Does Oral Tranexamic Acid 250mg Really Help with Melasma and Skin Whitening? - Pharmacology

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Depigmentation


Is it true that oral Tranexamic acid 250mg prescribed by a dermatologist for melasma has "spot reduction and whitening" effects?

Xiao Pang, 40~49 year old female. Ask Date: 2009/01/12

Dr. Hou Fangmin reply Pharmacology


Hello: Tranexamic acid was originally used to treat systemic and localized bleeding or hemorrhagic disorders.
It was later found to inhibit tyrosinase, rapidly modulating the activity of exogenous stimuli to prevent the activation of factors that cause skin darkening, thereby inhibiting the activity of tyrosinase and melanocytes.
This fundamentally regulates issues related to skin dullness and pigmentation, restoring a bright and refined complexion.

The second effect/whitening agent, tranexamic acid, has whitening properties while also preventing post-sun exposure pigmentation.
It is non-irritating, has low photosensitivity, and possesses soothing effects, reducing melanin and inhibiting tyrosinase.
However, it may have side effects that vary from person to person, including diarrhea, sexual dysfunction, nausea, vomiting, irregular menstruation, increased tear production, and skin rashes or itching, so it is important to be aware of these potential side effects.
Lastly, I wish you peace and happiness.

Reply Date: 2009/01/12

More Info


Tranexamic Acid (TXA) has gained attention in dermatology, particularly for its potential effects on melasma and skin whitening. Originally developed as a medication to treat bleeding disorders, TXA works by inhibiting the activation of plasminogen to plasmin, which is involved in the breakdown of fibrin in blood clots. However, its role in dermatology is primarily linked to its ability to inhibit the enzyme tyrosinase, which is crucial in the melanin production pathway.

Melasma is a common skin condition characterized by brown or gray-brown patches, often occurring on the face. It is typically triggered by factors such as sun exposure, hormonal changes (like those during pregnancy or with oral contraceptives), and certain medications. The pathophysiology of melasma involves an increase in melanin production by melanocytes, which can be exacerbated by UV exposure.
The use of oral Tranexamic Acid for melasma is based on its ability to reduce melanin synthesis. Studies have shown that TXA can effectively lighten melasma lesions and improve overall skin tone. The typical dosage for treating melasma is often around 250 mg to 500 mg taken orally, usually for a duration of several months. Patients may start to see improvements within a few weeks, but optimal results often require consistent use over a longer period.

In terms of skin whitening, TXA has been noted for its ability to not only reduce existing pigmentation but also to prevent the formation of new dark spots, particularly those induced by sun exposure. This dual action makes it a valuable option for individuals seeking to improve their skin tone and reduce hyperpigmentation.

However, it is essential to consider the potential side effects associated with Tranexamic Acid. While many patients tolerate it well, some may experience gastrointestinal issues such as nausea, diarrhea, or abdominal pain. Other reported side effects can include dizziness, headache, and, in rare cases, thromboembolic events due to its blood-clotting properties. Therefore, it is crucial for patients to discuss their medical history and any potential risks with their healthcare provider before starting treatment.

Moreover, while Tranexamic Acid can be effective, it is often recommended to be used in conjunction with other treatments for melasma, such as topical agents (like hydroquinone, retinoids, or azelaic acid) and sun protection measures. Sunscreen is vital, as UV exposure can worsen melasma and counteract the benefits of any treatment.

In conclusion, oral Tranexamic Acid 250 mg can indeed be effective for treating melasma and promoting skin whitening, but it should be part of a comprehensive skincare regimen. Patients should consult with their dermatologist to tailor a treatment plan that considers their specific skin type, the severity of melasma, and any underlying health conditions. Regular follow-ups can help monitor progress and adjust treatment as necessary to achieve the best results while minimizing side effects.

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