How should tranexamic acid be used?

Tranexamic acid is a synthetic derivative of lysine, originally employed in medicine for its antifibrinolytic properties, before being evaluated in dermatology for its effects on skin pigmentation. When applied topically, it chiefly 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 the stimulation of melanocytes, thereby reducing melanin overproduction. Tranexamic acid thus emerges as an interesting active ingredient for preventing and alleviating hyperpigmentation.

How should tranexamic acid be applied topically?

To achieve visible effects on pigmentation spots, tranexamic acid must be formulated at a concentration between 2 and 5%. Increasing this percentage does not improve its efficacy and primarily increases the risk of skin irritation. It is worth noting, however, that tranexamic acid is regarded as a relatively mild active ingredient and is generally well tolerated in topical applications. It can therefore be used up to twice daily, morning and evening, as it is not photosensitising. In sensitive or compromised skin, however, it is preferable to begin with a once-daily application to assess cutaneous tolerance. If no discomfort arises, the frequency may be increased gradually. Conversely, in case of persistent stinging, redness or irritation, discontinuing the treatment is advised.

Note : A tranexamic acid treatment can be applied topically, directly onto the spots you wish to fade (body and/or face) or across the entire face. For directions for use, please refer to the instructions provided on the product.

Tranexamic acid can also be administered orally. Originally, it is an antifibrinolytic agent, that is to say it inhibits the breakdown of blood clots by preventing plasminogen activation. This property explains its medical use in the prevention or reduction of certain bleeding (heavy menstrual bleeding, surgery, trauma, etc.). Moreover, clinical observations have revealed beneficial effects of oral tranexamic acid on certain forms of hyperpigmentation.

However, this oral administration remains under medical supervision, since tranexamic acid is a medication in its own right.

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

By way of 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 conjunction with sunscreen. Efficacy was assessed clinically and via digital photography throughout the follow-up period, which was extended by six months post-treatment to monitor for any recurrence. Good results were achieved and no serious systemic adverse effects were reported. Only a few patients experienced oligomenorrhoea, defined as a menstrual cycle exceeding 35 days, or mild gastrointestinal disturbances. Patient satisfaction was generally high.

In practice, oral tranexamic acid is sometimes combined with topical tranexamic acid to address hyperpigmentation on multiple levels. Tranexamic acid tablets can also be taken alongside the topical application of other depigmenting actives, such as alpha-arbutin or hydroquinone. Tranexamic acid thus emerges as a particularly promising active ingredient for targeting hyperpigmentation, whether applied locally to the skin or administered orally. Nevertheless, it should be reiterated that the latter requires prior medical advice, due to its status as a medicinal product 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 fibre.

• 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).