Rybak M
Department of Pharmacy, Detroit Receiving Hospital, Michigan 48201, USA.
Am J Med. 1996 Jun 24;100(6A):39S-44S. doi: 10.1016/s0002-9343(96)00106-4.
Cefepime, a fourth-generation cephalosporin with activity against both gram-negative and gram-positive organisms, has been investigated in healthy subjects and in special patient populations, including the elderly and those whose ability to eliminate drugs may be compromised. This review of seven pharmacokinetic studies indicates that the pharmacokinetic disposition of cefepime, administered either intravenously or intramuscularly, is similar to that of other cephalosporins with regard to dose linearity, renal excretion, and low serum protein binding. The elimination half-life of intravenous cefepime has been found to be approximately 2 hours, and peak serum concentrations approach 82 microg/mL for a 1-g dose and 164 microg/mL for a 2-g dose. Total body clearance is approximately 120 mL/min, independent of dose, and >80% of the drug is excreted unchanged by the kidneys. Dosage adjustment is warranted for patients with renal insufficiency but not hepatic dysfunction. The pharmacokinetic disposition of cefepime is altered in the elderly but not enough to necessitate additional dosage adjustment. Tissue penetration studies indicate similarity to other cephalosporins with low protein binding.
头孢吡肟是一种对革兰氏阴性菌和革兰氏阳性菌均有活性的第四代头孢菌素,已在健康受试者以及包括老年人和药物消除能力可能受损者在内的特殊患者群体中进行了研究。这篇对七项药代动力学研究的综述表明,静脉注射或肌肉注射的头孢吡肟的药代动力学处置在剂量线性、肾排泄和低血清蛋白结合方面与其他头孢菌素相似。已发现静脉注射头孢吡肟的消除半衰期约为2小时,1g剂量的血清峰值浓度接近82μg/mL,2g剂量的血清峰值浓度接近164μg/mL。总体清除率约为120 mL/分钟,与剂量无关,且>80%的药物以原形经肾脏排泄。肾功能不全患者需要调整剂量,但肝功能不全患者无需调整。头孢吡肟的药代动力学处置在老年人中有所改变,但不足以需要额外调整剂量。组织穿透性研究表明,其与其他低蛋白结合的头孢菌素相似。