Tranexamic acid is antifibrinolytic medication that has numerous applications. It is primarily used to control bleeding – in particular heavy menstrual bleeding and bleeding associated with oral surgeries. First discovered in the 1960s, tranexamic acid is now included on the World Health Organization’s list of essential medicines and is used regularly in clinics throughout the world. It is only recently that it has been recognized for its potential to save lives with large-scale clinical trials. If given within three hours of an injury, tranexamic acid may reduce the risk of death from bleeding by up to one third.

History of Tranexamic Acid

Tranexamic acid was first discovered in the early 1960s by the husband and wife researchers Shosuke and Utako Okamoto. They were looking for a drug that could help control post-partum bleeding – one of the leading causes of death after childbirth worldwide. Their results were published in 1962. At the time they were unable to convince obstetricians to conduct a trial with the drug for their intended use. It was not until 2010 that a large-scale study was started on the effects of tranexamic acid on mortality from hemorrhaging after childbirth. Utako Okamoto became a chair at Kobe Gakuin University in 1966 after she published her research and worked there until she retired in 1990, but died before the completion of the large-scale post-partum study was published in 2016.

Applications of Tranexamic Acid Include

The use of tranexamic acid has expanded over the years so that it now has applications across many specialties. Initially only used for minor dental procedures, it is now used in hospitals and clinics around the world as an effective way to prevent bleeding that could lead to serious complications.

Post-partum bleeding

A large, international study was conducted on the use of tranexamic acid after childbirth to prevent hemorrhaging.  Post-partum hemorrhage is the leading cause of maternal death worldwide. A majority of these deaths occur in low- and middle-income countries. The trial found that tranexamic acid significantly reduced the risk of death from hemorrhaging after childbirth. Although this was the application that the researchers who initially discovered tranexamic acid were mainly focused on, it was not for over 50 years that a large-scale study was completed.

Mouthwash for oral procedures

An antifibrinolytic mouthwash can be used for controlling bleeding after an oral procedure such as a tooth extraction. The tranexamic acid mouthwash is used prior to the procedure and immediately afterwards to prevent and reduce bleeding. It is then used daily for about a week after the procedure. This treatment is especially effective for patients with blood clotting disorders.

Heavy menstruation

Tranexamic acid can help with heavy menstruation. It is available commercially in tablet form and sold under the brand name Lysteda for this indication. The tablets are made in 650mg doses and for menstrual bleeding the dose is 3,900mg per day for a maximum of 5 days during menstruation.

Nose bleeds

A topically applied tranexamic acid solution can help reduce nose bleeds. Gauze can be soaked in the solution then held inside the nose for about an hour.  In a randomized, controlled trail, it was demonstrated that within 10 minutes of treatment with tranexamic acid, bleeding was stopped in 71% of patients compared to 31.2% who were given anterior nasal packing.

Melasma

Topically applied tranexamic acid has been shown to significantly improve the appearance of melasma. When compared to a combination of hydroquinone and dexamethasone, it produced no noticeable difference in results but had less side effects. Tranexamic acid is now combined with other ingredients like kojic acid and niacinamide in serums that reduce discoloration. Our pharmacy compounds a tranexamic acid cream with these ingredients.

CRASH-2 Trial

The CRASH-2 trial was a UK government-funded trial studying the effects of tranexamic acid on trauma patients. The study was published in 2010 and was undertaken in 274 hospitals in 40 countries. The results showed that all-cause mortality was reduced significantly by the use of tranexamic acid. In order to be effective, it must be administered within 3 hours after an injury. However, the strongest effects were seen in patients who received it within an hour. The study recommended that for patients who are admitted later than 3 hours after their injury, tranexamic acid should not be used as it could be harmful.

Compounding Tranexamic Acid Solution

At our compounding pharmacy we specialize in providing customized medications to provide optimal outcomes for patients. We frequently prepare a tranexamic acid 4.8% solution at our compounding pharmacy. However, we can make any dosage based on a prescriber’s needs. We ship this medication directly to a healthcare office or to the patient’s home if needed.

Research

• Topical tranexamic acid as a promising treatment for melasma –  Journal of Research in Medical Sciences
• Effect of early tranexamic acid administration on mortality, hysterectomy, and other morbidities in women with post-partum haemorrhage (WOMAN): an international, randomised, double-blind, placebo-controlled trial – The Lancet
• Utako Okamoto – Obituary – The Lancet
• The CRASH-2 trial: a randomised controlled trial and economic evaluation of the effects of tranexamic acid on death, vascular occlusive events and transfusion requirement in bleeding trauma patients. – PubMed
• A new and rapid method for epistaxis treatment using injectable form of tranexamic acid topically: a randomized controlled trial. – American Journal of Emergency Medicine