What is the role of oral tranexamic acid (TXA) in the treatment of melasma?

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Oral Tranexamic Acid for Melasma Treatment

Oral tranexamic acid (TXA) is an effective second-line treatment option for melasma with a favorable benefit-risk profile, demonstrating 49% reduction in modified Melasma Area and Severity Index (mMASI) scores after 3 months of treatment. 1

Efficacy of Oral TXA

  • Oral TXA provides rapid and sustained improvement in melasma treatment, with statistically significant decreases in MASI scores at 8 and 12 weeks compared to routine topical treatments alone 2
  • Studies show TXA is effective even at low doses (500 mg daily) over short periods (8-12 weeks), particularly in patients with moderate-to-severe melasma 3
  • Patients with severe melasma show greater improvement with oral TXA than those with moderate melasma 1
  • Treatment effects may persist for up to 3 months after discontinuation, with a 26% reduction in mMASI scores compared to baseline 1

Recommended Dosing Protocol

  • The typical dosage ranges from 250 mg twice daily to 650 mg twice daily 4, 3
  • Treatment duration is generally 3 months, with follow-up evaluation one month after the last treatment 2, 1
  • Maintenance treatments may be required as melasma is a chronic condition with high recurrence rates 5

Combination Therapy Approaches

  • PRP combined with oral TXA demonstrates higher efficacy (90.48%) compared to TXA alone (73.68%) with lower recurrence rates 5
  • TXA should be used alongside strict sun protection measures, which form the foundation of any melasma treatment regimen 6, 5
  • Sun protection should include broad-spectrum sunscreen (SPF 30 or higher, preferably SPF 50+) reapplied every 2-3 hours during outdoor exposure 5

Safety Profile

  • Oral TXA has a good safety profile with minimal side effects, making it suitable for long-term management of melasma 4, 1
  • Common side effects include headaches, gastrointestinal upset, malaise, nausea, and menstrual irregularities 4
  • Side effects are typically mild and resolve upon discontinuation of the medication 4
  • Patients should be screened for contraindications and risk factors prior to starting therapy 3

Treatment Algorithm

  • Begin with strict sun protection and first-line topical therapy (tretinoin, hydroquinone, corticosteroids) 6, 5
  • If inadequate response after 8-12 weeks, consider adding oral TXA at 250 mg twice daily for 3 months 5, 2
  • For maintenance, continue sun protection, consider intermittent use of topical agents, and evaluate the need for additional TXA courses 5
  • Consider PRP injections as an alternative or adjunct to oral TXA for enhanced efficacy 7, 5

Important Considerations

  • Oral TXA should be considered in cases unresponsive to topical hydroquinone and combination topical therapy over approximately 12 weeks 3
  • Additional sun protection measures should include wearing wide-brimmed hats, seeking shade during peak UV hours, and using UV-protective clothing 5
  • Patients should be counseled that melasma is a chronic condition requiring ongoing management 6, 5
  • Regular follow-up is essential to monitor treatment response and adjust therapy as needed 6

References

Research

Oral tranexamic acid for the treatment of melasma.

Kathmandu University medical journal (KUMJ), 2012

Research

Oral Tranexamic Acid for the Treatment of Melasma: A Review.

Dermatologic surgery : official publication for American Society for Dermatologic Surgery [et al.], 2018

Guideline

Treatment Options for Melasma

Praxis Medical Insights: Practical Summaries of Clinical Guidelines, 2025

Guideline

Melasma Treatment Guidelines

Praxis Medical Insights: Practical Summaries of Clinical Guidelines, 2025

Guideline

Guideline Directed Topic Overview

Dr.Oracle Medical Advisory Board & Editors, 2025

Professional Medical Disclaimer

This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.

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