What Is The Best Oral Tranexamic Acid Dosage For Hyperpigmentation?

What Is The Best Oral Tranexamic Acid Dosage For Hyperpigmentation?

Oral tranexamic acid is a promising skincare therapy with long-term benefits for stubborn melasma and other hyperpigmentation conditions. Putting aside the excitement for a moment, it’s important to remember that oral tranexamic acid is a prescription-only medicine used to treat bleeding disorders. As such, understanding oral tranexamic acid dosages is crucial to understanding how it works.

When used to treat skin hyperpigmentation disorders, it is said to be in use ‘off-label,’ that is, in a way that the original FDA approval does not indicate (Chauncey). Nevertheless, due to its safety and a lack of side effects at low dosages, it has found wide adoption among dermatologists who have been treating melasma patients with it for decades.

This article looks at the oral tranexamic acid dosage for hyperpigmentation, discussing both higher and lower levels and what each means.

Oral tranexamic acid dosage for hyperpigmentation

Tranexamic acid appears to have different effects on the body at different dosage levels. For example, at high dosage levels (over 3,000mg/day), its blood clotting properties are prominent, but at low ones (under 1,500mg/day), they are virtually non-existent.
Oral tranexamic acid dosages for hyperpigmentation typically fall on the lower end of the dosage spectrum compared to those given for bleeding disorders. However, within this lower range is a sub-range, normally ranging from 500mg to 1500mg per day.

When treating hyperpigmentation, dermatologists will typically prescribe a well-tolerated dosage that provides the maximum benefits. Since each individual has a different tolerance level and treatment needs, the exact dosage will vary from one person to another.

However, what does not change is the range. Dermatologists prescribe oral tranexamic acid below the 1500mg threshold because it is still effective at these levels. Doing so also reduces the risk of clotting, which can cause embolisms, deep vein thrombosis, and possibly stroke.

Conversely, doses lower than 250 mg appear not to have any visible effects on melasma and will not be effective.

The perfect oral tranexamic acid dosage for hyperpigmentation effectively treats hyperpigmentation without increasing the risk of blood clots.

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The effects of low oral tranexamic acid dosage for hyperpigmentation

A low oral tranexamic acid dosage for hyperpigmentation is typically between 500mg and 750mg per day, divided into two equal doses. For example, 500mg per day might be prescribed as one 250mg tablet twice a day.

One research study found that doses at this level effectively treated melasma and that test subjects were happy with the outcomes (Zhu). In another clinical trial, 250mg per day was used.

Based on current research, a low oral tranexamic acid dosage for hyperpigmentation is effective in treating hyperpigmentation. Although more research is required, the study found some side effects: mild stomach discomfort and decreased menstruation. The study concluded that taking oral tranexamic acid at dosages between 500mg and 750mg was safe for long-term hyperpigmentation treatment, with a low risk of severe side effects.

Effects of high oral tranexamic acid dosage for hyperpigmentation

High doses of oral tranexamic acid for hyperpigmentation are between 1000mg and 1500mg per day, divided into two equal doses. For example, 1500mg per day might be prescribed as one 750mg tablet twice a day.

When test subjects took high dosages for several weeks, researchers were surprised to find that the results were the same as for the test subjects who took between 500mg and 750mg per day (Zhu). While more research is needed to prove these findings further, it can be assumed based on current studies that taking higher doses will not provide better results.

On the other hand, higher doses might cause some additional side effects, albeit mild ones. In the study, some test subjects reported decreased menstruation, a known effect of oral tranexamic acid when taken at higher dosages.

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The verdict

From available research data, it appears that taking an oral tranexamic acid dosage for hyperpigmentation of between 500mg and 1500mg will give the same results (Zhu). However, at higher dosages, the possibility of clotting risk heightens. Therefore, the data appears to support taking lower doses to get positive results and lower the risk of clotting.


Brandon Kirsch

Brandon Kirsch, MD, FAAD, is a board-certified dermatologist specializing in clinical drug development and medical innovation. He is the founder of Kirsch Dermatology in Naples, Florida and is also the Chief of Dermatology at the Naples Community Hospital. Kirsch Dermatology Website Dr. Kirsch started his career as a lawyer and holds law degrees from the University of Western Ontario (LL.B.) and Georgetown (LL.M. Securities and Financial Regulation). Dr. Kirsch completed his pre-medical studies at the University of Pennsylvania, medical school at Brown University, internship at the Mayo Clinic (Florida) and dermatology residency at the University of North Carolina. In partnership with the Mayo Clinic, he filed to patent a novel topical composition for the treatment of skin hyperpigmentation that he co-developed and also oversaw a successful pilot study of the formulation. Dr. Kirsch has experience with therapeutic drug development programs from pre-clinical to Phase 3 studies. He is licensed to practice medicine in California, Colorado, Florida, and North Carolina and law in New York and Ontario.

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