Cattoir V, Daurel C
Equipe EA 2128, service de microbiologie, CHU Côte-de-Nacre, Interactions hôtes et microorganismes des épithéliums, faculté de médecine de Caen, université de Caen-Basse-Normandie, avenue Côte-de-Nacre, Caen cedex 9, France.
Med Mal Infect. 2010 Mar;40(3):135-54. doi: 10.1016/j.medmal.2009.10.009. Epub 2009 Dec 2.
There is a constant need for new antibacterial agents because of the unavoidable development of bacterial resistance that follows the introduction of antibiotics in clinical practice. As observed in many fields, innovation generally comes by series. For instance, a wide variety of broad-spectrum antibacterial agents became available between the 1970s and the 1990s, such as cephalosporins, penicillin/beta-lactamase inhibitor combinations, carbapenems, and fluoroquinolones. Over the last 2 decades, the arrival of new antibacterial drugs on the market has dramatically slowed, leaving a frequent gap between isolation of resistant pathogens and effective treatment options. In fact, many pharmaceutical companies focused on the development of narrow-spectrum antibiotics targeted at multidrug-resistant Gram-positive bacteria (e.g. methicillin-resistant Staphylococcus aureus, penicillin resistant Streptococcus pneumoniae, and vancomycin-resistant Enterococcus faecium). Therefore, multidrug-resistant Gram-negative bacteria (e.g. extended-spectrum beta-lactamase-producing Enterobacteriaceae, carbapenem-resistant Pseudomonas aeruginosa and Acinetobacter baumannii) recently emerged and rapidly spread worldwide. Even if some molecules were developed, new molecules for infections caused by these multidrug-resistant Gram-negative bacteria remain remarkably scarce compared to those for Gram-positive infections. This review summarises the major microbiological, pharmacological, and clinical properties of systemic antibiotics recently marketed in France (i.e. linezolid, daptomycin, tigecycline, ertapenem, and doripenem) as well as those of antibacterial drugs currently in development (i.e. ceftobiprole, ceftaroline, dalbavancin, telavancin, oritavancin, iclaprim, and ramoplanin) or available in other countries (i.e. garenoxacin, sitafloxacin, and temocillin).
由于在临床实践中引入抗生素后不可避免地会出现细菌耐药性，因此一直需要新型抗菌药物。正如在许多领域所观察到的那样，创新通常是一连串出现的。例如，在20世纪70年代至90年代期间出现了各种各样的广谱抗菌药物，如头孢菌素、青霉素/β-内酰胺酶抑制剂组合、碳青霉烯类和氟喹诺酮类。在过去的20年里，新抗菌药物进入市场的速度大幅放缓，耐药病原体的分离与有效的治疗选择之间常常存在差距。事实上，许多制药公司专注于开发针对多重耐药革兰氏阳性菌（如耐甲氧西林金黄色葡萄球菌、耐青霉素肺炎链球菌和耐万古霉素屎肠球菌）的窄谱抗生素。因此，多重耐药革兰氏阴性菌（如产超广谱β-内酰胺酶的肠杆菌科细菌、耐碳青霉烯类铜绿假单胞菌和鲍曼不动杆菌）最近出现并在全球迅速传播。即使研发出了一些药物，但与革兰氏阳性菌感染的药物相比，针对这些多重耐药革兰氏阴性菌感染的新药物仍然非常稀缺。本综述总结了最近在法国上市的全身用抗生素（即利奈唑胺、达托霉素、替加环素、厄他培南和多尼培南）以及目前正在研发（即头孢比普、头孢托罗、达巴万星、特拉万星、奥利万星、依拉普明和雷莫拉宁）或在其他国家可用（即加雷沙星、西他沙星和替莫西林）的抗菌药物的主要微生物学、药理学和临床特性。
