By addressing the vascular component of melasma, off-label use of oral tranexamic acid has been a beneficial adjunct for this difficult-to-treat condition. For on-label use treating menorrhagia (the oral form) and short-term prophylaxis of bleeding in hemophilia patients undergoing dental procedures – (the injectable form), tranexamic acid acts as an antifibrinolytic.
Dr. Naissan O. Wesley
By inhibiting plasminogen activation, according to a 2018 review article “tranexamic acid mitigates UV radiation–induced melanogenesis and neovascularization,” both exhibited in the clinical manifestations of melasma.1 In addition to inhibiting fibrinolysis, tranexamic acid has direct effects on UV-induced pigmentation, “via its inhibitory effects on UV light–induced plasminogen activator on keratinocytes and [subsequent] plasmin activity,” the article states. “Plasminogen activator induces tyrosinase activity, resulting in increased melanin synthesis. The presence of plasmin [which dissolves clots by degrading fibrin] results in increased production of both arachidonic acid and fibroblast growth factor, which stimulate melanogenesis and neovascularization, respectively.”
With oral use, the risk of clot formation, especially in those who have a history of blood clots, clotting disorders (such as factor V Leiden), smoking, or other hypercoagulability risks should be weighed.
Topical tranexamic acid used locally mitigates systemic risk, and according to published studies, has been found to be efficacious for hemostasis in knee and hip arthroplasty surgery and for epistaxis. However, clinical outcomes with the topical treatment have largely not been on par with regards to efficacy for melasma when compared with oral tranexamic acid.
pigmentation is with laser-assisted delivery. Topical tranexamic acid, in my experience, when applied immediately after fractional 1927-nm diode laser treatment, not only has been noted by patients to feel soothing, but anecdotally has been found to improve pigmentation.
Moreover, there are now several peer-reviewed studies showing some benefit for treating pigmentation from photodamage or melasma with laser-assisted delivery of topical tranexamic acid. Treatment of these conditions may also benefit from nonablative 1927-nm laser alone.
In one recently published study, 10 female melasma patients, Fitzpatrick skin types II-IV, underwent five full-face low-energy, low-density (power 4-5 W, fluence 2-8 mJ, 2-8 passes) 1927-nm fractional thulium fiber laser treatment.2 Topical tranexamic acid was applied immediately after laser treatment and continued twice daily for 7 days. Seven patients completed the study. Based on the Global Aesthetics Improvement Scale (GAIS) ratings, all seven patients noted improvement at day 180, at which time six of the patients were considered to have improved from baseline, according to the investigator GAIS ratings. Using the Melasma Area Severity Index (MASI) score, the greatest degree of improvement was seen at day 90; there were three recurrences of melasma with worsening of the MASI score between day 90 and day 180.
In a split-face, double-blind, randomized controlled study, 46 patients with Fitzpatrick skin types III-V, with recalcitrant melasma received four weekly treatments of full-face fractional 1927-nm thulium laser; topical tranexamic acid was applied to one side of the face and normal saline applied to the other side under occlusion, immediately after treatment.3 At 3 months, significant improvements from baseline were seen with Melanin Index (MI) and modified MASI (mMASI) scores for the sides treated with tranexamic acid and the control side, with no statistically significant differences between the two. However, at month 6, among the 29 patients available for follow-up, significant differences in MI and mMASI scores from baseline were still evident, with the exception of MI scores on the control sides.
No adverse events from using topical tranexamic acid with laser were noted in either study. Split-face randomized control studies with use of topical tranexamic acid after fractional 1927-nm diode laser in comparison to fractional 1927-nm thulium laser would be notable in this vascular and heat-sensitive condition as well.
Dr. Wesley and Dr. Talakoub are cocontributors to this column. Dr. Wesley practices dermatology in Beverly Hills, Calif. Dr. Talakoub is in private practice in McLean, Va. This month’s column is by Dr. Wesley. Write to them at dermnews@mdedge.com. They had no relevant disclosures.
References
1. Sheu SL. Cutis. 2018 Feb;101(2):E7-E8.
2. Wang, JV et al. J Cosmet Dermatol. 2021 Jan;20(1):105-9.
3. Wanitphakdeedecha R. et al. Lasers Med Sci. 2020 Dec;35(9):2015-21.