Yuk J H, Nightingale C H, Quintiliani R
Methodist Hospital, Department of Pharmacy Services, Texas Medical Center, Houston.
Clin Pharmacokinet. 1989 Oct;17(4):223-35. doi: 10.2165/00003088-198917040-00002.
Ceftriaxone is a third-generation cephalosporin that exhibits saturable plasma protein binding, which influences its pharmacokinetic parameters depending on the dose. Systemic clearance and volume of distribution of total drug show dependence on both concentration and time, whereas for unbound drug these parameters remain constant. The decrease in renal or non-renal clearance with age or in the presence of disease states is often compensated by the concurrent increase in free fraction, resulting in no apparent changes in half-life and no need for dose adjustment. Because of its unusually long plasma half-life, the availability of intramuscular administration and its high intrinsic activity against many organisms, ceftriaxone has become a popular agent in once-daily therapy of infections in paediatric patients, gonococcal infections and outpatient management of pneumonia and osteomyelitis.
头孢曲松是一种第三代头孢菌素，具有饱和性血浆蛋白结合特性，这会根据剂量影响其药代动力学参数。总药物的全身清除率和分布容积显示出对浓度和时间的依赖性，而对于游离药物，这些参数保持恒定。随着年龄增长或在疾病状态下，肾清除率或非肾清除率的降低通常会被游离分数的同时增加所补偿，导致半衰期无明显变化，无需调整剂量。由于其异常长的血浆半衰期、肌肉注射的便利性以及对多种病原体的高内在活性，头孢曲松已成为儿科患者感染、淋球菌感染以及肺炎和骨髓炎门诊治疗中每日一次治疗的常用药物。
