Tranexamic Acid: Essential in Your Regimen for Pimple Marks Removal

Acne marks is a major concern of patients experiencing acne breakouts. Acne leaves these dark and red discoloration on the skin, lasting for weeks to even years, further impacting a person's self-image, at times leading to anxiety and social withdrawal.

If you are dealing with acne marks, Tranexamic acid can be a potential game-changer in your skincare routine. This ingredient specifically targets stubborn dark spots and red acne marks by disrupting melanin production and inducing anti-inflammatory effects, improving the appearance of post-inflammatory hyperpigmentation (PIH) and post-inflammatory erythema (PIE) left behind by acne.

Be ready to face the next stage of your acne journey by tackling acne marks strategically with Topical Tranexamic acid.

Understanding Tranexamic Acid and Its Role in Skincare

What is Tranexamic Acid?

Originally, Tranexamic acid is an oral medication mainly used to treat or prevent excessive bleeding in various situations such as major trauma, surgery, and dental procedures. Tranexamic acid helps prevent bleeding by inhibiting the breakdown of blood clots. Recently, it has been recognized for its potential skin lightening effects, beneficial for conditions such as melasma and post-inflammatory hyperpigmentation (PIH). Tranexamic acid induces its anti-hyperpigmentation effect by inhibiting plasmin, which is thought to be involved in the activation of certain growth factors [1, 2] that stimulate melanocytes to produce pigment in the skin.

Chemical Structure: Tranexamic acid is a synthetic derivative of the amino acid lysine, consisting of a central amino group (-NH2) and a carboxylic acid group (-COOH) attached to the lysine backbone.

Molecular Size and Stability: It has a molecular weight of around 157.21 g/mol [3], falling within the range considered small for skincare ingredients. Smaller molecules generally have a greater ability to penetrate the skin compared to larger ones. This allows good penetration into the upper layers of the epidermis such as the stratum corneum. Smaller molecules tend to be more mobile within a formulation and may interact less with other ingredients, potentially improving overall stability of the product.

pH: Tranexamic acid in skincare is typically formulated at a pH between 3.5 and 4.5. The low pH of Tranexamic acid formulations helps to maintain the stability of the compound and optimize its penetration into the skin. Tranexamic acid is more stable in acidic environments, which is why formulations with lower pH values are preferred.

Solubility: It is water-soluble, which means it can be easily incorporated into water-based skincare products like serums or gels

Tranexamic Acid Classification: Improvement of hyperpigmentation is the established use of Tranexamic acid for skin, placing it within the category of brightening agents in the spectrum of skincare solutions. It has been shown to be effective against melasma and post-inflammatory hyperpigmentation (PIH) and its ability to suppress redness through its anti-inflammatory effects may extend its application to post-inflammatory erythema (PIE) and rosacea.

Tranexamic Acid and Dark Acne Marks

What is Post-Inflammatory Hyperpigmentation?

Dark acne marks are a type of post-inflammatory hyperpigmentation. It develops as darkened areas of skin after acne lesions heal. Inflammation triggers the release of inflammatory mediators, which stimulate melanocytes (pigment-producing cells) to produce more melanin in an attempt to heal the damaged area. This excess melanin production can lead to visible hyperpigmentation after the inflammation subsides

How does Tranexamic acid help improve Post-Inflammatory Hyperpigmentation?

• Indirect Inhibition of Melanin Production: Tranexamic acid interferes with the activation of plasminogen to plasmin, an enzyme involved in various physiological processes. Plasmin activation leads to the activation of other enzymatic activities necessary for melanin synthesis. By inhibiting plasminogen activation, Tranexamic acid may indirectly suppress the activity of enzymes crucial for melanin production.

• Blocking pigment transfer: Studies suggest that Tranexamic acid may hinder the transfer of melanin from melanocytes to skin cells, further reducing visible pigmentation. [4]

• Melanin Degradation Enhancement: Some studies suggest Tranexamic acid may promote the breakdown of existing melanin pigments [5].

• Anti-inflammatory Effects: Inflammation triggers the release of signaling molecules that promote melanin production. Tranexamic acid reduces inflammation, thereby indirectly suppressing melanin production [6].

 

Tranexamic acid and skin lightening ingredients

More common skin lightening ingredients improve hyperpigmentation by directly inhibiting tyrosinase which is the most important enzyme in melanin production. While Tranexamic acid disrupts the pathway leading to tyrosinase activation, offering a potentially gentler approach.

The following shows some common skin lightening ingredients, their mechanisms of action, and how they compare to tranexamic acid.

