Has tranexamic acid (TXA) been used orally in dermatology?

Oral Tranexamic Acid in Dermatology

Yes, oral tranexamic acid (TXA) has been extensively used in dermatology, primarily for treating melasma and other hyperpigmentation disorders, with demonstrated efficacy and safety when used at doses of 250-650 mg twice daily. 1, 2

Primary Dermatologic Indication: Melasma

Oral TXA is most commonly used for melasma treatment, particularly in refractory cases that fail topical therapies. 2, 3

• The American Academy of Dermatology recognizes oral TXA as part of the standard treatment algorithm for melasma, alongside strict sun protection and topical therapies. 2
• Oral TXA demonstrates superior efficacy compared to topical TXA formulations for hyperpigmentation disorders. 4
• The typical dosing regimen is 250 mg twice daily, though doses up to 650 mg twice daily have been studied with good results. 1, 5

Clinical Efficacy Data

When used as monotherapy, oral TXA produces significant improvement in melasma severity scores:

• Mean MASI score reductions of approximately 69% have been documented after 3-4 months of treatment. 6
• Treatment duration typically ranges from 8-12 weeks, with some protocols extending to 6 months. 7, 3
• Low-dose oral TXA (500 mg daily) over short periods (8-12 weeks) has demonstrated clear efficacy, particularly in Asian populations. 3

Combination therapy with PRP injections shows even better outcomes:

• Oral TXA 250 mg twice daily combined with monthly intradermal PRP injections achieves 90.48% total efficacy compared to 73.68% with TXA alone. 1, 4
• This combination therapy reduces disease recurrence rates and maintains normal levels of VEGF and α-MSH. 1
• Patient satisfaction exceeds 90% with combination PRP-oral TXA treatment. 1

Beyond Melasma: Other Hyperpigmentation Disorders

Oral TXA has been used off-label for various hyperpigmentation conditions beyond melasma:

• Post-inflammatory hyperpigmentation (treatment and prevention). 7
• Lichen planus pigmentosus. 7
• Ashy dermatosis. 7
• Riehl melanosis. 7
• Dosing for these conditions ranges from 250-1500 mg daily for 2 weeks to 6 months with variable efficacy. 7

Safety Profile and Side Effects

Oral TXA demonstrates a favorable safety profile in dermatologic use:

• Most common side effects include gastrointestinal upset, headaches, malaise, nausea, and menstrual irregularities (both hypo- and hypermenorrhea). 5
• In one retrospective study of 42 patients, only 7 experienced side effects, all of which resolved upon discontinuation. 5
• Studies have shown that TXA does not increase thromboembolic risk when used at dermatologic doses, though careful screening for contraindications is essential. 3

Important Contraindications and Precautions

Screen patients carefully before prescribing oral TXA:

• The pro-thrombotic nature of TXA requires assessment of thromboembolic risk factors prior to treatment. 8
• Contraindications include history of thromboembolic events, hypercoagulable states, and active bleeding disorders. 3
• Patients should be counseled about potential menstrual irregularities. 8

Treatment Algorithm Position

Oral TXA should be considered after first-line therapies fail:

• Begin with strict sun protection (SPF 50+, reapplied every 2-3 hours) and topical therapies (hydroquinone-based combinations). 4, 2
• If inadequate response after 8-12 weeks of topical therapy, add oral TXA 250 mg twice daily. 3
• For optimal outcomes in refractory melasma, combine oral TXA with monthly intradermal PRP injections. 1, 4
• Maintenance therapy may be required as melasma is a chronic condition with high recurrence rates. 4, 2

Common Pitfall to Avoid

Do not discontinue treatment prematurely—melasma requires sustained therapy and maintenance to prevent recurrence. 4 The combination of oral TXA with PRP specifically reduces recurrence rates compared to monotherapy. 1