Tranexamic Acid for Hyperpigmentation Disorders: A Literature Review on Efficacy and Safety in Melasma and PIH

Hyperpigmentation disorders, including melasma and post-inflammatory hyperpigmentation (PIH), are common dermatologic conditions associated with significant cosmetic and psychological burden. Tranexamic acid (TXA), an antifibrinolytic agent, has gained increasing attention due to its anti-inflammatory and antimelanogenic properties.

To review the current evidence on the efficacy and safety of tranexamic acid in the management of hyperpigmentation disorders, particularly melasma and PIH.

A narrative literature review was conducted using PubMed, Scopus, and Google Scholar to identify clinical and observational studies evaluating the efficacy, safety, and comparative outcomes of oral, topical, and intradermal tranexamic acid in hyperpigmentation disorders. Data were descriptively analyzed with comparison to standard treatments such as hydroquinone and laser therapies.

Evidence from randomized and comparative studies demonstrates that oral, topical, and intradermal TXA significantly reduce pigmentation indices and improve quality-of-life scores in patients with melasma and PIH. Oral TXA at doses of 250-500 mg twice daily showed sustained clinical improvement with minimal adverse effects, most commonly mild gastrointestinal symptoms and menstrual irregularities. Topical and intradermal formulations demonstrated comparable or superior efficacy to hydroquinone with fewer irritant reactions. Combination therapies (e.g., TXA with hydroquinone or laser) yielded enhanced and longer-lasting outcomes.

Tranexamic acid represents a promising and well-tolerated therapeutic option for hyperpigmentation disorders. Its efficacy across multiple administration routes, favorable safety profile, and synergistic potential with existing therapies support its expanding role as both a primary and adjunctive treatment in dermatologic pigment management.