【摘要】 <正> 氮脒青霉素(Mecillinam,FL1060)是一种作用机制不同于其他青霉素的窄谱抗生素。本文报道国产品体外抗菌作用和临床药理研究的结果。 以平板稀释法(多点接种器)测定52株产β-内酰胺酶金葡菌的药敏,本品8μg/ml的抑菌率为0,而羧苄青霉素(64μg/ml)达98.1％。以试管稀释法另测375株临床分离菌药敏,本品对肺炎球菌和金葡菌(不产酶)的抑菌率分更多还原

【Abstract】 Mecillinam is a new semisynthetic Penicillin with a substituted amidino group. The mechanism of antibacterial action is different from other penicillins.It’s antibacterial activity against 427 strains of clinical isolates was determined by agar dilution method and tube dilution method. The activity of mecillinam against Gram-positive bacteria was definitely lower than those of ampicillin and carbeni-cillin, its inhibition rate was 22.2% only, critical concentration set at 8 μg/ml. However its activity against Gram-negative bacteria was much stronger. Most species of Enterobacteriaceae, such as Esch. coli, Salmonella, Shigella, Enterobacter and Cit-robacter were usually susceptible to mecillinam. All strains of S. typhimurium were inhibited by a concentration of 2 μg/ml. It had some activity against H. influenzae. The inhibition rate on Gram-negative bacteria was 62.4%.In vitro synergy was demonstrated when mecillinam was combined with cefama-ndole or fosfomycin.After intramuscular infection of a 400 mg dose to 10 volunteers, a mean peak serum level of 13.63 μg/ml was reached 30 min. after the injection. After intravenous injection of a same dose, initial high serum level of 37.9μg/ml was obtained. Mecillinam was excreted mainly in the urine, 66~73% of the given dose being excreted by 12 hours.更多还原