抄録
The influence of protein binding displacement on sulfonamide blood levels was studied, using salicylic acid as the displacing drug. When five different sulfonamides were orally administered with salicylic acid to rabbits, blood levels of sulfadimethoxine and sulfisoxazole which shown high binding to bovine serum albumin (BSA) markedly decreased, whereas blood levels of sulfanilamide which shows low binding to BSA did not change. In addition, a significant correlation (r=-0.974) was observed between the decrease in sulfonamide blood levels and the increase in unbound sulfonamide concentrations. These results indicate that protein binding displacement is an important determinant affecting the blood levels of highly bound drugs.
