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环丙氟哌酸(简称CPFX,又称环丙沙星)1983年由西德拜耳制药有限公司首先研制成功,是目前活性最强、临床评价最高的第三代喹诺酮类抗菌新药.对革兰阴性和革兰阳性菌均有强大的杀灭作用,而且对分枝杆菌、麻疯杆菌及绿脓杆菌有高度抗菌活性,治疗厌氧菌感染优于头孢氨噻肟,治疗严重感染优于亚胺硫霉素,治疗心内膜炎优于头孢他定,治疗淋球菌感染比氟哌酸强15倍,MIC为0.01~2.00μg/ml,可口服或静脉注射给药.一般的抗菌药在1小时内杀灭细菌而本品仅以0.15μg/ml的浓度在19分钟内便能杀死病菌,大多数组织中浓度高于血清浓度,主要以原形从尿和粪便中排出,t_(1/2)4~5小时,生物利用度为80%,主要在肝脏代谢,24小时尿中含量为给药剂量的30%~50%.具有独特的后发性抗菌作用,在血药浓度降至MIC以下时,仍能保持6小时的抗菌活性,可抑制细菌再生,防止细菌再度繁殖而造成的重复感染,与抗生素之间无交叉耐药性.
Ciprofloxacin (referred to as CPFX, also known as ciprofloxacin) was first developed by West Bayer Pharmaceutical Co., Ltd. in 1983, is currently the most active and highest clinical evaluation of the third generation of quinolone antibacterial drugs against Gram Negative and Gram-positive bacteria have a strong killing effect, but also on mycobacteria, leprae and Pseudomonas aeruginosa has a high degree of antibacterial activity, treatment of anaerobic bacteria than cefotaxime, the treatment of serious infections than in Asia Amikacin, the treatment of endocarditis is superior to ceftazidime, gonococcal infection treatment than norfloxacin 15 times stronger, MIC was 0.01 ~ 2.00μg / ml, oral or intravenous administration of the general antimicrobial drugs 1 hour to kill bacteria and the goods only 0.15μg / ml concentration in 19 minutes to kill bacteria, the concentration of most tissues higher than the serum concentration, mainly in the prototype discharged from urine and feces, t_ (1 / 2) 4 ~ 5 hours, bioavailability of 80%, mainly in the liver metabolism, 24-hour urinary content of the dose of 30% to 50%. Has a unique secondary antimicrobial effect, decreased blood concentration To MIC the following, still can maintain 6 hours of antibacterial activity, can inhibit bacterial regeneration, to prevent bacteria from re-breeding caused Of the repeat infection, no cross-resistance with antibiotics.