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本类药物为合成抗菌药,是DNA螺旋酶抑制剂。其药理学特点:(1)抗菌谱,与其它抗菌药较少交叉耐药性。(2)抗菌作用强,抗菌范围新一代的左氟沙星抗菌活性比消旋的氧氟沙星强一倍,其他如司帕沙星、妥舒沙星等抗菌谱广,具有抗革兰氏阳性、厌氧菌、衣原体、支原体以及抗结核分枝杆菌作用,另有克林沙星,DU-6859a具有超广谱、高效特点。(3)药代动力学特性,口服吸收好,分布于体液和组织,V_d>21L/kg,远高于β-内酰胺类与气炎甙类,分布于支气管粘膜,骨、皮肤、前列腺,以及肺巨噬细胞内浓度高。若干品种如洛美沙星、司帕沙星、氟罗沙星口服芦氟沙星具有长半衰期(7～35h)给药次数明显减少,每日仅需1～2次,便于患者服用。后一药物除有效血药浓度持久外,还有增强机体免疫功能作用。(4)多种药物均可作注射剂使用,且不增加毒副反应,对急、重症患者的序贯疗法已在临床推广应用。
This class of drugs for the synthesis of antibacterial drugs, is a DNA helicase inhibitor. Its pharmacological characteristics: (1) antibacterial spectrum, less cross-resistance with other antibacterials. (2) strong antibacterial activity, antibacterial range The new generation of levofloxacin antibacterial activity than the racemic of ofloxacin twice as strong, such as sparfloxacin, tosufloxacin broad antimicrobial spectrum, with anti-Gram Positive, anaerobic bacteria, chlamydia, mycoplasma and anti-mycobacterium tuberculosis, and another clifloxacin, DU-6859a has broad-spectrum, high efficiency. Pharmacokinetics, oral absorption, distributed in body fluids and tissues, V_d> 21L / kg, much higher than β-lactams and glycosides glycosides distributed in the bronchial mucosa, bone, skin, prostate, And high concentrations of pulmonary macrophages. Some varieties such as lomefloxacin, sparfloxacin, fleroxacin oral oral rufloxacin has a long half-life (7 ~ 35h) significantly reduced the number of administration, only 1 or 2 times a day for patients to take. The latter drug in addition to lasting blood concentration, but also enhance the body’s immune function. (4) a variety of drugs can be used for injection, and does not increase the side effects, sequential treatment of acute and critically ill patients has been clinically applied.