Tranexamic Acid for Melasma: The Science, Safety & Success Rate in Malaysian Patients

Key Takeaways:

• Tranexamic acid (TXA): is an antifibrinolytic agent originally used to control bleeding, now repurposed as an effective treatment for melasma, especially in resistant cases.
• It’s available: in various forms, allowing for treatment through oral tablets, topical creams or serums, and sometimes, as targeted injections.
• TXA works: by blocking plasmin formation, which helps reduce melanocyte activity and melanin production, offering anti-inflammatory, anti-melanogenic, and anti-angiogenic effects.
• Most patients see results: within 8 to 16 weeks of oral TXA use (250 mg three times daily), though long-term use up to 28 months may be needed for maintenance in some cases.

Introduction

Melasma is a cutaneous hyperpigmentation disorder that affects one’s cheeks, chin, forehead, nose, and upper lip.

Because it’s difficult to conceal, many affected individuals often feel self-consciousness and diminished self-confidence.

Fortunately, several interventions have emerged to address both its physical and psychological impacts.

Among these is tranexamic acid (TXA). TXA is gaining traction as an effective treatment option for cases that don’t respond to traditional topical therapies.

Oral TXA has demonstrated significant improvements in melasma severity, with clinical trials demonstrating appreciable reductions in pigmentation.

Furthermore, high patient satisfaction has been reported as TXA has been linked to marked improvements in quality of life.

This article aims to explore this promising intervention, its scientific basis, safety profile, and success rate among Malaysian patients seeking effective treatment options

What is Tranexamic Acid?

Tranexamic acid (TXA) is essentially a synthetic medication classified as an antifibrinolytic agent. In practice, it prevents the breakdown of blood clots by inhibiting the transformation of plasminogen to plasmin, an enzyme responsible for clot degradation.

Available in mouthwash, tablet, and injection form, it effectively reduces or prevents excessive bleeding across various medical conditions.

For instance, heavy nosebleeds, menstrual bleeding, dental procedures, surgeries, trauma-related haemorrhage, and hereditary angioedema.

Originally prescribed for excessive bleeding, TXA has gained traction as an effective treatment for melasma patients who don’t respond to topical therapies.

In fact, research has shown that TXA reduces melanin synthesis by inhibiting plasmin activity in one’s skin.

In practice, plasmin plays an indispensable role in regulating melanocyte function and pigment production.

How Tranexamic Acid works for Melasma?

Tranexamic acid (TXA) primarily treats melasma by inhibiting the activation of plasminogen to plasmin in the skin.

Ultraviolet (UV) radiation natively induces keratinocytes to produce plasminogen activator, which then converts plasminogen into plasmin.

By increasing tyrosinase activity and stimulating the release of inflammatory mediators, plasmin subsequently promotes melanogenesis.

Melanogenesis is a complex biomolecular process that activates melanocytes to produce melanin.

In practice, TXA suppresses plasmin to achieve anti-inflammatory, anti-melanogenic, and anti-angiogenic actions. These actions enable it to be an effective intervention for treating melasma.

Since tranexamic acid doesn’t bleach the skin, it offers a safer profile for long-term use compared to other melasma treatment options, such as hydroquinone.

Hydroquinone is also a direct inhibitor of the tyrosinase enzyme. However, prolonged use may lead to ochronosis, skin irritation, and other adverse effects.

TXA, on the other hand, indirectly regulates melanogenesis without whitening the skin or producing toxicity.

Oral Tranexamic Acid for Melasma

Oral tranexamic acid (TXA) is a promising intervention for melasma, owing to its demonstrated efficacy, safety, and ease of administration.

Efficacy and dosage

• Optimal Dosage: Authoritative studies suggest that the most effective regimen for oral TXA in treating melasma is 250 mg taken three times daily for 12 consecutive weeks.

• Success Rate: Patients typically notice significant improvements in melasma severity within 8 to 16 weeks of consistent use.

In fact, many have reported fair to excellent results after just 1–2 months of treatment.

Tranexamic Acid tablets for Melasma side effects

• Common Side Effects: The most common reported side effects of TXA have been bloating, nausea, and stomach upset.

However, these mild gastrointestinal discomforts are generally well tolerated.

• Serious Side Effects: Although rare, serious adverse events like deep vein thrombosis (DVT) and stroke have also been reported.

This means medical supervision and screening for clotting risk factors before and during treatment are imperative.

Overall, oral TXA remains a safe and effective alternative for managing melasma when used under appropriate supervision.

Tranexamic Acid injections for Melasma

 

Tranexamic acid injections, also known as intradermal tranexamic acid, involve injecting the medication directly into hyperpigmented lesions.

This targeted intervention exhibits anti-inflammatory, anti-melanogenic, and anti-angiogenic properties to treat melasma patients who aren’t responding to topical treatments.

These are rarely required, and only considered for a small fraction of patients. They are given as spot treatment combined with other options.

Mechanism and efficacy

• Localised Treatment: Intradermal injections of TXA deliver the medication directly into melasma-affected skin, thereby allowing for highly targeted action with minimal systemic absorption.

