Tranexamic Acid

Why is tranexamic acid a breakthrough ingredient for melasma?

Trending over the past few years, learn why this skincare acid is the number one agent of choice for most dermatologists when it comes to treating melasma & disorders of pigmentation as it treats the cause of pigmentation.

How does it work?

Tranexamic acid is classified as a depigmenting agent. It interferes in a number of places with the chemical pathway which causes pigmentation & hence it is useful in managing conditions such as melasma & post inflammatory hyperpigmentation. 

It stops the uptake of the melanin producing cells into the superficial layers of the skin. It works well alongside other pigment correctors, lasers & chemical peels. 

What is it?

This acid comes in 3 formulations: tablets, serums & injectables. Serums are used most frequently, oral agents are prescribed by dermatologists, & injectables are for research purposes only. 

Serums & topicals do not require a prescription (read more to understand brands available), whilst tablets require a doctor’s prescription. 

How long does it take to work?

It takes 3-8 weeks before results can be seen. Faster results are achieved when this is combined with picosecond lasers or novel peels such as Cosmelan or Dermamelan. 

What do the studies say about tranexamic acid & melasma?

This works in 20 to 80% of melasma. The lower figure quoted is for serums, the higher figure is when it is used systemically with lasers, pigment inhibitors & chemical peels. 

Is it suitable for all skin types?

Unlike some of the other skincare acids that can irritate your skin & give rise to sensitized skin, you don’t have to worry as much with this. It is safe for all skin types and well tolerated, providing concentrations are around 1.8 to 2%. 

Higher concentrations can cause skin irritation, especially in patients with sensitive skin. Read more to understand how to start it.

Should I take a tablet, or should I try a cream formulation?

Difficult question to answer as it depends on several factors including extent of melasma, depth of pigmentation, previous treatment, your insight as well as risk factors. 

If you have not tried basic melasma management, you are better off trialing topicals over oral agents. Leave the oral tranexamic acid to clinicians who can guide you as to the risk benefit ratio of this medication. 

How should you apply tranexamic acid creams/serums?

As with all powerful formulations, start slowly. Apply every second night to affected areas of pigmentation, increasing to nightly dosing. It’s good practice to stick to recommended brands at around 1.5 to 3% tranexamic acid.

Moisturize your skin 15 to 30 minutes before application for maximum effect. As always, titrate your dosing if you are on other skin care products. 

What should I do if skin gets irritated with tranexamic acid creams?

Back off. Here are the steps to troubleshoot-

1. Reduce absorption; modulate delivery. Example lower density microneedling. 
2. Reduce application amount, frequency or concentration.
3. Moisturize after application.
4. Minimize interactions with other topicals (modulate), examples include retinoids, ascorbic acid, AHAs, etc. Titrate accordingly. 
5. Test patch prior to application. 
6. Be guided by your clinician. 

What brands are recommended?

Look for concentrations ranging between 2 to 10%, remembering that topical serums are equally as effective as other pigment inhibitors such as ascorbic acid & hydroquinone. Brands include-

• SkinCeuticals Discoloration Defense Serum 
• The Inkey List
• Exaglow

What happens if tranexamic acid serums don’t work?

This is not uncommon as serums rate dismally as compared to proper dosing of tranexamic acid (systemic or orally). Your clinician can –

• Add other pigment correctors (see below)
• Initiate systemic therapy.
• Add picolasers.
• Consider novel chemical peels.

What is frequently combined with t.acid?

Dermatologists frequently combine tranexamic acid with specific tyrosinase inhibitors, depending on if it is taken orally or topically. For the latter, interactions do occur with the irritant potential of combination creams. 

Combinations include-

• Arbutin
• Azelaic acid
• Kojic acid
• Hydroquinone
• Ascorbic acid
• Tocopherol
• Salicylic acid
• AHAs; glycolic, mandelic & lactic acid
• Botanicals; licorice root, green tea, bearberries

How long can I be on tranexamic acid?

There is no definitive answer, however long-term studies in the gynecology group have been promising regarding long term safety. 

Your clinician will guide you through the duration of treatment (different for oral, intradermal & topical regime). The specialists at The Melasma Clinic practice rotational therapy for t.acid. 

What about intradermal (injections) of tranexamic acid?

T.acid injected at 1 centimeter grids can help with melasma pigmentation, however this treatment method is purely academic. As the half-life (active lifespan) of this molecule is very short, weekly injections are required. 

Considering it can take 3-6 months for best results, it means 12 to 24 injection sessions. The pain/frequency/costs are not insignificant & hence why our specialists do not inject tranexamic acid for melasma pigmentation. 

Why is microneedling with tranexamic acid not the ideal delivery method?

3 main reasons.

1. Microneedling goes too deep in most cases. Ideally depths should be 0.2 mm at most. Over penetration of needles can lead to pigment dropout & worsening of melasma. 
2. Tranexamic acid has a very short half-life (2-4 hours). Intervals are too long for meaningful results. 
3. System therapy overcomes penetration issues.

What is the oral dose of tranexamic acid?

The optimal dose depends on what papers you cite. The most common dose is 500 mg, whilst the maximum dose is 2000 mg. Some studies suggest that higher doses are better, conversely other studies have shown that a lower dose is equally effective as higher doses. Be guided by your clinician. 

Is it safe in pregnancy?

