Lyon J A
Drug Intell Clin Pharm. 1985 Dec;19(12):895-9.
Imipenem/cilastatin is the first of a new class of beta-lactam antibiotics called carbapenems. The antibacterial spectrum of imipenem exceeds any antibiotic investigated to date and includes gram-positive, gram-negative, and anaerobic organisms. Only methicillin-resistant organisms, Strep. faecium, Pseudomonas cepacia, and Pseudomonas maltophilia have been shown to be resistant. Imipenem is administered in a 1:1 ratio with cilastatin, which inhibits a renal enzyme (dehydropeptidase) and improves urinary recovery of imipenem. The elimination half-life of both compounds is 1.0 hours and recommended doses are 0.25-0.5 g iv q6h. Adverse events are similar in nature and incidence to beta-lactam antibiotics, with phlebitis/thrombophlebitis, diarrhea, nausea, skin rash, and elevations of hepatic enzymes most common. Clinical studies in phase II and III trials have shown imipenem/cilastatin to be effective in soft tissue infections, endocarditis, obstetrics and gynecology, complicated urinary tract infections, mixed anaerobic-aerobic infections, osteomyelitis, bacteremias, and pneumonias. Several comparative clinical trials have shown imipenem/cilastatin to be equal in efficacy to combination therapy. Imipenem/cilastatin may prove to be an alternative to combination antibiotic therapy because of its extremely broad spectrum of activity.
亚胺培南/西司他丁是一类新型β-内酰胺抗生素(碳青霉烯类)中的首个药物。亚胺培南的抗菌谱超过了迄今所研究的任何一种抗生素,包括革兰氏阳性菌、革兰氏阴性菌和厌氧菌。仅耐甲氧西林菌、粪肠球菌、洋葱伯克霍尔德菌和嗜麦芽窄食单胞菌已显示出耐药性。亚胺培南与西司他丁按1:1的比例给药,西司他丁可抑制一种肾酶(脱氢肽酶)并提高亚胺培南的尿回收率。两种化合物的消除半衰期均为1.0小时,推荐剂量为0.25 - 0.5 g静脉注射,每6小时一次。不良事件在性质和发生率上与β-内酰胺类抗生素相似,最常见的有静脉炎/血栓性静脉炎、腹泻、恶心、皮疹和肝酶升高。II期和III期临床试验的临床研究表明,亚胺培南/西司他丁在软组织感染、心内膜炎、妇产科疾病、复杂性尿路感染、需氧菌与厌氧菌混合感染、骨髓炎、菌血症和肺炎中有效。多项比较性临床试验表明,亚胺培南/西司他丁的疗效与联合治疗相当。由于其极广的活性谱,亚胺培南/西司他丁可能被证明是联合抗生素治疗的一种替代方案。