Tranexamic Acid in the Treatment of Postsclerotherapy Hyperpigmentation

Abstract

Tranexamic acid (TA) is a well-known antifibrinolytic drug used in several medical fields. In Dermatology, it has been proposed as an off-label indication in acquired hyperpigmentation, especially for the treatment of melasma, a condition that shares similar histologic features with postsclerotherapy hyperpigmentation (PSH). TA has antiangiogenic effects that reduce the expression of vascular endothelial growth factor (VEGF), endothelin-1, and antimelanogenic effects by inhibiting the tyrosine kinase receptor. Sclerotherapy is a common treatment for chronic venous insufficiency that obliterates the vessels by a chemical endothelial reaction. One of its adverse effects is hyperpigmentation due to an accumulation of hemosiderin in the superficial dermis following erythrocyte extravasation; however, both, melasma and PSH patients, express an elevated number of melanocytes and blood vessels in the affected areas. Since there is a lack of studies in this field, we present a systematic review of TA usefulness in acquired hyperpigmentation. We conducted a systematic review of studies published between 1962 and 2020, available in the databases Pubmed, Web of Science, Scopus, and Google Scholar after searching the following MeSH terms: "tranexamic acid" and "sclerotherapy" or "hyperpigmentation" or "melasma." After extensive review 12 studies met eligibility criteria and were included. Despite no studies having been conducted assessing the role or effectiveness of TA in PSH, we found 12 articles about the use of TA in melasma, which is also an acquired pigmentary disorder with several histologic similarities with PSH. According to these studies, patients treated with TA 250 mg by mouth two times per day for 4 months reached a 90% rate of improvement, with a 27.2% rate of recurrence. Treated patients also expressed histologic resolution of the pigmentations, given by a reduced number of vessels, mast cell counts, and epidermal pigmentation. In vitro results exhibit effects on the neutralization of VEGF-1 and VEGF-2 and inhibiting tyrosinase activity, melanin production, and melanogenic proteins. TA has been proved to be effective in the treatment of melasma, due to its antiangiogenic and antimelanocytic properties. Therefore, we believe that TA might also be effective for treating PSH. We propose this agent as a valuable tool in vascular surgery due to its antiangiogenic and antimelanogenic properties. This study is the first step for the assessment of the clinical effectiveness of TA in PSH. It is also necessary to investigate if it could also help to remove hemosiderin residues from the epidermis in PSH.