Tranexamic acid

Tranexamic Acid - Is It Really THE Solution for Your Skin Discolouration? 

Skin discolouration results from excess production of melanin, the natural pigment that gives your skin its colour. This can be triggered by various conditions such as acne, chronic exposure to sunlight, hormonal fluctuations, and skin inflammation.

Among the many treatments for skin discolouration is the use of acids. Acids such as azelaic acid, hyaluronic, glycolic, retinoic, and malic are used or incorporated into skin care products to deal with skin hyperpigmentation. Another compound that is gradually joining the rest is Tranexamic acid (TXA). 

This begs the question; is tranexamic acid really THE solution for your skin discolouration or is it just another fad? Let’s find out below.

What is Tranexamic Acid?

TXA is a synthetic form of lysine, an amino acid necessary for the biosynthesis of proteins. This man-made acid is commonly used as a prescription medication to stop excess bleeding - such as in the case of major trauma, heavy menstruation and nosebleeds.  

It can be administered orally, by topical application, and sometimes by injection. It is an antifibrinolytic, a class of medications that work by improving the clotting property of blood.

This formed the basis of tranexamic acid use over the years, until in 1976 when a side effect stoked physicians - patients were showing improvement in the appearance of skin discolouration after tranexamic acid treatments. By 1979 the acid was found useful in the treatment of melasma.

Tranexamic Acid Mechanism in Treating Skin Discolouration?

Listed as an essential medicine by WHO, tranexamic acid treats skin discolouration by slowing down melanin synthesis. This it does by inhibiting the plasminogen/plasmin pathway- the system that interconnects melanocytes and keratinocytes. This interferes with melanin production in the skin, resulting in a lighter complexion and improvement of hyperpigmented areas.

The mechanism of TXA on skin conditions has been studied extensively. This interest has largely been attributed to the acid’s ability to treat even the most stubborn forms of skin discolouration. The treatment is rightfully considered a ‘game changer’ in the treatment of melasma by the Journal of the American Academy of Dermatology.

Forms of Tranexamic Acid Used to Treat Skin

To treat the skin, tranexamic acid is mainly administered orally and topically.

Tranexamic Acid Tablets  

Unless advised otherwise by your doctor, the usual dosage in pill form is 650 mg or 500 mg taken 2 to 4 times daily for 5 days when treating bleeds. For the treatment of discolouration, the dose is reduced and the treatment taken for a longer period of time.

Oral treatment is usually taken in combination with topical tranexamic acid creams. Topical application can also be used on its own especially in contraindicated cases. 

The dosage depends on physiological factors such as weight and age. The type and severity of the condition being treated also affect the dosage. To be on the safer side consult a dermatologist especially for serious conditions such as hyperpigmentation from chronic acne and melasma.   

Tranexamic Acid Creams

This colourless and water-soluble compound is infused in skin care creams to achieve depigmentation. These creams may contain 2% tranexamic acid at the maximum. Low dosage is considered safer but still effective; higher concentrations show no significant difference and are actually likely to cause more side effects.

Higher doses of up to 5% can, however, be used but with the explicit direction from a specialist. This kind of high doses are common in clinical trials where use is controlled and monitored. To optimize the effects, other melanin inhibitors are used as complementary ingredients.

“By 1979 tranexamic acid was found useful in the treatment of melasma."

Tranexamic acid is also administered in injection form. This is, however, a reserved for doctors in sterile conditions and only when there is a need to reduce bleeding. In such cases, 100mg of tranexamic acid is used in 1ml of IV solution.”

Tranexamic Acid Contraindications

Due to its procoagulant nature, oral Tranexamic acid is contraindicated in certain individuals. You should not use it if:

  • You are taking anti-coagulant medication
  • You have a family history of blood clotting
  • You are pregnant or breastfeeding
  • You are using the combined contraceptive pill or hormonal replacement therapy (HRT)
  • You have irregular periods
  • You have a history of retinal vein occlusion

Topical tranexamic acid, on the other hand, has minimal systemic absorption. It is, therefore, safer for use even by people limited by the contraindications.

Is Tranexamic Acid backed by Science?

Since its discovery in 1962 by Japanese researchers, tranexamic acid has been used for various treatments touching on blood clotting. However, for skin lightening and treatment of skin conditions, the acid has been in use for about four decades now.

During this time there have been many clinical trials assessing the efficacy of the acid in treating skin discolouration. Here are highlights of some of the leading scientific studies focusing on melasma, one of the most stubborn forms of discolouration, and other skin conditions;   

Tranexamic Acid vs Hydroquinone

In a split-face trial, 3% tranexamic acid was applied on one side, and 3% Hydroquinone plus 0.01% Dexamethasone on the other twice daily. The study involved 50 melasma patients with assessment being done in 4-week intervals. Before and after photographs were used to evaluate changes using the Melasma Area and Severity Index (MASI) score.    

From the 12-week study, both treatments were found to be efficacious with no significant differences. The side effects of the acid were however less prominent compared to Hydroquinone + Dexamethasone. The research concluded that topical application of tranexamic acid was “an effective and safe medication for the treatment of melasma.”      

