Cefepime is a broad-spectrum fourth-generation cephalosporin with activity against Gram-positive and Gram-negative pathogens. It is generally administered as an infusion over 30–60 min or as a prolonged infusion with infusion times from 3 h to continuous administration. Cefepime is widely distributed in biological fluids and tissues with an average volume of distribution of ~ 0.2 L/kg in healthy adults with normal renal function. Protein binding is relatively low (20%), and elimination is mainly renal. About 85% of the dose is excreted unchanged in the urine, with an elimination half-life of 2–2.3 h. The pharmacokinetics of cefepime is altered under certain pathophysiological conditions, resulting in high inter-individual variability in cefepime volume of distribution and clearance, which poses challenges for population dosing approaches. Consequently, therapeutic drug monitoring of cefepime may be beneficial in certain patients including those who are critically ill, have life-threatening infections, or are infected with more resistant pathogens. Cefepime is generally safe and efficacious, with a goal exposure target of 70% time of the free drug concentration over the minimum inhibitory concentration for clinical efficacy. In recent years, reports of neurotoxicity have increased, specifically in patients with impaired renal function. This review summarizes the pharmacokinetics, pharmacodynamics, and toxicodynamics of cefepime contemporarily in the setting of increasing cefepime exposures. We explore the potential benefits of extended or continuous infusions and therapeutic drug monitoring in special populations.

头孢吡肟是一种广谱第四代头孢菌素，具有抗革兰氏阳性和革兰氏阴性病原体的活性。一般输注时间为 30-60 分钟，或延长输注时间为 3 小时至连续给药。头孢吡肟广泛分布于生物体液和组织中，在肾功能正常的健康成人中平均分布容积约为 0.2 L/kg。蛋白结合相对较低（20%），主要通过肾脏消除。约85%的剂量以原形通过尿液排出，消除半衰期为2-2.3小时。头孢吡肟的药代动力学在某些病理生理条件下发生改变，导致头孢吡肟的分布和清除量存在较高的个体间差异，这对人群给药方法提出了挑战。因此，头孢吡肟的治疗药物监测可能对某些患者有益，包括病情危重、患有危及生命的感染或感染更具耐药性病原体的患者。头孢吡肟通常是安全有效的，其目标暴露目标是游离药物浓度超过临床疗效最低抑制浓度的 70% 时间。近年来，神经毒性的报道有所增加，特别是肾功能受损的患者。本综述总结了当前头孢吡肟暴露量增加情况下头孢吡肟的药代动力学、药效学和毒效动力学。我们探索延长或连续输注和治疗药物监测对特殊人群的潜在益处。