HomeENGLISH MAGAZINEMelasma management: tranexamic acid to overtake expectances in the treatments' midst

Melasma management: tranexamic acid to overtake expectances in the treatments’ midst

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.

Scientific references

Foss M et al. J Drugs Dermatol. 2022 Apr; 21(4):393-398. 

Perveen S et al. J Drugs Dermatol. 2022; 21(3):321-322. 

Neagu N, Conforti C et al. J Dermatol Treat 2021; 14:1–39.

Spierings NMK. J Cosmet Dermatol. 2020; 19:1284–1289.

Wang JV et al. J Clin Aesthet Dermatol. 2019; 12:E73–74.

Kwon SH, Na JI et al. Exper Dermatol. 2019; 28:704–708.

Saki N, Darayesh M et al. J Dermatol Treatm 2018; 29:405.

Kim SJ, Park JY et al. Clin Exp Dermatol. 2016; 41:480-85.

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Dott. Gianfrancesco Cormaci

Medico Chirurgo, Specialista; PhD. a CoFood s.r.l.
- Laurea in Medicina e Chirurgia nel 1998 (MD Degree in 1998) - Specialista in Biochimica Clinica nel 2002 (Clinical Biochemistry residency in 2002) - Dottorato in Neurobiologia nel 2006 (Neurobiology PhD in 2006) - Ha soggiornato negli Stati Uniti, Baltimora (MD) come ricercatore alle dipendenze del National Institute on Drug Abuse (NIDA/NIH) e poi alla Johns Hopkins University, dal 2004 al 2008. - Dal 2009 si occupa di Medicina personalizzata. - Guardia medica presso strutture private dal 2010 - Detentore di due brevetti sulla preparazione di prodotti gluten-free a partire da regolare farina di frumento immunologicamente neutralizzata (owner of patents concerning the production of bakery gluten-free products, starting from regular wheat flour). - Responsabile del reparto Ricerca e Sviluppo per la società CoFood s.r.l. (leader of the R&D for the partnership CoFood s.r.l.) - Autore di un libro riguardante la salute e l'alimentazione, con approfondimenti su come questa condizioni tutti i sistemi corporei. - Autore di articoli su informazione medica e salute sui siti web salutesicilia.com, medicomunicare.it e in lingua inglese sul sito www.medicomunicare.com
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