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