Giamarellou H, Tsagarakis J, Daikos G K
Rev Infect Dis. 1982 Nov-Dec;4 Suppl:S629-38. doi: 10.1093/clinids/4.supplement_3.s629.
Moxalactam was evaluated in vitro against 600 nosocomial isolates of gram-negative bacteria and was compared with cephalothin, cefoxitin, and cefotaxime. Moxalactam was superior to the other compounds, with minimal inhibitory concentrations of less than or equal to 4 micrograms/ml for 95% of the Enterobacteriaceae isolates and less than or equal to 8 micrograms/ml for 85% of the Bacteroides fragilis isolates; 70% of the Pseudomonas aeruginosa isolates were inhibited with less than or equal to 16 micrograms/ml. Moxalactam at doses ranging from 1 g every 12 hr to 2 g every 8 hr was given to patients with serious infections of the respiratory (14) or urinary (13) tract, abdominal abscess (4), osteomyelitis (4), meningitis (5), soft-tissue phlegmon (3), malignant external otitis (2), peritonitis (1), and panophthalmitis (1). The clinical response was excellent in 35 (74.5%) and improved in 12 (25.5%) of the 47 patients. The pathogen was eradicated in 29 (61.7%) patients, two patients had relapses, and bacteria persisted but in decreased numbers and without development of resistance in 16 patients. The half-life of moxalactam was 146 (+/- 21) and 125 (+/- 34) min after 2-g intravenous and 1-g intramuscular doses, respectively. Kinetic studies in sputum, bile, bone, aqueous humor, prostatic fluid, and cerebrospinal fluid showed moxalactam concentrations several times higher than the required MICs. No appreciable adverse effects or toxicity were observed.
对600株医院获得性革兰氏阴性菌进行了莫西拉坦的体外评估,并与头孢噻吩、头孢西丁和头孢噻肟进行了比较。莫西拉坦优于其他化合物,95%的肠杆菌科分离株的最低抑菌浓度小于或等于4微克/毫升,85%的脆弱拟杆菌分离株的最低抑菌浓度小于或等于8微克/毫升;70%的铜绿假单胞菌分离株在小于或等于16微克/毫升时受到抑制。对患有呼吸道严重感染(14例)、泌尿系统严重感染(13例)、腹腔脓肿(4例)、骨髓炎(4例)、脑膜炎(5例)、软组织蜂窝织炎(3例)、恶性外耳道炎(2例)、腹膜炎(1例)和全眼球炎(1例)的患者,给予每12小时1克至每8小时2克剂量的莫西拉坦。47例患者中,35例(74.5%)临床反应极佳,12例(25.5%)有所改善。29例(61.7%)患者的病原体被根除,2例患者复发,16例患者细菌持续存在但数量减少且未产生耐药性。静脉注射2克和肌肉注射1克剂量后,莫西拉坦的半衰期分别为146(±21)分钟和125(±34)分钟。在痰液、胆汁、骨骼、房水、前列腺液和脑脊液中的动力学研究表明,莫西拉坦浓度比所需的最低抑菌浓度高几倍。未观察到明显的不良反应或毒性。