
Hyperpigmentation is a topic that affects many people worldwide. This common skin condition, characterized by dark patches on the skin, can be a source of distress for those who experience it. But what if we told you there’s a promising solution in the form of a substance originally used to prevent excessive bleeding? Enter Tranexamic Acid.
Contents
Introduction to Hyperpigmentation and Tranexamic Acid
Hyperpigmentation is a common skin condition that causes certain areas or patches of skin to darken more than the surrounding skin. This occurs when an excess of melanin, the brown pigment that produces normal skin color, forms deposits in the skin. Hyperpigmentation can affect anyone, regardless of skin color or type, and can occur on any part of the body.
Tranexamic Acid, a synthetic derivative of the amino acid lysine, was originally used as a medication to help reduce bleeding. In recent years, it has gained attention in the dermatological field for its potential in treating hyperpigmentation. It works by inhibiting the activation of melanocytes, the cells that produce melanin, thereby reducing the overproduction of melanin that leads to hyperpigmentation.
Understanding Hyperpigmentation
Before we study the role of Tranexamic Acid in treating hyperpigmentation, it’s important to understand what hyperpigmentation is, what causes it, and how it can impact the quality of life of those who experience it.
Causes of Hyperpigmentation
Hyperpigmentation is often a result of either external or internal factors that lead to an overproduction of melanin, the pigment responsible for the color of our skin, hair, and eyes [1].
Sun Exposure
The most common cause of hyperpigmentation is sun exposure. When our skin is exposed to the sun, it produces more melanin to protect itself, which can lead to dark spots or patches. These are often referred to as sun spots or age spots.
Hormonal Changes
Hormonal changes, particularly those occurring during pregnancy or due to the use of hormonal contraceptives, can also lead to hyperpigmentation. This type is often referred to as melasma or the “mask of pregnancy.”
Inflammation or Injury
Post-inflammatory hyperpigmentation (PIH) occurs following skin injury or inflammation, such as acne, eczema, or psoriasis. The skin’s response to inflammation or injury can result in an overproduction of melanin, leading to dark spots or patches.
Types of Hyperpigmentation
There are several types of hyperpigmentation, each with its unique characteristics and causes.
Melasma
Melasma is a type of hyperpigmentation that often occurs during pregnancy or in women taking hormonal contraceptives. It’s characterized by dark, irregular patches commonly found on the upper cheek, nose, lips, upper lip, and forehead.
Post-Inflammatory Hyperpigmentation (PIH)
PIH is a response to injury or inflammation. It can occur anywhere on the body and is often caused by acne lesions, psoriasis, burns, or certain skin care treatments.
Age Spots
Also known as liver spots or solar lentigines, age spots are small, dark patches that are often a result of sun exposure over time. They typically occur on areas of the skin that have been exposed to the sun, such as the face, hands, and arms.
Impact on Quality of Life
Hyperpigmentation, while usually harmless, can have a significant impact on a person’s quality of life. It can lead to feelings of self-consciousness and can affect a person’s self-esteem. Many people with hyperpigmentation seek treatment to help even out their skin tone and improve their confidence.

Overview of Tranexamic Acid
Now that we have a solid understanding of hyperpigmentation, let’s turn our attention to Tranexamic Acid. This compound, while not originally intended for dermatological use, has shown promising results in the treatment of hyperpigmentation.
History and Original Use of Tranexamic Acid
Tranexamic Acid, also known as TXA, is a synthetic derivative of the amino acid lysine. It was originally developed in the 1960s as a medication to reduce or prevent excessive bleeding during surgery or following trauma. It works by blocking the conversion of plasminogen to plasmin, a molecule that breaks down blood clots. By doing so, it helps to prevent excessive bleeding.
How Tranexamic Acid Works
In the context of skincare, Tranexamic Acid works a bit differently. It’s believed to inhibit the activation of melanocytes, the cells that produce melanin. This is achieved by blocking the plasminogen binding sites on the surface of keratinocytes, the predominant cell type in the outer layer of the skin. When plasminogen is activated (by UV radiation, for example), it can stimulate melanocytes to produce more melanin. By blocking this activation, Tranexamic Acid can help to reduce the overproduction of melanin that leads to hyperpigmentation [2].
Safety Profile of Tranexamic Acid
Tranexamic Acid has a well-established safety profile when used systemically to prevent bleeding. In dermatological use, it’s generally well-tolerated, with few side effects. Topical application may cause minor skin irritation in some people, while oral use can occasionally lead to gastrointestinal upset. As with any treatment, it’s important to discuss the use of Tranexamic Acid with a healthcare provider to ensure it’s suitable for your individual circumstances.

