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 concern. 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).

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

How it works

In melasma lesions, 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.

What the trials actually show

A 2024 meta-analysis of randomized controlled trials found that adding oral tranexamic acid to standard triple-combination cream improved MASI scores significantly more than the cream alone (mean difference −3.10) and was associated with a roughly 72% lower relative risk of melasma recurrence (risk ratio 0.28, 95% CI 0.16–0.49) (PMID 38848545). Korean clinical data indicates similar results for combination care: patients who took oral tranexamic acid alongside IPL and low-fluence laser treatment improved more than those treated with light and laser alone — with the difference most visible during periods of higher sun exposure (PMID 22103770).

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 can discuss them 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.