Fillastre J P, Leroy A, Humbert G
Antimicrob Agents Chemother. 1987 Feb;31(2):156-60. doi: 10.1128/AAC.31.2.156.
The pharmacokinetics of ofloxacin were investigated in 12 normal subjects and 21 uremic patients after the administration of a single oral 200-mg dose. An open three-compartment body model was used to calculate ofloxacin pharmacokinetic parameters. In healthy subjects, the peak plasma level averaged 2.24 +/- 0.90 micrograms/ml and was obtained at 0.83 +/- 0.31 h. The absorption rate constant was 4.22 +/- 1.64 h-1. The terminal half-life was 7.86 +/- 1.81 h. The apparent volume of distribution was 2.53 +/- 0.78 liters/kg. Total body and renal clearances were 241.4 +/- 53.8 and 196.5 +/- 42.9 ml/min per 1.73 m2, respectively. A total of 68.4 +/- 11.9% of the dose was recovered unchanged in 24-h urine. In uremic patients, the terminal half-life increased in relation to the degree of renal failure: from 8 h in normal subjects to 37 h in severely uremic patients. Renal insufficiency did not significantly modify the peak plasma level, the apparent volume of distribution, the fractional clearance, or the nonrenal clearance of ofloxacin. However, the time to peak level was delayed in patients with creatinine clearance of less than 30 ml/min. Linear relationships were found between ofloxacin pharmacokinetic parameters and glomerular filtration rate data. Ofloxacin is only very slightly removed by hemodialysis. Dosage adjustments of ofloxacin in uremic patients are proposed.
对12名正常受试者和21名尿毒症患者单次口服200毫克剂量的氧氟沙星后的药代动力学进行了研究。采用开放三室人体模型计算氧氟沙星的药代动力学参数。在健康受试者中，血浆峰值水平平均为2.24±0.90微克/毫升，在0.83±0.31小时达到。吸收速率常数为4.22±1.64小时-1。末端半衰期为7.86±1.81小时。表观分布容积为2.53±0.78升/千克。每1.73平方米的全身清除率和肾脏清除率分别为241.4±53.8和196.5±42.9毫升/分钟。24小时尿液中回收的未变化剂量占总剂量的68.4±11.9%。在尿毒症患者中，末端半衰期随肾衰竭程度增加：从正常受试者的8小时增加到严重尿毒症患者的37小时。肾功能不全并未显著改变氧氟沙星的血浆峰值水平、表观分布容积、清除分数或非肾脏清除率。然而，肌酐清除率低于30毫升/分钟的患者达到峰值水平的时间延迟。发现氧氟沙星药代动力学参数与肾小球滤过率数据之间存在线性关系。血液透析对氧氟沙星的清除作用非常轻微。提出了尿毒症患者氧氟沙星的剂量调整建议。
