For my melasma, should I take tranexamic acid 250 mg twice daily or three times daily, does it affect sleep, and should it be taken with food?

Tranexamic Acid Dosing for Melasma

For melasma treatment, take tranexamic acid 250 mg three times daily (total 750 mg/day) for optimal efficacy, though 250 mg twice daily is an acceptable alternative if adherence is a concern. 1

Dosing Recommendations

Optimal Regimen

• The highest quality evidence demonstrates that 750 mg per day (250 mg three times daily) for 12 consecutive weeks provides superior efficacy compared to lower doses. 1
• This dosing achieved the best balance between therapeutic effect and safety in network meta-analysis of randomized controlled trials. 1

Alternative Dosing for Poor Adherence

• 250 mg twice daily (total 500 mg/day) is an acceptable alternative if you anticipate difficulty taking three daily doses. 2, 3, 1
• This regimen showed a 49% reduction in melasma severity scores at 3 months in placebo-controlled trials. 3
• The twice-daily regimen demonstrated statistically significant improvement starting at 8 weeks and sustained through 12 weeks. 2

Lower Dose Considerations

• 250 mg once daily showed delayed onset of improvement (not significant until 8 weeks) compared to higher doses, though it eventually achieved comparable efficacy by 16 weeks. 4
• The once-daily regimen had a lower relapse rate (4.7%) compared to twice-daily dosing (10.8%) at 28 weeks follow-up, suggesting potential benefit for maintenance. 4

Food Intake Considerations

No specific guidance exists in the dermatology literature regarding food intake with tranexamic acid for melasma. The studies reviewed did not specify whether to take tranexamic acid with or without food. 5, 2, 3, 1, 4

Given that tranexamic acid is well-absorbed orally and the melasma studies did not mandate specific timing relative to meals, you may take it with or without food based on personal preference and gastrointestinal tolerance.

Sleep Impact

Tranexamic acid does not have documented effects on sleep patterns. 5, 2, 3, 1, 4

The side effect profile in melasma trials included mild gastrointestinal symptoms and rare menstrual irregularities, but sleep disturbances were not reported. 5, 3, 4

Treatment Duration and Monitoring

• Continue treatment for 12 weeks for optimal results, with evaluation at 4-week intervals. 2, 1
• Patients with severe melasma show greater improvement than those with moderate disease. 3
• Sustained improvement persists for at least 3 months after discontinuation, though some relapse may occur. 3, 4

Safety Considerations

Screening Before Starting

• You must be screened for contraindications including history of thrombosis, atrial fibrillation, known thrombophilia, or current use of oral contraceptives. 6, 7
• Renal function should be assessed, as tranexamic acid is renally excreted. 7

Side Effect Profile

• Tranexamic acid is safe for melasma treatment with minimal side effects, primarily mild gastrointestinal discomfort and occasional oligomenorrhea. 5, 3, 4
• Large studies demonstrate no increased thromboembolic risk at doses used for melasma (500-750 mg/day). 5
• Side effects rarely necessitate treatment discontinuation. 4

Clinical Algorithm

1. Start with 250 mg three times daily (750 mg total) if you can maintain adherence to three daily doses. 1
2. If adherence is challenging, use 250 mg twice daily (500 mg total) as an effective alternative. 2, 3, 1
3. Take consistently for 12 weeks before assessing full response. 2, 1
4. Combine with daily sunscreen for optimal results. 3
5. Expect initial improvement around 8 weeks, with maximal benefit at 12 weeks. 2, 1

Common Pitfalls to Avoid

• Do not discontinue prematurely before 8 weeks, as significant improvement may not be apparent until this timepoint. 2, 4
• Do not use tranexamic acid if you have contraindications to antifibrinolytic therapy, particularly recent thrombosis or concurrent oral contraceptive use. 6, 7
• Do not expect immediate results; this is a gradual treatment requiring patience and consistent adherence. 2, 1