Renal Tubular Mechanisms for Excretion of Cefpiramide (SM-1652) in Association with Its Long-Lasting Pharmacokinetic Properties

概要

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To investigate possible mechanisms for the long-lasting pharmacokinetic properties of cefpiramide, pharmacokinetic and renal clearance studies were carried out using rabbits. Cefazolin was employed as a reference compound. In pharmacokinetic studies, the plasma half-life (t_<1/(2β)>) for cefpiramide was 2.7 times as long as that for cefazolin. The total body clearance (Cl_T) and renal clearance (Cl_R) for cefazolin were approximately 2.3 times larger than those for cefpiramide. In renal clearance studies, the clearance by glomerular filtration (Cl_f) for cefpiramide exceeded Cl_f for cefazolin by 2.5 times, because of lower plasma protein binding of cefpiramide. In contrast, the clearance by tubular secretion (Cl_s) for cefpiramide was one-fifth as small as Cl_s for cefazolin. The overall renal clearance (Cl_r) for cefazolin was 3.6 times as large as Cl_r for cefpiramide, being in good agreement with the cefazolin/cefpiramide ratios of Cl_T and Cl_R. Therefore, the long-lasting pharmacokinetic properties of cefpiramide was suggested to be due to the fact that cefpiramide undergoes renal tubular secretion to less extent.
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