| Source | Synthetic |
| Hyperpigmentation | Rank : 5 |
| Anti-Inflammation | Rank : 5 |
| Skin Barrier Function | Rank : 5 |
| Side Effects | Rare, Allergic Reactions & Irritations |
| Synergy | Vitamin C, AHAs, Hyaluronic Acid, Retinoids |
| Optimal pH Level | Between 5.0 and 7.0 |
| Counteract Ingredients | Strong Expoliants, Alkaline Products, Excessive Sun |
| Alternatives | Vitamin C, Nianinamide, AHAs, Arbutin, Kjoic Acid |
| Normal Skin | Brightening and prevent hyperpigmentation |
| Dry Skin | Hydrating and prevent hyperpigmentation |
| Oily Skin | Reduce dark spots, and control excess sebum production |
| Combination Skin | Target hyperpigmentation for dry and oily areas. |
| Sensitive Skin | Gently diminishing the appearance of hyperpigmentation |
| Acne-Prone Skin | Lightening post-inflammatory hyperpigmentation |
| Mature Skin | Brightening, texture improvement |
Tranexamic acid
Originally known for its use in preventing and treating excessive blood loss during surgery and in conditions like heavy menstrual bleeding, tranexamic acid has found its way into the realm of dermatology and skincare due to its impressive effects on hyperpigmentation and skin brightening.
History
Tranexamic acid was synthesized and studied in the 1960s, initially used to reduce bleeding by inhibiting plasmin. Its ability to reduce bleeding made it valuable in surgeries and specific medical conditions where blood loss was a concern.
Topical Tranexamic Acid for Hyperpigmentation
Studies demonstrated that both oral and topical forms of tranexamic acid could significantly reduce the appearance of melasma, a challenging condition to treat, characterized by dark, discolored patches on the skin.
Current Use in Skincare
Its inclusion in serums, creams, and masks is touted for its ability to target stubborn dark spots without the irritation or side effects associated with other skin-lightening agents like hydroquinone or high-concentration retinoids.
Safety and Efficacy
Topical tranexamic acid is generally considered safe for most skin types, with minimal side effects. It is often recommended as part of a comprehensive skincare routine that includes sun protection, given that UV exposure can exacerbate hyperpigmentation issues.
The synthesis of tranexamic acid involves the chemical reaction of lysine with certain reagents to form the cyclohexane derivative that characterizes tranexamic acid. This synthetic route allows for the production of a pure, consistent compound, which is crucial for its effectiveness and safety in medical and cosmetic applications.
Molecular Formula
The molecular elements of tranexamic acid interact with the skin in a targeted manner that influences melanogenesis, the process by which the skin produces melanin, the pigment responsible for skin color.
Inhibition of Plasmin
At the molecular level, tranexamic acid's interaction with the skin primarily involves its ability to inhibit plasmin, an enzyme that, when activated, can lead to increased melanin production.
Reduction of Inflammatory Mediators
Tranexamic acid also influences the skin's inflammatory response, which can be a precursor to hyperpigmentation, especially in conditions like melasma, where UV exposure causes inflammation that stimulates melanin production.
Interference with Melanocyte-Keratinocyte Interaction
In the skin, melanocytes transfer melanin to keratinocytes, the most common cells in the epidermis. This process is essential for pigmentation. Tranexamic acid's interference in this process can lead to a reduction in melanin transfer.
Effects
Tranexamic acid has gained prominence in addressing hyperpigmentation and improving skin tone. While it was originally used to treat or prevent excessive blood loss, its benefits for skin care have made it a sought-after ingredient.
Reduces Hyperpigmentation
Tranexamic acid is highly effective in reducing the appearance of melasma, a condition characterized by dark, discolored patches on the skin, usually on the face. It works by inhibiting the plasminogen/plasmin pathway in the skin, which can otherwise stimulate melanin production by melanocytes. This action helps to lighten dark spots and even out skin tone.
Minimizes Inflammation
It has anti-inflammatory properties that help to calm the skin and reduce redness. This makes it beneficial not only for hyperpigmentation but also for soothing irritated skin. By decreasing inflammation, tranexamic acid helps to prevent the inflammatory cascade that can lead to an increase in melanin production.
Improves Skin Barrier Function
While its primary use in skincare is for pigmentation issues, tranexamic acid can also contribute to a healthier skin barrier by reducing inflammation and potentially influencing the skin’s hydration levels.
