One skin care ingredient that has been discussed a lot recently is tranexamic acid. This product was initially developed to reduce bleeding and is still most commonly used for this purpose. However many dermatologists are now prescribing tranexamic acid to treat conditions of the skin including melasma. This ingredient has a favorable side effect profile compared to some others used to treat melasma and has been shown to be effective in clinical trials in both oral and topical form. Recent articles in InStyle and Allure have discussed the ingredient’s benefits and current prevalence in skin care.
Tranexamic acid works well with other skincare products, which means that you can safely use it with many other ingredients. Our compounding pharmacy makes tranexamic cream in various strengths as well as a combination cream with tranexamic acid, kojic acid, and niacinamide.
Does tranexamic acid have side effects?
Topical tranexamic acid has been shown to have few side effects. However its use as an agent to stop bleeding means that it should be carefully prescribed for people with cardiovascular disease, cerebrovascular disease, and who are using hemostatic agents. Although topical use should not result in any side effects, using other topical medications concurrently with the cream can result in increased irritation. Abrasive soaps, cleansers, and cosmetics, and topical products with high levels of alcohol or astringents, can also increase irritation. Salicylic acid, resorcinol, and sulfur containing products should not be used with tranexamic acid cream.
Comparison with hydroquinone
One of the most commonly prescribed treatments for changing the pigment of the skin is hydroquinone. Hydroquinone is a bleaching agent that is highly effective at treating hyperpigmentation from various causes. In studies to-date, tranexamic acid has been found to be less irritating than hydroquinone but equally effective (not necessarily more effective).
Tranexamic acid is potentially less irritating than hydroquinone and has less of a risk of unwanted pigmentation changes. In a study comparing hydroquinone with tranexamic acid, it was shown that 19/50 patients in the hydroquinone group experienced erythema and irritation while only 3/50 patients in the tranexamic acid group experience the same side effects. The reduction in MASI in both groups was similar – showing that tranexamic acid is as effective as hydroquinone. However patient satisfaction scores in the tranexamic acid group were higher, likely due to the reduced incidence of side effects.
In a separate study comparing the same treatments – hydroquinone and tranexamic acid – the researches similarly found that the results were comparable. However, they concluded that “a low complication rate in the group receiving TXA [tranexamic acid] could lead to the high patient satisfaction, while the prescription of hydroquinone led to skin irritation and erythema in 10% of cases, resulting in high dissatisfaction of treatment protocol.” The satisfaction level for the tranexamic acid group was 33% vs. 6.7% in the hydroquinone group.
How does it work to treat melasma?
The exact mechanism of action of tranexamic acid for dermatological conditions is not completely understood. For melasma, it decreases the production of melanin in the skin likely by inhibiting the interaction by keratinocytes and melanocytes. Melanin production creates the dark brown patches on the face, which are a defining characteristic of the condition. It is possible that tranexamic acid both reduces melasma patches and prevents UV-induced melasma.
One theory is that tranexamic acid’s plasmin inhibition results in prevention of UV triggered melasma. Ultraviolet (UV) radiation is significantly correlated to flare-ups of melasma. Sun exposure starts a series of reactions in the skin that increases plasmin activity in skin cells and stimulates the production of melanin. Plasmin is also crucial in the release of basic fibroblast growth factor (FGF) which is a potent melanocyte growth factor. Tranexamic acid is a plasmin inhibitor that prevents UV-induced pigmentation changes. However it does not affect healthy skin that was not exposed to UV radiation.
Oral tranexamic acid has been studied extensively as it is commercially available. Studies show that it can effectively treat melasma and has few side effects (though there are some important contraindications to consider).
Tranexamic Acid as a Combination Treatment
Tranexamic acid has been shown to be effective when combined with other in-office dermatological treatments like lasers and microneedling. Microneedling has been used in conjunction with many different topical treatments. The small perforations in the skin that are made during microneedling may improve dispersion and penetration of a topically applied medication. In a small study, it has been shown that the combination of topical tranexamic acid with microneedling provides better results than microinjections (mesotherapy) of tranexamic acid. Another study that was a split-face study (one side control, the other side medication) demonstrated that on the test side, there was 65.92% improvement in the mean MASI score compared with 20.75% on the control side at the end of 8 weeks.
Is Tranexamic Acid Cream Commercially Available?
Tranexamic acid tablets are available commercially. They are sold as a generic medication and under the brand name Lysteda. Lysteda is an oral tablet that comes in 650mg doses and is primarily indicate for managing heavy menstrual bleeding. Tranexamic acid also is available as a solution, which is often what has been used in studies to examine topical effects. A cream that can be applied to the affected area is not available and must be made by a compounding pharmacy. Many medications that are used to treat skin conditions are applied as a cream and this is generally an effective way to get the medication to the area while minimizing systemic effects.
In addition to 2-5% tranexamic acid creams, our pharmacy also makes a combination cream with tranexamic acid 3%, kojic acid 4%, and niacinamide 5%.
Articles
A Randomized Controlled Study Comparing the Efficacy of Topical 5% Tranexamic Acid Solution versus 3% Hydroquinone Cream in Melasma – Journal of Cutaneous and Aesthetic Surgery
Therapeutic Effects of Topical Tranexamic Acid in Comparison with Hydroquinone in Treatment of Women with Melasma – Dermatology and Therapy
A Randomised, Open-label, Comparative Study of Tranexamic Acid Microinjections and Tranexamic Acid with Microneedling in Patients with Melasma – Journal of Cutaneous and Aesthetics Surgery
Clinical Efficacy of Topical Tranexamic Acid With Microneedling in Melasma – Dermatologic Surgery
Oral Tranexamic Acid for the Treatment of Melasma: A Review – Dermatologic Surgery