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Irischen1/sandbox
Clinical data
Pronunciation\ˌtran-eks-ˌam-ik-\
AHFS/Drugs.comConsumer Drug Information
Pregnancy
category
  • B
Routes of
administration		Injection and oral
ATC code
Legal status
Legal status
  • P (UK)
Pharmacokinetic data
Bioavailability34%
Elimination half-life3.1 h
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
Chemical and physical data
FormulaC8H15NO2
Molar mass157.21 g/mol g·mol−1
3D model (JSmol)
  • NC[C@@H]1CC[C@H](CC1)C(O)=O
  • InChI=1S/C8H15NO2/c9-5-6-1-3-7(4-2-6)8(10)11/h6-7H,1-5,9H2,(H,10,11)/t6-,7- checkY
  • Key:GYDJEQRTZSCIOI-LJGSYFOKSA-N checkY
  (verify)

Tranexamic acid or TXA is used to treat or prevent excessive blood loss during surgery and in various medical conditions or disorders including hemophilia and heavy menstrual bleeding[1]. Side effects are rare (<10%) and include gastrointestinal effects, dizziness, fatigue, headache, and hypersensitivity reactions [2]. Use of tranexamic acid has a potential risk of thrombosis[3].Care should be used in those with kidney disease and high risk of blood clots[1].Tranexamic is safe to use in pregnant women. However, caution should be used in lactating women[1]. It comes in oral and intravenous forms [1]. It is on the World Health Organization's List of Essential Medicines, the most important medications needed in a basic health system.[4]

Mechanism of action

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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.

Medical uses

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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 such as heart, orthopedic, craniofacial, and other procedures.

Prophylactic Tooth Extraction in Hemophilia Patients

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In the United States, tranexamic acid is FDA approved for short-term use in patients with severe bleeding disorders who are about to have dental surgery [1]. Transexamic 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 this patient population [5]. In hemophilia patients, combinations of transexamic acid and factor VII or IX have effectively decreased blood loss and the need for transfusions after dental surgery In one patient with mild hemophilia, a combination of tranexamic acid and demopressin effectively stopped bleeding[6]

Heavy Menstrual Bleeding

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In the United States, tranexamic acid is FDA approved to treat heavy menstrual bleeding that occurs repeatedly [2]. Two randomized, double-blind placebo controlled studies demonstrated that oral tranexamic acid tablets safely and effectively treated regularly occurring heavy menstrual bleeding [7] [2]. Another study demonstrated that the dose does not need to be adjusted in patients who are between ages 12 and 16 [2]. Tranexamic acid is also used to treat abnormal heavy bleeding during menstruation, including abnormal heavy bleeding patterns that were caused by an intrauterine device [8]

Orthopedic surgery

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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. However, the hidden blood loss is not reduced. Still, it is becoming an important tool in the anaesthetist's arsenal. It is commonly used in joint replacement surgery.

Craniofacial surgery

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Use of tranexamic acid in surgical corrections of craniosynostosis in children reduces the need for blood transfusions.[9]

Other uses

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  • In obstetrics, tranexamic acid is used after delivery to reduce bleeding, often with syntocinon/oxytocin and fundal massage. A major trial is in progress worldwide to establish the efficacy of the drug to arrest postpartum haemorrhage (PPH). 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 cardiac surgery, e.g. coronary artery bypass surgery, it is used to prevent excessive blood loss.
  • In spine surgery, e.g. scoliosis correction with posterior spinal fusion using instrumentation, to prevent excessive blood loss. [10]
  • In hereditary angioedema[11]
  • 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.[12]
  • In melasma - Tranexamic acid has shown to provide rapid and sustained lightening in melasma by decreasing melanogenesis in epidermal melanocytes.[13]
  • In hyphema - Tranexamic acid has been shown to be effective in reducing risk of secondary hemorrhage outcomes in patients with traumatic hyphema.[14]

Adverse effects

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Common side effects include: [2]

  • Headaches (50.4 - 60.4%)
  • Backaches (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: [2]

  • Pulmonary embolism
  • Deep vein thrombosis
  • Anaphylaxis
  • Visual disturbances

Precautions in Special Populations

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Tranexamic acid is categorized as pregnancy category B. No harm to the fetus was observed in reproductive studies with mice, rats and rabbits. [2]

