药代动力学、药效学疗法及pradofloxacin的狗和猫。

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药代动力学、药效学疗法及pradofloxacin的狗和猫。

J兽医杂志。2013年6月,36(3):209 - 21所示。doi: 10.1111 / jvp.12036。Epub 2013年2月14。

PubMed ID

23406008 (在PubMed

]

文摘

Pradofloxacin第三代氟喹诺酮类,在欧盟授权使用的迹象在狗和猫和授权在美国最近一个治疗指示(皮肤感染)猫。本文总结和评价当前知识物化,药理(药物动力学(PK)和药效学(PD)],安全性和治疗属性的pradofloxacin目标物种。Pradofloxacin包含两个不对称中心,是纯粹的党卫军对映体。口服给药后的平板电脑(狗)或平板电脑和口服悬挂(cat),最大血浆浓度(Cmax)实现在小于3.0 h,和终端的半衰期是5 - 10 h。积累的顺序是轻微或没有每天一次口服给药。免费药物在血浆浓度在63 - 71%的总浓度。至于其他氟喹诺酮类原料药,抗菌活性是由于抑制细菌复制在两个站点,单元拓扑异构酶II和拓扑异构酶IV。抗菌谱包括革兰氏阴性和革兰氏阳性微生物、厌氧菌、支原体种虫害和一些细胞内生物(立克次氏体种虫害和分枝杆菌spp)。。浓度的杀戮行动类型。Pradofloxacin效能高(低麦克风值)与第一代和第二代氟喹诺酮类原料药相比。体内PK和体外PD数据集成提供的值Cmax /麦克风和血浆浓度时间曲线下面积(AUC24 h) /麦克风比率预测好的临床疗效与敏感的生物,当服用推荐剂量率。pradofloxacin临床试验评价,与其他授权抗菌药物相比,表明非或pradofloxacin的优越性。 Data indicating clinical and, in some instances, bacteriological cure have been reported: (i) in cats, for wound infections, abscesses, upper respiratory tract infections, conjunctivitis, feline infectious anaemia and lower urinary tract infections and (ii) in dogs, for wound infections, superficial and deep pyoderma, acute urinary tract infections and adjunctive treatment of infections of gingival and periodontal tissues. At clinical dose rates pradofloxacin was well tolerated in preclinical studies and in clinical trials. Among the advantages of pradofloxacin are (i) successful treatment of infections caused by strains resistant to some other fluoroquinolones, as predicted by PK/PD data, but depending on the specific MIC of the target strain and (ii) a reduced propensity for resistance development based on MPC measurements. The preclinical and clinical data on pradofloxacin suggest that this drug should commonly be the fluoroquinolone of choice when a drug of this class is indicated. However, the PK/PD data on pradofloxacin, in comparison with other fluoroquinolones, are not a factor that leads automatically to greater clinical efficacy.

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药物

Pradofloxacin