Zhanel George G, Karlowsky James A, Rubinstein Ethan, Hoban Daryl J
Department of Medical Microbiology, Faculty of Medicine, Health Sciences Centre, University of Manitoba, Winnipeg, Manitoba, Canada.
Expert Rev Anti Infect Ther. 2006 Feb;4(1):9-25. doi: 10.1586/14787210.4.1.9.
Tigecycline, the first-in-class glycylcycline, was developed to recapture the broad spectrum of activity of the tetracycline class and to treat patients with difficult-to-treat bacterial infections. Tigecycline's in vitro spectrum of activity encompasses aerobic, facultative and anaerobic Gram-positive and -negative bacteria, including antimicrobial-resistant bacteria such as methicillin-resistant Staphylococcus aureus, vancomycin-resistant Enterococcus faecalis and Enterococcus faecium, and extended-spectrum beta-lactamase-producing Enterobacteriaceae. Clinical trials involving patients with complicated skin and skin-structure infections and complicated intra-abdominal infections, including patients infected with methicillin-resistant S. aureus, demonstrated that tigecycline was bacteriologically and clinically effective with mild-to-moderate gastrointestinal adverse events (i.e., nausea, vomiting and diarrhea) the most commonly reported. Tigecycline is a promising new broad-spectrum parenteral monotherapy for the treatment of patients with Gram-positive and -negative bacterial infections.
替加环素是首个甘氨酰环素类药物，其研发旨在恢复四环素类药物的广谱抗菌活性，用于治疗难治性细菌感染患者。替加环素的体外抗菌谱涵盖需氧菌、兼性厌氧菌和厌氧菌，包括革兰氏阳性菌和革兰氏阴性菌，其中有耐甲氧西林金黄色葡萄球菌、耐万古霉素粪肠球菌和屎肠球菌等耐药菌，以及产超广谱β-内酰胺酶的肠杆菌科细菌。涉及复杂皮肤及皮肤结构感染和复杂腹腔内感染患者（包括感染耐甲氧西林金黄色葡萄球菌的患者）的临床试验表明，替加环素在细菌学和临床方面均有效，最常报告的是轻至中度胃肠道不良事件（即恶心、呕吐和腹泻）。替加环素是一种有前景的新型广谱肠外单药疗法，用于治疗革兰氏阳性菌和革兰氏阴性菌感染患者。
