Ernst M E, Ernst E J, Klepser M E
College of Pharmacy, University of Iowa (UI), Iowa City 52242-1112, USA.
Am J Health Syst Pharm. 1997 Nov 15;54(22):2569-84. doi: 10.1093/ajhp/54.22.2569.
The pharmacology, spectrum of activity, pharmacokinetics, clinical efficacy, and adverse effects of levofloxacin, recently approved by FDA, and trovafloxacin, currently undergoing clinical trials, are reviewed. Compared with quinolones in current use, levofloxacin is more potent against gram-negative bacteria and exhibits better antipseudomonal activity as well as greater oral bioavailability. Trovafloxacin is more potent than existing quinolones against gram-positive bacteria. Both agents exert their antibacterial effects by inhibiting bacterial DNA synthesis. Compared with other quinolones, levofloxacin and trovafloxacin both demonstrate superior activity against the Bacteroides fragilis group, Chlamydia spp., Mycoplasma pneumoniae, and Mycobacterium spp. The half-life (t1/2) of levofloxacin is nearly eight hours. Levofloxacin can therefore be administered once daily for mild to moderate infections and twice daily for more serious infections. The recommended daily dose is 500 mg. Trovafloxacin has a t1/2 of 12 hours, which allows for single daily doses, and is extensively metabolized. Levofloxacin has demonstrated clinical efficacy in the treatment of community-acquired respiratory-tract infections, genitourinary infections, skin and skin-structure infections, acute bacterial sinusitis, and infections of the head and neck. Trovafloxacin may have a role in treating skin and skin-structure or soft-tissue infections respiratory-tract infections, sexually transmitted diseases, and meningitis. Both agents are well tolerated, with central-nervous-system and gastrointestinal adverse effects reported most frequently. Concomitant administration of antacids or compounds containing meal cations decreases absorption of these quinolones. Levofloxacin and trovafloxacin have favorable antimicrobial and pharmacokinetic profiles, offering the advantages of once-daily doses as well as superior potency and spectrum of activity compared with currently available quinolones.
对最近获美国食品药品管理局（FDA）批准的左氧氟沙星以及目前正在进行临床试验的曲伐沙星的药理作用、活性谱、药代动力学、临床疗效和不良反应进行了综述。与目前使用的喹诺酮类药物相比，左氧氟沙星对革兰氏阴性菌的抗菌活性更强，对铜绿假单胞菌具有更好的抗菌活性，口服生物利用度也更高。曲伐沙星对革兰氏阳性菌的抗菌活性比现有的喹诺酮类药物更强。两种药物均通过抑制细菌DNA合成发挥抗菌作用。与其他喹诺酮类药物相比，左氧氟沙星和曲伐沙星对脆弱拟杆菌属、衣原体属、肺炎支原体和分枝杆菌属均表现出更强的活性。左氧氟沙星的半衰期（t1/2）约为8小时。因此，对于轻至中度感染，左氧氟沙星可每日给药1次；对于更严重的感染，则每日给药2次。推荐日剂量为500mg。曲伐沙星的t1/2为12小时，允许每日单次给药，且代谢广泛。左氧氟沙星已在社区获得性呼吸道感染、泌尿生殖系统感染、皮肤及皮肤结构感染、急性细菌性鼻窦炎以及头颈部感染的治疗中显示出临床疗效。曲伐沙星可能在治疗皮肤及皮肤结构或软组织感染、呼吸道感染、性传播疾病和脑膜炎方面发挥作用。两种药物耐受性良好，最常报告的不良反应为中枢神经系统和胃肠道不良反应。同时服用抗酸剂或含金属阳离子的化合物会降低这些喹诺酮类药物的吸收。左氧氟沙星和曲伐沙星具有良好的抗菌和药代动力学特性，与目前可用的喹诺酮类药物相比，具有每日单次给药的优势，以及更强的活性和更广的活性谱。
