Alvarez-Lerma Francisco, Grau Santiago, Ferrández Olivia
Intensive Care Unit, Pharmacy Department, Hospital Del Mar, Passeig Marítim 25-29, Barcelona, Spain.
Drug Des Devel Ther. 2009 Sep 21;3:173-90. doi: 10.2147/dddt.s3083.
Doripenem (S-4661) is a new parenteral antibiotic from the carbapenem class; similarly to imipenem and meropenem, it has a broad-spectrum activity against Gram-positive, Gram-negative, and anaerobic bacteria. It is active against multiresistant Gram-negative bacilli such as extended-spectrum beta-lactamase-producing (ESBL) Gram-negative Enterobacteriaceae and nonfermentative Gram-negative bacilli including some strains of Pseudomonas aeruginosa that are resistant to other carbapenems. Doripenem's chemical structure is similar to that of meropenem (substitution of one sulfamoxil-aminomethyl chain for the dimethyl-carboxyl chain), and has one 1-beta-methyl chain which provides resistance to dehydropeptidase-I enzyme. The clinical trials conducted so far have focused on the treatment of severe infections such as complicated intra-abdominal infections, complicated urinary tract infections and pyelonephritis, nosocomial pneumonia, and ventilator-associated pneumonia. Given its activity profile and the results from the clinical trials, this antibiotic may be used for empirical treatment of multibacterial infections produced by potentially multiresistant Gram-negative bacilli. In 2007, the US Food and Drug Administration approved the use of doripenem for the treatment of complicated intra-abdominal infections and complicated urinary tract infections. The European Medicines Agency has approved the use of doripenem for the same indications in addition to nosocomial pneumonia regardless of whether it is ventilator-associated or not.
多利培南(S-4661)是一种新型的碳青霉烯类肠外抗生素;与亚胺培南和美罗培南类似,它对革兰氏阳性菌、革兰氏阴性菌和厌氧菌具有广谱活性。它对多重耐药革兰氏阴性杆菌有效,如产超广谱β-内酰胺酶(ESBL)的革兰氏阴性肠杆菌科细菌以及非发酵革兰氏阴性杆菌,包括一些对其他碳青霉烯类耐药的铜绿假单胞菌菌株。多利培南的化学结构与美罗培南相似(用一个氨磺酰氨甲基链取代二甲基羧基链),并且有一个1-β-甲基链,可提供对脱氢肽酶-I的耐药性。迄今为止进行的临床试验主要集中在治疗严重感染,如复杂性腹腔内感染、复杂性尿路感染和肾盂肾炎、医院获得性肺炎以及呼吸机相关性肺炎。鉴于其活性谱和临床试验结果,这种抗生素可用于经验性治疗由潜在多重耐药革兰氏阴性杆菌引起的多菌感染。2007年,美国食品药品监督管理局批准多利培南用于治疗复杂性腹腔内感染和复杂性尿路感染。欧洲药品管理局已批准多利培南用于相同适应症,此外还可用于医院获得性肺炎,无论是否为呼吸机相关性肺炎。