Tranexamic Acid (often abbreviated as TXA or TA) is a synthesized amino acid that is used to treat moderate to severe melasma, especially in patients that have not had success with other treatments like lasers, skincare (sunscreen), and other prescription medication.

This is a new and promising treatment for melasma that’s been slowly gaining support for almost a decade now as an off-label use of this FDA-Approved drug, and now has some really good science behind its use in adults with melasma.

Tranexamic Acid in Melasma

Tranexamic acid is the only therapeutic agent that can prevent the activation of the pigment cells (melanocytes) by ultraviolet light, hormones, and injury to the skin. It acts by inhibition of the activation of a protein called plasminogen. Besides reducing the formation of melasma, Tranexamic acid is suggested to reduce the probability of recurrence upon discontinuation of other treatment modalities.

TA significantly reduces the recurrence rate of melasma upon discontinuation of the medicine. A good skin care regimen with carefully prescribed topical agents and laser technologies should be continued to be performed for maintenance.

In addition, strict avoidance of sun exposure is suggested as well as year round full spectrum sunblock.

Most patients respond to the combination of oral tranexamic acid, topical hydroquinone and either Q switched Nd:Yag or clear and brilliant laser treatments within 3-4 weeks. Normally a total of 3-4 laser treatments are provided approximately 2-4 weeks apart (Q switched Yag interval is 2-3 weeks apart and Clear and Brilliant interval is 3-4 weeks) apart.

Tranexamic acid has to reach to the bottom layers of the skin to interact with the melanocytes, the cells responsible for creating melanin and darker coloration in the skin, in order to be effective.

Tranexamic acid can reach to the proper skin depth 1 of 4 ways currently:

  1. Oral prescription medication: doctor prescribes you a pill to take daily. The problem with this is that tranexamic acid then interacts with and impacts the entire body, not just the skin, and this medication can have real side effects. Patients should not take Tranexamic acid pills if they have a history of venous or arterial clots, actively smoke, or are taking oral contraceptive pills.
  2. Microneedling the Skin and Applying Topically (rubbing into the skin through puncture channels) this method is problematic because the dosage is not precise: the channels close very quickly and at an uneven rate – and you never really know how deeply the product you’re rubbing in is penetrating, or how evenly it’s entering those channels.
  3. Skincare serums and creams containing tranexamic acid: claim to to able to deliver the molecules of TA through the skin to the required depths, but the science is lacking, and because this is a non-prescription strength, its weaker than the other options. We’ve seen many patients try a variety of products with little to no success and there is no science to say this method is viable.
  4. tranexamic acid microinjections were tedious and incredibly difficult using individual handheld syringes – it’s nearly impossible to precisely inject at the same depth, the same tiny amount, for hundreds of injections – so this method was untenable for both doctor and patient (due to discomfort and length of that method), until we created a computer-controlled precision micro-injection technique called TXA Restore.



Topical Tranexamic Acid

Historically, we’ve know that topical TA is really the ideal, but it has been a struggle to find a way to get the TXA evenly deposited throughout the skin at the depths it works best. Topical use of medications is almost always preferred, when possible, as it reduces the risk of systemic interference or side effects that are inherent when you take a pill form of any medication.

It’s only been in the last year that we’ve developed a method of precisely depositing the TXA in uniform droplets at a uniform depth, and this is done through our own proprietary treatment, called TXA Restore. This microneedling injection device has 3 important distinctions from traditional microneedling in that 1. the needles are depositing the TXA through hollow tips, 2. the amount of TXA being deposited is controlled through a precision injection tool, and 3. the depth is also precisely controlled by the device. This also means the treatment is much faster and more comfortable for the patient.

Oral Tranexamic Acid

Oral tranexamic acid(TXA prescription pills) have been shown to be an effective way of managing melasma, to decrease the creation of new pigment – so that the effects of laser treatment and hydroquinone to remove existing pigment are long-lasting. However, this pill format means that the TXA is dispersed throughout the entire body, and TA will have some side effects, which make it not a good choice for every patient, especially in pill format, where the effects are much more widespread than in a topical or injected formula.

Frequently Asked Questions about Treatment of Melasma with TXA


Sources Cited:

  1. Lajevardi, Vahideh, et al. “Comparison of the Therapeutic Efficacy and Safety of Combined Oral Tranexamic Acid and Topical Hydroquinone 4% Treatment vs. Topical Hydroquinone 4% Alone in Melasma: A Parallel-Group, Assessor- and Analyst-Blinded, Randomized Controlled Trial with a Short-Term Follow-Up.” Journal of Cosmetic Dermatology, vol. 16, no. 2, 2016, pp. 235–42. Crossref, doi:10.1111/jocd.12291.
  2. Saki, Nasrin, et al. “Comparing the Efficacy of Topical Hydroquinone 2 versus Intradermal Tranexamic Acid Microinjections in Treating Melasma: A Split-Face Controlled Trial.” Journal of Dermatological Treatment, vol. 29, no. 4, 2017, pp. 405–10. Crossref, doi:10.1080/09546634.2017.1392476.
  3. Lee, Hwee Chyen, et al. “Oral Tranexamic Acid (TA) in the Treatment of Melasma: A Retrospective Analysis.” Journal of the American Academy of Dermatology, vol. 75, no. 2, 2016, pp. 385–92. Crossref, doi:10.1016/j.jaad.2016.03.001.
Medical Director at Reflections Center

Dr. Mitchell Chasin founded Reflections Center for skin & body as a place where physicians specializing in cosmetic medicine could focus on helping empower patients to feel their most beautiful. Dr. Chasin believes strongly that the best cosmetic physicians are those who are dedicated to mastering their craft through continuing education and collaboration with the industry’s top doctors.