Prevents UV-Induced Pigmentation
Tranexamic acid can help prevent the formation of UV-induced pigmentation by inhibiting the UV-induced plasmin activity in the skin. This makes it a valuable ingredient for use in conjunction with sunscreen to protect the skin.
Reduces the Appearance of Acne Scars
Tranexamic acid can also help lighten post-inflammatory hyperpigmentation (PIH) associated with acne scars. By reducing the overproduction of melanin that occurs after inflammatory acne, it helps to diminish the appearance of these scars.
Side Effects
Topical tranexamic acid, used in skincare products for hyperpigmentation and evening skin tone, is generally well-tolerated. However, some individuals may experience:
- Mild Irritation: Redness, itching, or burning, especially if the skin barrier is compromised or if used in conjunction with other irritating products.
- Allergic Reactions: Although rare, allergic reactions can occur, presenting as rash, hives, or extreme irritation at the application site.
Synergy
Tranexamic acid, a powerhouse ingredient for tackling hyperpigmentation, works even more effectively when combined with certain other skincare ingredients.
Vitamin C
Vitamin C is a potent antioxidant that inhibits melanin production, brightens the skin, and protects against environmental damage. When used with tranexamic acid, it enhances the skin-brightening effects and provides added protection against oxidative stress.
Alpha Hydroxy Acids (AHAs)
AHAs like glycolic acid and lactic acid promote cell turnover, removing the upper layer of the skin and fading dark spots. When used with tranexamic acid, the accelerated cell renewal helps to more quickly diminish the appearance of hyperpigmentation.
Hyaluronic Acid
While hyaluronic acid doesn't directly impact pigmentation, its powerful hydrating properties can enhance the skin's absorption of tranexamic acid. A well-hydrated skin barrier allows for better penetration and effectiveness of active ingredients.
Retinoids
Retinoids accelerate cellular turnover and have a profound impact on collagen production, aiding in the reduction of hyperpigmentation and improvement of skin texture. Used with tranexamic acid, this combination can significantly improve the clarity and evenness of the skin tone.
Sunscreen
While not an active ingredient that directly synergizes with tranexamic acid, sunscreen is essential in any routine targeting hyperpigmentation. It protects the skin from UV radiation, preventing further darkening of hyperpigmented spots and maximizing the effects of tranexamic acid.
pH Level
The optimal pH range for tranexamic acid in topical formulations is typically between 5.0 and 7.0. This range ensures that the acid remains stable and effective, providing maximum benefits without causing skin irritation.
Why pH Matters for Tranexamic Acid
- Stability: Tranexamic acid’s stability in skincare formulations is pH-dependent. Maintaining a pH within the optimal range helps preserve its integrity and effectiveness over time.
- Skin Compatibility: The skin's natural pH ranges from about 4.7 to 5.75, slightly acidic, which helps protect the skin from harmful microorganisms and maintains barrier function. Formulating tranexamic acid products within this range ensures better compatibility with the skin, minimizing potential irritation and allowing for more effective absorption.
- Efficacy in Treating Hyperpigmentation: For tranexamic acid to effectively target melanogenesis (the process of melanin production), it needs to penetrate the upper layers of the skin. A formulation within the optimal pH range facilitates better absorption into the skin, enhancing its ability to reduce hyperpigmentation and even out skin tone.
Counteract Ingredients
When incorporating tranexamic acid into your skincare routine, especially if targeting hyperpigmentation or seeking to improve skin tone, it's important to be mindful of certain ingredients.
Direct Acids and Strong Exfoliants
Combining tranexamic acid with high concentrations of direct acids (e.g., glycolic acid, salicylic acid) or strong exfoliants can potentially lead to increased skin sensitivity and irritation. Over-exfoliation can compromise the skin barrier too.
Highly Alkaline Products
Products with a high pH (alkaline) can disrupt the skin's natural acid mantle, potentially affecting the absorption and efficacy of tranexamic acid.
Excessive Sun Exposure
While tranexamic acid itself does not increase photosensitivity, treating hyperpigmentation requires diligent sun protection to prevent further UV-induced pigmentation. Excessive sun exposure can counteract the benefits of tranexamic acid in reducing dark spots.
Unstable Vitamin C Formulations
Although vitamin C and tranexamic acid can be complementary in treating hyperpigmentation, using unstable or improperly formulated vitamin C products can lead to irritation and reduce the effectiveness of both ingredients.
Incorporating To Skin Routine
Morning Routine
- Cleanser Start with a gentle, pH-balanced cleanser to remove overnight buildup without stripping the skin.
