el Guinaidy M A, Nawishy S, Abd el Bary M, Sabbour M S
Department of Medicine and Pharmacology, Ain-Shams University, Cairo, Egypt.
Chemotherapy. 1991;37(2):77-85. doi: 10.1159/000238837.
The pharmacokinetics of cefodizime (HR 221) were studied in 6 healthy male individuals and 12 male patients with various degrees of chronic renal failure following intravenous bolus injection of 1 g of the drug. Serum pharmacokinetics were described by an open two-compartment kinetic model. The serum levels of cefodizime exceeded the MIC90 for Enterobacteriaceae, Haemophilus influenzae and Neisseria gonorrhoeae for more than 12 h in healthy individuals and 24 h in renal failure patients. The half-life of elimination was significantly prolonged (p less than 0.001) from 2.7 +/- 0.2 h in healthy volunteers to 7.7 +/- 1.5 h in renal failure patients. The total systemic clearance decreased significantly (p less than 0.001) from 43.3 +/- 5.8 ml/h/kg in healthy volunteers to 23.2 +/- 5.6 ml/h/kg in renal failure patients. A linear correlation (r = 0.9; p less than 0.001) was found between creatinine clearance and the total systemic clearance of cefodizime. The AUC0-infinity in patients with renal failure was more than double the value in healthy volunteers. An equation to calculate the 1-gram dose interval of cefodizime in patients with compromised renal function is provided.
在6名健康男性个体和12名患有不同程度慢性肾功能衰竭的男性患者静脉推注1克头孢地嗪（HR 221）后，对其药代动力学进行了研究。血清药代动力学用开放二室动力学模型描述。在健康个体中，头孢地嗪的血清水平超过肠杆菌科、流感嗜血杆菌和淋病奈瑟菌的MIC90超过12小时，在肾功能衰竭患者中超过24小时。消除半衰期从健康志愿者的2.7±0.2小时显著延长（p<0.001）至肾功能衰竭患者的7.7±1.5小时。总全身清除率从健康志愿者的43.3±5.8毫升/小时/千克显著降低（p<0.001）至肾功能衰竭患者的23.2±5.6毫升/小时/千克。发现肌酐清除率与头孢地嗪的总全身清除率之间存在线性相关性（r = 0.9；p<0.001）。肾功能衰竭患者的AUC0-∞是健康志愿者的两倍多。提供了一个计算肾功能受损患者中头孢地嗪1克剂量间隔的公式。
