Objective: The current study was to examines the effects of tranexamic acid and its derivatives (N-Acetyl-Tranexamic acid and N-Phthaloyl-Tranexamic acid) on the metabolism and chemical modulation of glutathione (GSH)/ thiol in freshly isolated leukocytes from human blood. Method: Blood from human volunteers was taken and leukocytes were isolated, by avoiding oxidation and coagulation of the blood. The pH of phosphate buffer solution on was adjusted to pH 7.62 and absorbances were measured at 412 nm using U.V/ Visible spectroscopy. Results: The effect of the different concentrations of N-Acetyl tranexamic acid on the metabolism of thiol in leukocytes was found to exhibit greater changes as compared to the effects of tranexamic acid and phthaloyl tranexamic acid. Furthermore, these changes in thiol concentration were found to be time dependent. Conclusions: It appears that N-Acetyl tranexamic acid causes the depletion of GSH markedly on thiols in leukocytes solutions due to the oxidation while N-Phthaloyl tranexamic acid shows slight change.