Are There Any Possible Side Effects Of Oral Tranexamic Acid?

Oral tranexamic acid is an FDA-approved prescription-only clotting drug used in treating bleeding conditions like heavy periods and excessive postoperative bleeding. During the clotting process, oral tranexamic acid inhibits plasminogen activation, a key process linked to the formation of darker skin patches in conditions like melasma and hyperpigmentation.

Due to this action, oral tranexamic acid has been used to successfully treat melasma either as a stand-alone therapy or in combination with other topical formulations. The drug also has potential extended uses in the treatment of post-inflammatory hyperpigmentation and rosacea (Kim).

However, as with any drug, knowing its possible side effects is essential to understanding the tradeoff between benefits and side effects.

How to understand oral tranexamic acid side effects

Oral tranexamic acid side effects are vastly dissimilar at different dosages.

When prescribed for bleeding conditions, a typical oral tranexamic acid prescription has between 30 to 40 mg/kg, working out to around 3900 mg per day on average. On average, oral tranexamic acid for melasma prescriptions are comparatively low, ranging from 4 to 16 mg/kg or 500 to 1500 mg per day.

The best way to understand the side effects of oral tranexamic acid is to consider them separately at these two dosage levels because, in most cases, the side effects at a higher dosage are not the same as those at a lower one.

High dosage oral tranexamic acid side effects

The side effects of oral tranexamic acid at high dosages can emerge from four causes: the body getting used to a new drug, an allergic reaction, a preexisting condition, or an interaction with a medication you are currently taking.

If your body is getting used to the drug, you might experience common side effects of oral tranexamic acid. In contrast, severe side effects might be because of the three other causes: allergic reaction, preexisting conditions, or drug interactions.

Oral tranexamic acid: common side effects

Common oral tranexamic acid side effects can include:

• Nausea
• Vomiting
• Diarrhea
• Abdominal or stomach pain, discomfort, or tenderness
• Headache (severe and throbbing)
• Chills
• Fever
• Back or joint pain
• Muscle stiffness
• Muscle pain
• Difficulty moving
• Runny or stuffy nose

In most cases, these side effects are minor and tend to go away after some time. They also might not be pronounced enough to require medical treatment. However, if these symptoms persist or get worse, you should seek medical attention.

Oral tranexamic acid: serious side effects

Serious oral tranexamic acid side effects include:

• Pale skin
• Anxiety
• Confusion
• Cough
• Unusual tiredness or weakness
• Change in vision
• Chest pain or tightness
• Difficulty with swallowing
• Trouble breathing when exerting oneself
• Numbness of the hands
• Pain, redness, or swelling in the arm or leg
• Unusual bleeding or bruising
• Dizziness or lightheadedness
• Fainting
• Fast heartbeat
• Puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue
• Skin rash, hives, or itching

If you experience any of these side effects, they might be indicative of a life-threatening reaction to the drug (anaphylaxis), and you must seek medical help immediately.

Side effects of low-dosage oral tranexamic acid for melasma

Oral tranexamic acid for melasma side effects are not as many or as severe as those at high dosages.

Although more research is needed to determine the full extent of OTA side effects at low dosages, current data suggests it may be safe to take with few to no side effects (Lee).

Here’s a quick round-up of possible oral tranexamic acid for melasma side effects:

Oral tranexamic acid for melasma: common side effects

The most common side effect of oral tranexamic acid for melasma is abdominal bloating and pain. In general, OTA is well-tolerated by most people, and in those with abdominal discomfort, the symptoms are mostly mild and go away after a short time.

However, some common high-dosage side effects like headaches, fever, and runny nose might occur at lower doses. It is therefore necessary to speak with a healthcare professional before and while taking oral tranexamic acid for melasma. They will evaluate your dosage based on your level of tolerance and side effects and adjust or replace it accordingly.

Oral tranexamic acid for melasma: serious side effects

Current research shows that oral tranexamic acid for melasma has relatively few serious side effects, mainly because the drug is well tolerated at low dosages (Colferai).

However, the risk of more serious side effects like deep vein thrombosis, acute myocardial infarction, acute renal cortical necrosis, and pulmonary embolism still exist, especially if you have underlying conditions that might make you more susceptible.

Since these side effects can be life-threatening, it is critical to undergo screening by a medical professional to eliminate any factors that might lead to serious side effects after taking OTA for melasma.

Underlying conditions, drug interactions, and COVID-19

Oral tranexamic acid is unsuitable for individuals with a history of any of the following conditions:

• Increased risk of blood clotting
• Deep vein thrombosis
• Use of anticoagulants
• Moderate to severe kidney impairment
• Heart valve disease

Moreover, some adverse drug interactions might occur if you are currently taking the following drugs:

• Hormonal birth control like birth control pills, the patch, IUD, or vaginal ring because they increase your risk of a blood clot, stroke, or heart attack.
• Anti-inhibitor coagulant complex drugs used to reduce and prevent excessive bleeding.
• Chlorpromazine, an antipsychotic medicine.
• Tretinoin, a drug used to treat acute promyelocytic leukemia, which might lead to bleeding issues when combined with oral tranexamic acid.

Additionally, COVID-19 increases blood clotting in the body, so you should not take oral tranexamic acid because it can heighten the risk of embolism.

Key takeaways

Oral tranexamic acid side effects differ when taken at high dosages and low ones. OTA dosages for melasma tend to be on the low end, and current research and meta-analyses indicate that at low dosages, it is safe and effective for treating melasma (Tan).

Nevertheless, while side effects at lower dosages are limited, allergic reactions, underlying conditions, and drug interactions can mean oral tranexamic acid is safe for one person but dangerous for another.

Before taking it at high or low dosages, it is critical to first speak with a medical professional to screen for any factors that might make it dangerous for you. In addition, monitoring side effects after taking it can help determine whether you should keep taking it or discontinue and replace it with a different treatment.

References

• Colferai MMT, Miquelin GM, Steiner D. Evaluation of oral tranexamic acid in the treatment of melasma [published online ahead of print, 2018 Dec 9]. J Cosmet Dermatol. 2018;10.1111/jocd.12830. doi:10.1111/jocd.12830
• Kim MS, Bang SH, Kim JH, Shin HJ, Choi JH, Chang SE. Tranexamic Acid Diminishes Laser-Induced Melanogenesis. Ann Dermatol. 2015;27(3):250-256. doi:10.5021/ad.2015.27.3.250
• Lee HC, Thng TG, Goh CL. Oral tranexamic acid (TA) in the treatment of melasma: A retrospective analysis. J Am Acad Dermatol. 2016;75(2):385-392. doi:10.1016/j.jaad.2016.03.001
• Tan AWM, Sen P, Chua SH, Goh BK. Oral tranexamic acid lightens refractory melasma. Australas J Dermatol. 2017;58(3):e105-e108. doi:10.1111/ajd.12474

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Brandon Kirsch, MD

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.