Transexamic acid works differently from other skin lightening ingredients to treat skin hyperpigmentation.

It can be combined with other skin whitening products in your skin care routine.

But- the best products have at least 1% TXA in them.

• SkinCeuticals Discoloration defense
• Derma Made Mela fade
• Murad Replenishing Multi-Acid Peel
• La Roche-Posay Glycolic B5 10% Serum
• PCA Skin Pigment Gel PRO

SkinCeuticals Daily Brightening UV Defense SPF

TXA blocks melanin production through a 3 step process:

1. Inhibits plasmin
2. Decreases tyrosinase activity in melanocytes
3. Reduces prostaglandin synthesis

It only works well on hyperpigmentation caused by increased blood flow to the skin. (at least that is the current belief but studies are ongoing.)

Tranexamic acid is use to treat hyperpigmentation. When used orally and topically it can improve:

• melasma
• post inflammatory hyperpigmentation (PIH) ⁽⁴⁾
• hyperpigmentation
• solar lentigos

Topical tranexamic does not prevent PIH, but has been shown to speed clearing of post inflammatory pigmentation. ⁽¹⁾

Injected intradermal tranexamic acid has been shown to prevent PIH. ⁽⁴⁾

Topical tranexamic acid should not be used if you have an allergy to TXA.

No. Tranexamic is not an exfoliant.

Hydroquinone is usually much more effective than TXA topically.

This is because topical TXA is usually a very low dose in cosmeceuticals while hydroquinone is prescription and is usually 4-10%.

TXA does not absorb as well into the skin as hydroquinone does.

In research trials that use 3-5% of TXA, we see that TXA might work as well as hydroquinone.

Here are the research studies:

2014: A randomized, split-face trial compared 3% topical TXA versus 3% HQ and 0.01% dexamethasone used twice daily for 12 weeks. The improvement was better in the TXA group but the difference was not statistically significant. ⁽⁹⁾

2015: A study compared 5% TXA versus 4% HQ cream for the treatment of melasma and did not find a statistically significant difference between the 2 groups. ⁽¹⁰⁾

2017: Another study in 2017 compared 5% TXA with 2% hydroquinone and did not show a statistical difference. ⁽¹¹⁾

Oral tranexamic acid is much more effective than topical hydroquinone for treating melasma.

The topical formulations of TXA are not as effective as TXA orally or injected into the skin.

TXA pills and injections work much better than hydroquinone.

TXA does not tend to react with other ingredients so it can be mixed with retinol, AHA, BHA, hydroquinone, vitamin C, kojic acid, arbutin and other skin lightening ingredients.

These are good skin lightening ingredients to use together because they work in 2 different ways.

These are great ingredients to use together but they should be used at different times in your skin care routine.

It is a good idea to use HA serums and TXA together because:

• TXA absorbs poorly
• HA increases absorption of TXA into the skin

Is TXA right for you? When is the best time to use it in your skin care routine?

We can help you build the best skin care routine for your Baumann Skin Type.

TXA is used in 3 main ways:

1. topically in skin serums and creams
2. injected into dark spots
3. orally in a tablet pill form

Topical TXA is included in skin care products with formulations at a dose of up to 5% ^(8).

The most effective TXA skin care products have at least 1% of TXA.

TXA absorbs poorly so the products that you combine with it in your skin care routine matters a lot!

TXA is injected into skin and after microneedling i to treat dyschromia.

It comes in a liquid form and most protocols use 4–100 mg/mL.

Several studies have looked at intradermal TXA or TXA applied after microneedling, however there is no consensus on dose and how often to inject.

At this time it is too early to say if TXA is an effective treatment when used in this manner. ⁽¹²⁾

Oral tranexamic acid is not approved by the FDA but it is often used to treat melasma.

It works by decreasing blood flow to the skin.

This means that TXA will NOT work on dark spots that are not caused by an increased blood flow.

The most commonly used dose of TXA for melasma is350 mg two times a day. a 600mg tablet is broken in half to give a dose of 350 mg.

Many studies show oral TXA works well to treat melasma.

In one study, 44 patients with melasma took 250mg of TXA by mouth two times a day for 3 months. ⁽⁷⁾

They had a 49% improvement of melasma as assessed by the MASI score.

Many other studies have shown efficacy as well.

It is unknown how long the skin whitening effects of TXA will last, but they are not permanent.

Melasma tends to recur and relapse. This is seen after TXA treatment as with any other melasma treatments.

In one study ^(7), 26% of patients continued to show improvement at 3 months (49% had improvement at end of the study)- so only about half still showed improvement at 3 months.

You can help prevent recurrence of melasma after stopping tranexamic acid with:

Two skin care routines for melasma- a maintenance regimen and a treatment regimen

Habits to minimize pigmentation and help get rid of melasma

Treating melasma from the inside with anti-inflammatory diet and supplements

There is no consensus on how long TXA should be used. Most doctors have you take it until melasma clears or for 3 months.

We do not know many things about using TXA for melasma:

1. Should be a treatment holiday?
2. How long it is safe to take?
3. How common is relapse?
4. How long after stopping tranexamic acid does it recur?

TXA is a promising medication for the treatment of melasma, but more studies and clinical experience is needed to determine the most effective treatment and maintenance protocols.

The most common side effects are GI complaints such as nausea and diarrhea.

