Are there any oral medications (oral meds) that can lighten skin?

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Last updated: June 10, 2025View editorial policy

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From the Guidelines

There are no FDA-approved oral medications specifically designed to lighten skin, and attempting to change natural skin tone through oral medications can pose significant health risks without reliable results. While some oral medications like glutathione, tranexamic acid, and certain antioxidants are sometimes promoted for skin lightening, they lack substantial scientific evidence supporting their effectiveness and safety for this purpose 1. Tranexamic acid (typically 250mg twice daily for several months) has shown some promise in treating melasma when used under medical supervision, but it's not approved specifically for skin lightening and carries risks including blood clots. Oral glutathione supplements, despite their popularity, have insufficient evidence regarding both efficacy and safety for skin lightening. Some key points to consider:

  • The most effective and safest approaches for addressing hyperpigmentation include topical treatments (hydroquinone, retinoids, vitamin C), sun protection, and procedures performed by dermatologists 1.
  • Skin color is largely determined by genetics, and attempting to change your natural skin tone through oral medications can pose significant health risks without reliable results.
  • If you're concerned about specific pigmentation issues, consulting with a dermatologist is recommended for safe, evidence-based treatment options tailored to your needs. It's also worth noting that some medications, such as those used to treat acne, may have a lightening effect on the skin as a secondary benefit, but this is not their primary purpose and should not be used as a justification for taking them for skin lightening alone 1.

From the Research

Oral Medications for Skin Lightening

There are several oral medications that have been studied for their potential to lighten skin, including:

  • Oral carotenoids
  • Glutathione
  • Melatonin
  • Polypodium leucotomos hydrophilic extract
  • Procyanidin
  • Tranexamic acid 2

Efficacy and Safety of Oral Medications

Preliminary data on the use of these oral medications for skin lightening are promising, and they appear to be safe 2. However, it is not recommended to use intravenous glutathione for skin lightening due to the increased risk of adverse events 2. Oral tranexamic acid has also been shown to be a promising treatment for moderate and severe recurrent melasma 3.

Comparison with Topical Treatments

While topical treatments are commonly used for skin lightening, oral medications may offer an alternative for patients who do not respond to topical treatments or who have widespread pigmentation disorders. Hydroquinone is still considered the gold standard for the treatment of hyperpigmentation, but oral medications may be used in combination with topical treatments for enhanced efficacy 4, 3.

Important Considerations

It is essential for dermatologists to understand the properties, efficacy, and adverse events profile of each oral medication to ensure proper use and counseling of patients 2. Additionally, patients should be aware of the potential risks and benefits of using oral medications for skin lightening and should be monitored closely for any adverse events 3, 5.

References

Guideline

Guideline Directed Topic Overview

Dr.Oracle Medical Advisory Board & Editors, 2025

Research

The role of systemic treatments for skin lightening.

Journal of cosmetic dermatology, 2018

Research

Melasma Treatment: An Evidence-Based Review.

American journal of clinical dermatology, 2020

Research

[Topical treatment of pigmentation disorders with cosmetic and pharmaceutical agents].

Der Hautarzt; Zeitschrift fur Dermatologie, Venerologie, und verwandte Gebiete, 2020

Research

Skin lightening: causes and complications.

Clinical and experimental dermatology, 2022

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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