- Vitamin C Serum Apply a vitamin C serum for its antioxidant protection and to enhance the brightening effects of tranexamic acid. Vitamin C also helps fend off free radical damage and boosts sun protection.
- Tranexamic Acid Product While tranexamic acid can be used both morning and night, if you prefer using it once a day, consider your overall routine. For those using retinoids or acids at night, the morning might be a better time for tranexamic acid.
- Moisturizer Use a hydrating moisturizer suitable for your skin type to help lock in moisture and maintain your skin barrier.
- Sunscreen Finish with a broad-spectrum SPF 30 or higher sunscreen. Sun protection is crucial, especially when targeting hyperpigmentation, to prevent further darkening of spots.
Night Routine
- Cleanser Use the same gentle cleanser or a slightly more hydrating option if your skin feels drier at night.
- Exfoliating Acid (Optional) On alternate nights or less frequently, use an AHA/BHA exfoliant to promote cell turnover and enhance skin texture. Ensure there's no irritation when combining with tranexamic acid in your routine.
- Tranexamic Acid Product If not applied in the morning, use your tranexamic acid product in the evening. Its ability to reduce melanin production works well overnight as the skin repairs itself.
- Retinol (Alternate Nights) If you’re incorporating retinol into your routine, alternate it with tranexamic acid to prevent potential irritation unless your skin can tolerate both.
- Moisturizer Apply a richer moisturizer at night if your skin requires extra hydration.
- Face Oil (Optional) For added moisture, especially in dry climates or seasons, a few drops of a non-comedogenic face oil can be beneficial.
Tips
Start Slowly
- Why: To minimize irritation and allow your skin to adjust.
- How: Begin with a lower concentration of tranexamic acid and use it every other day or twice a week, gradually increasing frequency based on your skin's tolerance.
Patch Test
- Why: To ensure you don't have an adverse reaction.
- How: Apply a small amount of the product containing tranexamic acid to your inner forearm or behind your ear and wait 24-48 hours to observe any reactions.
Combine Wisely
- Why: Certain ingredients can enhance the effects of tranexamic acid, while others may cause irritation when used together.
- How: Pair tranexamic acid with complementary ingredients like niacinamide, vitamin C, and hyaluronic acid for added benefits. Be cautious with direct acids and retinoids, and space their application apart if necessary.
Use Sun Protection
- Why: UV exposure can worsen hyperpigmentation, counteracting the benefits of tranexamic acid.
- How: Apply a broad-spectrum sunscreen with SPF 30 or higher every morning, and reapply as needed throughout the day.
- Cleanser Start with a gentle, pH-balanced cleanser to remove overnight buildup without stripping the skin.
- Vitamin C Serum Apply a vitamin C serum for its antioxidant protection and to enhance the brightening effects of tranexamic acid. Vitamin C also helps fend off free radical damage and boosts sun protection.
- Tranexamic Acid Product While tranexamic acid can be used both morning and night, if you prefer using it once a day, consider your overall routine. For those using retinoids or acids at night, the morning might be a better time for tranexamic acid.
- Moisturizer Use a hydrating moisturizer suitable for your skin type to help lock in moisture and maintain your skin barrier.
- Sunscreen Finish with a broad-spectrum SPF 30 or higher sunscreen. Sun protection is crucial, especially when targeting hyperpigmentation, to prevent further darkening of spots.
- Cleanser Use the same gentle cleanser or a slightly more hydrating option if your skin feels drier at night.
- Exfoliating Acid (Optional) On alternate nights or less frequently, use an AHA/BHA exfoliant to promote cell turnover and enhance skin texture. Ensure there's no irritation when combining with tranexamic acid in your routine.
- Tranexamic Acid Product If not applied in the morning, use your tranexamic acid product in the evening. Its ability to reduce melanin production works well overnight as the skin repairs itself.
- Retinol (Alternate Nights) If you’re incorporating retinol into your routine, alternate it with tranexamic acid to prevent potential irritation unless your skin can tolerate both.
- Moisturizer Apply a richer moisturizer at night if your skin requires extra hydration.
- Face Oil (Optional) For added moisture, especially in dry climates or seasons, a few drops of a non-comedogenic face oil can be beneficial.
For Each Skin Type
Tranexamic acid is versatile and can be beneficial for various skin types when incorporated appropriately into skincare routines. Here's how it can be used effectively for each skin type:
Normal Skin
- Goal: Enhance overall skin tone and prevent hyperpigmentation.
