Wiseman L R, Wagstaff A J, Brogden R N, Bryson H M
Adis International Limited, Auckland, New Zealand.
Drugs. 1995 Jul;50(1):73-101. doi: 10.2165/00003495-199550010-00007.
The parenteral carbapenem meropenem is relatively stable to inactivation by human renal dehydropeptidase (DHP-1) and does not require concomitant administration of a DHP-1 inhibitor such as cilastatin. It has a broad spectrum of antibacterial activity in vitro, the majority of Gram-negative, Gram-positive and anaerobic pathogens being highly susceptible to the drug. Meropenem has shown clinical and bacteriological efficacy in the treatment of a wide range of serious infections in adults and children which is at least comparable with that of currently available treatment options. Its clinical and bacteriological efficacy is similar to that of imipenem/cilastatin, clindamycin plus tobramycin and cefotaxime plus metronidazole in the treatment of intraabdominal infections; cefotaxime or ceftriaxone in the treatment of meningitis; imipenem/cilastatin, and ceftazidime with or without an aminoglycoside, in lower respiratory tract infections; and imipenem/cilastatin or ceftazidime in the treatment of urinary tract infections. Satisfactory clinical and bacteriological response rates have also been achieved in patients with skin and skin structure infections, obstetric and gynaecological infections or septicaemia, and in immunocompromised patients with febrile episodes. Preliminary findings also indicate efficacy in the treatment of respiratory tract infections in patients with cystic fibrosis. The tolerability profile of meropenem is generally similar to that of comparator agents, although it is associated with a lower incidence of adverse gastrointestinal effects (nausea and vomiting) than imipenem/cilastatin. Importantly, the incidence of seizures in patients with meningitis is not increased following administration of meropenem. Thus, meropenem is an effective broad spectrum antibacterial drug for the treatment of a wide range of infections including polymicrobial infections in both adults and children, with comparable efficacy to imipenem/cilastatin and various other treatment regimens. Meropenem is likely to be of greatest value as empiric monotherapy in the treatment of serious infections for those caused by multiply-resistant pathogens. Further clinical experience is necessary, however, to ultimately define its place in therapy.
肠外碳青霉烯类药物美罗培南对人肾脱氢肽酶(DHP - 1)的灭活作用相对稳定,无需同时使用DHP - 1抑制剂如西司他丁。它在体外具有广泛的抗菌活性,大多数革兰氏阴性菌、革兰氏阳性菌和厌氧菌对该药高度敏感。美罗培南在治疗成人和儿童的多种严重感染方面已显示出临床和细菌学疗效,至少与目前可用的治疗方案相当。在治疗腹腔内感染方面,其临床和细菌学疗效与亚胺培南/西司他丁、克林霉素加妥布霉素以及头孢噻肟加甲硝唑相似;在治疗脑膜炎方面与头孢噻肟或头孢曲松相似;在治疗下呼吸道感染方面与亚胺培南/西司他丁以及头孢他啶(加或不加氨基糖苷类药物)相似;在治疗尿路感染方面与亚胺培南/西司他丁或头孢他啶相似。在皮肤和皮肤结构感染、妇产科感染或败血症患者以及有发热发作的免疫功能低下患者中也取得了令人满意的临床和细菌学反应率。初步研究结果还表明其在治疗囊性纤维化患者的呼吸道感染方面有效。美罗培南的耐受性总体上与对照药物相似,尽管与亚胺培南/西司他丁相比,其胃肠道不良反应(恶心和呕吐)的发生率较低。重要的是,脑膜炎患者使用美罗培南后癫痫发作的发生率并未增加。因此,美罗培南是一种有效的广谱抗菌药物,可用于治疗包括成人和儿童的多种微生物感染在内的广泛感染,其疗效与亚胺培南/西司他丁及其他各种治疗方案相当。美罗培南作为经验性单药治疗多重耐药病原体引起的严重感染可能具有最大价值。然而,最终确定其在治疗中的地位还需要进一步的临床经验。