Meropenem一个新的碳青霉烯类抗生素

MEROPENEM: A NOVEL CARBAPENEM ANTIBIOTIC

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 was a novel carbapenem antibiotic which had excellent bactericidal activity in vitro against almost clinically significant aerobes and anaerobes.It had an antibacterial spectrum which was broadly similar to that of imipenem.Although it was slightly less active against Staphylococci,it was more active against Pseudomonas aeruginosa, all enterobacteriaceae , Haemophilis influenzae and anaerobes.Meropenem was stable to group1 and group2 serine-based β-lactamase including those which hydrolysed third-generation cephalosporins. The stability of meropenem to metallo-β-lactamase was less than that of imipenem. However, it was more stable to carbapenem-hydrolyzing enzyme Sme-1 than that of imipenem.Moreover, meropenm had high affinity for PBPs in Staphylococcus aerus, E.coli and P.aeruginosa.The clinical trials showed meropenem was effective for treatment of severe bacterial exacerbation of chronic bronchitis, bacterial meningitis, bacterial infections of the urinary tract and lower respiratory tract,intra-abdominal infections and septicaemia.Meropenem was rapidly and readily distributed into interstitial fluid producing concentration in tissue likely to be clinically effective.The frequencies of adverse events with meropenem were similar to those of the other β-lactam antibiotics with which it was compared . The most frequently reported adverse events were diarrhoea, rash, nausea and vomiting, and changing in hepatis biochemistry.Abnormal laboratory tests occured with similar frequencies between meropenem and the comparator agents.