Expanding Inclusivity: Tranexamic Acid for the Treatment of Melasma in Males

April 2024 | Volume 23 | Issue 4 | e110 | Copyright © April 2024


Published online March 20, 2024

Nicole E. Chin BAa,b, Andrea Hui Austin MDb

aLoyola Stritch School of Medicine, Maywood, IL 
bBay Area Cosmetic Dermatology, San Francisco, CA 
 




Case 3: 
This 56-year-old gentleman had a combination of severe melasma superimposed with sun damage. He began a regimen of oral tranexamic acid 650 mg daily, along with topical retinol 1% (AlphaRet by SkinBetter Science, Phoenix, AZ) every evening along with physical sunblock daily. He received two chemical peels (Vitalize peel by Allergan, Irvine, CA) and two treatments of Q-switched Alexandrite laser (Alex Trivantage by Candela, Marlborough, MA) with near-complete resolution. He has maintained his results with the same oral and topical regimen as of publication. 
 

DISCUSSION

Melasma is a common, acquired skin condition that can be caused by a multitude of factors including genetics, radiation, hormones, cosmetics, and phototoxic drug usage.6 TXA can be administered for all severities of melasma. The exact mechanism for how TXA reduces melanogenesis is not yet fully understood. What we believe is a probable explanation for its effectiveness is TXA's ability to inhibit the activity of plasmin. Plasmin can stimulate melanocytes, the cells that are responsible for producing melanin. By inhibiting plasmin, TXA can reduce the stimulation of melanocytes thus decreasing melanin synthesis.7 TXA may also be involved with the interference of melanin synthesis. TXA is structurally similar to tyrosinase, an enzyme that plays a crucial role in melanin production and may work by competitively antagonizing its function.3 Additionally, it has been found that TXA has anti-inflammatory properties and can modulate the inflammatory response by influencing cytokine levels.8 Normally, chronic inflammation can trigger melanogenesis and contribute to hyperpigmentation. Thereby, with the reduction of this inflammation, TXA can indirectly inhibit melanin production. While more research is needed to fully understand the exact mechanisms behind TXA's dermatologic effectiveness, TXA has brought great success in the many melasma patients we have seen.

There are a few studies in the current literature that support the use of TXA in treating melasma, although currently, there are no studies that only focus on men. Even so, when studies do include a male population, few males make up a portion of the sample size. In one of the largest studies of oral TXA, 561 patients were enrolled, while only 8.6% of those patients were male. The majority of patients found an improvement in their melasma symptoms.9 A randomized controlled trial of 96 patients compared the effect of TXA on intraoperative blood loss (IOB) based on gender. Interestingly, it was found that there was an effect in women, but none in men. However, the paper noted that future studies should include larger sample sizes of men.10 All in all, within current literature, it is clear that there is no consensus when it comes to TXA and men.

TXA is effective at treating melasma. One randomized controlled trial compared 20 patients taking 250 mg TXA twice a day and 17 patients receiving the placebo for 12 weeks. They found that melasma improved in 50% of the patients in the experimental group versus only 5.9% in the placebo group.11 Another trial compared a group of 18 taking the same dosage as the previous study, with 21 patients taking the placebo. Only the group taking TXA saw significant improvement.12  

TXA also has a well-established safety profile. Previous studies have reported adverse side effects associated with TXA, however, we must note that these negative side effects occurred at significantly higher doses than what our findings suggest as effective for treating