Melasma is a common and acquired skin disorder with pigmentation that predominantly affects women with darker skin types. Melasma presents with bilateral, irregularly shaped, dark brown spots and usually appears on the cheeks, forehead, nose, or upper lip of the face. The etiology of melasma is complicated; Multiple factors may be involved, such as genetics, UV exposure, pregnancy, and the use of contraceptives. Treatment of melasma has been difficult due to its unclear etiology, stubbornly refractory nature and frequent relapses. Also, post-treatment hyperpigmentation and long-term treatment make it more difficult. At present, melasma therapies can generally be divided into two categories: chemical-dependent and energy-dependent therapies. These latest therapies include intense pulsed light, Q-switched lasers, picosecond lasers and fractional lasers, to name the most used.
The chemical interventions are local applications based on hydroquinone, triple combined cream, based on azelaic acid, protective cream from visible and UV light, derivatives of vitamin A such as tretinoin, chemical peels, plasma rich in platelets and ultrasounds. Chemical peel is the recommended second-line treatment for melasma and can accelerate epidermal renewal and collagen regeneration to remove epidermal melanin and suspend melanosome transfer. A systematic review and meta-analysis showed that glycolic acid peel had no obvious advantage over tretinoin. In 2018, the use of tranexamic acid was introduced in an attempt to add options other than the current ones which, on their own, all have limited effectiveness. The review of the most recent scientific literature, in fact, has confirmed that single treatments are either ineffective or their duration is almost always followed by relapses.
Tranexamic acid has shown superior effects on melasma over the past few years. Even in the very popular TV program “Dr. Pimplepopper”, Dr. Lee had some patients with melasma, explaining the past options, their limits and introducing tranexamic acid as last resort. This drug, branded as Tranex into clinical practice to clot blood (fibrinolysis), in melasma targets melanocytes, endothelial cells, mast cells and keratinocytes to remove pigmentation. It was initially not clear what his target was in this context. In fact, in the case of blood coagulation, it blocks the production of plasmin, inhibiting the function of plasminogen activators. As for melasma, however, it seems to target the hormone endothelin-1 and the growth factor TGF-beta. Due to the effects, oral tranexamic acid was recommended as a first-line therapy also in a recent review. Over the past couple of years, interest has grown in studying its effects in various formulations for melasma.
In a meta-analysis, the oral form demonstrated the greatest improvement over the topical and intradermal formulations. By mouth, in fact, the drug has a bioavailability of 50%, a half-life of 2 hours and is not metabolized by the liver except for 5-10%. Furthermore, it seems to be preferred over tretinoin and hydroquinone due to a lower toxicity than the latter. Several dozen clinical trials have already been published on its single effects and in combination with steroids, vitamin C, hydroquinone and laser therapy. Everyone agrees on its superiority and synergy with other treatments. But how long does it take to see results? Field experiences indicate that it takes 8 to 12 weeks, and there are no equal timings for everyone. Furthermore, the recruitment cannot be indefinite; periods of “detachment” and new evaluation by the dermatologist are needed. That is why more studies are needed to determine its long-term safety and efficacy.
Finally, despite its safety at doses of 250-500mg per day, its use must be under strict medical supervision for patients who have contemporary medical problems such as thrombophilia, severe heart disease, renal insufficiency and tendency to venous thrombosis starting from the lower limbs. from varicose veins.
- Edited by Dr. Gianfrancesco Cormaci, PhD, specialist in Clinical Biochemistry.
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Dott. Gianfrancesco Cormaci
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