Effect of Renal Excretion Rate on Intrarenal Distribution of Sulfonamides
A study of the distribution of sulfadimethoxine and sulfisoxazole in plasma, kidney cortex and medullopapillary tissue is presented. Equimolar amounts of each sulfonamide were fed to separate groups of hydropenic rats, and measurements carried out after one hour and five hours. Similar plasma concentrations of either drug were encountered one hour after the ingestion. A significant increase in the plasma concentration of sulfadimethoxine and a significant decrease in the plasma concentration of sulfisoxazole were observed five hours after ingestion. There was no change in the kidney tissue/plasma concentration ratios between one and five hours after the ingestion of sulfadimethoxine or sulfisoxazole. However, the ratios were significantly higher for sulfisoxazole, a fact that can be explained by its higher renal excretion rate. Likewise, the significant higher cortico-papillary concentration gradient observed for sulfisoxazole is interpreted to be a result of its slower rate of back diffusion in the distal segments of the nephron (on account of its lower pKa) and in contrast to sulfadimethoxine to the lack of active reabsorption of sulfisoxazole.
Key-WordsSulfonamides Plasma Concentration Kidney Excretion
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