Walstad R A, Nilsen O G, Berg K J
Eur J Clin Pharmacol. 1983;24(3):391-8. doi: 10.1007/BF00610061.
The pharmacokinetics and clinical effects of cefuroxime were investigated in 5 patients with severe impairment of renal function (creatinine clearance less than or equal to 23 ml/min), suffering from an urinary tract infection. Bolus i.v. injections of cefuroxime 750 mg b.i.d. or 750 mg once daily were given to the patients depending on the degree of renal impairment. The concentration of drug in serum and urine was measured during treatment, and pharmacokinetic parameters were evaluated on the second and last days; the parameters obtained on the 2 days did not differ significantly. Drug elimination half-life increased from 4.2 h (creatinine clearance 23.0 ml/min) to 22.3 h (creatinine clearance 5.0 ml/min) with decreasing renal function. The apparent volume of distribution ranged from 11.6 to 17.9 l, and showed a substantial increase to 29.6 l in the patient with the poorest renal function. A linear correlation was found between the total and renal clearance of cefuroxime and the creatinine clearance; the extrarenal clearance was 8.24 ml/min. Concomitant treatment with furosemide did not impair renal function and no evidence of nephrotoxicity was found. The clinical efficacy of the drug was good. Symptoms of infection subsided after 3-4 days and the isolated pathogens were eradicated. No relapse or episodes of reinfection were observed in a following-up period of 3 months. The drug was well tolerated and no side effects or changes in haematological or biochemical values were seen.
对5例肾功能严重受损（肌酐清除率小于或等于23ml/min）且患有尿路感染的患者，研究了头孢呋辛的药代动力学和临床效果。根据肾功能损害程度，对患者静脉推注头孢呋辛750mg，每日两次或每日一次。治疗期间测定血清和尿液中的药物浓度，并在第二天和最后一天评估药代动力学参数；两天获得的参数无显著差异。随着肾功能下降，药物消除半衰期从4.2小时（肌酐清除率23.0ml/min）增加到22.3小时（肌酐清除率5.0ml/min）。表观分布容积为11.6至17.9升，在肾功能最差的患者中显著增加至29.6升。发现头孢呋辛的总清除率和肾清除率与肌酐清除率之间呈线性相关；肾外清除率为8.24ml/min。与呋塞米联合治疗未损害肾功能，未发现肾毒性证据。该药物临床疗效良好。感染症状在3-4天后消退，分离出的病原体被根除。在3个月的随访期内未观察到复发或再感染情况。该药物耐受性良好，未出现副作用，血液学或生化值也无变化。
