Dowzicky M, Nadler H, Dorr M B, Acusta A, Talbot G H
Rhône-Poulenc Rorer Pharmaceuticals Inc., Collegeville, Pennsylvania 19426-0800, USA.
Clin Ther. 1999 May;21(5):790-805; discussion 789. doi: 10.1016/s0149-2918(99)80002-2.
The in vitro activity of and pathogen responses to sparfloxacin were compared with those of standard therapies for the treatment of patients with community-acquired pneumonia, complicated skin or skin-structure infections, urinary tract infections, acute bacterial exacerbations of chronic bronchitis, and acute maxillary sinusitis in 7 multicenter controlled trials in North America. Sparfloxacin was administered orally as a 400-mg loading dose followed by 200 mg once daily for up to 10 days. The bacteriologic efficacy of sparfloxacin (84% to 95%) was comparable to that of comparator drugs (77% to 100%). Sparfloxacin was generally 2 to 8 times more active (minimum inhibitory concentration for 90% of strains tested [MIC90]: 0.03 to 0.5 microg/mL) than comparators against common pathogens isolated in community-acquired infections, especially Streptococcus pneumoniae, including penicillin-resistant strains; Moraxella catarrhalis; Haemophilus influenzae; Streptococcus pyogenes; and Staphylococcus aureus. Sparfloxacin was also effective against Chlamydia and Mycoplasma species. The emergence of resistance was uncommon during sparfloxacin therapy (0.3% of 1100 cases). Higher area under the plasma concentration-time curve/MIC and maximum plasma concentration/MIC ratios for sparfloxacin were associated with clinical and bacteriologic efficacy, whereas lower ratios were associated with clinical and bacteriologic failure. The clinical efficacy of sparfloxacin (80% to 95%) was comparable to that obtained with the comparator drugs (71% to 92%). In addition, sparfloxacin was well tolerated and had an overall frequency of related adverse events similar to that of the comparators. There was a higher frequency of photosensitivity reactions but a lower level of digestive adverse events with sparfloxacin compared with comparators. Sparfloxacin is a suitable therapeutic alternative for the empiric treatment of respiratory tract infections owing to its favorable pharmacokinetic profile and activity against typical and atypical respiratory tract pathogens, even in geographic areas with a high incidence of penicillin resistance.
在北美进行的7项多中心对照试验中,将司帕沙星的体外活性及病原体对其的反应与治疗社区获得性肺炎、复杂性皮肤或皮肤结构感染、尿路感染、慢性支气管炎急性细菌感染以及急性上颌窦炎患者的标准疗法进行了比较。司帕沙星口服给药,负荷剂量为400mg,随后每日一次,每次200mg,疗程最长10天。司帕沙星的细菌学疗效(84%至95%)与对照药物(77%至100%)相当。在社区获得性感染中分离出的常见病原体,尤其是肺炎链球菌(包括耐青霉素菌株)、卡他莫拉菌、流感嗜血杆菌、化脓性链球菌和金黄色葡萄球菌方面,司帕沙星的活性通常比对照药物高2至8倍(对90%受试菌株的最低抑菌浓度[MIC90]:0.03至0.5μg/mL)。司帕沙星对衣原体和支原体属也有效。在司帕沙星治疗期间,耐药性的出现并不常见(1100例中的0.3%)。司帕沙星的血浆浓度 - 时间曲线下面积/MIC和最大血浆浓度/MIC比值较高与临床和细菌学疗效相关,而较低比值则与临床和细菌学治疗失败相关。司帕沙星的临床疗效(80%至95%)与对照药物(71%至92%)相当。此外,司帕沙星耐受性良好,相关不良事件的总体发生率与对照药物相似。与对照药物相比,司帕沙星的光敏反应发生率较高,但消化系统不良事件的发生率较低。由于司帕沙星具有良好的药代动力学特性以及对典型和非典型呼吸道病原体的活性,即使在青霉素耐药率高的地区,它也是呼吸道感染经验性治疗的合适替代药物。