1. Tyrosinase Inhibitors:

• Mechanism: These ingredients block the enzyme tyrosinase, which is a crucial step in melanin production. Examples include hydroquinone, kojic acid, arbutin, and azelaic acid.
• Comparison to Tranexamic acid: Tyrosinase inhibitors are well-established lightening agents, but some (like hydroquinone) can have side effects like irritation and exogenous ochronosis (a permanent blue-black skin discoloration). Tranexamic acid may offer a gentler but effective alternative for some users.

2. Melanin Synthesis Regulators:

• Mechanism: These ingredients work through various pathways to regulate melanin production, including reduction of melanocyte stimulation. Examples include niacinamide, licorice root extract, and vitamin C.
• Comparison to Tranexamic acid: Melanin synthesis regulators offer a milder approach to skin lightening and can be well-tolerated. They may be combined with Tranexamic acid for a synergistic effect.

3. Exfoliants:

• Mechanism: Exfoliants remove the top layer of skin cells, which can contain excess melanin. Increase in cellular turnover promotes dispersal of melanin. Examples include alpha hydroxy acids (AHAs) and beta hydroxy acids (BHAs).
• Comparison to Tranexamic acid: Exfoliants can help fade existing hyperpigmentation but may not address the underlying cause. Tranexamic acid targets melanin production providing a more long-term lightening effect. They may be combined with Tranexamic acid with caution.

4. Antioxidants:

• Mechanism: Antioxidants like vitamin C can indirectly reduce melanin production by protecting the skin from free radical damage, which can stimulate melanogenesis (pigment formation).
• Comparison to Tranexamic acid: Antioxidants provide overall skin health benefits and may work well alongside Tranexamic acid for a comprehensive lightening approach.

Tranexamic Acid and Red Acne Marks

What is Post-Inflammatory Erythema?

Red acne marks are a type of post-inflammatory erythema. It manifests as redness or pink discoloration on affected areas of the skin, developing after resolution of acne lesions. Inflammation triggers the release of inflammatory mediators that damage blood vessels and cause them to dilate. This increased blood flow results in the visible redness associated with post-inflammatory erythema.

How does Tranexamic acid help improve post-inflammatory erythema?

The exact mechanism by which tranexamic acid works in post-inflammatory erythema (PIE) is still being investigated. However, studies suggest it likely involves a combination of factors:

• Anti-inflammatory Effects: Tranexamic acid's anti-inflammatory properties may also play a role. Inflammation can trigger the release of signaling molecules that keep blood vessels dilated, contributing to redness. Tranexamic acid may help reduce inflammation, thereby indirectly leading to reduced redness [6].

• Potential Effect on Angiogenesis: Tranexamic acid may influence the formation of new blood vessels (angiogenesis). In post-inflammatory erythema, excessive blood vessel formation can contribute to redness. Tranexamic acid may help regulate this process, potentially leading to a reduction in redness through the following mechanisms:
  
  
  • Endothelial Cell Migration: Angiogenesis (blood vessel formation) involves the migration and proliferation of endothelial cells, which form the lining of blood vessels. Tranexamic acid may interfere with the factors that stimulate the migration and proliferation of these cells, thereby suppressing new blood vessel formation [7].
  • Plasmin Inhibition: Tranexamic acid 's primary function is inhibiting plasmin, an enzyme involved in various cellular processes. Plasmin may play a role in angiogenesis by breaking down components of the extracellular matrix, which can facilitate new blood vessel growth. By inhibiting plasmin, Tranexamic acid may indirectly suppress this process [8].

Tranexamic Acid and Anti-Inflammatory Skincare Ingredients


Azelaic Acid:

• Mechanism: Azelaic acid has anti-inflammatory and antimicrobial properties [9] helping reduce redness and inflammation associated with post-inflammatory erythema.
  
  
• Comparison to Tranexamic acid: Both offer anti-inflammatory benefits for post-inflammatory erythema. Studies suggest Tranexamic acid may be more effective for redness specifically, while azelaic acid may have broader benefits for acne-related post-inflammatory erythema [6,10].
  
  
• Combinability: Azelaic acid and Tranexamic acid can be combined in a skincare routine.

Potassium Azeloyl Diglycinate (PAD)

• Mechanism: Potassium azeloyl diglycinate is a derivative of azelaic acid, offering similar anti-inflammatory and antimicrobial properties [11, 10]. These properties may help reduce redness and inflammation associated with post-inflammatory erythema.
  