Blood clots are a risk with TXA, but clots have not to my knowledge been reported in patients taking TXA for melasma treatment.

Oral TXA Tranexamic acid can increase the risk of blood clots when used orally.

Do not take the tranexamic acid pills if you:

• are on estrogen containing oral contraceptives
• are taking estrogen for hormone replacement therapy
• have a history of blood clots
• have an increased risk of blood clots
• are planning a very long flight or time period of inactivity such as bed rest
• are pregnant

Do not take tranexamic acid pills if you have any of these medical issues:

• Acute promyelocytic leukemia patients on oral tretinoin
• History of blood clots,
• History of deep vein thrombosis
• History of pulmonary embolism
• History of stroke
• Stroke
• Kidney disease—The effects may be increased because of slower removal of the medicine from the body.
• Pregnancy
• Breastfeeding

Discuss with your doctor before taking TXA if you are on any of these because of increased risk of blood clots:

• Desogestrel
• Dienogest
• Drospirenone
• Estradiol
• Ethinyl Estradiol
• Ethynodiol
• Etonogestrel
• Gestodene
• Levonorgestrel
• Medroxyprogesterone
• Mestranol
• Nomegestrol
• Norelgestromin
• Norethindrone
• Norgestimate
• Norgestrel
• Segesterone

The best way to know if oral or injected TXA is a good option for you is to see one of our doctors or medical providers.

• Trans-4-aminomethylcyclohexanecarboxylic acid
• trans-AMCHA
• TXA
• Melasma pill
• Melasma tablet

Wondering if topical TXA is good for your skin type?

WE can help!

1. Rutnin, S., Pruettivorawongse, D., Thadanipon, K., & Vachiramon, V. (2019). A prospective randomized controlled study of oral tranexamic acid for the prevention of postinflammatory hyperpigmentation after Q?switched 532?nm Nd: YAG laser for solar lentigines. Lasers in Surgery and Medicine, 51(10), 850-858.
2. Sirithanabadeekul, P., & Srieakpanit, R. (2018). Intradermal tranexamic acid injections to prevent post-inflammatory hyperpigmentation after solar lentigo removal with a Q-switched 532-nm Nd: YAG laser. Journal of Cosmetic and Laser Therapy, 20(7-8), 398-404.
3. Forbat, E., Al?Niaimi, F., & Ali, F. R. (2020). The emerging importance of tranexamic acid in dermatology. Clinical and Experimental Dermatology, 45(4), 445-449.
4. Lindgren, A. L., Austin, A. H., & Welsh, K. M. (2021). The use of tranexamic acid to prevent and treat post-inflammatory hyperpigmentation. J Drugs Dermatol, 20(3), 344-345.
5. Hasegawa, K., Fujiwara, R., Sato, K., Park, J. Y., Kim, S. J., Kim, M., & Kang, H. Y. (2016). Increased blood flow and vasculature in solar lentigo. The Journal of dermatology, 43(10), 1209-1213.
6. Baumann L. Ch 41 Depigmenting Ingredients in Baumann's Cosmetic Dermatology 3rd edition (McGraw hill 2022)
7. Del Rosario, E., Florez-Pollack, S., Zapata Jr, L., Hernandez, K., Tovar-Garza, A., Rodrigues, M., ... & Pandya, A. G. (2018). Randomized, placebo-controlled, double-blind study of oral tranexamic acid in the treatment of moderate-to-severe melasma. Journal of the American Academy of Dermatology, 78(2), 363-369.
8. McKesey, J., Tovar-Garza, A., & Pandya, A. G. (2020). Melasma treatment: an evidence-based review. American journal of clinical dermatology, 21(2), 173-225.
9. Ebrahimi B, Naeini FF. Topical tranexamic acid as a promising treatment for melasma. J Res Med Sci. 2014;19(8):753–7.
10. Banihashemi M, Zabolinejad N, Jaafari MR, Salehi M, Jabari A.Comparison of therapeutic effects of liposomal Tranexamic Acid and conventional Hydroquinone on melasma. J Cosmet Dermatol. 2015;14(3):174–7.
11. Atef N, Dalvand B, Ghassemi M, Mehran G, Heydarian A. Theraputic effects of topical tranexamic acid in comparison with hydroquinone in treatment of women with Melasma. Dermatol Ther (Heidelb). 2017;7(3):417–24.
12. McKesey, J., Tovar-Garza, A., & Pandya, A. G. (2020). Melasma treatment: an evidence-based review. American journal of clinical dermatology, 21(2), 173-225.
13. Wang, J. V., Jhawar, N., & Saedi, N. (2019). Tranexamic acid for melasma: evaluating the various formulations. The Journal of clinical and aesthetic dermatology, 12(8), E73.
14. Hasegawa, K., Fujiwara, R., Sato, K., Park, J. Y., Kim, S. J., Kim, M., & Kang, H. Y. (2016). Increased blood flow and vasculature in solar lentigo. The Journal of dermatology, 43(10), 1209-1213.
15. Nakamura, M., Morita, A., Seité, S., Haarmann?Stemmann, T., Grether?Beck, S., & Krutmann, J. (2015). Environment?induced lentigines: formation of solar lentigines beyond ultraviolet radiation. Experimental dermatology, 24(6), 407-411.