Tranexamic acid has been used for many years for managing blood loss. It is also an effective treatment for melasma that has fewer side effects than hydroquinone. This makes it an appealing option for a skin condition that is resistant to medication and may require repeated treatment courses. While there is no commercially available preparation of tranexamic acid in topical form, it can still be obtained by taking advantage of the services of a compounding pharmacy.

What is Melasma?

Melasma describes pigmentation changes in the skin that include brown, discolored patches – most often on the face. The condition is most common in women and is associated with hormonal changes, genetics, and sun exposure although its exact cause is unknown. Exposure to UV rays tends to be a major trigger for a flare-up of melasma for most individuals.

What is Tranexamic Acid?

Tranexamic has been available since the 1960s and has an interesting history. Its main mechanism of action is preventing fibrinolyis, which reduces blood loss. It was first used to prevent heavy menstruation in women and then become more broadly used to control blood loss in a variety of situations. It may be used in surgery, to prevent postpartum bleeding, and to control nosebleeds. Dentists started using it in the form of a mouthwash in patients with bleeding disorders. The most recent use for tranexamic acid actually has nothing to do with controlling bleeding but utilizes a different mechanism of action of this drug. Tranexamic acid for melasma is being studied as an effective alternative to other medications that may have more severe adverse effects. While this drug was known to have an effect on melasma since at least 1979, it was not until recent studies comparing it to hydroquinone were published that doctors started to take notice.

How Does Tranexamic Acid Help Melasma?

Tranexamic acid competitively inhibits the activation of plasminogen activator. The anti-plasmin activity of tranexamic acid is thought to be the reason it is so effective for treating melasma.  When UV-radiation reaches the skin, it initiates processes that lead to the conversion of plasminogen to plasmin. This conversion leads to increased melanin synthesis. When plasmin activity is limited by tranexamic acid, this inhibits the melanin synthesis that causes pigmentation changes associated with melasma.

Research on Tranexamic Acid for Melasma

Most studies on topical treatment for melasma utilize the Modified Melasma Area and Severity Index (MASI). The index divides the face into four regions that are rated on their darkness and area of involvement. This includes the forehead, right malar, left malar, and chin. The rating system has been found to be reliable across different reviewers and provides a consistent measurement of melasma treatment across studies. The effectiveness of tranexamic acid for melasma is determined by comparing MASI scores with either a placebo or another anti-pigmentation agent like hydroquinone.

Many studies have demonstrated that tranexamic acid is effective orally, in a topical cream, and in the form of an intradermal injection. A topically applied cream on its own may be effective, and eliminates possible gastrointestinal or systemic effects associated oral administration of a drug. Thromboembolism may be a rare but serious risk associated with oral administration of topical tranexamic acid. Less serious side effects of orally administration of this drug include abdominal bloating, nausea, and heartburn.

Some studies have shown that topical tranexamic acid is just as effective as hydroquinone but produces fewer side effects. One study compared topical tranexamic acid 5% with hydroquinone 2%. Group A was the tranexamic acid group and group B was the hydroquinone group:

“The mean MASI score in both treatment groups decreased considerably after completion of treatment and was not significant between the two groups. No side effects were detected in group A, but 10% of those in group B complained of drug-related side effects including erythema and skin irritation (p = 0.131).”

As was demonstrated in this small-scale study, tranexamic acid and hydroquinone are both effective at reducing melasma. However there may be less skin irritation associated with tranexamic acid. Especially for patients who have sensitive skin, an alternative to hydroquinone can be a great benefit.

When using a topical medication, one problem is making sure that the product penetrates the skin to the targeted treatment area. A study was conducted that used topical tranexamic acid combined with microneedling to achieve this. Medications can often more effectively penetrate the outer layers of the skin when they are applied topically in combination with a microneedling treatment. The small needles of the device puncture the skin and provide a way for the medication to reach deeper. When using microneedling, a topical numbing cream like BLT cream is often required.

Side Effects of Tranexamic Acid Compared to Hydroquinone

Hydroquinone has long been the gold standard for managing melasma and hyperpigmentation in general. Topically applied hydroquinone is effective at reducing melasma but can cause severe irritation and redness for some patients. One of the main benefits of using tranexamic acid cream over hydroquinone is that it offers a lower incidence of side effects and decreased irritation. In the majority of studies to-date, patients have not discontinued treatment with topical tranexamic cream due to side effects.

Tranexamic acid cream is often made by our compounding pharmacy in 2%, 3%, and 5% strengths. Contact us today for more information about this treatment for melasma.

Articles

Interpretability of the Modified Melasma Area and Severity Index (mMASI) – JAMA

Therapeutic Effects of Topical Tranexamic Acid in Comparison with Hydroquinone in Treatment of Women with Melasma. – PubMed

Tranexamic Acid for Adults with Melasma: A Systematic Review and Meta-Analysis – BioMed Research International