What are the risks or side effects of using tranexamic acid (TXA) for hyperpigmentation?

From the FDA Drug Label

5 WARNINGS AND PRECAUTIONS

5. 1 Thromboembolic Risk Tranexamic acid is contraindicated in patients with active intravascular clotting. Tranexamic acid is an antifibrinolytic and may increase the risk of thromboembolic events. Venous and arterial thrombosis or thromboembolism has been reported in patients treated with Tranexamic acid Avoid concomitant use of Tranexamic acid and medical products that are pro-thrombotic, as the risk of thrombosis may be increased. These medications include but are not limited to, Factor IX Complex concentrates, Anti-inhibitor Coagulant concentrates, and hormonal contraceptives [see Drug Interactions (7.1), Use in Specific Populations (8.3)].
6. 2 Risk of Medication Errors Due to Incorrect Route of Administration Tranexamic acid injection is for intravenous use only. Serious adverse reactions including seizures and cardiac arrythmias have occurred when Tranexamic acid injection was inadvertently administered intrathecally instead of intravenously Confirm the correct route of administration for Tranexamic acid injection and avoid confusion with other injectable solutions that might be administered at the same time as Tranexamic acid injection. Syringes containing Tranexamic acid injection should be clearly labeled with the intravenous route of administration.
7. 3 Seizures Tranexamic acid may cause seizures, including focal and generalized seizures. The most common setting for tranexamic acid-induced seizures has been during cardiovascular surgery (a setting in which Tranexamic acid is not FDA-approved and which uses doses of up to 10-fold higher than the recommended human dose and in patients inadvertently given tranexamic acid into the neuraxial system) Tranexamic acid is not approved and not recommended for neuraxial administration. Consider dose reduction during surgery and dose adjustments for patients with clinical conditions such as renal dysfunction. Closely monitor the patient during surgery Consider electroencephalogram (EEG) monitoring for patients with history of seizures or who experience myoclonic movements, twitching, or show evidence of focal seizures. Discontinue Tranexamic acid if seizures occur.
8. 4 Hypersensitivity Reactions Cases of hypersensitivity reactions, including anaphylactic reactions, have occurred with use of intravenous tranexamic acid. Discontinue treatment with Tranexamic acid if serious reaction occurs, provide appropriate medical management, and do not restart treatment. Tranexamic acid is contraindicated in patients with a history of hypersensitivity to tranexamic acid.
9. 5 Visual Disturbances Although not seen in humans, focal areas of retinal degeneration have been observed in cats and dogs following oral or intravenous tranexamic acid at doses between 250 to 1600 mg/kg/day (1. 6 to 22 times the recommended usual human dose based on body surface area) from 6 days to 1 year. No retinal changes have been observed in eye examinations of patients treated with tranexamic acid for up to 8 years. Patients expected to be treated for greater than 3 months may consider ophthalmic monitoring including visual acuity and optical coherence tomography at regular intervals. Discontinue Tranexamic acid if changes in ophthalmological examination occurs.
10. 6 Dizziness Tranexamic acid may cause dizziness. Concomitant use of other drugs that may also cause dizziness may worsen this effect. Advise patients to avoid driving or using machines until they know how Tranexamic acid affects them.

The FDA drug label does not mention hyper pigmentation as a specific condition being treated with tranexamic acid. However, it does list several potential side effects and risks associated with the use of tranexamic acid, including:

• Thromboembolic risk: increased risk of thromboembolic events
• Seizures: may cause seizures, including focal and generalized seizures
• Hypersensitivity reactions: cases of hypersensitivity reactions, including anaphylactic reactions, have occurred
• Visual disturbances: although not seen in humans, focal areas of retinal degeneration have been observed in cats and dogs
• Dizziness: may cause dizziness It is essential to note that the label does not provide information on the use of tranexamic acid for hyperpigmentation, and therefore, no conclusion can be drawn about the safety and efficacy of tranexamic acid for this specific condition 1.

From the Research

Yes, there are risks and side effects when using tranexamic acid for hyperpigmentation, but recent studies suggest that the risks may be lower than previously thought, especially when used orally in low doses. Tranexamic acid, typically used in oral doses of 250-500mg twice daily for 8-12 weeks, can cause potential side effects, including gastrointestinal disturbances (nausea, diarrhea), headaches, and most importantly, increased risk of blood clots such as deep vein thrombosis or pulmonary embolism 2. However, a recent systematic review and meta-analysis found that intravenous tranexamic acid was not associated with an increased risk of thromboembolic events or mortality 2.

Common Side Effects

• Mild irritation, redness, dryness, and occasional stinging upon application (topical use)
• Gastrointestinal disturbances (nausea, diarrhea)
• Headaches
• Increased risk of blood clots (oral use)

Special Considerations

• Individuals with current or past history of blood clots, stroke, heart disease, hormonal conditions, or those taking birth control pills should avoid tranexamic acid
• Pregnant or breastfeeding women should also avoid it
• The medication works by inhibiting plasminogen activator, which reduces melanin production in skin cells, but this same mechanism affects blood clotting pathways

Recent Studies

• A 2024 study found that oral tranexamic acid was effective in preventing and treating postinflammatory hyperpigmentation without significant adverse effects 3
• A 2023 review found that tranexamic acid has anti-inflammatory and anti-melanin-producing properties, and may have more uses in dermatology, including the treatment of rosacea, urticaria, and post-inflammatory hyperpigmentation 4
• A 2024 update on the use of tranexamic acid for hyperpigmentation and telangiectatic disorders found that it has been tried as a treatment for various conditions, including post-inflammatory hyperpigmentation, Riehl's melanosis, rosacea, and post-acne erythema 5

Recommendation

Always consult with a dermatologist before starting tranexamic acid treatment, especially if considering oral formulations, as they can monitor for adverse effects and determine if it's appropriate for your specific situation. The most recent and highest quality study suggests that oral tranexamic acid may be a safe and effective treatment option for hyperpigmentation disorders, but more evidence is needed to confirm its efficacy and safety in different patient populations 3.