• Efficacy: Clinical studies have demonstrated appreciable improvement in melasma severity when intradermal TXA injections are employed.

For example, this study showed a 40% reduction in the Melasma Area and Severity Index (MASI) score for all participants. However, recurrence occurred without maintenance therapy.

Tranexamic Acid injection side effects

• Common Side Effects: TXA injections for melasma may occasionally cause mild reactions such as swelling, bruising, erythema, and a burning sensation at the injection site. However, these localised side effects are generally transient and easily tolerated.

• Serious Side Effects: Rare allergic reactions have been noted in some patients. This highlights the mission-critical nature of medical supervision during treatment.

Overall, systemic side effects are uncommon due to the low doses utilised in intradermal injections compared to oral administration.

Topical Tranexamic Acid for Melasma

Topical TXA for melasma is a treatment applied directly to one’s skin in the form of creams, serums, or gels.

However, it may have limited penetration compared to oral or injectable forms, which can affect its potency in treating deeper melasma lesions.

Formulations and applications

• Creams and Serums: Topical TXA is available in cream and serum forms, with concentrations ranging from 2% to 5%.

• Application: These TXA products are typically applied once daily, preferably at night. However, it is essential to cleanse and moisturise the skin before application to maximise absorption and minimise sun exposure during treatment.

Topical Tranexamic Acid safety

• Efficacy: Topical TXA has been found effective, particularly for epidermal-type melasma.

Reputable studies have shown significant reductions in pigmentation and Melasma Area and Severity Index (MASI) scores, although results may vary depending on an individual’s skin type and severity.

• Safety: Topical TXA is generally well-tolerated, with a lower incidence of irritation compared to traditional agents, such as hydroquinone.

However, individuals with sensitive skin are advised to always perform a patch test before application to avoid potential irritation.

How long can you take Tranexamic Acid for Melasma?

According to clinical research, most people experience measurable improvements between 8 and 16 weeks of regular TXA use. This is with an ideal dosage of 250 mg, taken three times daily.

Some patients continue oral TXA medication for longer than six months, often up to 28 months. This routine significantly improves pigmentation and reduces the severity of melasma.

Since TXA works by temporarily inhibiting melanin synthesis rather than curing melasma, melasma may recur after the medication is stopped.

As such, dermatologists often recommend individualised treatment plans that may dictate maintenance dosing with periodic breaks.

Remember, careful medical supervision is essential, especially for patients with risk factors for thromboembolism.

Can Tranexamic Acid be used with other Melasma treatments?

Tranexamic acid (TXA) is generally considered safe for use in conjunction with other common melasma treatments.

When combined with topical therapies like hydroquinone, retinoids, or corticosteroids, TXA doesn’t interfere with their efficacy.

In fact, most studies report no significant adverse interactions. Rather, an enhancement in overall results is achieved by targeting different pathways in melanogenesis.

Overall, most dermatologists emphasise that TXA is most effective as part of a multimodal regimen, particularly for refractory cases.

Tranexamic acid for Melasma in Malaysian patients

In Malaysia, melasma is a prevalent pigmentary illness that primarily affects women with darker skin tones. In fact, Malaysian women are disproportionately affected, with a female-to-male ratio of between 4:1 to 6:1.

In Malaysia, the management of melasma is considerably influenced by environmental and cultural factors.

Sun exposure is a key cause of melasma exacerbations in the country’s tropical environment. As such, strict sun protection is an essential component of any treatment plan.

To reduce UV exposure during therapy, patients are encouraged to employ physical barriers like umbrellas and caps as well as broad-spectrum sunscreens.

Furthermore, oral and topical tranexamic acid (TXA) is slowly becoming more common as a therapeutic alternative. However, accessibility varies depending on the healthcare setting and geographical location.

To ensure safe and efficient management tailored to each patient’s needs and cultural customs, patients are recommended to specialist facilities like Clique Clinic.

Patients can avail of customised individual treatment plans that may include TXA, in addition to other topical medications or procedures.

Conclusion

Melasma is a very common acquired disorder of hyperpigmentation. Fortunately, interventions like Tranexamic acid (TXA) offer an effective multimodal mechanism of action to counteract its effects.

Mechanistically, TXA inhibits plasminogen activation. Thereby, appreciably reducing melanocyte activity and subsequent pigmentation. It may be administered either orally, topically, or via intralesional injection.

TXA is generally a safe and efficacious intervention for refractory melasma. Topical and intralesional TXA applications tend to have mild, localised side effects such as transient erythema or burning.

Oral TXA may cause systemic side effects like abdominal pain and nausea. In rare cases, melasma patients may experience severe complications due to clotting disorders or other contraindications.

However, its use should be individualised, with careful screening for risk factors and ongoing monitoring by a dermatologist for adverse effects.

Book a consultation with us today at Clique Clinic and take the first step toward healthier, glowing skin. WhatsApp our team: wa.me/60123537960.