Goldstein Ellie J C, Citron Diane M
RM Alden Research Laboratory, Culver City, CA 90230, USA.
Diagn Microbiol Infect Dis. 2009 Apr;63(4):447-54. doi: 10.1016/j.diagmicrobio.2009.01.022. Epub 2009 Feb 26.
Doripenem, a synthetic 1-beta-methyl carbapenem, has a broad-spectrum of activity against almost all species of anaerobic bacteria, including all Bacteroides fragilis group species, most with MIC(90) results at <or=1 microg/mL (with the exception of Sutterella wadsworthensis). Against Clostridium difficile strains, it has a narrow range of inhibitory concentrations (1-4 microg/mL) that "may be achievable in the colon", potentially resulting in lower disease rates. It has been shown to be active in vitro against strains isolated from a variety of clinical infections, including bacteremias, diabetic foot and other soft tissues infections and in intra-abdominal and pelvic sites. In addition, a study of a pyometrium animal model of mixed infections noted a better microbiologic response than with imipenem. Two phase 3 multinational clinical trials of complicated mixed aerobic/anaerobic intra-abdominal infections noted "noninferiority" of doripenem when compared with meropenem, but in vitro against the anaerobes, it was "more potent than meropenem, ertapenem, ... and similar to imipenem". Doripenem activity against anaerobes seems comparable with the other extant carbapenems. Although resistance among anaerobic bacteria to this agent is possible, it remains relatively rare.
多利培南是一种合成的1-β-甲基碳青霉烯类药物，对几乎所有厌氧菌都具有广谱活性，包括所有脆弱拟杆菌属菌种，大多数菌种的MIC（90）结果≤1微克/毫升（沃兹沃思萨特菌除外）。对于艰难梭菌菌株，它的抑制浓度范围较窄（1 - 4微克/毫升），“在结肠中可能达到”，这可能会降低发病率。已证明它在体外对从各种临床感染中分离出的菌株具有活性，包括菌血症、糖尿病足和其他软组织感染以及腹腔和盆腔部位的感染。此外，一项关于混合感染脓性子宫炎动物模型的研究表明，与亚胺培南相比，多利培南具有更好的微生物学反应。两项关于复杂的需氧菌/厌氧菌混合腹腔内感染的3期跨国临床试验表明，与美罗培南相比，多利培南具有“非劣效性”，但在体外对厌氧菌的活性方面，它“比美罗培南、厄他培南……更强，与亚胺培南相似”。多利培南对厌氧菌的活性似乎与其他现有的碳青霉烯类药物相当。虽然厌氧菌对该药物可能产生耐药性，但仍然相对少见。
