Oral Tranexamic Acid Guidelines for Melasma in Adult Women
Recommended Dosage and Treatment Protocol
Oral tranexamic acid should be prescribed at 250 mg twice daily (total 500 mg/day) for 12-16 weeks as adjunctive therapy to topical treatments and strict sun protection, with consideration for combination with intradermal PRP injections for enhanced efficacy. 1, 2
Optimal Dosing Strategy
The evidence supports a tiered approach to oral tranexamic acid dosing:
- Start with 250 mg twice daily (500 mg total daily dose) as this represents the optimal balance between efficacy, safety, and long-term tolerability 3, 4
- The network meta-analysis identified 750 mg per day (250 mg three times daily) for 12 weeks as the optimal dose, though 250 mg twice daily remains acceptable for patients with adherence concerns 3
- Treatment duration should be minimum 12-16 weeks to achieve meaningful improvement, as MASI score reductions become statistically significant only after 8 weeks with lower doses 4
- Higher doses (1000-1500 mg/day) show dose-dependent efficacy but are not necessary for most patients and may increase side effects 5
Position in Treatment Algorithm
Oral tranexamic acid functions as adjunctive therapy, not first-line monotherapy:
- First-line treatment remains triple combination cream (hydroquinone 4%, tretinoin 0.05%, fluocinolone acetonide 0.01%) plus strict sun protection (SPF 50+ reapplied every 2-3 hours) 1, 2
- Add oral tranexamic acid 250 mg twice daily if inadequate response after 8-12 weeks of topical therapy 1, 6
- For moderate-to-severe melasma, combine oral tranexamic acid with intradermal PRP injections (4 sessions every 2-3 weeks), which achieves 90.48% total efficacy versus 73.68% with tranexamic acid alone 7, 1, 2
Safety Screening and Contraindications
Before prescribing, screen for absolute and relative contraindications:
- Absolute contraindications: Recent thrombosis (within 6 months), active thromboembolic disease 7
- Relative contraindications: Atrial fibrillation, known thrombophilia, history of venous thromboembolism 7
- Monitor for side effects: Oligomenorrhea, decreased menstruation, mild gastrointestinal upset (stomach discomfort) 5, 4
- Reassuring safety data: Studies demonstrate tranexamic acid does not increase thromboembolic risk in appropriately screened patients 8
Measuring Treatment Success
- Use modified MASI (mMASI) scores to objectively track improvement at baseline, 4 weeks, 8 weeks, and end of treatment 1, 2, 5
- Response grading: >90% MASI reduction = excellent; 60-90% = moderate improvement; 20-60% = mild improvement 7, 1
- Expect gradual improvement: Significant MASI reduction typically occurs after 8 weeks, with continued improvement through 12-16 weeks 4
- Patient satisfaction should complement objective measurements, as subjective improvement often correlates with adherence 7, 2
Maintenance and Long-Term Management
Melasma is a chronic relapsing condition requiring ongoing management:
- Continue strict sun protection indefinitely: SPF 50+ broad-spectrum sunscreen reapplied every 2-3 hours, wide-brimmed hats (>3-inch brim), UV-protective clothing, shade-seeking during peak hours (10 AM-4 PM) 1, 2
- Lower relapse rates with combination therapy: PRP plus oral tranexamic acid shows reduced recurrence at 3 and 6 months compared to tranexamic acid alone 7, 1
- Consider maintenance PRP treatments every 6 months after initial treatment course 1, 2, 6
- Lower doses (250 mg once daily) may have lower relapse rates (4.7%) compared to higher doses (10.8% with 500 mg twice daily), though this requires further validation 4
Critical Pitfalls to Avoid
- Do not use oral tranexamic acid as monotherapy—it must be combined with topical treatments and sun protection for optimal results 1, 8
- Do not discontinue treatment prematurely—minimum 12 weeks required for meaningful improvement 3, 4
- Do not forget to reapply sunscreen after swimming, sweating, or every 2-3 hours during continuous outdoor exposure 1, 2
- Do not overlook hormonal triggers—counsel patients about oral contraceptives, pregnancy, and hormone replacement therapy that may limit treatment success 1
- Do not ignore lifestyle factors—advise smoking cessation as smoking worsens melasma 1, 2
Enhanced Efficacy Strategy
For patients requiring maximum efficacy:
- Combine oral tranexamic acid 250 mg twice daily with intradermal PRP injections administered monthly for 3-5 sessions, spaced 2-3 weeks apart 7, 1, 2, 6
- This combination maintains normal VEGF and α-MSH levels while reducing disease recurrence 7, 2
- PRP demonstrates superior efficacy compared to intradermal tranexamic acid injections with similar safety profiles 2, 6
- Follow-up evaluation one month after the last PRP treatment 1, 6