Tranexamic acid (TA) is a synthetic analog of the amino acid lysine with a long history of medical use to stop bleeding. Its mechanism of action is based on the inhibition of fibrinolysis, which also affects the vascular changes and inflammation associated with rosacea. It has been relatively recently established that TA can directly affect keratinocytes and, through them, indirectly affect other skin cells, triggering processes leading to [1]:

• Restoration of skin barrier function
• Reduction of inflammation
• Suppression of angiogenesis (formation of new blood vessels)

These properties make TA particularly promising for treating the erythematous-teleangiectatic form of rosacea, characterized by severe redness and dilated blood vessels.

What is the best way to apply tranexamic acid for rosacea?

There are several ways to use TA for rosacea:

1. Topical application: application of preparations with TK to the skin. TK is a water-soluble substance, so the topical preparation should contain an aqueous phase, i.e., an aqueous solution or emulsion (cream). TA has a small molecular weight, so it can be expected to pass through the stratum corneum [2]. However, the base of the preparation with TA strongly affects the diffusion of TA across the lipid barrier, so topical agents will differ in their efficacy even if the concentration of TA in them is the same.
2. Oral administration: a study by Kwon et al. (2016) investigated using 250 mg of TA per day in combination with propranolol and minocycline. This combination reduced the patient's rosacea symptoms, including erythema and subjective discomfort, without side effects for two months [3].
3. Injections: intradermal injections of 5% TA solution were used in six patients in a study by Daadaa et al. (2021). After 3-6 months of therapy, a significant reduction in the severity of rosacea symptoms was observed with minimal side effects (mild redness and swelling) [4].
4. Microneedling: Bageorgou et al. (2018) compared the effect of 10% TA solution alone with the impact of a combination of 10% TA solution and microneedling for treating rosacea. In their study, ten patients treated erythematous-teleangiectatic rosacea with a moist dressing moistened with 10% TA solution applied to the affected area for 15 days over four sessions; another 10 patients were treated with a combination of microneedling and moist dressing. The results showed significant improvement in the severity of clinical manifestations and quality of life in both groups, but the improvement of erythema was more pronounced in the microneedling group [5].

The critical advantage of TA is the low rate of side effects. Only in rare cases were temporary redness and swelling after injections observed. At the same time, topical and oral administration caused almost no complications [1].

Conclusion

Tranexamic acid has proven to be a promising tool for treating rosacea, especially in cases with pronounced vascular changes. The drug combines efficacy and safety, making it a valuable adjunct to standard therapy.

Despite encouraging study results and numerous clinical observations, more research is needed to incorporate TA preparations into rosacea treatment protocols. The key challenges are:

• Determining optimal dosages and methods of administration
• Developing treatment standards for different forms of rosacea
• Conducting large-scale clinical trials

References

1. Zhang J., Gu D., Yan Y. et al. Potential role of tranexamic acid in rosacea treatment: conquering flushing beyond melasma. Clin Cosmet Investig Dermatol. 2024; 17: 1405–1412.
2. Kim M.S., Chang S.E., Haw S. et al. Tranexamic acid solution soaking is an excellent approach for rosacea patients: a preliminary observation in six patients. J Dermatol. 2013; 40(1): 70–71.
3. Kwon H.J,. Suh J.H., Ko E.J., Kim B.J. Combination treatment of propranolol, minocycline, and tranexamic acid for effective control of rosacea. Dermatol Ther. 2017; 30(3).
4. Daadaa N., Litaiem N., Karray M., Bacha T. Intradermal tranexamic acid microinjections: a novel treatment option for erythematotelangiectatic rosacea. J Cosmet Dermatol. 2021; 20(10): 3324–3329.
5. Bageorgou F., Vasalou V., Tzanetakou V., Kontochristopoulos G. The new therapeutic choice of tranexamic acid solution in treatment of erythematotelangiectatic rosacea. J Cosmet Dermatol. 2019; 18(2): 563–567.