- Approach: Use tranexamic acid formulations in moderate concentrations as part of your evening routine. Combine with antioxidants like vitamin C during the day for added protection and brightening effects.
Dry Skin
- Goal: Address hyperpigmentation while maintaining hydration.
- Approach: Opt for tranexamic acid products that also contain hydrating ingredients like hyaluronic acid or glycerin. Apply a rich moisturizer afterward to lock in hydration and support the skin barrier.
Oily Skin
- Goal: Reduce dark spots and control excess sebum production.
- Approach: Look for lightweight, non-comedogenic tranexamic acid serums that won't clog pores. Pairing tranexamic acid with niacinamide can be particularly effective, as niacinamide helps regulate oil production.
Combination Skin
- Goal: Target hyperpigmentation while balancing dry and oily areas.
- Approach: Use tranexamic acid selectively on areas prone to dark spots and hyperpigmentation. Consider layering different products to address the varying needs of your skin—lighter formulations for oily areas and more hydrating ones for dry patches.
Sensitive Skin
- Goal: Gently diminish the appearance of hyperpigmentation without causing irritation.
- Approach: Start with low-concentration tranexamic acid products and introduce them slowly into your routine. Ensure the rest of your skincare is formulated for sensitive skin to minimize the risk of irritation.
Acne-Prone Skin
- Goal: Lighten post-inflammatory hyperpigmentation (PIH) from acne without exacerbating breakouts.
- Approach: Tranexamic acid can be safely used on acne-prone skin to treat PIH. Pair it with salicylic acid (BHA) to keep pores clear, but be mindful to not over-irritate the skin. Alternate between using BHA and tranexamic acid in different routines (morning vs. evening) or on alternate days.
Mature Skin
- Goal: Improve skin tone and texture while addressing signs of aging.
- Approach: Combine tranexamic acid with ingredients that target aging, such as retinol or peptides. Since these combinations can be potent, apply them on alternate nights or as part of a routine that gradually layers products to build tolerance.
Tips for All Skin Types
- Sun Protection: Regardless of skin type, daily sunscreen application is crucial when using tranexamic acid to prevent further UV-induced pigmentation.
- Consistent Use: For best results, use tranexamic acid consistently as part of your skincare routine.
- Patch Test: Before fully incorporating tranexamic acid into your routine, perform a patch test to ensure compatibility with your skin, especially if you have sensitive or reactive skin.
Alternatives
| Ingredient | Benefits | Typical Uses |
| Vitamin C (Ascorbic Acid) | Antioxidant properties, brightens skin, reduces pigmentation | Serums, creams, lotions |
| Niacinamide (Vitamin B3) | Reduces redness, minimizes appearance of pores, evens skin tone, reduces pigmentation | Serums, moisturizers, toners |
| Alpha Hydroxy Acids (AHAs) | Exfoliates, reveals brighter skin, improves texture, reduces pigmentation | Exfoliating toners, serums, peels |
| Arbutin | Inhibits melanin production, fades hyperpigmentation | Serums, creams, spot treatments |
| Kojic Acid | Lightens visible sun damage, age spots, and scars | Serums, cleansers, creams |
| Azelaic Acid | Reduces inflammation, fades hyperpigmentation and blemishes, antibacterial | Creams, gels, foams |
| Licorice Extract | Contains glabridin which inhibits pigmentation, anti-inflammatory, soothes skin | Serums, creams, gels |
| Retinoids | Promotes cell turnover, fades pigmentation, fights signs of aging | Serums, creams, prescription treatments |
| Hydroquinone | Lightens dark spots (use under dermatologist supervision due to potential side effects) | Prescription creams, spot treatments |
| Glycolic Acid (AHA) | Exfoliates, fades pigmentation, increases cell turnover | Cleansers, toners, peels, creams |
Misconceptions
Tranexamic Acid Exfoliates the Skin
Unlike alpha-hydroxy acids (AHAs) or beta-hydroxy acids (BHAs) that exfoliate the skin by removing dead skin cells, tranexamic acid works by inhibiting melanin production and reducing inflammation. It does not exfoliate or remove dead skin cells.
It’s Only Effective When Taken Orally
While oral tranexamic acid is used for treating melasma and has systemic effects, topical formulations have also been proven effective for reducing hyperpigmentation with fewer systemic side effects. Topical tranexamic acid is a viable option for those seeking targeted skin benefits.
