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亚胺培南/西司他丁/雷巴他定:治疗革兰氏阴性菌感染的综述。

Imipenem/Cilastatin/Relebactam: A Review in Gram-Negative Bacterial Infections.

机构信息

Springer Nature, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand.

出版信息

Drugs. 2021 Feb;81(3):377-388. doi: 10.1007/s40265-021-01471-8. Epub 2021 Feb 25.

Abstract

Imipenem/cilastatin/relebactam (Recarbrio™) is an intravenously administered combination of the carbapenem imipenem, the renal dehydropeptidase-I inhibitor cilastatin, and the novel β-lactamase inhibitor relebactam. Relebactam is a potent inhibitor of class A and class C β-lactamases, conferring imipenem activity against many imipenem-nonsusceptible strains. Imipenem/cilastatin/relebactam is approved in the USA and EU for the treatment of hospital-acquired bacterial pneumonia (HABP) and ventilator-associated bacterial pneumonia (VABP) in adults and other gram-negative infections, including complicated urinary tract infections (cUTIs) [including pyelonephritis] and complicated intra-abdominal infections (cIAIs), in adults with limited or no alternative treatment options. In pivotal phase II and III trials, imipenem/cilastatin/relebactam was noninferior to piperacillin/tazobactam in patients with HABP/VABP and to imipenem/cilastatin in patients with cUTIs and cIAIs. It was also effective in imipenem-nonsusceptible infections. Imipenem/cilastatin/relebactam was generally well tolerated, with a safety profile consistent with that of imipenem/cilastatin. Available evidence indicates that imipenem/cilastatin/relebactam is an effective and generally well tolerated option for gram-negative infections in adults, including critically ill and/or high-risk patients, and a potential therapy for infections caused by carbapenem-resistant pathogens.

摘要

亚胺培南/西司他丁/雷巴他定(瑞来巴坦)是一种静脉内给予的碳青霉烯类药物亚胺培南、肾去氢肽酶-1 抑制剂西司他丁和新型β-内酰胺酶抑制剂雷巴他定的组合。雷巴他定是一种强效的 A 类和 C 类β-内酰胺酶抑制剂,赋予亚胺培南对许多亚胺培南不敏感的菌株的活性。亚胺培南/西司他丁/雷巴他定在美国和欧盟被批准用于治疗成人医院获得性细菌性肺炎(HABP)和呼吸机相关性细菌性肺炎(VABP)以及其他革兰氏阴性感染,包括复杂尿路感染(cUTI)[包括肾盂肾炎]和复杂腹腔内感染(cIAI),在有有限或无其他替代治疗选择的成人中。在关键的 II 期和 III 期试验中,亚胺培南/西司他丁/雷巴他定在 HABP/VABP 患者中与哌拉西林/他唑巴坦无差异,在 cUTI 和 cIAI 患者中与亚胺培南/西司他丁无差异。它在亚胺培南不敏感的感染中也有效。亚胺培南/西司他丁/雷巴他定通常具有良好的耐受性,安全性与亚胺培南/西司他丁一致。现有证据表明,亚胺培南/西司他丁/雷巴他定是成人革兰氏阴性感染的一种有效且通常具有良好耐受性的选择,包括重症和/或高危患者,也是治疗由耐碳青霉烯类病原体引起的感染的潜在疗法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6724/7905759/7b53d1168ba5/40265_2021_1471_Fig1_HTML.jpg

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