Mellin H E, Welling P G, Madsen P O
Antimicrob Agents Chemother. 1977 Feb;11(2):262-6. doi: 10.1128/AAC.11.2.262.
The pharmacokinetics of cefamandole, a new cephalosporin, were investigated in 23 patients with urinary tract infections and normal or varying degrees of impairment of renal function. A daily dose of 1.5 to 3.0 g administered intramuscularly was tolerated well and resulted in very high urine concentrations. The pharmacokinetics of the antibiotic were compared with isotopically labeled [(131)I]hippurate and [(125)I]iothalamate, which were used for determination of effective renal plasma flow and glomerular filtration rate, respectively. It was shown that cefamandole was excreted by glomerular filtration as well as by active tubular secretion. Probenecid inhibited the tubular secretion of cefamandole. The serum half-life of cefamandole in patients with normal renal function was approximately 1.5 h and increased in patients along with increasing impairment of renal function. Our studies indicate that a dosage regimen of 1 g of cefamandole every 8 h in patients with normal renal function results in urine concentrations sufficiently high for treatment of most common urinary tract infections. In patients with impaired renal function, the dosage interval should be increased or the dosage lowered according to the serum creatinine values.
对23例患有尿路感染且肾功能正常或有不同程度损害的患者,研究了新型头孢菌素头孢孟多的药代动力学。每日1.5至3.0 g的肌内注射剂量耐受性良好,并导致尿液中药物浓度很高。将该抗生素的药代动力学与分别用于测定有效肾血浆流量和肾小球滤过率的同位素标记的[(131)I]马尿酸盐和[(125)I]碘肽酸盐进行了比较。结果表明,头孢孟多通过肾小球滤过以及肾小管主动分泌排出。丙磺舒抑制头孢孟多的肾小管分泌。肾功能正常患者中头孢孟多的血清半衰期约为1.5小时,并随肾功能损害的加重而延长。我们的研究表明,肾功能正常的患者每8小时服用1 g头孢孟多的给药方案可使尿液浓度足够高,足以治疗大多数常见的尿路感染。对于肾功能受损的患者,应根据血清肌酐值延长给药间隔或降低剂量。