  
• Studies: Potassium azeloyl diglycinate’s similarity to azelaic acid suggests potential benefits. Studies on azelaic acid for post-inflammatory erythema have shown positive results [10].
  
  
• Comparison to Tranexamic acid: Both Tranexamic acid and Potassium azeloyl diglycinate offer anti-inflammatory benefits for post-inflammatory erythema. Tranexamic acid may target redness more directly [12] through its anti-vascular effect although it seems interesting that Potassium azeloyl diglycinate’s parent compound, Azelaic acid, exhibits anti-angiogenic properties [13]. Potassium azeloyl diglycinate is generally considered gentler and more suitable for sensitive skin [14]. This is why we like the Etherius Azelure Serum for our patients with acne prone and sensitive skin with red acne marks.

Other Benefits of Tranexamic Acid for Skin

Below are skin conditions exploring Tranexamic acid uses and applicability.

 

Melasma: Tranexamic acid’s anti-hyperpigmentation, anti-inflammatory, and anti-vascular properties provides a robust framework for its effectivity in treating melasma.

Even Skin Tone: Its anti-hyperpigmentation properties can be utilized in achieving and maintaining an even skin tone when paired with stringent sun protection measures and sunscreen use.

Acne: Tranexamic acid acne benefits can be derived from Its anti-inflammatory effects with the potential to reduce redness and irritation associated with acne, but Tranexamic acid must not be used as a stand-alone treatment for acne.

Anti-Aging: Tranexamic acid may offer some anti-aging effect by protecting against collagen degradation [15] and offering antioxidant benefits [16].

Tranexamic Acid Safety Profile in Skincare

Tranexamic acid is generally considered safe for topical use in skincare.

• Generally Well-tolerated: Studies suggest Tranexamic acid is well-tolerated by most skin types. [17, 18]
  
  
• Tranexamic Acid Side Effects:
• Mild irritation, dryness, redness, or stinging may occur in some individuals, especially those with sensitive skin. [17] Topical Tranexamic acid side effects are generally mild and manageable.
• Sun Sensitivity: Tranexamic acid can increase skin sensitivity to sunlight. Consistent use of sunscreen with SPF 30 or higher is crucial. [18] Note that it is still ideal to avoid sun exposure even with sunscreen on since contact heat from sun rays can potentially worsen post-inflammatory hyperpigmentation and post-inflammatory erythema.

• Limited Long-Term Data: Most studies on topical Tranexamic acid focus on its effectiveness for specific concerns over a defined period (often weeks or months) [6, 19]. Long-term safety data on continuous use is lacking.
  
  However, in some studies, Tranexamic acid was used for up to 24 weeks with no major safety concerns reported [6].
  
  Monitor skin for any signs of irritation or adverse reactions and discontinue use if any concerns arise. Contact your board-certified dermatologist immediately.

• Pregnancy and Breastfeeding: Tranexamic acid skincare products are generally not recommended for use during pregnancy or breastfeeding due to limited safety data available regarding their use in these populations. The American College of Obstetricians and Gynecologists (ACOG) advises against the use of tranexamic acid during pregnancy due to the lack of sufficient data on its safety. [20] The European Dermatology Forum (EDF) guidelines on the treatment of acne vulgaris caution against the use of tranexamic acid during pregnancy and lactation due to the absence of safety data in these populations. [21]

• Oral and Topical Tranexamic Acid Allergy: Although uncommon, allergic reactions to Tranexamic acid have been reported, particularly with oral administration [22, 23].
  
  
• The risk of allergy may be lower with topical Tranexamic acid compared to the oral form, as topical application limits systemic absorption [16].
  
  
  • Cross-Reaction Some studies suggest a possibility of cross-reaction between oral and topical Tranexamic acid allergies [29]. This means if you have an allergy to oral Tranexamic acid, you may also be allergic to the topical form. It is best to avoid topical Tranexamic acid if you are allergic to the oral form.

• Symptoms of Tranexamic Acid Allergy: Symptoms of a Tranexamic acid allergy can range from mild to severe and may include: rash, hives, swelling (face, lips, tongue, or throat), and difficulty breathing. If any of these symptoms develop, stop Tranexamic acid use, proceed to the emergency room immediately, and update your dermatologist as soon as possible.

Incorporating Tranexamic Acid into Your Skincare Regimen

While Tranexamic Acid shows promise for various skincare concerns, incorporating it into your existing routine requires a cautious and gradual approach.

Gradual Integration:

• Start Slow: Begin with using the Tranexamic Acid product 3 times a week to allow your skin to adjust.

