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Tranexamic Acid Treatment for Melasma: Causes & Side effects

An oral approach to melasma

Published on 09/14/2019
Tranexamic Acid Melasma Treatment

Melasma is a very common skin condition that causes darkened discoloration of the skin known as hyperpigmentation. Though harmless, it is a cosmetic disturbance and can cause psychological distress for many of the individuals it afflicts.

What is Melasma?

Melasma causes brown to gray-brown patches, that appear symmetrically on the face, typically on the cheeks, forehead, bridge of the nose, chin, and upper lips.[1] Melasma is a result of overproduction of melanin, which is the dark pigment of the skin that is produced by cells called melanocytes. The hyperpigmentation can be localized superficially in the epidermis (known as epidermal melasma), more deep in the dermis (known as dermal melasma), or a combination of both. The location of the hyperpigmentation will affect the treatment plan.[1]

Who does melasma affect?

Melasma typically affects women during their reproductive years (20-50 years old), with men accounting for <10% of the overall cases. Individuals with darker skin, such as Latinos, African Americans, and Asians, are more prone to developing melasma, as they are predisposed to having more active melanocytes that produce melanin, compared to lighter-skin individuals.[2] Melasma is also common during pregnancy and is known as chlolasma or “the mask of pregnancy”.

Common causes of melasma

The exact cause of melasma remains unclear, but genetics, UV radiation, hormones, and heat exposure are all implicated in development of melasma. It is believed that all of these components play a part in its pathogenesis. However, one of the most important factors that causes melasma is sun overexposure. UV and blue light from the sun can stimulate melanocytes to produce more melanin, resulting in hyperpigmentation.[2]

Birth control pills, hormone replacement therapy with estrogen and/or progesterone, and pregnancy can trigger melasma in women because of increased levels of estrogen. In these cases, the melasma tends to disappear after the mother delivers the baby, or if the woman stops the birth control or hormone replacement therapy. However, it is always important to discuss medications with a physician before they are stopped.

Another possible cause of melasma is heat exposure. Any activity that involves exposing the skin to high temperatures, such as going to a sauna, can cause or worsen melasma. This may also explain why laser treatments can sometimes make melasma worse in certain individuals. Laser treatments can sometimes be too strong and create too much heat on the skin that damage skin cells known as keratinocytes and over-activate melanocytes to produce more melanin, resulting in postinflammatory pigmentation.[3]

Tranexamic Acid Treatment for Melasma

Tranexamic acid (TA) is an antifibrinolytic compound that functions to prevent the breakdown of fibrin which is important for forming clots. Essentially tranexamic acid prevents the breakdown of clots.[4] TA has been used to treat excessive blood loss in a variety of conditions such as an upper gastrointestinal bleeding and heavy menstrual bleeding, It can also be used to prevent bleeding when given prior to a surgery.[5]

Effectiveness of tranexamic acid treatment

Although hydroquinone is considered the gold standard for melasma treatment, it may provide only minimal to no resolution in many individuals with melasma. Furthermore, with its adverse effects including erythema, irritation, allergic skin rash, and paradoxical postinflammatory hypermelanosis, where the skin becomes even darker after hydroquinone treatment, many patients are seeking safer alternative treatments.[6] Compared to hydroquinone, TA may be as effective at reducing epidermal pigmentation. Therefore TA may be considered as another therapy for the treatment of melasma.[7]

There are three preparations of TA that can be used for the treatment of melasma:[8]

1) An injection into the dermis known as intradermal microinjection

2) Topical cream

3) Oral tablet

Patients typically start to notice lightening of the melasma around 2 months of treatment, with the average length of treatment lasting 4 to 6 months.[9]

TA treatment of melasma can be used as a monotherapy or as an adjuvant treatment with other current available treatments such as hydroquinone creams, glycolic acid peels, or laser treatments. As with any current treatment for melasma, wearing and reapplying sunscreen, particularly those that contains zinc oxide and titanium dioxide to fully block UV-A and UV-B, is a required regimen for the treatment and prevention of melasma.[1]

Side effects and contraindications

Side effects are rare, but include nausea, diarrhea, changes in color vision, blood clots, and allergic reactions.[4] For topical preparations, common side effects include erythema and irritation to the skin.

Inform your doctor if you pregnant before using TA. TA treatment is contraindicated in individuals with: 1) a previous history of stroke and/ or blood clots, 2) hypersensitivity or an allergic reaction to tranexamic acid, and 3) severe renal failure. Avoid concurrent use of any forms of tranexamic acid with any forms of birth control, as this can increase the risk of blood clot formation and stroke.[4]


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