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美洛培南是一个新的碳青霉烯类抗生素。它对需氧菌及厌氧菌都有很好的杀菌活性,虽然对葡萄球菌属的抗菌活性较弱,但它对绿脓杆菌、肠杆菌属、流感嗜血杆菌及厌氧菌的抗菌活性强。美洛培南对group1和group2丝氨酸酶及能水解三代头孢菌素的β-内酰胺酶稳定。它对金属酶的稳定性不如亚胺培南,但对碳青霉烯酶Sme-1的稳定性强于亚胺培南,并且对金黄色葡萄球菌、大肠杆菌、绿脓杆菌的青霉素结合蛋白的亲和力强。临床试验结果表明美洛培南用于治疗慢性支气管炎急性恶化、下呼吸道感染、泌尿系感染、腹腔感染、细菌性脑膜炎及败血症是安全有效的。药代动力学研究表明美洛培南能迅速分布于组织间隙产生临床治疗浓度。美洛培南的药物不良反应发生率与对照药相似,常见的为腹泻、皮肤红斑、恶心呕吐、及肝功改变。
Meropenem is a new carbapenem antibiotic. It aerobic bacteria and anaerobic bacteria have good bactericidal activity, although the antimicrobial activity of Staphylococcus is weak, but its antibacterial activity of Pseudomonas aeruginosa, Enterobacter, Haemophilus influenzae and anaerobic bacteria Strong. Meropenem is stable against group 1 and group 2 serine enzymes and β-lactamase enzymes capable of hydrolyzing the third generation cephalosporins. It is less stable to metalloenzyme than imipenem, but more stable to carbapenemase Sme-1 than imipenem and to penicillin-binding proteins of Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa Strong affinity. Clinical trials show that meropenem is safe and effective for the treatment of acute exacerbations of chronic bronchitis, lower respiratory tract infections, urinary tract infections, abdominal infections, bacterial meningitis and septicemia. Pharmacokinetic studies have shown that meropenem can rapidly distribute in interstitial spaces to produce clinically relevant concentrations. The incidence of adverse drug reactions in meropenem is similar to that of the control drugs. Diarrhea, skin erythema, nausea and vomiting, and changes in liver function are common.