Blog > Acne > Tranexamic Acid for Melasma: Benefits & Side Effects  

Tranexamic Acid for Melasma: Benefits & Side Effects  

Melasma is a hyperpigmentation disorder quite often seen in women, and some men. When it comes to skin brightening and lightening hyperpigmentation, the most common ingredients that come to mind are Vitamin C, Niacinamide, Glutathione, Kojic Acid and Hydroquinone. But in recent years, Tranexamic Acid has risen the ranks to become one of the popular ingredients that contains skin whitening benefits to fade several types of skin discolorations - pigmentation such as dark spots and melasma.  

Tranexamic acid has now emerged as the new kid on the block in the skincare treatments sector. It is regularly prescribed as a pigmentation treatment such as melasma and other similar pigmentary conditions.

In this article, let’s explore the benefits and side effects of Tranexamic Acid and how it works to reduce pigmentation.  

What is Tranexamic Acid?  

Tranexamic acid (TXA) is a synthetic derivative of lysine, an amino acid present naturally in our bodies. Due to its antifibrinolytic and procoagulant properties, was initially utilized as an oral medication for managing severe bleeding from trauma or post-surgery. They also used it control heavy postpartum or menstrual bleeding.

In addition to this, lysine is an essential amino acid which helps to produce collagen as well as inhibit the production of melanin. The topical application of tranexamic acid skin care was found to alter the cell mechanism for producing melanin.

This discovery led to the use of tranexamic acid in the treatment and resolution of hyperpigmentation. Today, tranexamic acid is extensively used in the treatment of skin pigmentation and other related skin issues. Treatment outcomes with tranexamic acid range from a brighter skin complexion to lightened pigmentation.

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How does Tranexamic Acid work on the skin? 

TXA essentially works to lighten hyperpigmentation in two ways – by blocking melanin production as well as the transfer of melanin to the outer skin layer. At the physiological level, TXA typically acts as an antiplasmin. It prevents the bonding of plasminogen with the keratinocytes. This adversely impacts the activity of melanocyte tyrosinase, leading to a decrease in arachidonic acid and prostaglandins[1].

Arachidonic acid is known to contribute to inflammation leading to melanogenesis, especially in the facial region. Melanogenesis is recognized as a primary contributor to the aging of the skin. 

What are the Benefits of Tranexamic Acid?  

The anti-inflammatory properties of TXA, coupled with its ability to inhibit melanin production, point to its immense potential in dermatology. TXA restricts the pathway connecting the keratinocytes and melanocytes, effectively reducing the interaction between the skin cells and the melanin-forming cells.  This helps to effectively resolve skin concerns such as: 

Reduced Dark Spots and Discoloration 

A study of 100 participants conducted in 2019 probed the relative benefits of 2 different treatments on melasma [2]. 84 women and 16 men received TXA and hydroquinone, a skin-lightening bleaching agent, as topical treatments.

At the end of 12 weeks, the study findings showed that the severity of melasma had decreased by 27% in the group using TXA. This is almost equal to the number of participants who had opted for treatment with hydroquinone. However, higher satisfaction levels were reported by the participants who had used TXA, citing fewer side effects like skin irritation [3].   

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Reduced Post-inflammatory Hyperpigmentation and Sun Damage  

Acne breakouts often leave behind permanent marks in the form of post-inflammatory hyperpigmentation. Better known as skin blemishes, these red or brown colored patches of discoloration can be quite stubborn when it comes to treating them.   

A 2022 review observed that TXA was useful for reducing the appearance of these lesions, with minimal risk of serious side effects [4]. Similarly, a small study conducted a year earlier also opined that TXA could enhance skin tone, reduced redness and dark spots.

In a 2021 study, the participants applied cetyltranexamate mesylate, a derivative of TXA, twice every day for 8 weeks. After just 2 weeks treatment, the majority of the participants reported improvements in skin tone and reduction of redness and dark spots. The participants also noticed continued improvement throughout the study [3].   

Stronger Skin Barrier   

The skin barrier is the outermost layer of the skin and acts as a protective shield that helps keep moisture locked in while keeping toxins and irritants out.   

A 2016 review noted that rosacea symptoms can be greatly reduced through strengthening of the skin barrier with the use of TXA [5].   

Another small study from 2015 demonstrated that treatment with topical application of a 3% tranexamic acid for 2 weeks. The study resulted in fewer signs of rosacea compared to people who didn’t use this treatment. Researchers correlated the reduction in symptoms with improved skin barrier function [6].  

Potential Risks & Side Effects of Tranexamic Acid

Compared to other brightening agents, TXA is deemed to be safe as well tolerated by all skin types.

However, some of the common side effects identified by a small study in 2014 include [7]:   

  • Dryness   

  • Irritation   

  • Flaking   


Oral TXA usage is also not advised for people with the following conditions:   

  • Thrombosis and similar blood clotting disorders  

  • Convulsions   

  • Poor kidney function   

  • Personal or family history of coagulopathy   

  • Stroke   

  • Ischemic heart disease   

  • Fibrinolytic conditions  

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Tranexamic Acid – The Bottom Line 

As a late entrant in skincare, TXA is gaining recognition for treating UV-induced hyperpigmentation, scars, and various skin spots. Its unexpected benefits are also capturing increasing attention. Nevertheless, because every skin type is unique and differs in various ways. It is important to consult your doctor to understand the potential benefits and possible risks of tranexamic acid as well as the other alternatives to melasma treatment