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Practice Therapeutics

Efficacy and safety of tranexamic acid in acute haemorrhage

BMJ 2024; 384 doi: https://doi.org/10.1136/bmj-2023-075720 (Published 04 January 2024) Cite this as: BMJ 2024;384:e075720

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The antiplasmin drug tranexamic acid is effective against hemoptysis, epistaxis and melasma, as well as trauma and peripartum hemorrhage.

Dear Editor

Clinical trials suggest that tranexamic acid may offer a modest improvement in mortality in patients at risk of major bleeding due to trauma, but is not beneficial for spontaneous intracranial or gastrointestinal bleeding.[1] Nevertheless, tranexamic acid has been incorporated into the treatment algorithm for the management of a variety of bleeding disorders and angiotensin-converting enzyme inhibitor-induced angioedema. It is currently on the WHO Model List of Essential Medicines as a drug that affects coagulation.[2] It has been included in the treatment algorithm not only for trauma and peripartum hemorrhage, but also for hemoptysis, epistaxis, and oropharyngeal hemorrhage.[3]

Tranexamic acid binds strongly to the lysine binding sites of plasmin and plasminogen, preventing plasmin and plasminogen from binding to fibrin and inhibiting fibrin degradation by plasmin. This antiplasmin effect is the mechanism of hemostatic action.

In addition to hemostasis, antiplasmin action also has a skin whitening effect. When ultraviolet rays act on keratinocytes in the skin, they produce plasmin, a melanocyte activating factor, and melanin production by melanocytes begins. Tranexamic acid blocks the action of plasmin, preventing the activation signal from reaching the melanocytes.

Tranexamic acid has been shown to be effective in the treatment of melasma at an average dose of 250 mg twice daily.[4-6] Although the doses used to treat melasma are significantly lower than those used to treat hemorrhagic disease, tranexamic acid's propensity to induce thromboembolism should be considered. Patients should be screened for thrombotic risk factors prior to initiating oral dosing.

Acknowledgments: none.
Sources of Funding: none.
Disclosure: none.

References:
1. Franchini M, Focosi D, Zaffanello M, Mannucci PM. Efficacy and safety of tranexamic acid in acute haemorrhage. BMJ 2024;384:e075720.
2. WHO Model List of Essential Medicines - 23rd list, 26 July 2023 https://www.who.int/publications/i/item/WHO-MHP-HPS-EML-2023.02
3. Wang K, Santiago R. Tranexamic acid - A narrative review for the emergency medicine clinician. Am J Emerg Med 2022;56:33-44.
4. Del Rosario E, Florez-Pollack S, Zapata L Jr, et al. Randomized, placebo-controlled, double-blind study of oral tranexamic acid in the treatment of moderate-to-severe melasma. J Am Acad Dermatol 2018;78:363-369.
5. Colferai MMT, Miquelin GM, Steiner D. Evaluation of oral tranexamic acid in the treatment of melasma. J Cosmet Dermatol 2019;18:1495-1501.
6. Zhang L, Tan WQ, Fang QQ, et al. Tranexamic Acid for Adults with Melasma: A Systematic Review and Meta-Analysis. Biomed Res Int 2018;2018:1683414.

Competing interests: No competing interests

15 February 2024
Kazuo Komamura
Physician
Mitsunori Iwase
Affiliate Professor, Cardiovascular Research Institute, Yokohama City University, School of Medicine
3-9 Fukuura, Kanazawa-ku, Yokohama-city 236-0004 Japan
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