Graninger W
Department of Infectious Diseases, Internal Medicine I, University of Vienna, Vienna, Austria.
Int J Antimicrob Agents. 2003 Oct;22 Suppl 2:73-8. doi: 10.1016/s0924-8579(03)00235-8.
Pivmecillinam is the pro-drug of mecillinam, a beta-lactam antibiotic with a novel site of action and with specific and high activity against Gram-negative organisms such as Escherichia coli and other Enterobacteriaceae. Since its introduction, it has been widely used for the treatment of acute lower urinary tract infections (UTI), primarily in the Nordic countries. In contrast to the increasing resistance of urinary pathogens to other beta-lactams particularly ampicillin/amoxycillin and to other UTI antibiotics such as trimethoprim and trimethoprim/sulphamethoxazole (TMP/SMX), the level of resistance has remained on a low level. Less than 2% of E. coli community isolates are resistant to mecillinam. This paper reviews the clinical data on pivmecillinam with a special focus on the safety aspects. A large number of studies from the 70s to 80s have proven the clinical efficacy and safety of pivmecillinam for empirical treatment of acute cystitis. More recent studies confirm short-term treatment with pivmecillinam results in clinical and bacteriological cure rates similar to those obtained with other UTI agents. Both clinical studies in pregnant women with UTI and large epidemiological studies have confirmed the safety of pivmecillinam used in pregnancy. In the Nordic countries pivmecillinam has been the most widely used agent for treatment of UTI in pregnancy for many years. Ecological aspects of antibiotic treatment are important both with regard to adverse effects and development of resistance due to disturbance of the normal micro flora. Studies have shown that pivmecillinam has a very minor impact on the normal oropharyngeal, intestinal and skin microflora. The clinical implications of this are a low frequency of diarrhoea and Candida vaginitis as confirmed in the clinical studies. The high and increasing level of resistance among E. coli to currently recommended first-line agents for acute cystitis requires a re-evaluation of treatment guidelines. With the low resistance, its proven efficacy and favourable safety profile, pivmecillinam is a suitable first-line agent for empirical treatment of acute cystitis.
匹美西林是美西林的前体药物，美西林是一种β-内酰胺类抗生素，具有新颖的作用位点，对革兰氏阴性菌如大肠杆菌和其他肠杆菌科细菌具有特异性且高活性。自上市以来，它已广泛用于治疗急性下尿路感染（UTI），主要在北欧国家。与尿路病原体对其他β-内酰胺类药物（特别是氨苄西林/阿莫西林）以及对其他UTI抗生素（如甲氧苄啶和甲氧苄啶/磺胺甲恶唑（TMP/SMX））的耐药性不断增加形成对比的是，对美西林的耐药水平一直保持在较低水平。不到2%的社区分离大肠杆菌对美西林耐药。本文回顾了匹美西林的临床数据，特别关注其安全性方面。20世纪70年代至80年代的大量研究证明了匹美西林经验性治疗急性膀胱炎的临床疗效和安全性。最近的研究证实，匹美西林短期治疗的临床和细菌学治愈率与其他UTI药物相似。对患有UTI的孕妇进行的临床研究以及大型流行病学研究均证实了孕期使用匹美西林的安全性。在北欧国家，多年来匹美西林一直是孕期治疗UTI最广泛使用的药物。抗生素治疗的生态学方面在不良反应和由于正常微生物群落受到干扰而导致的耐药性发展方面都很重要。研究表明，匹美西林对正常口咽、肠道和皮肤微生物群落的影响非常小。临床研究证实，这在临床上表现为腹泻和念珠菌性阴道炎的发生率较低。大肠杆菌对目前推荐的急性膀胱炎一线药物的耐药水平不断升高，这需要重新评估治疗指南。鉴于其低耐药性、已证实的疗效和良好的安全性，匹美西林是急性膀胱炎经验性治疗的合适一线药物。
