Alghasham A A, Nahata M C
College of Medicine, Riyadh, Saudi Arabia.
Ann Pharmacother. 1999 Jan;33(1):48-60. doi: 10.1345/aph.17460.
To review the pharmacology, antimicrobial activity, pharmacokinetics, clinical efficacy, and safety of trovafloxacin.
A MEDLINE search (January 1966-April 1998) was conducted for relevant literature using the terms CP-99,219, CP-116,519, trovafloxacin, and alatrofloxacin. Abstracts published by the American Society of Microbiology during 1995-1997 meetings were also reviewed.
All in vitro, animal, and human studies were reviewed for the antimicrobial activity, pharmacokinetics, efficacy, and safety of trovafloxacin.
Trovafloxacin is a new fluoroquinolone with enhanced activity against gram-positive and anaerobic microorganisms. The oral bioavailability under fasting conditions is approximately 88%. The elimination half-life of trovafloxacin is approximately 10 hours. Less than 10% of trovafloxacin is eliminated unchanged in the urine. Trovafloxacin is effective in the treatment of community-acquired pneumonia and nosocomial pneumonia with cure rates of > 90% and 77%, respectively. Trovafloxacin is comparable with ceftriaxone in the treatment of meningococcal meningitis in children; each produces a cure rate of approximately 90%. In treatment of uncomplicated urinary tract infection, both ciprofloxacin and trovafloxacin achieve an eradication rate of > or = 93%. Trovafloxacin is similar to ofloxacin in the treatment of urogenital Chlamydia trachomatis and acute exacerbations of chronic bronchitis, with clinical success in 97% of patients with each drug. The common adverse effects of trovafloxacin include dizziness, headache, and gastrointestinal intolerance.
The advantages of once-daily dosing and enhanced activity of trovafloxacin against gram-positive and anaerobic organisms may expand its use over available fluoroquinolones. Further studies are needed to define its role in the treatment of various infectious diseases.
综述曲伐沙星的药理学、抗菌活性、药代动力学、临床疗效及安全性。
利用“CP-99,219”“CP-116,519”“曲伐沙星”和“阿拉曲伐沙星”等检索词,对MEDLINE(1966年1月至1998年4月)进行相关文献检索。还查阅了美国微生物学会在1995 - 1997年会议上发表的摘要。
对所有关于曲伐沙星抗菌活性、药代动力学、疗效及安全性的体外、动物和人体研究进行综述。
曲伐沙星是一种新型氟喹诺酮类药物,对革兰氏阳性菌和厌氧菌的活性增强。空腹条件下口服生物利用度约为88%。曲伐沙星的消除半衰期约为10小时。不到10%的曲伐沙星以原形经尿液排出。曲伐沙星治疗社区获得性肺炎和医院获得性肺炎有效,治愈率分别>90%和77%。在治疗儿童脑膜炎球菌性脑膜炎方面,曲伐沙星与头孢曲松相当;二者治愈率均约为90%。在治疗单纯性尿路感染时,环丙沙星和曲伐沙星的根除率均>或 = 93%。在治疗泌尿生殖系统沙眼衣原体感染和慢性支气管炎急性加重方面,曲伐沙星与氧氟沙星相似,两种药物治疗的患者临床成功率均为97%。曲伐沙星的常见不良反应包括头晕、头痛和胃肠道不耐受。
曲伐沙星每日一次给药的优势以及对革兰氏阳性菌和厌氧菌活性增强,可能使其比现有氟喹诺酮类药物的应用范围更广。需要进一步研究以明确其在各种传染病治疗中的作用。