T.acid is class B in pregnancy.  Animal studies have not detected a risk to the baby; however, no well-controlled human studies have been conducted. T.acid crosses the placental barrier and appears in cord blood with a concentration as high as maternal blood. 

On this basis, most dermatologists will not prescribe this drug if you are contemplating pregnancy or are pregnant. In the context of melasma pigmentation, the risks of morbidity (even as class B) is not warranted. 

What are the side effects of tranexamic acid?

Side effects are uncommon with tranexamic acid. 

• Oral (pill/tablet) side effects: irregular period cycles, tummy upsets, blood clots (very rare).

• Topical (cream) side effects: redness, skin irritation, stinging, dryness, flaking. More common after microneedling, higher incidence of side effects with higher concentrations of tranexamic acid. 

How do I incorporate Tranexamic Acid in my daily skin care routine?

AM: Gentle cleanser, then antioxidants*, SPF 50+ with iron oxide, 

PM: Cleanser, Tranexamic Acid 1.5 to 3% topically during the weekdays, option for other pigment correctors such as arbutin, azelaic acid, hydroquinone, or retinoids during the weekend. 

There are many different combinations, be guided by your clinician.

Give me some data on tranexamic acid & melasma- Please!

Here are some papers that you may want to research regarding tranexamic acid. 

Comparison of oral versus topical tranexamic acid for treatment of melasma

M Agrawal, Krishnendra Varma, Ujjwal Kumar, Shashank Bhargava 

Jul 2023-IP Indian journal of clinical and experimental dermatology-Vol. 9, Iss: 2, pp 84-89

Paper summary

• Oral tranexamic acid demonstrated a more promising therapeutic effectiveness compared to topical tranexamic acid for the treatment of melasma, as evidenced by a statistically significant difference in the mean percentage of reduction in MASI score from baseline at 12 weeks .

• Despite the gastrointestinal side effects observed with oral tranexamic acid, it had higher patient compliance, suggesting it could be a viable therapeutic approach for melasma .

• Topical tranexamic acid treatment was associated with side effects such as erythema, skin irritation, and xerosis .

• The study highlights the importance of considering both the efficacy and side effect profiles when choosing between oral and topical tranexamic acid for the treatment of melasma. 

Optimizing Melasma Management With Topical Tranexamic Acid: An Expert Consensus.

Desai, Chan, Handog, Lim. Mar 2023–Journal of Drugs in Dermatology–Vol. 22 4, pp 386-392

Paper summary

• Melasma is a challenging skin disorder that requires long-term management .
• Topical treatments, such as hydroquinone, are often used as first-line therapy for melasma, however there are concerns regarding long term use of HQ
• Topical tranexamic acid (TXA) alone or in combination with other modalities, such as patented delivery technology, is an alternative treatment option for certain patient profiles who have had prior therapy and/or are refractory to treatment .
• The paper aims to fill knowledge gaps by providing a summary of current evidence on topical TXA as a treatment for certain case profiles, highlighting its role in melasma management 

Use of Tranexamic Acid for Melasma

Taylor Bullock, Shilpi Khetarpal

01 May 2023–Advances in Cosmetic Surgery–Vol. 6, Iss: 1, pp 43-52

Paper summary

• Tranexamic acid is an effective off-label treatment for melasma, which can be used orally and/or topically with minimal side effects.
• Oral administration of tranexamic acid may be more effective than other routes of administration, but it comes with the risk of possible systemic side effects.
• Topical administration of tranexamic acid has been shown to be as effective as standard melasma treatments, but with fewer side effects. 

Intradermal Injection of 100mg Tranexamic Acid Versus Topical 4% Hydroquinone for the Treatment of Melasma: A Randomized, Controlled Trial.

Nader Pazyar, Motahareh Babazadeh Dezfuly, Maryam Hadibarhaghtalab, Seyedeh Yasamin Parvar

Jan 2023. The Journal of clinical and aesthetic dermatology–Vol. 16 1, pp 35-40

Paper summary

• Both intradermal injection of 100mg/mL tranexamic acid (TA) and topical application of 4% hydroquinone (HQ) significantly reduced the Melasma Area and Severity Index (MASI) score in female patients with melasma.
• There were no significant differences in the efficacy of TA and HQ in reducing the MASI score.
• Both treatments were well-tolerated, with participants experiencing only mild degrees of burning pain at the injection site.
• The study highlights the challenge of treating melasma, as it has a high recurrence rate even after treatment.

Comparison of oral versus topical tranexamic acid for treatment of melasma

M Agrawal, Krishnendra Varma, Ujjwal Kumar, Shashank Bhargava  +1 more

July 2023 Indian journal of clinical and experimental dermatology–Vol. 9, Iss: 2, pp 84-89

Paper summary

• Oral tranexamic acid demonstrated a more promising therapeutic effectiveness compared to topical tranexamic acid for the treatment of melasma, as evidenced by a statistically significant difference in the mean percentage of reduction in MASI score from baseline at 12 weeks .
• Despite the gastrointestinal side effects observed with oral tranexamic acid, it had higher patient compliance, suggesting it could be a viable therapeutic approach for melasma .
• Topical tranexamic acid treatment was associated with side effects such as erythema, skin irritation, and xerosis .
• The study highlights the importance of considering both the efficacy and side effect profiles when choosing between oral and topical tranexamic acid for the treatment of melasma.