Graninger W
Wien Klin Wochenschr Suppl. 1983;142:11-5.
Apart from their antimicrobial activity pattern the cephalosporins differ by their pharmacokinetics. Most cephalosporins have a plasma half life of 30 to 120 minutes. Only ceftriaxon has a half life of about 8 hours, which implicates extended dose intervals. Cephalosporins are excreted renally. Cefoperazone and ceftriaxon, however, are excreted with the bile up to 30%. Cefalotin, cefacetril and cefotaxime are metabolized to a significant degree. Only the main-metabolite of cefotaxime shows mentionable antimicrobial activity. With regard to renal insufficiency (creatinine clearance greater than 5 ml/min) dose reduction is not necessary with cefoperazone and with ceftriaxon because of hepatic excretion and with cefotaxime because of metabolism.
除了抗菌活性模式不同外,头孢菌素类药物在药代动力学方面也存在差异。大多数头孢菌素类药物的血浆半衰期为30至120分钟。只有头孢曲松的半衰期约为8小时,这意味着给药间隔时间可以延长。头孢菌素类药物经肾脏排泄。然而,头孢哌酮和头孢曲松有高达30%经胆汁排泄。头孢噻吩、头孢乙腈和头孢噻肟有相当程度的代谢。只有头孢噻肟的主要代谢产物显示出明显的抗菌活性。对于肾功能不全(肌酐清除率大于5 ml/min)的患者,由于头孢哌酮和头孢曲松经肝脏排泄,头孢噻肟经代谢,因此无需减少剂量。