Clissold S P, Todd P A, Campoli-Richards D M
Drugs. 1987 Mar;33(3):183-241. doi: 10.2165/00003495-198733030-00001.
Imipenem is the first available semisynthetic thienamycin and is administered intravenously in combination with cilastatin, a renal dipeptidase inhibitor that increases urinary excretion of active drug. In vitro studies have demonstrated that imipenem has an extremely wide spectrum of antibacterial activity against Gram-negative and Gram-positive aerobic and anaerobic bacteria, even against many multiresistant strains of bacteria. It is very potent against species which elaborate beta-lactamases. Imipenem in combination with equal doses of cilastatin has been shown to be generally well tolerated and an effective antimicrobial for the treatment of infections of various body systems. It is likely to be most valuable as empirical treatment of mixed aerobic and anaerobic infections, bacteraemia in non-neutropenic patients and serious hospital-acquired infections.
亚胺培南是首个可用的半合成硫霉素,需与西司他丁联合静脉给药,西司他丁是一种肾脏二肽酶抑制剂,可增加活性药物的尿排泄量。体外研究表明,亚胺培南对革兰氏阴性菌和革兰氏阳性需氧菌及厌氧菌具有极广的抗菌活性,甚至对许多多重耐药菌株也有效。它对产生β-内酰胺酶的菌种非常有效。亚胺培南与等量西司他丁联合使用已证明一般耐受性良好,是治疗各种身体系统感染的有效抗菌药物。作为需氧菌和厌氧菌混合感染、非中性粒细胞减少患者的菌血症以及严重医院获得性感染的经验性治疗,它可能最具价值。