Comparative pharmacokinetic study of four different sulfonamides in combination with trimethoprim in human volunteers.

The pharmacokinetics of four different sulfonamides i. e., sulfamethoxazole (SMZ). Sulfamoxole (SMO), Sulfadiazine (SDZ) and Sulfadimidine (SDD) in combination with trimethoprim (TMP) were studied in 12 healthy volunteers. Plasma and urine concentrations of sulfonamides were measured at different time intervals. No significant difference was observed in the area under the plasma curve (AUC) of SMZ, SMO and SDZ, while AUC of SMO was significantly higher than SDD only. Free (unmetabolized) SDZ urinary excretion during a 10-25 h period was significantly higher than SMZ, SMO and SDD. The results suggest that SDZ alone or in combination with TMP would be more effective in urinary tract infections as compared to other sulfonamides studied.