Oral Tranexamic Acid effective and well tolerated treatment for melasma

Oral Tranexamic Acid for the Treatment of Melasma- IJD consensus guidelines

Melasma, a chronic, acquired pigmentary disorder due to dysfunction in melanogenesis affecting exposed body parts, mainly the face. It is associated with significant psychological disturbance and impaired quality of life. Although several treatment options are available they do not show promising results in many patients.

Tranexamic acid (TCA), an anti‑fibrinolytic agent, inhibits plasminogen activator pathway in skin, prevents melanocytes activation due to ultraviolet (UV) light, hormones, and injured keratinocyte. Reduction in the activity of melanocyte tyrosinase by reducing prostaglandins and decreased angiogenesis in dermal blood vessels by inhibition of vascular endothelium growth factor are other proposed mechanisms of TXA in melasma. Oral, topical, as well intradermal formulations have been evaluated for its efficacy and safety in patients with melasma. Currently, there is no consensus or published guideline for use of TXA in melasma. Recently a experience‑based consensus of Indian experts on currently available evidence was published in the Indian Journal of Dermatology.

A total of 25 clinical studies published from 2012 to 2022 involving more than 2000 patients were retrieved. Large number of clinical studies with different designs and from several countries have evaluated effects of oral TXA in melasma. Most of the studies retrieved were prospective and only three studies were retrospective in design. A study evaluating TXA doses from 500‑1500 mg have showed no significant difference in efficacy. Usual doses of TXA in studies range from 250 mg twice daily or thrice daily. TXA has been used alone as well as an adjuvant therapy in melasma. It has been shown to be effective in moderate to severe melasma. Duration of therapy ranges from 4 weeks to about 6 months. Clinical studies have showed clinical and histological improvements in patients with melasma. Reduction of dermal blood flow in melasma affected areas has also been demonstrated. Recurrence has been reported after discontinuation of therapy. Adverse event profile is not of concern. Gastrointestinal adverse events and hypomenorrhea are seen in few patients. Oral TXA should be stopped if patients receiving develops visual or ocular symptoms or severe allergic reaction.

Expert consensus statements for use of oral TXA in melasma

 Considering the mechanism of action, TXA has an important role in melasma treatment.

 Prospective and retrospective studies from different countries have documented the effectiveness of oral TXA in melasma

 TXA is not approved for the treatment of melasma. Clinicians should inform this to the patient, obtain full history to rule out complications, provide full information and document same in the case notes.

 Overall, oral TXA 250 mg twice daily seems to be promising treatment option for melasma especially in refractory cases.

 Oral TX can be used as monotherapy or along with other modalities.

 Minimum of three-month treatment with oral TXA is required for the results. Although optimal duration of treatment is unknown, tranexamic acid may be given for up to six months.

 Patients with history hypersensitivity to TXA should not receive this treatment

 Females on combination hormonal contraception should not be treated with oral TXA.

 Presence of active thromboembolic condition or history/ risk of thrombosis or thromboembolism should be excluded before initiation of treatment with oral TXA,

 According to experts, in case of relapse, TXA may be repeated. However, for the duration of the gap, there is no specific recommendation.

In conclusion oral TXA is an effective and well tolerated treatment for melasma and other adjuvant therapies and sun protection should be advised along with TXA so as to prevent the recurrence of melasma.

Source- Godse K, Sarkar R, Mysore V, Shenoy MM, Chatterjee M, Damisetty R, et al. Oral tranexamic acid for the treatment of melasma: Evidence and experience‑based consensus statement from Indian experts. Indian J Dermatol 2023;68:178‑85.