Kowalsky S F, Echols R M, Parker M A
Clin Pharm. 1985 Mar-Apr;4(2):177-81.
The pharmacokinetics of ceftriaxone was studied in 14 men and women volunteers with renal insufficiency. Subjects were grouped by renal function: those with end-stage renal disease (CLcr less than 15 mL/min/1.73 sq m) but not receiving dialysis, those with severe renal insufficiency (CLcr 16-30 mL/min/1.73 sq m), and those with moderate renal insufficiency (CLcr 31-60 mL/min/1.73 sq m). Ceftriaxone 1 g as the sodium salt was administered by i.v. infusion over 30 minutes, and blood and urine samples were collected before and up to 48 hours after drug administration. The pharmacokinetic data were described using a nonlinear least-squares computer program. For volunteers with a creatinine clearance of less than 15 mL/min/1.73 sq m, the mean half-life was 15.6 hours. For subjects with a creatinine clearance of 31-60 mL/min/1.73 sq m, the mean half-life was 11.9 hours. Plasma ceftriaxone concentrations measured at the conclusion of the infusion (mean peak concentration 122 +/- 53.1 micrograms/mL) or 24 hours after the infusion (mean concentration 20.2 +/- 6.14 micrograms/mL) were similar in each study group. A dose of ceftriaxone 1 g every 24 hours in patients with renal insufficiency is probably adequate for inhibiting most susceptible gram-positive and gram-negative microorganisms.
在14名患有肾功能不全的男性和女性志愿者中研究了头孢曲松的药代动力学。受试者按肾功能分组:终末期肾病患者(肌酐清除率低于15 mL/分钟/1.73平方米)但未接受透析,严重肾功能不全患者(肌酐清除率16 - 30 mL/分钟/1.73平方米),以及中度肾功能不全患者(肌酐清除率31 - 60 mL/分钟/1.73平方米)。以钠盐形式的1g头孢曲松通过静脉输注30分钟给药,在给药前及给药后长达48小时收集血液和尿液样本。使用非线性最小二乘法计算机程序描述药代动力学数据。对于肌酐清除率低于15 mL/分钟/1.73平方米的志愿者,平均半衰期为15.6小时。对于肌酐清除率为31 - 60 mL/分钟/1.73平方米的受试者,平均半衰期为11.9小时。在每个研究组中,输注结束时测得的血浆头孢曲松浓度(平均峰值浓度122±53.1微克/毫升)或输注后24小时的浓度(平均浓度20.2±6.14微克/毫升)相似。对于肾功能不全患者,每24小时给予1g头孢曲松的剂量可能足以抑制大多数易感革兰氏阳性和革兰氏阴性微生物。