Tranexamic Acid Dosing for Melasma
For adult patients with melasma, oral tranexamic acid should be prescribed at 250 mg twice daily for 12-16 weeks as adjunctive therapy to topical treatments and strict sun protection. 1
Optimal Dosing Regimen
The standard dose is 250 mg orally twice daily for 12-16 weeks, which represents the most practical balance between efficacy and adherence. 1
Network meta-analysis data suggests that 750 mg per day (250 mg three times daily) for 12 weeks may be optimal for maximum efficacy, but 250 mg twice daily remains an acceptable alternative for patients with adherence concerns. 2
Lower doses (500 mg daily total) have demonstrated efficacy in Asian populations over 8-12 weeks, though twice-daily dosing appears more consistently effective across studies. 3
Treatment Algorithm and Positioning
First-line therapy should consist of triple combination cream plus strict sun protection (SPF 50+ broad-spectrum sunscreen). 1
Add oral tranexamic acid 250 mg twice daily only if inadequate response occurs after 8-12 weeks of topical therapy alone. 1
For moderate-to-severe melasma requiring maximum efficacy, combine oral tranexamic acid with intradermal PRP injections administered monthly for 3-5 sessions, spaced 2-3 weeks apart, which achieves 90.48% total efficacy versus 73.68% with tranexamic acid alone. 1
Monitoring Treatment Response
Use the Melasma Area and Severity Index (MASI) scores at baseline, 4 weeks, 8 weeks, and end of treatment to objectively track improvement. 1
Response grading: >90% MASI reduction = excellent; 60-90% = moderate improvement; 20-60% = mild improvement. 1
Clinical studies show approximately 50% of patients achieve meaningful improvement with oral tranexamic acid compared to 5.9% with placebo when evaluated by multiple methods including MASI, colorimetry, and quality of life measures. 4
Safety Screening Requirements
Absolute contraindications include recent thrombosis and active thromboembolic disease. 1
Relative contraindications include atrial fibrillation, known thrombophilia, and history of venous thromboembolism. 1
Despite theoretical thrombotic concerns, studies demonstrate that tranexamic acid does not increase thromboembolic risk in appropriately screened patients, though careful pre-treatment evaluation remains essential. 3
Common side effects are mild and include gastrointestinal upset, menstrual irregularities (both hypo- and hypermenorrhea), headaches, and malaise, with most patients able to continue therapy. 5
Maintenance Strategy
Continue strict sun protection indefinitely with SPF 50+ broad-spectrum sunscreen reapplied every 2-3 hours, wide-brimmed hats, UV-protective clothing, and shade-seeking during peak hours. 1
Consider maintenance PRP treatments every 6 months after the initial treatment course for sustained results. 1
Common Pitfalls to Avoid
Do not use tranexamic acid as monotherapy—it must be combined with topical treatments and rigorous sun protection for optimal results. 1
Oral administration is more effective than topical application alone, particularly for refractory cases, though topical formulations can be combined with other cosmeceuticals. 6
The evidence provided regarding trauma dosing (1 g IV loading dose followed by 1 g over 8 hours) is irrelevant to melasma treatment and should not be confused with the dermatologic indication. 7, 8, 9