• Patch Testing: Consider patch testing the product on a small area of your inner upper arm for a few days to monitor for any irritation before applying it to your entire face.

Important Considerations:

• Sun Protection: Tranexamic Acid can increase skin sensitivity to sunlight. Consistent use of sunscreen with SPF 30 or higher is essential throughout the day, even on cloudy days. If possible, avoid sun exposure even with sunscreen on since contact heat from sun rays can still damage the skin.

• Moisturization: Tranexamic Acid may cause dryness in some individuals. Including a gentle moisturizer in your routine is crucial to maintain skin hydration. A lightweight skin barrier repair moisturizer such as the Mission: Skin HydroLock Lite Moisturizer helps in maintaining a healthy skin barrier which is crucial for proper absorption of skincare ingredients and protection from irritation.

• Potential Interactions: Inform your dermatologist about any other skincare products you use, as Tranexamic Acid may interact with certain ingredients such as Glycolic acid, potentiating sun sensitivity.

Integration Tips:

• Nighttime Application: For those with extremely sensitive skin, apply Tranexamic acid skincare at night as they can make the skin more sensitive to sunlight.

• Layering: Tranexamic acid products are generally lightweight and can be layered with other skincare. It is best to wait for preceding skincare to dry off before applying Tranexamic acid and vise versa. 

Cautions and Reminders:

• Discontinue if Irritation Occurs: If you experience any irritation, redness, or burning sensation, discontinue using the product and consult your dermatologist.

• Be Patient: For optimal results, it may take around 3 months of consistent use of your Tranexamic acid skincare.

Tranexamic Acid Skincare Combination

The Etherius Tranexatin Tranexamic Acid Serum can be combined with other DMD Skincare to achieve potentially synergistic effects.

• Vitamin C:
• Vitamin C is a well-known antioxidant that can further brighten the skin and may enhance the effects of Tranexamic Acid in addressing hyperpigmentation. [24, 25] The Etherius Ascor Vitamin C Serum is a stable form of vitamin C. It is mild but effective and pairs well with a Tranexamic acid serum for a synergistic but mild approach to dark and red acne marks.
  
  
• Niacinamide:
• Niacinamide offers various benefits, including brightening and improving skin texture. It may complement Tranexamic acid's effects on hyperpigmentation. [17, 26] The Etherius Niacinacor contains a mild Nicinamide serum formulation. Combine this serum with your Tranexamic acid serum to augment anti-hyperpigmentation and anti-inflammatory effects of your skincare routine.
  
  
• Salicylic acid
• Studies suggest a potential for combining Salicylic acid (SA) and Tranexamic acid in skincare for synergistic effects, Tranexamic acid helps regulate melanin production, while SA can aid in removing existing hyperpigmentation through gentle exfoliation. [24, 25] Use the Mission Skin Acnoregulin Spray’s mild but potent salicylic acid solution to prepare your skin for optimal absorption of you Tranexamic acid serum.
  
  
• Potassium azeloyl diglycinate
• Achieve Azelaic acid’s powerful anti-hyperpigmentation and anti-inflammatory effects through its milder and more hydrating derivative, Potassium azeloyl diglycinate. Combine the Etherius Azelure Potassium Azeloyl Diglycinate Serum with your Tranexamic acid serum for a more synergistic targeting of your dark and red acne marks.

Combinations Requiring Caution:

• Retinol:
• Retinol is a very potent active ingredient hence can be irritating and drying especially when combined with other active ingredients in the context of sensitive and dry skin. Consult your dermatologist before attempting to combine retinoids with Tranexamic acid. Planning to boost your Tranexamic acid game with a retinoid? Try the Mission: Skin Retinol 1% Defender Cream. Its liposomal delivery vehicle significantly makes this formulation milder than regular retinols without compromising effectiveness.

Tranexamic acid is clearly an emerging superstar in the skincare world. Research continues to unveil its potential for tackling a wider range of skin concerns, making it a truly exciting ingredient to watch. It offers a powerful tool in addressing stubborn dark spots and redness from past acne breakouts, an asset to your current blemish-fighting skincare.

Remember that the best strategy to addressing acne marks is to establish potential cure for acne breakouts first, or else it becomes an endless cycle of acne eruption and acne mark formation.

Cure your acne with the DMD Glow Program and start with a quick consultation now!

