Tranexamic acid

Updated on Oct 21, 2023

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Trade names Cyklokapron, others Routes of administration by mouth, injection Formula C8H15NO2 Molar mass 157.21 g/mol ATC code B02AA02 (WHO) DrugBank DB00302		Pregnancy category B Bioavailability 34% CAS ID 1197-18-8 Biological half-life 3.1 h Pronunciation ˌtran-eks-ˌam-ik-

AHFS/Drugs.com FDA Professional Drug Information Legal status UK: P (Pharmacy medicines)

Tranexamic acid in the emergency department

Tranexamic acid (TXA) is a medication used to treat or prevent excessive blood loss from major trauma, surgery, tooth removal, nose bleeds, and heavy menstruation. It is also used for hereditary angioedema. It is taken either by mouth or injection into a vein.

Side effects are rare. Some include changes in color vision, blood clots and allergic reactions. Greater caution is recommended in people with kidney disease. Tranexamic appears to be safe for use during pregnancy and breastfeeding. Tranexamic acid is in the antifibrinolytic family of medications.

Tranexamic acid was discovered in 1962 by Utako Okamoto. It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system. Tranexamic acid is available as a generic medication. The wholesale cost in the developing world is about 4.38 to 4.89 USD for a course of treatment. In the United States a course of treatment costs 100 to 200 USD.

Tranexamic acid for the treatment of heavy menstrual bleeding

Medical uses

Tranexamic acid is frequently used following major trauma. Tranexamic acid is used to prevent and treat blood loss in a variety of situations, such as dental procedures for hemophiliacs, heavy menstrual bleeding, and surgeries with high risk of blood loss.

Trauma

Tranexamic acid has been found to decrease the risk of death in people who have significant bleeding due to trauma. Its main benefit is if taken within the first three hours.

Heavy menstrual bleeding

Tranexamic acid is used to treat heavy menstrual bleeding. When taken by mouth it both safely and effectively treats regularly occurring heavy menstrual bleeding. Another study demonstrated that the dose does not need to be adjusted in females who are between ages 12 and 16.

Surgery

Tranexamic acid is used in orthopedic surgery to reduce blood loss, to the extent of reducing or altogether abolishing the need for perioperative blood collection. It is of proven value in clearing the field of surgery and reducing blood loss when given before or after surgery. Drain and number of transfusions are reduced.

In surgical corrections of craniosynostosis in children it reduces the need for blood transfusions.

In spine surgery, e.g. scoliosis correction with posterior spinal fusion using instrumentation, to prevent excessive blood loss.

In cardiac surgery, both with and without cardiopulmonary bypass e.g. coronary artery bypass surgery, it is used to prevent excessive blood loss. It replaces aprotinin.

Dentistry

In the United States, tranexamic acid is FDA approved for short-term use in people with severe bleeding disorders who are about to have dental surgery. Tranexamic acid is used for a short period of time before and after the surgery to prevent major blood loss and decrease the need for blood transfusions. In people with hemophilia, combinations of tranexamic acid and factor VII or IX have effectively decreased blood loss and the need for transfusions after dental surgery In one person with mild hemophilia, a combination of tranexamic acid and desmopressin effectively stopped bleeding

Tranexamic acid is used in dentistry in the form of a 5% mouth rinse after extractions or surgery in patients with prolonged bleeding time, e.g. from acquired or inherited disorders.

Other uses

In obstetrics, tranexamic acid is used after delivery to reduce bleeding, often with syntocinon/oxytocin and fundal massage. Since 2010, the WOMAN (World Maternal Antifibrinolytic) trial has been in progress worldwide to establish the efficacy of the drug to arrest postpartum haemorrhage (PPH) in 15 000 women, due to be completed in 2016. Since the drug can be administered orally, it has great potential to reduce maternal mortality rates in developing countries where primary healthcare is often unavailable.

In hereditary angioedema

In hereditary hemorrhagic telangiectasia - Tranexamic acid has been shown to reduce frequency of epistaxis in patients suffering severe and frequent nosebleed episodes from hereditary hemorrhagic telangiectasia.

In melasma - tranexamic acid is sometimes used in skin whitening as a topical agent, injected into a lesion, or taken by mouth, both alone and as an adjunct to laser therapy; as of 2017 its safety seemed reasonable but its efficacy for this purpose was uncertain because there had been no large scale randomized controlled studies nor long term follow-up studies.

In hyphema - Tranexamic acid has been shown to be effective in reducing risk of secondary hemorrhage outcomes in patients with traumatic hyphema.

Adverse effects

Common side effects include:

Headaches (50.4 - 60.4%)

Back aches (20.7 - 31.4%)

Nasal sinus problem (25.4%)

Abdominal pain (12 - 19.8%)

Diarrhea (12.2%)

Fatigue (5.2%)

Anemia (5.6%)

Rare side effects include:

Pulmonary embolism

Deep vein thrombosis

Anaphylaxis

Visual disturbances

These rare side effects were reported in post marketing experience and frequencies cannot be determined.

Special populations

Tranexamic acid is categorized as pregnancy category B. No harm has been found in animal studies.

Small amounts appears in breast milk if taken during lactation. If it is required for other reasons, breastfeeding may be continued.

Tranexamic acid is also not indicated for postmenopausal women and geriatrics.

In kidney impairment, tranexamic acid is not well studied. However, due to the fact that it is 95% excreted unchanged in the urine, it should be dose adjusted in patients with renal impairment.

In liver impairment, dose change is not needed as only a small amount of the drug is metabolized through the liver.

Mechanism of action

Tranexamic acid is a synthetic analog of the amino acid lysine. It serves as an antifibrinolytic by reversibly binding four to five lysine receptor sites on plasminogen or plasmin. This prevents plasmin from binding to and degrading fibrin and preserves the framework of fibrin's matrix structure. Tranexamic acid has roughly eight times the antifibrinolytic activity of an older analogue, ε-aminocaproic acid.

Society and culture

TXA was discovered in 1962 by Utako Okamoto. It has been included in the WHO list of essential medicines. TXA is inexpensive and treatment would be considered highly cost effective in high, middle and low income countries.

Brand names

Tranexamic acid is marketed in the U.S. and Australia in tablet form as Lysteda and in Australia and Jordan it is marketed in an IV form and tablet form as Cyklokapron, in the UK as Cyclo-F and Femstrual, in Asia as Transcam, in Bangladesh as Traxyl, in India as Pause, in South America as Espercil, in Japan as Nicolda, in France and Romania as Exacyl and in Egypt as Kapron. In the Philippines, its capsule form is marketed as Hemostan and In Israel as Hexakapron.

Approval

The U.S. Food and Drug Administration (FDA) approved tranexamic acid oral tablets (brand name Lysteda) for treatment of heavy menstrual bleeding on 13 November 2009.

In March 2011 the status of tranexamic acid for treatment of heavy menstrual bleeding was changed in the UK, from PoM (Prescription only Medicines) to P (Pharmacy Medicines) and became available over the counter in UK pharmacies under the brand names of Cyklo-F and Femstrual, initially exclusively for Boots pharmacy, which has sparked some discussion about availability. (In parts of Europe - like Sweden - it had then been available OTC for over a decade.) Regular liver function tests are recommended when using tranexamic acid over a long period of time.

References

Tranexamic acid Wikipedia

(Text) CC BY-SA

Jean Guihen Queyras

Christina Scott