Kropp H, Gerckens L, Sundelof J G, Kahan F M
Rev Infect Dis. 1985 Jul-Aug;7 Suppl 3:S389-410. doi: 10.1093/clinids/7.supplement_3.s389.
Imipenem (N-formimidoyl thienamycin) is the first representative of a new class of beta-lactam antibiotics--the carbapenems. Imipenem has an unusually broad spectrum, high potency, and no cross-resistance with other beta-lactam antibiotics. Susceptible gram-negative species include Pseudomonas aeruginosa, Serratia, and Enterobacter. Activity is high against Staphylococcus aureus, most group D streptococci, and Staphylococcus epidermidis but is variable against methicillin-resistant S. aureus. Imipenem is more active against Bacteroides than are other beta-lactam agents, chloramphenicol, metronidazole, and clindamycin. The minimal inhibitory concentrations (MICs) for 98% of 30,655 isolates--excluding those of the three resistant species (Pseudomonas maltophilia, Pseudomonas cepacia, and Streptococcus faecium)--were less than 8 micrograms/ml, the susceptibility breakpoint adopted for clinical trials. Imipenem is bactericidal (minimal bactericidal concentrations (MBCs] less than twice the MICs). For P. aeruginosa, MBCs of imipenem are less influenced by high inoculum density rather than are MBCs of antipseudomonal penicillins and cephalosporins. Stability of imipenem to diverse classes of plasmid-mediated and chromosomal beta-lactamases accounts for its lack of cross-resistance with other beta-lactam antibiotics. Imipenem is also active against P. aeruginosa with non-lactamase-mediated resistance to classical beta-lactam agents. Efficacy of imipenem was shown in animal models, including septicemia in normal and neutropenic rodents and P. aeruginosa pneumonia. Imipenem also has a unique postantibiotic effect against P. aeruginosa in vivo.
亚胺培南(N-甲酰亚胺硫霉素)是新型β-内酰胺类抗生素——碳青霉烯类的首个代表药物。亚胺培南具有异常广泛的抗菌谱、高效力,且与其他β-内酰胺类抗生素无交叉耐药性。敏感的革兰阴性菌包括铜绿假单胞菌、沙雷菌属和肠杆菌属。对金黄色葡萄球菌、多数D组链球菌和表皮葡萄球菌活性高,但对耐甲氧西林金黄色葡萄球菌活性不一。亚胺培南对拟杆菌属的活性比其他β-内酰胺类药物、氯霉素、甲硝唑和克林霉素更强。在30655株分离菌中,98%(不包括三种耐药菌:嗜麦芽窄食单胞菌、洋葱伯克霍尔德菌和粪肠球菌)的最低抑菌浓度(MIC)低于8微克/毫升,这是临床试验采用的敏感折点。亚胺培南具有杀菌作用(最低杀菌浓度[MBC]低于MIC的两倍)。对于铜绿假单胞菌,亚胺培南的MBC受高接种量密度的影响小于抗假单胞菌青霉素和头孢菌素的MBC。亚胺培南对多种类型的质粒介导和染色体β-内酰胺酶稳定,这解释了其与其他β-内酰胺类抗生素无交叉耐药性的原因。亚胺培南对具有非β-内酰胺酶介导的对经典β-内酰胺类药物耐药的铜绿假单胞菌也有活性。亚胺培南在动物模型中显示出疗效,包括正常和中性粒细胞减少的啮齿动物的败血症以及铜绿假单胞菌肺炎。亚胺培南在体内对铜绿假单胞菌还具有独特的抗生素后效应。