Brown J, Yang Y J, Livermore D M
Department of Medical Microbiology, London Hospital Medical College, UK.
J Antimicrob Chemother. 1989 Feb;23(2):201-7. doi: 10.1093/jac/23.2.201.
Tigemonam was compared in vitro with other orally active beta-lactams, aztreonam and ciprofloxacin against a selection of Gram-negative clinical isolates and laboratory-derived beta-lactamase-producing variants. Of the orally active beta-lactams, tigemonam was the most potent, with a spectrum of activity similar to that of aztreonam. This included stability to plasmid-mediated beta-lactamases and poor induction of chromosomal beta-lactamases. The susceptibility to Class I enzymes was only clinically significant for derepressed Enterobacter cloacae mutants. Tigemonam may have a valuable role in the management of infection caused by enterobacteria, particularly if bioavailability following oral administration is confirmed in human subjects.
将替吉莫南在体外与其他口服活性β-内酰胺类药物、氨曲南和环丙沙星进行比较,以对抗一系列革兰氏阴性临床分离株以及实验室衍生的产β-内酰胺酶变体。在口服活性β-内酰胺类药物中,替吉莫南效力最强,其活性谱与氨曲南相似。这包括对质粒介导的β-内酰胺酶的稳定性以及对染色体β-内酰胺酶的低诱导性。对I类酶的敏感性仅对去阻遏的阴沟肠杆菌突变体具有临床意义。替吉莫南在肠杆菌引起的感染管理中可能具有重要作用,特别是如果在人类受试者中证实口服给药后的生物利用度。