TRANEXAMIC ACID (CYKLOKAPRON) FOR MELASMA print home print home

WHAT IS TRANEXAMIC ACID?

Tranexamic acid

( brand name Cyklokapron ) is a medication used to treat and prevent bleeding in patients with an increased tendency to bleed. It is given to patients with the blood clotting disorders hemophilia A and B, and to women with heavy menstrual bleeding. It

was discovered by chance, long ago, that tranexamic acid can also be used to reduce dark discoloration ( hyperpigmentation ) in adults with a persistent form of melasma , and to reduce dark circles around the eyes caused by excessive pigment production in the skin.

HOW DOES TRANEXAMIC ACID WORK FOR MELASMA?

It is not known exactly how tranexamic acid works for melasma. Tranexamic acid likely inhibits the action of tyrosinase. Tyrosinase is an enzyme necessary for the production of pigment in the skin. If this enzyme is less effective, pigment production in the skin is slowed down or inhibited. This causes the skin to lighten again over time. The dosage of tranexamic acid for melasma is 250 mg twice daily. This is much lower (six times lower) than the amount used for blood clotting disorders. Therefore, there are few side effects. The drug is not registered in the Netherlands for the treatment of melasma. However, several studies have since been published demonstrating that tranexamic acid is effective and safe for melasma. Therefore, the drug can be used for this condition even though it was not originally intended for this purpose.

WHEN SHOULD YOU NOT USE THIS MEDICINE?

- If you have or have had clotting problems such as a leg thrombosis or pulmonary embolism; or if these types of clotting problems occur in your family.
- If your kidneys are not functioning properly.
- If you have a malignant disease.
- If you are taking medicines for cardiovascular diseases.
- If you are using anticoagulants.
- If you smoke.
- If you are taking oral contraception (the pill). When using tranexamic acid in combination with oral contraception, there is theoretically a slightly increased risk of thrombosis. In practice, women with melasma usually do not use oral contraception because it can cause and worsen melasma.
- If you are pregnant. It is not 100% certain whether tranexamic acid is safe to use during pregnancy. When used in the second half of pregnancy, clotting problems or other adverse effects in the newborn have never occurred. However, it is wiser to avoid using medication during pregnancy unless absolutely necessary.
- If you are breastfeeding. A small amount of tranexamic acid passes into the baby through breast milk. Problems have never been observed in children of women who received a single dose of tranexamic acid after birth for postpartum bleeding, but the effects of long-term use for melasma are unknown. If you intend to use tranexamic acid for melasma immediately after delivery, choose not to breastfeed.
- If you are allergic to any of the ingredients of the medicine.
- If you have previously suffered from seizures (convulsions).
- In case of a cerebral hemorrhage (subarachnoid hemorrhage).

WHEN SHOULD YOU BE EXTRA CAUTION WHEN USING THIS MEDICINE?

- If your kidney function decreases, your dose may need to be adjusted.
- If you have an increased risk of thrombosis, you should only use Cyklokapron if it is strictly necessary.
- In case of irregular menstruation, Cyklokapron should only be used once the cause of the bleeding has been established.
- In case of disseminated intravascular coagulation (DIC), you may only use Cyklokapron in combination with heparin.
- When treating with drugs that inhibit clotting (anticoagulants), Cyklokapron should only be prescribed under strict supervision of a physician experienced in this field.

WHAT SUBSTANCES ARE CONTAINED IN THIS PRODUCT?

The active substance in this medicine is tranexamic acid. Each film-coated tablet contains 500 mg tranexamic acid. The other ingredients are microcrystalline cellulose (E460), hydroxypropyl cellulose (E463), talc (E553B), magnesium stearate (E470B), colloidal silicon dioxide (E551), povidone (E1201), Eudragit E100, titanium dioxide (E171), polypropylene glycol 8000, and vanillin.

HOW DO YOU USE TRANEXAMIC ACID FOR MELASMA?

For melasma, take 250 mg twice a day (half a 500 mg tablet twice a day). This is usually prescribed for a maximum of 6 months. The 500 mg tablet has a score line so you can break it in half. Take the tablet with plenty of water, preferably after a meal, to prevent nausea.

WHAT ARE THE POSSIBLE SIDE EFFECTS OF TRANEXAMIC ACID?

Often

(affects less than 1 in 10 users):
Nausea, vomiting, diarrhea.

Sometimes

(affects less than 1 in 100 users):
Allergic skin reactions.

Seldom

(may affect up to 1 in 1,000 people):
Thrombotic and embolic events (blood clots, including those that break away and block other vessels), such as pulmonary embolism and cerebrovascular accident (stroke). Thrombocytopenia (decrease in platelet count) and the development of prolonged bleeding time. Colour vision disturbances and other visual disturbances, and dizziness have been reported.

Not known

(frequency cannot be estimated from the available data):
Seizures (convulsions), especially at high doses.

The above-mentioned side effects have been reported with the higher doses of tranexamic acid used for bleeding disorders. At the low dose used to treat melasma, the most common side effects are nausea and decreased menstruation.

WHAT SHOULD I DO IF I HAVE TAKEN TOO MUCH TRANEXAMIC ACID?

Contact your doctor or the nearest hospital. Sometimes treatment with activated charcoal, gastric lavage, or inducing a gag reflex is necessary. Symptoms of overdose may include nausea, diarrhea, dizziness, headache, drop in blood pressure, and muscle weakness (myopathy). In patients with a tendency to thrombosis or a history of thrombosis, thrombosis (formation of a blood clot) may occur. Seizures (convulsions) may also occur.

WHAT SHOULD I DO IF I FORGET TO TAKE A TABLET?

Skipping a dose isn't a problem for melasma. Don't take a double dose to make up for a forgotten tablet.

WHAT CAN I EXPECT FROM TRANEXAMIC ACID FOR MELASMA?

The medication usually works well. The dark spots will lighten after 1-2 months and may even disappear completely. The effect is not the same for every patient. After stopping, there is a small chance of the pigment returning. The medication can be represcribed if necessary.
Source: www.skin-diseases.eu 2023
13-12-2023 ( JRM ) www.skin-diseases.eu pocketbook

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