Active Ingredients

Tranexamic acid – effect, application & risks

Tranexamic acid

Tranexamic acid is an antifibrinolytic and inhibits the dissolution of blood clots . The substance is used to stop and prevent bleeding caused by hyperfibrinolysis.

What is tranexamic acid?

The substance tranexamic acid is an antifibrinolytic. It inhibits the fibrinolysis system and thus ultimately inhibits clot dissolution ( fibrinolysis ).

Tranexamic acid is produced exclusively synthetically and is similar to lysine . The substance belongs to the group of para-aminocarboxylic acids. Tranexamic acid is readily soluble in water, but poorly soluble in ethanol and diethyl ether.

The substance is in a solid state as a beige-colored solid, the melting point is between 386 and 392 degrees Celsius. At these temperatures, the substance decomposes. The molar mass of tranexamic acid is 157.21g x mol ^-1. The chemical molecular formula of the substance is C8H15NO2.

Pharmacological action

Tranexamic acid is administered orally, intravenously or locally. The bioavailability of the substance is 30-50% after oral administration and is not affected by simultaneous food intake. The plasma protein binding is 3%, with the substance being bound almost exclusively to plasmin .

Tranexamic acid crosses the placenta 100%, but only 1% crosses breast milk. Metabolism occurs to a small extent in the liver , 95% of the substance is excreted unchanged in the urine . There is no excretion in the stool . The half-life of tranexamic acid is 2 hours.

Pharmacodynamically, the drug works by blocking the formation of plasmin. This blockage occurs by inhibiting the proteolytic activity of plasminogen activators. Overall, this leads to the plasmin being hindered in its ability or task to dissolve (lyse) fibrin. At low doses, tranexamic acid acts as a competitive inhibitor of plasmin, but at higher doses it is a non-competitive inhibitor.

As already mentioned, the metabolism in the liver takes place only to a very small extent, and 95% of the elimination is renal. If tranexamic acid is administered together with factor IX, the risk of thrombosis increases. Due to the almost exclusively renal elimination, the dose must be adjusted in the case of renal insufficiency .

The active substance is administered orally in the form of tablets or effervescent tablets. Intravenous administration is also possible. Since the substance is also active in urine, it can also be used to treat bleeding in the urinary tract .

Medical Application & Use

Tranexamic acid is an antifibrinolytic. The substance is used medically for the treatment of bleeding due to hyperfibrinolysis, increased blood clot dissolution, and for the prophylaxis of bleeding due to possible hiberfibrinolysis.

In addition, tranexamic acid is used as an antidote for bleeding during fibrinolytic therapy. Further indications are the promotion of coagulation in postpartum bleeding, the prophylaxis of bleeding during dental procedures in patients at risk and the prophylaxis of bleeding in surgical procedures with a high risk of bleeding.

Furthermore, tranexamic acid is used in hypermenorrhea , as an accompanying medication when fibrinogen is administered, and in hereditary angioedema . For nosebleeds , it can be applied using a nebulizer.

Risks & side effects

The side effects of tranexamic acid include allergies , skin rashes , an increased risk of theombosis in patients with a corresponding predisposition (which can result in heart attacks , strokes and pulmonary embolism ), atrial fibrillation and visual disturbances . If factor IX is administered at the same time, the risk of thrombosis increases further.

Tranexamic acid should not be taken in the case of pre-existing thrombosis , or during breastfeeding . Heavy bleeding in the urinary tract can cause clots (“blood clots”) to form, which can lead to urinary retention .

There are also relative contraindications, for example in consumption coagulopathy . Here the individual risk must be weighed up by the doctor. The same applies to bleeding in the urinary tract. While tranexamic acid works well here, there is a risk of clots forming, which can cause urinary retention. This means that there is also a relative contraindication here, for which the risk must be weighed up by the doctor.

Tranexamic acid requires a prescription and may therefore only be administered or prescribed by a doctor, since the administration must always be preceded by a diagnosis and an assessment of the individual risk.

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Hello! I am Lisa Newlon, and I am a medical writer and researcher with over 10 years of experience in the healthcare industry. I have a Master’s degree in Medicine, and my deep understanding of medical terminology, practices, and procedures has made me a trusted source of information in the medical world.