Tranexamic Acid and Hyperpigmentation
Having understood the basics of hyperpigmentation and Tranexamic Acid, let’s now explore how this compound can be used to treat hyperpigmentation.
Scientific Evidence Supporting the Use of Tranexamic Acid for Hyperpigmentation
Over the past few years, Tranexamic Acid has gained attention in the field of dermatology for its potential in treating hyperpigmentation.
Clinical Studies
Several clinical studies have demonstrated the efficacy of Tranexamic Acid in reducing hyperpigmentation. For instance, a study published in the Journal of Dermatology found that patients with melasma who were treated with Tranexamic Acid showed significant improvement compared to a control group. Another study in the British Journal of Dermatology found that Tranexamic Acid was effective in treating not only melasma but also post-inflammatory hyperpigmentation [3].
Mechanism of Action
The mechanism of action of Tranexamic Acid in treating hyperpigmentation is believed to be its ability to inhibit the activation of melanocytes, thereby reducing the overproduction of melanin. It does this by blocking the plasminogen binding sites on keratinocytes, preventing the activation of plasminogen which can stimulate melanocytes to produce more melanin.
How to Use Tranexamic Acid for Hyperpigmentation
Tranexamic Acid can be used in several ways to treat hyperpigmentation [4].
Topical Application
Topical Tranexamic Acid is often found in creams, serums, or lotions. It’s applied directly to the areas of hyperpigmentation. This method is generally well-tolerated, with minor skin irritation being the most common side effect.
Oral Intake
Oral Tranexamic Acid is typically prescribed for more severe cases of hyperpigmentation, such as widespread melasma. It’s important to note that oral Tranexamic Acid should only be taken under the supervision of a healthcare provider due to potential side effects, including gastrointestinal upset.
Intradermal Injections
In some cases, Tranexamic Acid may be administered via intradermal injections. This method is often used for localized areas of hyperpigmentation and is typically performed by a dermatologist or other trained healthcare provider.
Potential Side Effects and Precautions
While Tranexamic Acid is generally well-tolerated, it’s not without potential side effects. Topical application can cause minor skin irritation in some individuals. Oral intake can lead to gastrointestinal upset, and in rare cases, it can increase the risk of blood clots. Therefore, it’s not recommended for individuals with a history of thromboembolic disease. Intradermal injections can cause discomfort at the injection site and, in rare cases, may lead to skin necrosis [5].

Comparing Tranexamic Acid to Other Hyperpigmentation Treatments
While Tranexamic Acid is a promising treatment for hyperpigmentation, it’s not the only option available.
Hydroquinone
Hydroquinone is a well-known skin-lightening agent that has been used for many years to treat hyperpigmentation. It works by inhibiting the enzyme tyrosinase, which is necessary for melanin production. While effective, Hydroquinone has been associated with some side effects, including skin irritation and, in rare cases, a condition called ochronosis which results in darkening of the skin. Compared to Hydroquinone, Tranexamic Acid has a better safety profile and is less likely to cause skin irritation.
Retinoids
Retinoids, derivatives of Vitamin A, are commonly used in skincare for their ability to speed up cell turnover and reduce the appearance of hyperpigmentation. While effective, they can cause skin irritation, dryness, and sensitivity to the sun. Tranexamic Acid, on the other hand, is generally well-tolerated and does not increase sun sensitivity.
Chemical Peels
Chemical peels, which use acids to exfoliate the top layers of the skin, can also be used to treat hyperpigmentation. While they can be effective, they often require downtime for the skin to heal and can lead to skin irritation and changes in skin color. Tranexamic Acid does not require downtime and is less likely to cause skin irritation.
Laser Treatments
Laser treatments can be very effective in treating hyperpigmentation. They work by targeting the melanin in the skin, breaking it up so it can be removed by the body’s natural processes. However, laser treatments can be expensive, may require multiple sessions, and can sometimes lead to post-inflammatory hyperpigmentation, especially in darker skin tones. Tranexamic Acid is a more affordable option and does not carry the risk of causing post-inflammatory hyperpigmentation.
References
[1] Why Tranexamic Acid Is the New Secret to Fading Dark Spots
[2] Topical tranexamic acid as a promising treatment for melasma
[3] Oral tranexamic acid in the treatment of hyperpigmentation disorder beyond melasma
[4] The Use of Tranexamic Acid to Prevent and Treat Post-Inflammatory Hyperpigmentation
[5] Mechanism of Action of Topical Tranexamic Acid in the Treatment of Melasma and Sun-Induced Skin Hyperpigmentation