The pharmacokinetics of sulfamethoxazole were investigated in rabbits with folate-induced renal failure. The blood level, area under the blood concentration curve (AUC) and biological half-life were increased significantly, and the urinary excretion was decreased significantly compared with those of normal rabbits. Correlation of serum creatinine concentration and AUC, biological half-life, and correlation of creatinine clearance and renal clearance have linear relationship respectively. From these results, dosage regimen of sulfamethoxazole is considered to be adjusted for effective and safe therapy in renal failure.