Cazzola Mario, Salvatori Enrica, Dionisio Paolo, Allegra Luigi
Department of Pneumology, Unit of Pneumology and Allergology, A. Cardarelli Hospital, Via del Parco Margherita 24, 80121 Naples, Italy.
Pulm Pharmacol Ther. 2006;19 Suppl 1:30-7. doi: 10.1016/j.pupt.2005.09.007. Epub 2005 Dec 15.
Empiric therapy with oral antibiotics is normal practice in the treatment of acute exacerbations of chronic bronchitis (AECB), but there is growing concern regarding efficacy of the currently available antimicrobials. Prulifloxacin, the lipophilic prodrug of ulifloxacin, is an oral fluoroquinolone antibacterial agent with a broad-spectrum in vitro activity against Gram-negative and -positive bacteria, and a long elimination half-life, which allows the once-daily administration. In addition, it penetrates extensively into lung tissues. Statistical analyses indicated a significant linear trend between the prulifloxacin 300, 450, and 600 mg doses, which would point to an interesting relationship between dose employed and response obtained. The 600 mg once-daily dose showed the best risk/benefit ratio, and was selected for use in the pivotal clinical trials. In well-designed clinical trials, prulifloxacin 600 mg administered once daily for 10 days in patients with AECB showed good clinical and bacteriological efficacy (similar to that of ciprofloxacin or co-amoxiclav). In particular, the clinical response rates were favourable in all clinical trials, with eradication rates in patients with pneumococcal infections at least as high as the comparators. It can be concluded that prulifloxacin 600 mg once daily is a new therapeutic prospect in the antimicrobial therapy of AECB. In particular, since good patient compliance is a key factor in the successful treatment of any infection, the once daily treatment with prulifloxacin may have some compliance advantages compared to the twice-daily treatment with agents such as ciprofloxacin or co-amoxiclav.
口服抗生素的经验性治疗是慢性支气管炎急性加重期(AECB)治疗的常规做法,但人们越来越关注目前可用抗菌药物的疗效。普利沙星是乌利沙星的亲脂性前体药物,是一种口服氟喹诺酮类抗菌剂,对革兰氏阴性菌和阳性菌具有广谱体外活性,且消除半衰期长,允许每日一次给药。此外,它能广泛渗透到肺组织中。统计分析表明,普利沙星300、450和600毫克剂量之间存在显著的线性趋势,这表明所用剂量与获得的反应之间存在有趣的关系。每日一次600毫克的剂量显示出最佳的风险/效益比,并被选用于关键的临床试验。在精心设计的临床试验中,AECB患者每日一次服用600毫克普利沙星,持续10天,显示出良好的临床和细菌学疗效(与环丙沙星或阿莫西林克拉维酸相似)。特别是,在所有临床试验中临床反应率都很理想,肺炎球菌感染患者的根除率至少与对照药物一样高。可以得出结论,每日一次600毫克普利沙星是AECB抗菌治疗的一种新的治疗前景。特别是,由于良好的患者依从性是任何感染成功治疗的关键因素,与环丙沙星或阿莫西林克拉维酸等药物每日两次治疗相比,普利沙星每日一次治疗可能在依从性方面具有一些优势。