Meyers B R, Wilkinson P, Mendelson M H, Bournazos C, Tejero C, Hirschman S Z
Department of Medicine, Mount Sinai Medical Center, New York, NY 10029-6574.
J Clin Pharmacol. 1993 May;33(5):470-4. doi: 10.1002/j.1552-4604.1993.tb04690.x.
Aztreonam is a monobactam exhibiting an antibacterial spectrum similar to that of the aminoglycosides, with activity against aerobic gram-negative bacilli, and is the only related drug that may be given to patients hypersensitive to beta-lactams. The pharmacokinetics of aztreonam were compared in two groups of healthy volunteers. The young group comprised 10 adults between the ages of 18 and 30 years, and the elderly group included 10 adults older than 65 years of age. The two groups each received two doses (1 and 2 g) aztreonam, separated by 1 week. Although the mean peak serum concentrations of aztreonam for the two groups were similar, there were differences in other pharmacokinetic parameters. For example, for the 2-g dose the mean half-life (1.8 +/- .51 versus 3.1 +/- .9 hour), and area under the curve (AUC) (294.42 +/- 64.08 versus 469.01 +/- 144.02 micrograms x hour/mL per 1.73 m2) were less for the younger group compared with the elderly group. The mean total body clearance of aztreonam was greater for the younger than the elderly group. The results were similar to the pharmacokinetic parameters derived from the 1-g dose. These results mirror the lower creatinine clearances and higher serum creatinine levels found in the elderly group. The data suggest that lower doses of aztreonam given at less frequent intervals may be appropriate in the elderly population.
氨曲南是一种单环β-内酰胺类抗生素,其抗菌谱与氨基糖苷类相似,对需氧革兰氏阴性杆菌有活性,并且是唯一可用于对β-内酰胺类过敏患者的相关药物。在两组健康志愿者中比较了氨曲南的药代动力学。年轻组由10名年龄在18至30岁之间的成年人组成,老年组包括10名年龄超过65岁的成年人。两组均接受两剂(1克和2克)氨曲南,间隔1周。虽然两组氨曲南的平均血清峰值浓度相似,但在其他药代动力学参数上存在差异。例如,对于2克剂量,年轻组的平均半衰期(1.8±0.51对3.1±0.9小时)和曲线下面积(AUC)(294.42±64.08对469.01±144.02微克·小时/毫升每1.73平方米)低于老年组。氨曲南的平均全身清除率年轻组高于老年组。1克剂量得出的药代动力学参数结果与之相似。这些结果反映了老年组较低的肌酐清除率和较高的血清肌酐水平。数据表明,在老年人群中,可能适当给予较低剂量且给药间隔较长的氨曲南。