What is the oral treatment for melasma (hyperpigmentation)?

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Last updated: April 8, 2025View editorial policy

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From the FDA Drug Label

HYDROQUINONE USP, 4% SKIN BLEACHING CREAM is indicated for the gradual bleaching of hyperpigmented skin conditions such as chloasma, melasma, freckles, senile lentigines, and other unwanted areas of melanin hyperpigmentation. The oral treatment for melasma is not mentioned in the provided drug labels.

  • The labels discuss topical application of hydroquinone for skin bleaching.
  • There is no information about oral treatment options for melasma. 1

From the Research

Oral tranexamic acid is the most effective treatment for melasma, especially in cases of refractory melasma, and should be prescribed at a dose of 250mg twice daily for 8-12 weeks, as it has been shown to improve MASI scores and reduce hyperpigmentation 2. When considering oral treatments for melasma, it is essential to prioritize the most recent and highest quality study, which in this case is the 2023 review on tranexamic acid in melasma 2. This study found that oral tranexamic acid is safe and effective for the treatment of melasma, with significant improvements in MASI scores. Some key points to consider when prescribing oral tranexamic acid for melasma include:

  • The recommended dose is 250mg twice daily for 8-12 weeks 2
  • Patients should be aware of potential side effects, such as GI upset and menstrual irregularities 2
  • Tranexamic acid should be used with caution in patients with a history of blood clotting disorders or those who are pregnant 2
  • Combination therapy with other treatments, such as topical hydroquinone or chemical peels, may be considered for optimal results 3
  • Strict sun protection, including daily broad-spectrum sunscreen with SPF 30 or higher, is essential to prevent worsening of melasma 4

References

Research

Melasma Treatment: An Evidence-Based Review.

American journal of clinical dermatology, 2020

Research

Melasma: an Up-to-Date Comprehensive Review.

Dermatology and therapy, 2017

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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