Tranexamic Acid Increases Sun Sensitivity
Tranexamic acid does not increase the skin's sensitivity to the sun, unlike some other skincare ingredients such as retinoids and AHAs. However, using sunscreen is crucial when treating hyperpigmentation to prevent further UV damage and pigmentation.
It’s Only for Severe Hyperpigmentation
While tranexamic acid is effective for treating melasma and pronounced hyperpigmentation, it's also beneficial for lighter pigmentation issues, evening out skin tone, and preventing future pigmentation when used in skincare routines.
Immediate Results Should Be Expected
Like many skincare treatments, tranexamic acid requires consistent use over time to see significant results. It may take several weeks to months to notice a reduction in hyperpigmentation.
It's Unsafe for Long-Term Use
Topical tranexamic acid is considered safe for long-term use, with minimal side effects. However, as with any active ingredient, it's important to monitor your skin's response and consult with a dermatologist, especially if combining it with other treatments.
Note About Tranexamic Acid
Tranexamic acid works by targeting the overproduction of melanin that leads to hyperpigmentation, rather than altering the skin's natural pigmentation. When used as directed, it helps to fade dark spots and even out skin tone without bleaching the skin or affecting its natural color.
People Also Ask About Tranexamic Acid
A: While primarily known for reducing hyperpigmentation and melasma, tranexamic acid can also help fade post-inflammatory hyperpigmentation (PIH) associated with acne scars. However, its effectiveness directly on textured acne scars is limited; it's more effective on the dark marks that can be left behind after an acne breakout.
A: Tranexamic acid is not directly known to improve skin elasticity or firmness. Its primary role in skincare is to address hyperpigmentation and even out skin tone. Ingredients known for enhancing skin elasticity include retinoids, peptides, and vitamin C.
A: Yes, tranexamic acid can be used in conjunction with microneedling treatments, especially to address melasma and hyperpigmentation more effectively. Some studies suggest that applying tranexamic acid topically after microneedling can enhance its penetration and efficacy. Always consult with a dermatologist or skincare professional before combining treatments.
A: Refrigerating tranexamic acid products is not necessary for maintaining their efficacy. However, storing skincare products in a cool, dark place can help preserve their stability, especially if they contain multiple active ingredients. Always follow the storage instructions provided by the manufacturer.
A: The timeframe to see visible results from tranexamic acid can vary, typically ranging from several weeks to a few months of consistent use. Factors such as the severity of hyperpigmentation, the concentration of tranexamic acid, and how it's incorporated into your skincare routine can influence the results.
Recommended Products
(!) We are not affiliated with the brand listed below. We measure carefully to find the best ones.
For Dry Skin
The Inkey List Tranexamic Acid Night Treatment ($17)
This night treatment combines tranexamic acid with vitamin C and aloe vera, offering hydration alongside pigmentation reduction, making it ideal for dry skin types.
For Oily Skin
Good Molecules Discoloration Correcting Serum ($12)
Lightweight and effective, this serum combines tranexamic acid with niacinamide, making it ideal for oily skin prone to dark spots without contributing to oiliness.
For Combination Skin
Inkey List Tranexamic Acid Hyperpigmentation Treatment ($17)
This treatment is specifically designed to target dark spots and uneven skin tone, providing a balanced formulation that won't over-moisturize or dry out different areas of combination skin.
For Sensitive Skin
COSRX Pure Fit Cica Serum ($28)
While not solely focused on tranexamic acid, this serum includes a soothing CICA-7 complex and a small concentration of tranexamic acid, making it gentle enough for sensitive skin types looking to address redness and mild hyperpigmentation.
For Normal Skin
Shiseido White Lucent MicroTargeting Spot Corrector ($135)
Suitable for normal skin types, this overnight treatment works to reduce hyperpigmentation and even out skin tone while you sleep, featuring a blend of tranexamic acid and vitamin C.
For Mature Skin
Derma E Scar Gel ($23.95)
Though not exclusively a tranexamic acid product, this gel includes allantoin, panthenol, and onion extract, which work alongside tranexamic acid to improve the appearance of scars and hyperpigmentation, making it suitable for mature skin with concerns about texture and clarity.
For Acne-Prone Skin
Acure Radically Rejuvenating Dual Phase Bakuchiol Serum ($21.99)
This serum incorporates bakuchiol, a gentle retinol alternative, alongside other beneficial ingredients, making it suitable for acne-prone skin. While it doesn't contain tranexamic acid, it's effective for similar concerns and is a good alternative for those sensitive to direct acids.
