What is the preferred treatment approach for melasma and other hyperpigmentation disorders, oral (Tranexamic Acid (TXA)) versus topical Tranexamic Acid (TXA)?

Tranexamic Acid for Melasma and Hyperpigmentation: Oral vs. Topical Administration

Intradermal PRP injections are more effective than intradermal tranexamic acid (TXA) for treating melasma, while oral TXA is more effective than topical TXA for hyperpigmentation disorders. 1

Efficacy Comparison

Oral Tranexamic Acid

• Oral TXA has demonstrated superior efficacy for melasma treatment, especially in refractory cases, with significant improvement in mMASI scores 2, 3
• The optimal dosage is 750 mg daily (250 mg three times daily) for 12 consecutive weeks, though 500 mg daily (250 mg twice daily) may be acceptable for patients with adherence concerns 4
• Oral TXA combined with other therapies shows higher efficacy (90.48%) compared to TXA alone (73.68%) with lower recurrence rates 5

Topical Tranexamic Acid

• Topical TXA alone is less effective than oral administration but better tolerated than hydroquinone 2
• Topical TXA can be combined with other cosmeceuticals or delivery methods (like microneedling) to improve outcomes 2
• Topical TXA is included in first-line treatment approaches along with hydroquinone, tretinoin, and corticosteroids 6

Administration Methods and Protocols

Oral Administration

• Dosage ranges from 250-1500 mg daily, with 750 mg daily for 12 weeks showing optimal results 4
• Treatment duration typically ranges from 8-12 weeks 3, 4
• Regular follow-up is essential as melasma is a chronic condition requiring maintenance therapy 6, 5

Topical and Other Administration Methods

• Intradermal injections and microneedling with topical TXA are effective alternatives to oral treatment 2
• PRP intradermal injections have shown higher efficacy compared to intradermal TXA injections with similar side effect profiles 1
• Four PRP treatment sessions administered every 2-3 weeks with follow-up evaluation one month after the last treatment 5

Safety Considerations

Oral TXA Safety Profile

• Oral TXA is generally safe but may cause gastrointestinal upset and menstrual irregularities in some patients 2, 7
• The pro-thrombotic nature of TXA requires careful patient screening for contraindications and risk factors 3
• Studies have shown that TXA does not significantly increase thromboembolic risk when used appropriately 3

Topical TXA Safety Profile

• Topical TXA has fewer systemic side effects compared to oral administration 2
• Better tolerated than traditional topical treatments like hydroquinone 2

Treatment Algorithm for Hyperpigmentation Disorders

1. Begin with strict sun protection (SPF 50+, reapplication every 2-3 hours) as the foundation of any treatment regimen 6, 5
2. First-line therapy: Topical agents (hydroquinone, tretinoin, corticosteroids, topical TXA) 6
3. If inadequate response after 8-12 weeks:
   • For moderate cases: Consider intradermal TXA injections or PRP (with PRP showing superior results) 1
   • For severe or refractory cases: Consider oral TXA (750 mg daily for 12 weeks) 3, 4
4. Maintenance therapy:
   • Continue sun protection measures 6, 5
   • Consider intermittent use of topical agents 5
   • Maintenance PRP treatments every 6 months for sustained results 5

Common Pitfalls and Caveats

• Discontinuing treatment too early - melasma is a chronic condition requiring ongoing management 5
• Neglecting sun protection - this is essential regardless of which TXA administration route is chosen 6
• Not screening patients for contraindications to oral TXA (history of thromboembolism, coagulation disorders) 3
• Expecting immediate results - significant improvement typically requires 8-12 weeks of consistent treatment 3, 4