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氟喹诺酮是一类具有浓度依赖性杀菌作用的广谱抗菌药,目前在临床上被广泛用于治疗院内重度感染。其作用机制是抑制细菌DNA促旋酶和拓扑异构酶IV,耐药机制主要包括靶酶突变、外排机制和质粒介导耐药。游离药物的药时曲线下面积(AUC)与其最小抑菌浓度的比值(AUC:MIC)是决定这类药物能否达到最佳杀菌效果以及预防出现耐药性的关键药效学参数。除对肾功能损害患者应考虑适当调整氟喹诺酮给药剂量外,肝功能不全、细胞外液累积及烧伤患者均无需调整剂量。对重症患者而言,氟喹诺酮治疗方案的优化涉及多个因素,应视患者个体的具体实际情况而定,并在综合考虑致病菌的MIC、氟喹诺酮的药效学/药动学性质以及患者的特殊病理生理学状态等因素的基础上制定给药方案。
Fluoroquinolones are a class of broad-spectrum antimicrobial agents with a concentration-dependent bactericidal effect and are currently widely used clinically to treat nosocomial infections. Its mechanism of action is to inhibit bacterial DNA gyrase and topoisomerase IV. The mechanism of resistance mainly includes mutation of target enzyme, efflux mechanism and plasmid-mediated resistance. The ratio of the area under the curve (AUC) to the minimum inhibitory concentration (AUC: MIC) of free drug is the key pharmacodynamic parameter that determines the optimal bactericidal effect of such drug and the prevention of drug resistance. In addition to renal dysfunction patients should consider appropriate dosage of fluoroquinolone treatment, liver dysfunction, extracellular fluid accumulation and burn patients do not need to adjust the dose. For critically ill patients, the optimization of the fluoroquinolone regimen involves a number of factors and should be tailored to the individual circumstances of the individual patient, taking into account the MIC of the pathogen, the pharmacodynamic / pharmacokinetic properties of the fluoroquinolone and Patients with special pathophysiological status and other factors based on the formulation of drug delivery program.