From the Guidelines
Tranexamic Acid (TXA) is not the most effective treatment for hyperpigmentation, particularly when compared to other options like PRP, as evidenced by a recent study 1. When considering TXA for hyperpigmentation, it's essential to weigh its benefits against other available treatments. TXA can be used to treat hyperpigmentation, particularly melasma and post-inflammatory hyperpigmentation, in both topical and oral formulations. For topical use, concentrations typically range from 2-5% in serums or creams applied once or twice daily for several months. Oral TXA is sometimes prescribed at doses of 250-500mg twice daily for 8-12 weeks, though this requires medical supervision due to potential side effects. Some key points to consider about TXA for hyperpigmentation include:
- TXA works by inhibiting plasmin activity, which reduces melanocyte tyrosinase activity and melanin production.
- It also decreases vascular endothelial growth factor and mast cell activity, addressing both pigmentary and vascular components of conditions like melasma.
- While generally well-tolerated, topical TXA may cause mild irritation, and oral TXA carries risks including potential blood clots, making it unsuitable for those with clotting disorders or thromboembolic disease history.
- Results typically appear after 8-12 weeks of consistent use, and TXA works best as part of a comprehensive regimen including sun protection. However, a study from 2025 1 suggests that PRP can be a more effective treatment for melasma, with significant improvement in mMASI scores and patient satisfaction. Therefore, based on the most recent evidence, PRP may be a better option for treating hyperpigmentation than TXA alone 1.
From the Research
Tranexamic Acid for Hyperpigmentation
- Tranexamic acid (TXA) has been used off-label in dermatology for the treatment of melasma and other hyperpigmentation disorders 2, 3, 4, 5, 6.
- Studies have shown that oral TXA can be effective in treating hyperpigmentation disorders, including postinflammatory hyperpigmentation, lichen planus pigmentosus, ashy dermatosis, and Riehl melanosis, with a good safety profile 2, 6.
- The dose range of TXA used in these studies varied from 250mg per day to 1500mg per day, and the treatment period ranged from 2 weeks to 6 months 2.
- TXA has been shown to be a promising treatment option for melasma, with efficacy demonstrated in several studies 3, 4, 5.
- The use of TXA for hyperpigmentation disorders other than melasma is still an area of ongoing research, and more evidence from blinded randomized controlled trials and case-control studies is needed to determine its efficacy 2, 6.
Mechanism of Action
- TXA works by inhibiting ultraviolet (UV)-induced plasmin activity in keratinocytes, which contributes to its anti-melanogenesis effects 4.
- TXA also has anti-inflammatory, anti-angiogenic, and skin barrier recovery-promoting effects, making it a potential treatment for various hyperpigmentation and telangiectatic disorders 6.
Administration and Safety
- TXA can be administered orally, topically, through intradermal injections, or via microneedling 6.
- The safety profile of TXA is generally good, with few and mild side effects reported in studies 2, 3, 5.
- However, patients should be screened carefully for contraindications and risk factors prior to commencement of TXA therapy 3.