What Is Oral Tranexamic Acid And Why Is It Used In Skincare?

Tranexamic acid (TA or TXA) is a synthetic compound derived from lysine, an essential amino acid used in making proteins in the body. TXA comes in many forms, including oral, topical, and intravenous formulations.

Tranexamic acid is a fibrinolytic (blood clotting) compound whose primary role is preventing excessive bleeding. While oral TXA is historically associated with treating blood disorders (it’s even on the World Health Organization’s list of essential medicines), today, its use has expanded to include oral TXA for skincare.

This article unpacks this new and exciting frontier in skincare, starting with a brief history lesson.

A brief history of oral tranexamic acid and its uses

Japanese researchers first made tranexamic acid in 1962. Its blood clotting mechanism meant it was used exclusively in treating heavy periods, post-surgery bleeding, and chronic nosebleeds.

Over the years, doctors used the drug to treat bleeding conditions successfully, but in 1979, a researcher discovered an exciting, unexpected effect of TXA: it appeared to treat melasma in a patient undergoing treatment for a different condition (Bagherani). This discovery led to the realization that oral TXA could be used for skincare, with several subsequent studies further exploring its efficacy.

Why is oral tranexamic acid used for skincare?

Oral TXA is used for skincare due to its effectiveness in treating melasma, hyperpigmentation, and sunspots. In one study, researchers found that oral TXA reduced MASI (Melasma Area and Severity Index) by up to 69%, with little to no side effects (Tan). Another study supported these findings by showing that oral TXA effectively reduces melasma at low doses after eight to twelve weeks (Bala).

This relative safety and visible effectiveness of oral TXA treatment confirmed it as one of the most promising skincare therapies on the market today. These studies all point to a generally agreed consensus among scientists that oral TXA can be effective in the long-term treatment of melasma.

Oral tranexamic acid vs. topical and intradermal applications

TXA can be administered orally, topically, or intradermally, but which one is the most effective at treating melasma and other hyperpigmentation conditions?

In general, topical and intradermal applications of TXA have positive effects in the treatment of melasma, but results are usually limited. For instance, one research paper found that topical applications of TXA were only as effective as topical hydroquinone applications, showing no comparative improvements even with long-term treatment (Wang). In addition, topical TXA requires additional components like Kojic Acid and Vitamin C to enhance the skin’s brightness and overall appearance.

On the other hand, oral TXA appears to have better and more sustained results without adding additional components. At low doses, oral TXA significantly reduces signs of melasma, resulting in a clear and evenly toned skin appearance.

The main reason oral TXA appears to work better than topical TXA is that it enters the bloodstream and inhibits the melanin synthesis process at a cellular level. The result is a more natural inside-out renewal of the skin, something topical applications struggle to achieve because their mechanism of action is limited to the skin’s surface.

How does oral tranexamic acid work to reduce hyperpigmentation?

The science behind oral TXA’s effectiveness in treating melasma borrows from its action in enhancing blood clotting.

In general, the process follows the following steps:

• Oral TXA blocks the conversion of plasminogen to plasmin
• Which prevents the binding of plasminogen to keratinocytes (skin cells that produce keratin)
• Which lowers arachidonic acid release, prostaglandin synthesis, and fibroblast growth factors (FGF)
• Which decreases melanin synthesis and reduces angiogenesis (the development of new blood vessels)
• Resulting in an even-toned complexion

In the entire process, the two fundamental processes TXA inhibits to treat melasma effectively are:

• Melanogenesis, the formation of melanocytes/pigment cells), and
• Angiogenesis, the formation of tiny blood cells thought to play a role in the development of melasma (Kim)

Is oral tranexamic acid better than hydroquinone?

Hydroquinone is often the first line of treatment for melasma. Although its effectiveness has long been established, it does have some limitations. For example, it is not recommended for prolonged continual use due to possible side effects like dryness, redness, and inflammation.

Oral TXA overcomes hydroquinone’s limitations by lacking significant side effects, making it the perfect candidate for long-term melasma treatment.

Although the general results of each treatment are comparable, the mode of action (TXA works from the inside out while hydroquinone depigments the skin) means oral TXA shows more promise as a superior treatment.

The benefits of oral tranexamic acid on the skin

We’ve discussed how oral TXA can treat melasma, and that’s a great thing, but what are the other benefits of oral TXA?

Here are the top benefits of using oral TXA for skincare:

• Exceptional results within a short time: Within twelve weeks, individuals taking oral TXA see a significant reduction in pigmentation.
• Persistent results: If oral TXA is taken continually, melasma symptoms remain suppressed, and the skin stays clear and evenly toned.
• Effective for a wide range of skin types: Unlike topical applications that rely on skin type, oral TXA can be used for any skin type with equally positive results across the board.
• Can be used alone or as part of a regimen: TXA’s neutrality allows the use of combination topical therapies to enhance results without the risk of side effects.
• Almost no side effects: TXA used at low doses does not have any significant side effects that might discourage long-term use. In general, scientists have found few reasons to doubt the safety or effectiveness of oral TXA for skincare, a rare conclusion in the beauty sciences field.

Potential side effects of oral tranexamic acid

Since we’ve discussed how oral TXA has almost no side effects, it’s time to discuss the ‘almost’ in that statement.

Here are the main side effects of oral TXA for skincare:

• Loss of gains within three months of halting oral TXA
• Risk of deep vein thrombosis
• Mild gastrointestinal discomfort
• Hypomenorrhea (short periods or light menstrual blood flow)
• Allergic skin rashes
• Alopecia (hair loss)

How to use oral tranexamic acid for skin care

Although topical TXA is available in many skin care products that you can buy over the counter, oral TXA is a prescription-only drug that must be administered by a medical professional.

Before writing a prescription, your dermatologist will analyze your blood profile to screen for hereditary blood disorders, deep vein thrombosis (DVT), and kidney disease. If you have any of these risk factors, the doctor may recommend not taking oral TXA due to the heightened possibility of severe side effects.

If you are cleared, the doctor will generally prescribe a low dose (around 250 mg twice daily) for at least three months. In most cases, visible results start appearing after eight weeks. Depending on the doctor’s evaluation at that time, they may put you on an equal or lower long-term maintenance dose.

References

• Bala HR, Lee S, Wong C, Pandya AG, Rodrigues M. Oral Tranexamic Acid for the Treatment of Melasma: A Review. Dermatol Surg. 2018;44(6):814-825. doi:10.1097/DSS.0000000000001518
• Bagherani, N. (2015), The efficacy of tranexamic acid in the treatment of melasma. Dermatol Ther, 28: 265-265. https://doi.org/10.1111/dth.12200
• Kim EH, Kim YC, Lee ES, Kang HY. The vascular characteristics of melasma. J Dermatol Sci. 2007;46(2):111-116. doi:10.1016/j.jdermsci.2007.01.009
• Tan AWM, Sen P, Chua SH, Goh BK. Oral tranexamic acid lightens refractory melasma. Australas J Dermatol. 2017;58(3):e105-e108. doi:10.1111/ajd.12474
• Wang JV, Jhawar N, Saedi N. Tranexamic Acid for Melasma: Evaluating the Various Formulations. J Clin Aesthet Dermatol. 2019;12(8):E73-E74.

Share this Article

Brandon Kirsch, MD

Brandon Kirsch, MD, FAAD, is a board-certified dermatologist specializing in clinical drug development and medical innovation. He is the founder of Kirsch Dermatology in Naples, Florida and is also the Chief of Dermatology at the Naples Community Hospital.