Tranexamic Acid for Melasma: How It Works & Dosing

This is an English adaptation of a clinical article Dr. SangYoul Yun — board-certified dermatologist and Medical Director of Delight Dermatology in Gangnam, Seoul — originally published in Korean. Read the Korean original on Naver. It has been restructured and translated for international readers.

Melasma is a common source of worry. It develops from a range of causes — hormonal changes, oral contraceptives, sun exposure — and because the causes are varied, it is not easy to treat. One of the medications used for melasma is tranexamic acid (known in Korea by the brand Doransamin). Let's take a closer look.

Tranexamic acid comes as an orange-and-yellow capsule. It has long been used as a hemostatic (bleeding-control) agent, but once its effect on melasma became clear, it has been available over the counter in Japan since 2007.

How it works

If you examine a melasma lesion, the number of mast cells is increased. These mast cells produce vascular endothelial growth factor (VEGF), transforming growth factor-beta and fibroblast growth factor, all of which contribute to the development of melasma. However, using an antihistamine alone to reduce mast cells did not prove effective for melasma.

Separately, a factor called plasmin stimulates melanocytes and promotes melanin production. Tranexamic acid is an anti-plasmin agent: it suppresses melanin production, which is how it treats melasma and pigmentary conditions.

Dosing

For adults, tranexamic acid is taken orally at 750–2000 mg per day, divided into 3–4 doses. One capsule is generally 250 mg. In my practice I typically prescribe 250 mg twice daily.

Precautions

Tranexamic acid should be used with caution in patients who have a clot — such as cerebral thrombosis, myocardial infarction or thrombophlebitis — or who are at risk of thrombosis. That said, the dose generally used for melasma is only about one-sixth of the dose used to treat clotting disorders, so it is a relatively small amount and the likelihood of side effects is low.

Side effects

Possible side effects include reduced menstrual flow, headache, skin rash and abdominal pain. If these occur, we discuss it and may adjust the dose or provide appropriate treatment.

Tranexamic acid is one part of melasma care

Because melasma is genuinely difficult to treat, it often requires more than tranexamic acid alone — laser treatment, radiofrequency, chemical peels and other approaches are frequently combined. You can read more about our combined approach to melasma treatment and broader pigmentation treatment. Medications similar to tranexamic acid include Melasmin and Transino II.

Medical disclaimer. This article is general information and does not replace individual consultation. Tranexamic acid is a prescription medication with contraindications (for example, thrombotic disease), so the decision to take it — and the dose — must be made only after consulting a dermatologist.