Oral Tranexamic Acid for the Treatment of Melasma 

Tranexamic acid blocks the production of melanin (skin pigment) and decreases inflammation.  In numerous studies it has been shown to improve melasma when other treatments have failed, and side effects, if present, are mild.   

Should be used in combination with good sun protection and topical regimen

Side effects reported for the treatment of melasma are mild and may include: 

• Gastrointestinal discomfort - nausea, heartburn, vomiting 
• Gynecological – reduced or absent menses, abdominal cramps or backpain 
• Other: head headaches, muscle or joint aches, sinus pain

Contraindications 

• Women who are pregnant or nursing, have had two or more spontaneous abortions. 
• Women taking oral contraceptives or other hormone-based birth control- for less than 30 days are at highest risk.  On long term OCP (many years)– lower risk.  Progesterone only or IUD – very low risk. 
• Women who have a history or a strong family history of thromboembolic disease, such as deep vein thrombosis, pulmonary embolism, cerebral thrombosis (stroke) or any other kind of blood clots or bleeding disorders (Factor V Leiden, protein S deficiency). 
• Women who have a history of subarachnoid hemorrhage. 
• Women who are on blood thinners. 
• Women who smoke. 
• Women with significant kidney, cardiovascular or respiratory disease. 
• Women with an active cancer. 



Dosage 

• 325 mg twice a day (1/2 a 650mg pill twice a day) for 3 months to a year 
• 650mg once a day 
• Low dose (250mg ) can be used longer periods 

So once you stop the tranexamic acid, melasma may return. Patients should use triple combination cream or a skin brightener without hydroquinone when they stop taking tranexamic acid.