In lactating mothers, transexamic acid is present in the mother's milk and should only be used if there is a clear indication for the medication. [2]

Tranexamic acid is indicated for lactating women and is not well studied nor intended for use in premenarchial girls (<12 years of age). [2]

Tranexamic acid is also not indicated for postmenopausal women and geriatrics. [2]

In renal 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. [2]

In hepatic impairment, dose adjustment is not needed as only a small fraction of the drug is metabolized through the liver. [2]

Society and culture

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Tranexamic acid has been included in the WHO list of essential medicines.[15] Tranexamic acid is inexpensive and treatment would be considered highly cost effective in high, middle and low income countries.[16]

Brand names

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Tranexamic acid is marketed in the U.S. and Australia in tablet form as Lysteda and in IV form as Cyklokapron and Transamin, 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

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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)[17] 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.[18] (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.[19]

References

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  1. ^ a b c d e "Cyklokapron (tranexamic acid) Product Information" (PDF). Retrieved 3 November 2015.
  2. ^ a b c d e f g h i j k l m "Lysteda (tranexamic acid) Package Insert" (PDF). accessdata.FDA.gov. Retrieved 2 November 2015.
  3. ^ "Pitt Trauma Experts Aim to Reduce Deaths by Providing Blood-Clotting Agent on Medical Helicopters".
  4. ^ "19th WHO Model List of Essential Medicines" (PDF).
  5. ^ 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 (809): 311–3. doi:10.1136/bmj.2.5809.311. PMC 1788188. PMID 4553818. {{cite journal}}: Explicit use of et al. in: |last1= (help)CS1 maint: multiple names: authors list (link)
  6. ^ Shankar S & Lee R (1984). "DDAVP and tranexamic acid for dental extractions in a mild hemophiliac". Br Dent J. 156 (12): 450–2. doi:10.1038/sj.bdj.4805387. PMID 6235829. S2CID 27253611.
  7. ^ 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:10.2147/IJWH.S13840. PMC 3430088. PMID 22956886.{{cite journal}}: CS1 maint: unflagged free DOI (link)
  8. ^ Ylikorkala, O; Viinikka, L (1983). "Comparison between antifibrinolytic and antiprostaglandin treatment in the reduction of increased menstrual blood loss in women with intrauterine contraceptive devices". Br J Obstet Gynaecol. 90 (1): 78–83. doi:10.1111/j.1471-0528.1983.tb06751.x. PMID 6336951. S2CID 38361178. Retrieved 3 November 2015.
  9. ^ RCPCH. "Evidence Statement Major trauma and the use of tranexamic acid in children Nov 2012" (PDF). Retrieved 17 December 2012.
  10. ^ 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. S2CID 790638.
  11. ^ Rod Flower; Humphrey P. Rang; Maureen M. Dale; Ritter, James M. (2007). Rang & Dale's pharmacology. Edinburgh: Churchill Livingstone. ISBN 978-0-443-06911-6.{{cite book}}: CS1 maint: multiple names: authors list (link)[page needed]
  12. ^ 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.
  13. ^ 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.
  14. ^ Gharaibeh, Almutez; Savage, Howard I; Scherer, Roberta W; Goldberg, Morton F; Lindsley, Kristina (2011). Scherer, Roberta W (ed.). "Medical interventions for traumatic hyphema". Cochrane Database of Systematic Reviews (1): CD005431. doi:10.1002/14651858.CD005431.pub2. PMC 3437611. PMID 21249670.
  15. ^ WHO. "Summary of the report of the 18th meeting of the WHO Expert Committee on the Selection and Use of Essential Medicines" (PDF). {{cite journal}}: Cite journal requires |journal= (help)
  16. ^ 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 3086904. PMID 21559279. {{cite journal}}: |first6= has generic name (help)CS1 maint: numeric names: authors list (link) CS1 maint: unflagged free DOI (link)
  17. ^ Tranexamic Acid to be available OtC[full citation needed]
  18. ^ In defence of multiple pharmacies[full citation needed]
  19. ^ Allen, Helen (13 June 2012). "Tranexamic acid for bleeding". Patient UK.
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Category:Antifibrinolytics Category:Amino acids Category:Cyclohexanecarboxylic acids

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