Tranexamic acid

Tranexamic acid
Clinical data
Pronunciation \ˌtran-eks-ˌam-ik-\
AHFS/Drugs.com Consumer Drug Information
Pregnancy
category
  • B
Routes of
administration		 Injection and oral
ATC code B02AA02 (WHO)
Legal status
Legal status
  • P (UK)
Pharmacokinetic data
Bioavailability 34%
Biological half-life 3.1 h
Identifiers
CAS Number 1197-18-8 YesY
PubChem (CID) 5526
IUPHAR/BPS 6573
DrugBank DB00302 YesY
ChemSpider 10482000 YesY
UNII 6T84R30KC1 YesY
KEGG D01136 YesY
ChEBI CHEBI:48669 YesY
ChEMBL CHEMBL877 YesY
ECHA InfoCard 100.013.471
Chemical and physical data
Formula C8H15NO2
Molar mass 157.21 g/mol
3D model (Jmol) Interactive image
  (verify)

Tranexamic acid (TXA) is a medication used to treat or prevent excessive blood loss from trauma, surgery, and in various medical conditions including hemophilia and heavy menstrual bleeding.[1] It comes in oral and intravenous forms.[1]

Side effects are uncommon and include gastrointestinal effects, dizziness, fatigue, headache, and hypersensitivity reactions.[2] The medication needs to be used cautiously in people with kidney disease and who are at a high risk for blood clots.[1] Tranexamic is safe to use in pregnant women. However, caution should be used in lactating women.[1] It is an antifibrinolytic.

It was discovered in 1962 by Utako Okamoto[3] and has been on the World Health Organization's List of Essential Medicines, the most important medications needed in a basic health system.[4]

Medical uses

Tranexamic acid is frequently used following major trauma.[5] 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.[6][7]

Trauma

Tranexamic acid has been found to decrease the risk of death in people who have significant bleeding due to trauma.[8][9] Its main benefit is if taken within the first three hours.[10]

Heavy menstrual bleeding

Tranexamic acid is used to treat heavy menstrual bleeding.[7] When taken by mouth it both safely and effectively treats regularly occurring heavy menstrual bleeding.[2][11] Another study demonstrated that the dose does not need to be adjusted in females who are between ages 12 and 16.[2]

Surgery

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.[1] 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.[14] 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 demopressin effectively stopped bleeding[15]

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

Adverse effects

Common side effects include:[2]

Rare side effects include:[2]

These rare side effects were reported in post marketing experience and frequencies cannot be determined.[2]

Special populations

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.[2] 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.[3] It has been included in the WHO list of essential medicines.[4] TXA is inexpensive and treatment would be considered highly cost effective in high, middle and low income countries.[22]

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)[23] 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.[24] (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.[25]