Tranexamic Acid on Melasma

Tranexamic acid for melasma

A retrospective study on the effectiveness of oral ingestion of tranexamic acid concluded in favour of the treatment. The study involved 561 melasma patients over a period of 4½ years. 530 (95%) of the study group were classified as having therapy-resistant melasma, having had other treatments with no satisfactory results.

From the results, 90% of the patients showed improved lightening with a median response time of 2 months. Of the improvement cases, only about 28% (137) relapsed after stopping the treatment- after about 7 months.

This is one of the most extensive and quoted study on the use of oral tranexamic acid for the skin. Its touted to have “changed the practice of dermatology” by the American Academy of Dermatology.  

Tranexamic Acid in Combination Therapy on Post Acne Erythema

This study investigated the effectiveness of topical tranexamic acid + vitamin C serum vs. Microneedling. The therapy was targeted at improving persistent acne which also helps in preventing the resulting acne scarring. In the trial, 32 patients participated in a split-face study with treatment being done 4 times, 15 days apart over a period of 2 months.      

Observation was carried out every 2 weeks for 6 weeks after the treatment. Results showed a greater decrease in post-acne macules on the side under tranexamic acid treatment compared to the microneedling side.

Also, no side effects were reported after the treatment. The study concluded that “A combination of skin micro-needling and topical application of TXA and vitamin C may be considered as a new and fast treatment for post acne erythema.”

Tranexamic Acid on Post Inflammatory Hyperpigmentation

The effectiveness of tranexamic acid on hyperpigmentation was studied in a group of 40 patients suffering from solar lentigines- harmless patches of hyperpigmented skin from long term exposure to sunlight. After skin laser surgery, one section of the group was treated with oral tranexamic acid while the other took a placebo.

The treatment ran for 6 weeks with evaluation being done at the baseline and every 2 weeks thereafter for 3 months. From the results, the “tranexamic acid group tended to demonstrate superior lightening of the lesions than the placebo group”. This led to the conclusion that taking the acid orally may help to prevent PIH.

FDA Approval of Tranexamic Acid 

Tranexamic acid is FDA approved but only for use by patients with heavy menstrual bleeding and as a short term remedy for those suffering from haemophilia. Its formulation and use in cosmetics and for the purpose of treating hyperpigmentation is purely based on the evaluation of the clinical trials.

How to Use Tranexamic Acid

Based on clinical trials, the dosage for oral TXA for the treatment of hyperpigmentation should be 250mg tablets twice daily for up to 12 weeks. This should be done under the assessment of a doctor prior to and during the entire treatment period.

The reason behind this is because the medication may require constant monitoring due to the possibility of adverse effects. You should not change the dosage unless advised to do so by your doctor. The tablets can be taken with or without food.

Topical TXA is applied twice daily on the affected skin for about 12 weeks. Alternatively, you can opt for skin lightening creams/serums that incorporate tranexamic acid into their formulations; TXA combines well with other skin lightening ingredients such as kojic acid, hydroquinone, niacinamide, and vitamin C among others. In such cases, the percentage of TXA can be as little as 0.1%.

Another use of topical TXA is post-procedurally with procedures like laser therapy and microneedling to prevent post-inflammatory hyperpigmentation in prone skin types.

Side Effects of Tranexamic Acid

Very minimal side effects are linked to topical use of TXA if any. Depending on the sensitivity of your skin, some of the side effects to expect include:

  • Reddening of the skin
  • Mild irritation
  • Dry skin
  • Scaling

With oral use, it is possible to experience:

  • Nausea
  • Diarrhoea
  • Abdominal discomfort
  • Bloating
  • Allergic skin rash

NOTE; Oral Tranexamic acid is procoagulant medication; this means that it promotes coagulation of blood. With long term use, it can lead to health issues such as;

  • Deep vein thrombosis
  • Pulmonary embolism
  • Myocardial infarction
  • Changes in vision

Where to buy Tranexamic acid

Currently, shopping for products labelled as pure tranexamic acid might prove futile as most are labelled as ‘currently unavailable’ in online stores. However, TXA infused creams and serums are numerous and available on Amazon and other online stores and come at various prices depending on the brands and the purpose of the products. Most are sold as skin brightening, lightening, bleaching or whitening creams.

TXA tablets are available over the counter (OTC) in many pharmacies at $0.50 and above. However, they are usually 500mg and are sold for heavy menstrual flow. These are not meant to be used for more than 5 days, which necessitates a doctor’s advice.

Conclusion

Besides its original purpose, tranexamic acid has shown the ability to effectively deal with hyperpigmentation. However, the lack of data on the long-term effects of the acid on the subjects plus the potential risks that come with oral TXA cannot be ignored.

So, is Tranexamic acid really the solution for your skin discolouration? Use of the topical TXA has not been linked to serious side effects. Unfortunately, the highest efficacy has been achieved through oral administration or a combination of both. All is not lost though; a combination of TXA and safe skin lightening ingredients might prove helpful in your case.

Oral TXA is another story altogether; before embarking on that road, consult a doctor to weigh the risks against the benefits. If you don’t have a good gut feeling about it, there are plenty of safer, natural and effective topical skin lightening alternatives for you to try.

About:

sonia knight

Sonia Knight is the founder of be:skinformed.

Apart from having her own experience with hyperpigmentation, Sonia has gained vast knowledge in the dermatology field. For more info on this, check out our about us page.
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