A growing body of evidence supports treating melasma with systemic or intradermal tranexamic acid. But melasma patients often relapse when they stop taking the antifibrinolytic agent, and research on tranexamic acid’s long-term efficacy and safety is limited, according to a recent review of studies looking at the use of tranexamic acid for melasma and other dermatologic conditions published in Clinical and Experimental Dermatology.1
Discovered serendipitously as a urticaria and angioedema treatment, tranexamic acid’s popularity as a treatment for a wide variety of dermatologic conditions appears to be growing. Studies looking at using tranexamic acid for not only melasma but also post-inflammatory hyperpigmentation, urticaria, angioedema and hemostasis offer both encouraging and discouraging results.
And while the FDA has approved oral tranexamic acid for menorrhagia it has not yet approved it for treating skin conditions, including melasma.
Tranexamic Acid for Melasma
The most promising evidence supporting tranexamic acid as dermatologic monotherapy is in melasma treatment. Scientists believe tranexamic acid’s antiangiogenic and anti-melanogenic properties contribute to its efficacy in reducing melasma symptoms, according to the paper.
Researchers have studied treating patients with various doses and forms of tranexamic acid. They’ve found that the optimal dose depends on the condition being treated. In the cases of melasma and post-inflammatory hyperpigmentation, doses range from 4 mg/mL to 50 mg/mL, whereas the optimal dose for hemorrhage prevention is 100 mg/mL.
Most researchers have reported on oral or intradermal tranexamic acid administration. Fewer studies have focused on using topical tranexamic acid for melasma, according to the paper.
In what the authors say is the largest retrospective study of melasma and oral tranexamic acid treatment,2 researchers studied 561 melasma patients treated with 250 mg tranexamic acid taken twice daily, for an average of four months. Nearly 90% of patients improved within two months of treatment. The relapse rate among those who improved was 27.2%.
Adverse events occurred in 7.1% of patients studied, including one case of deep vein thrombosis, according to the study, published August 2016 in the Journal of the American Academy of Dermatology.2
In a study published October 2017 in Clinical and Experimental Dermatology, researchers compared tranexamic acid taken orally 250 mg twice daily vs intradermal microinjections of 4 mg/mL every four weeks for 12 weeks.3
The treatment methods were equally effective, reducing Melasma Area and Severity Index scores by about 78 in the oral group and 79 in the intradermal group at 12 weeks. Two patients had relapses at 24 weeks in the oral group but none relapsed in the intradermal group. Adverse events were mild.
- Forbat E, Ali F, Al-niaimi F. The emerging importance of tranexamic acid in dermatology. Clin Exp Dermatol. 2019. Epub ahead of print.
- Lee HC, Thng TG, Goh CL. Oral tranexamic acid (TA) in the treatment of melasma: A retrospective analysis. J Am Acad Dermatol. 2016;75(2):385-92.
- Atefi N, Dalvand B, Ghassemi M, Mehran G, Heydarian A. Therapeutic Effects of Topical Tranexamic Acid in Comparison with Hydroquinone in Treatment of Women with Melasma. Dermatol Ther (Heidelb). 2017;7(3):417-424.
- Sharma R, Mahajan VK, Mehta KS, Chauhan PS, Rawat R, Shiny TN. Therapeutic efficacy and safety of oral tranexamic acid and that of tranexamic acid local infiltration with microinjections in patients with melasma: a comparative study. Clin Exp Dermatol. 2017;42(7):728-734.