References

  1. 1 2 3 4 5 "Cyklokapron (tranexamic acid) Product Information" (PDF). Retrieved 3 November 2015.
  2. 1 2 3 4 5 6 7 8 9 10 11 12 "Lysteda (tranexamic acid) Package Insert" (PDF). accessdata.FDA.gov. Retrieved 2 November 2015.
  3. 1 2 Geoff Watts (2016). "Obituary Utako Okamoto". The Lancet. 387 (10035): 2286. doi:10.1016/S0140-6736(16)30697-3.
  4. 1 2 "19th WHO Model List of Essential Medicines (April 2015)" (PDF). WHO. April 2015. Retrieved May 10, 2015.
  5. ↑ Binz, S; McCollester, J; Thomas, S; Miller, J; Pohlman, T; Waxman, D; Shariff, F; Tracy, R; Walsh, M (2015). "CRASH-2 Study of Tranexamic Acid to Treat Bleeding in Trauma Patients: A Controversy Fueled by Science and Social Media.". Journal of blood transfusion. 2015: 874920. doi:10.1155/2015/874920. PMID 26448897.
  6. ↑ Melvin, JS; Stryker, LS; Sierra, RJ (22 October 2015). "Tranexamic Acid in Hip and Knee Arthroplasty.". The Journal of the American Academy of Orthopaedic Surgeons. 23: 732–40. doi:10.5435/JAAOS-D-14-00223. PMID 26493971.
  7. 1 2 Tengborn, L; Blombäck, M; Berntorp, E (February 2015). "Tranexamic acid--an old drug still going strong and making a revival.". Thrombosis research. 135 (2): 231–42. doi:10.1016/j.thromres.2014.11.012. PMID 25559460.
  8. ↑ Cherkas, David (Nov 2011). "Traumatic Hemorrhagic Shock: Advances In Fluid Management". Emergency Medicine Practice. 13 (11).
  9. ↑ "Drug will save lives of accident victims, says study". BBC News. 2010. Retrieved 3 June 2016.
  10. ↑ Napolitano, Lena M.; Cohen, Mitchell J.; Cotton, Bryan A.; Schreiber, Martin A.; Moore, Ernest E. (2013). "Tranexamic acid in trauma". Journal of Trauma and Acute Care Surgery. 74 (6): 1575–86. doi:10.1097/TA.0b013e318292cc54. PMID 23694890.
  11. ↑ Lukes, AS; Moore, KA; Muse, KN (2010). "Tranexamic acid treatment for heavy menstrual bleeding: a randomized controlled trial". Obstet Gynecol. 116 (4): 865–875. doi:10.1097/AOG.0b013e3181f20177. PMID 20859150.
  12. ↑ RCPCH. "Evidence Statement Major trauma and the use of tranexamic acid in children Nov 2012" (PDF). Retrieved 17 December 2012.
  13. ↑ Sethna, N. F.; Zurakowski, D; Brustowicz, R. M.; Bacsik, J; Sullivan, L. J.; Shapiro, F (2005). "Tranexamic acid reduces intraoperative blood loss in pediatric patients undergoing scoliosis surgery". Anesthesiology. 102 (4): 727–32. doi:10.1097/00000542-200504000-00006. PMID 15791100.
  14. ↑ Forbes CD, Barr RD, Reid G; et al. (1972). "Tranexamic acid in control of haemorrhage after dental extraction in haemophilia and Christmas disease". Br Med J. 2 (5809): 311–313. doi:10.1136/bmj.2.5809.311.
  15. ↑ Shankar S & Lee R (1984). "DDAVP and tranexamic acid for dental extractions in a mild hemophiliac". Br Dent J. 156 (12): 450–452. doi:10.1038/sj.bdj.4805387.
  16. ↑ "Protocol 09PRT/4179:Tranexamic acid for the treatment of postpartum haemorrhage: an international, randomised, double blind, placebo controlled trial (the WOMAN Trial)". The Lancet. Elsevier Limited. n.d. Retrieved 3 June 2016.
  17. ↑ Rod Flower; Humphrey P. Rang; Maureen M. Dale; Ritter, James M. (2007). Rang & Dale's pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-06911-5.
  18. ↑ Klepfish, A; Berrebi, A; Schattner, A (2001). "Intranasal tranexamic acid treatment for severe epistaxis in hereditary hemorrhagic telangiectasia". Archives of Internal Medicine. 161 (5): 767. doi:10.1001/archinte.161.5.767. PMID 11231712.
  19. ↑ Karn, D; Kc, S; Amatya, A; Razouria, E. A.; Timalsina, M (2012). "Oral tranexamic acid for the treatment of melasma". Kathmandu University Medical Journal. 10 (40): 40–3. doi:10.3126/kumj.v10i4.10993. PMID 23575051.
  20. ↑ Gharaibeh, Almutez; Savage, Howard I; Scherer, Roberta W; Goldberg, Morton F; Lindsley, Kristina (2011). "Medical interventions for traumatic hyphema". Cochrane Database of Systematic Reviews (1): CD005431. doi:10.1002/14651858.CD005431.pub2. PMC 3437611Freely accessible. PMID 21249670.
  21. ↑ "Tranexamic Acid use while Breastfeeding". www.drugs.com. 7 Nov 2014. Retrieved 27 May 2016.
  22. ↑ Guerriero, Carla; Cairns, John; Perel, Pablo; Shakur, Haleema; Roberts, Ian; Crash 2 Trial, Collaborators (2011). "Cost-Effectiveness Analysis of Administering Tranexamic Acid to Bleeding Trauma Patients Using Evidence from the CRASH-2 Trial". PLoS ONE. 6 (5): e18987. Bibcode:2011PLoSO...618987G. doi:10.1371/journal.pone.0018987. PMC 3086904Freely accessible. PMID 21559279.
  23. ↑ Tranexamic Acid to be available OtC
  24. ↑ In defence of multiple pharmacies
  25. ↑ Allen, Helen (June 13, 2012). "Tranexamic acid for bleeding". Patient UK.
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