Ido M, Ihara T, Kamiya H, Sakurai M
Jpn J Antibiot. 1985 Nov;38(11):3294-9.
Pharmacokinetics, in vitro, and in vivo effect of aztreonam (SQ 26,776, AZT), a newly synthesized monobactam antibiotic, were investigated in pediatric patients. The pharmacokinetics were studied in 12 children without renal or hepatic impairment, each of whom received single 10, 20 and 40 mg/kg intravenous doses of drug. Serial samples of serum and urine were assayed for AZT. Serum pharmacokinetics of AZT were described by an open, linear, two-compartment kinetic model. After intravenous administration, AZT was eliminated primarily by urinary excretion of unchanged drug (60.4%). The average biological half-lives of AZT in serum were 1.33 (10 mg/kg, n = 1), 1.69 +/- 0.40 (20 mg/kg, n = 8), and 1.51 +/- 0.61 (40 mg/kg, n = 3) hours. The antibacterial activity of AZT against E. coli and P. aeruginosa was equal or slightly stronger than that of CPZ, LMOX, and CTX. It had no antimicrobial activity against Gram-positive cocci. In vivo effect of AZT was evaluated in 13 children with various infections. The result was excellent in 7 cases, good in 1 case, fair in 3 cases and poor in 1 case, with effective ratio of 66.7%. Exanthema or elevation of GOT and GPT were noticed in 3 patients.
对一种新合成的单环β-内酰胺抗生素氨曲南(SQ 26,776,AZT)在儿科患者中的药代动力学、体外及体内效应进行了研究。在12名无肾或肝功能损害的儿童中研究了其药代动力学,每名儿童静脉注射单剂量10、20和40mg/kg的药物。对血清和尿液的系列样本进行了氨曲南检测。氨曲南的血清药代动力学用开放、线性、二室动力学模型进行描述。静脉给药后,氨曲南主要通过原形药物经尿液排泄而消除(60.4%)。氨曲南在血清中的平均生物半衰期分别为1.33小时(10mg/kg,n = 1)、1.69±0.40小时(20mg/kg,n = 8)和1.51±0.61小时(40mg/kg,n = 3)。氨曲南对大肠杆菌和铜绿假单胞菌的抗菌活性与头孢哌酮、拉氧头孢和头孢噻肟相当或略强。它对革兰氏阳性球菌无抗菌活性。在13名患有各种感染的儿童中评估了氨曲南的体内效应。结果7例为优,1例为良,3例为中,1例为差,有效率为66.7%。3名患者出现皮疹或谷草转氨酶和谷丙转氨酶升高。