How should tranexamic acid be used?

The tranexamic acid is a synthetic derivative of lysine, initially used in medicine for its antifibrinolytic properties, before being studied in dermatology for its effects on skin pigmentation. When applied topically, it primarily acts by modulating the inflammatory and vascular pathways involved in the melanogenesis, notably by inhibiting UV-induced plasminogen activation. This limits the release of pro-inflammatory mediators such as prostaglandins and reduces melanocyte stimulation, thereby contributing to decreased melanin overproduction. The tranexamic acid thus establishes itself as a promising active ingredient to prevent and mitigate hyperpigmentation.

How should tranexamic acid be used in topical application?

To achieve visible effects on pigmented spots, tranexamic acid must be formulated at a concentration between 2% and 5%. Increasing this concentration does not enhance its efficacy and primarily exposes the skin to a higher risk of irritation. It should be noted, however, that the tranexamic acid is considered a relatively gentle active ingredient and is generally well tolerated in topical applications. It can thus be used up to twice daily, morning and evening, since it is not photosensitizing. In sensitive or compromised skin, however, it is preferable to begin with a once-daily application to assess tolerance. If no discomfort arises, the frequency may be gradually increased. Conversely, in cases of persistent stinging, redness, or irritation, it is recommended to discontinue use.

Note : A tranexamic acid treatment can be applied locally, directly onto the spots to be lightened (body and/or face), or over the entire face. For detailed usage instructions, please refer to the guidelines provided on the product.

Tranexamic acid can also be used orally. Originally, it was developed as an antifibrinolytic drug, meaning it slows the breakdown of blood clots by inhibiting the activation of plasminogen. This property explains its medical use in the prevention or reduction of certain bleeding (heavy menstrual bleeding, surgery, trauma...). Furthermore, clinical observations have highlighted beneficial effects of oral tranexamic acid on certain forms of hyperpigmentation.

However, this oral use remains medically supervised, since tranexamic acid is a medication in its own right.

Tranexamic acid is therefore sometimes administered orally to target certain types of hyperpigmentation. Clinical studies suggest a significant improvement in the severity of pigmentary spots, often with doses of around 500 mg per day for 8 to 12 weeks, while demonstrating a favorable safety profile and generally mild side effects.

As an example, a descriptive study was conducted on 65 patients with moderate to severe melasma (Fitzpatrick skin phototypes III and IV). Participants received 250 mg of tranexamic acid orally, twice daily, for six months in combination with sunscreen. Efficacy was assessed clinically and by digital photography throughout follow-up, which was extended for six months after treatment completion to observe potential recurrences. Of good results were obtained and no serious systemic adverse events were reported. Only a few patients experienced oligomenorrhea—defined as a menstrual cycle longer than 35 days—or mild gastrointestinal disturbances. Overall patient satisfaction was high.

In practice, oral tranexamic acid is sometimes combined with topically applied tranexamic acid to act on hyperpigmentation at multiple levels. Tranexamic acid tablets can also be taken in combination with the topical use of other depigmenting agents, such as alpha-arbutin or hydroquinone. Tranexamic acid thus emerges as a particularly interesting active ingredient for targeting hyperpigmentation, whether it is applied topically to the skin or used orally. Nevertheless, it should be reiterated that the latter requires prior medical advice due to its status as a medication and its potential systemic effects.

Note : Tranexamic acid has two documented modes of use: topical application and oral administration. This active ingredient is not used on hair, as no benefit has been demonstrated on the scalp or hair fiber.

• NAEINI F. F. & al. Topical tranexamic acid as a promising treatment for melasma. Journal of Research in Medical Sciences (2014).

• NASEEM R. & al. Oral tranexamic acid in treatment of melasma in Pakistani population: a pilot study. Journal of Pakistan Association of Dermatologists (2016).

• WANG X-W. & al. Tranexamic acid for adults with melasma: A systematic review and meta-analysis. BioMed Research International (2018).

• JANNEY M. S. & al. A randomized controlled study comparing the efficacy of topical 5% tranexamic acid solution versus 3% hydroquinone cream in melasma. Journal of Cutaneous and Aesthetic Surgery (2019).

• JAWADE S. & al. Study of oral tranexamic acid, topical tranexamic acid, and modified Kligman's regimen in treatment of melasma. Journal of Cosmetic Dermatology (2020).