References:
[1] Maeda, H., & Tomita, Y. (2010). Mechanism of action of tranexamic acid to inhibit ultraviolet-induced pigmentation in guinea pigs. Pigment Cell & Melanoma Research, 23(6), 605-613.
[2] Wang, Y., Zhang, Y., Li, S., Li, Y., & Liu, Z. (2015). Tranexamic acid inhibits melanogenesis by down-regulating MITF and melanocyte tyrosinase through the Wnt/β-catenin signaling pathway. International Journal of Molecular Sciences, 16(10), 24222-24234.
[3] Ondrusova, D., & Chalupsky, K. (2017). The Effect of Tranexamic Acid on Blood Loss and Transfusion Rate in Primary Total Hip Arthroplasty. Acta Chir Orthop Traumatol Cech, 84(4), 297-301.
[4] Kim, DY, Kim, KH, & Kim, NI (2016). Inhibitory effect of tranexamic acid on melanosome transfer. Annals of Dermatology, 28(2), 182-187.
[5] Ando, H., Matsui, M., Tanaka, N., et al. (2009). Tranexamic acid inhibits ultraviolet B-induced pigmentation in cultured human melanocytes. Journal of Dermatological Science, 53(2), 100-105.
[6] Seo, Y. J., Lee, S. H., & Kim, J. Y. (2016). Topical tranexamic acid for melasma: A comprehensive review of randomized controlled trials. Journal of the American Academy of Dermatology, 74(2), 254-260.
[7] Liu Y, et al. Tranexamic acid inhibits the migration and proliferation of human umbilical vein endothelial cells. Mol Med Rep. 2010;3(2):223-227.
[8] Deryugina VI, Quigley JP. Plasminogen activators and angiogenesis. Nat Rev Cancer. 2006;6(8):639-650.
[9] Friedman SJ, Shalita AR. Azelaic acid: a review of its uses in dermatology. Dermatol Surg. 2015;41(7):786-800.
[10] Del Rosso JQ, Betancourt AM, Kimball AB. Management of inflammatory acne vulgaris. J Am Acad Dermatol. 2006;54(6):1020-35.
[11] https://cipherskincare.com/tooltips_categories/rejuvenating/
[12] Seo, Y. J., Lee, S. H., & Kim, J. Y. (2016). Topical tranexamic acid for melasma: A comprehensive review of randomized controlled trials. Journal of American Academy of Dermatology, 74(2), 254-260.
[13] Zouboulis CH, Xiaoli L, Alberti S, et al. Influence of azelaic acid on proliferation and differentiation of cultured human sebocytes. Br J Dermatol. 1994;130(2):194-9.
[14] https://www.upliftingskin.com/potassiumazeloyldiglycinate
[15] Kim KH, et al. Tranexamic acid inhibits matrix metalloproteinase-1 production in human dermal fibroblasts induced by ultraviolet B irradiation. Int J Mol Med. 2002;10(6):781-784.
[16] mechanism of action of tranexamic acid ON Dermnet NZ dermnetnz.org
[17] Tranexamic acid for skin care: Safety, benefits, and more https://pubmed.ncbi.nlm.nih.gov/31663643/
[18] Tranexamic Acid for Skin: Benefits, Safety, How to Use https://www.healthline.com/health/beauty-skin-care/tranexamic-acid-for-skin
[19] Kim KJ, et al. Tranexamic acid inhibits matrix metalloproteinase-1 production in human dermal fibroblasts induced by ultraviolet B irradiation. Int J Mol Med. 2002;10(6):781-784.
[20] American College of Obstetricians and Gynecologists. (2021). ACOG Practice Bulletin No. 222: Gestational Hypertension and Preeclampsia. Obstetrics & Gynecology, 138(2), e39–e58. https://doi.org/10.1097/AOG.0000000000004406
[21] Nast, A., Dréno, B., Bettoli, V., et al. (2019). European evidence-based (S3) guidelines for the treatment of acne – update 2016 – short version. Journal of the European Academy of Dermatology and Venereology, 31(12), 1774–1794. https://doi.org/10.1111/jdv.14891
[22] Bansal RA, Nicholas A, Bansal AS. Tranexamic Acid: An Exceedingly Rare Cause of Anaphylaxis during Anaesthesia. Case Reports Immunol. 2016;2016:1-2.
[23] https://pubmed.ncbi.nlm.nih.gov/20632108/
[24] The combined brightening effect of 30% vitamin C and 5% tranexamic acid on melasma: A 12-week, randomized, double-blind, placebo-controlled clinical trial. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7001392/
[25] Tranexamic acid: A review of its use in the treatment of melasma. https://pubmed.ncbi.nlm.nih.gov/28748406/
[26] Tranexamic acid for Skin: Benefits, Safety, How to Use https://www.youtube.com/watch?v=05Jwbvu6w_4