Hartstein A I, Patrick K E, Jones S R, Miller M J, Bryant R E
Antimicrob Agents Chemother. 1977 Jul;12(1):93-7. doi: 10.1128/AAC.12.1.93.
Pharmacological and antimicrobial properties of cefadroxil, a new cephalosporin antibiotic, were compared with cephalexin. Absorption and excretion were studied in 20 healthy men. Peak concentrations of the drugs in serum were similar after ingestion of single 500-mg tablets. The concentration of cefadroxil in serum was more sustained than that of cephalexin. Levels of cefadroxil in serum after a dose of 1,000 mg were approximately twice those after a 500-mg dose through 6 h. Each drug administered in a dose of 500 mg every 6 h for 24 h resulted in concentrations in serum that were similar to a single dose without accumulation. Ninety-three percent of the cefadroxil and 85% of the cephalexin were excreted in urine after ingestions of single 500-mg tablets. The urine concentration of cefadroxil was more sustained than cephalexin. Minimal inhibitory and minimal bactericidal concentrations for clinical isolates were comparable with each drug. Cefadroxil compares favorably with cephalexin in this study. Sustained levels of cefadroxil in serum and urine suggest that this drug may be given at less frequent intervals than cephalexin.
将一种新型头孢菌素抗生素头孢羟氨苄的药理特性及抗菌特性与头孢氨苄进行了比较。对20名健康男性进行了吸收和排泄研究。服用单剂500毫克片剂后,两种药物在血清中的峰值浓度相似。头孢羟氨苄在血清中的浓度比头孢氨苄更持久。服用1000毫克剂量后,头孢羟氨苄在血清中的浓度在6小时内约为500毫克剂量后的两倍。每6小时服用500毫克剂量的每种药物,持续24小时,血清中的浓度与单剂量相似,无蓄积现象。服用单剂500毫克片剂后,93%的头孢羟氨苄和85%的头孢氨苄经尿液排泄。头孢羟氨苄在尿液中的浓度比头孢氨苄更持久。两种药物对临床分离株的最低抑菌浓度和最低杀菌浓度相当。在本研究中,头孢羟氨苄与头孢氨苄相比具有优势。头孢羟氨苄在血清和尿液中的浓度持续存在,表明该药物给药间隔时间可能比头孢氨苄更长。