of the drug in serum of 1.8, 3, and 8.5 micrograms/ml at 8.5 h for the three doses, respectively. The half-life was approximately 2 h for all three doses. The total serum clearance averaged 1 ml/min per kg. The apparent volume of distribution averaged 0.17 liter/kg for the three doses. Overall excretion of the drug in urine was 61%, with mean levels in urine of 23, 52, and 109 micrograms/ml at 8.5 to 12.5 h after 0.5, 1, and 2 g of aztreonam, respectively. Concentrations of the drug in serum after a 1-g dose exceeded the minimal inhibitory concentration for 90% of the members of the Enterobacteriaceae by four- to eightfold for 8 h and exceeded the minimal inhibitory concentration for P. aeruginosa isolates for 4 h.
氨曲南是一种单环β-内酰胺类抗生素，在浓度低于1微克/毫升时可抑制大多数肠杆菌科细菌，在浓度低于16微克/毫升时可抑制大多数铜绿假单胞菌菌株。在健康男性志愿者中，静脉输注0.5克、1克和2克该药30分钟后，对其药代动力学进行了研究。输注结束时血清中药物的平均峰值水平在给予0.5克、1克和2克后分别为65.5、164、255微克/毫升，三个剂量在8.5小时时血清中药物水平分别为1.8、3和8.5微克/毫升。三个剂量的半衰期均约为2小时。总血清清除率平均为每千克体重1毫升/分钟。三个剂量的表观分布容积平均为0.17升/千克。药物在尿液中的总排泄率为61%，给予0.5克、1克和2克氨曲南后，在8.5至12.5小时尿液中的平均水平分别为23、52和109微克/毫升。给予1克剂量后，血清中药物浓度超过肠杆菌科90%成员的最低抑菌浓度4至8倍，持续8小时，超过铜绿假单胞菌菌株的最低抑菌浓度，持续4小时。
