tranexamic acid (Cyklokapron, Lysteda)
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Indications
- prevention of bleeding with dental procedures in patients with hemophilia
- reduction of bleeding in trauma patients*[3]
- reduction in menorrhagia[4][5]
- systemic fibrinolysis
- amniotic fluid embolism
- dental procedures
- postpartum hemorrhage*[8]
- nebulized tranexamic acid of benefit in patients with hemoptysis <200 mL[10]
- used routinely to reduce bleeding during cardiac surgery & orthopedic surgery[14]
* effectiveness decreases 10% for every 15-minute delay & is negligible at 3 hours[9]
Contraindications
- history of thrombosis
- high risk of hypercoagulable disorder
- valvular heart disease
- atrial fibrillation
- acute gastrointestinal hemorrhage (ineffective)
- prehospital of tranexamic acid administration may increase mortality in patients with isolated severe traumatic brain injury[12]
- prehospital administration of tranexamic acid after injury does not lower 30 day mortality, but may be safe & associated with survival benefit in specific subgroups of patients[13]
- hemodynamically significant anemia; RBC transfusion indicated[15]
Benefit/risk
- number needed to treat when given within 8 hours of trauma*
- 67 to save 1 life[3]
* effectiveness decreases 10% for every 15-minute delay & is negligible at 3 hours[9]
Dosage
- trauma: 1 g IV over 10 min then 1 g IV over 8 h[3]
- menorrhagia: 1300 mg PO TID for maximum of 5 days ,
Tabs: 650 mg
Dosage adjustment in renal failure
- dosages for menorrhagia
| serum creatinine | dosage < 1.4 mg/dL | 1300 mg TID 1.4-2.7 mg/dL | 1300 mg BID 2.8-5.6 mg/dL | 1300 mg QD >= 5.7 mg/dL | 650 mg QD |
|---|
Adverse effects
- nausea/vomiting
- diarrhea
- musculoskeletal pain, including back pain
- disturbances in color vision
- venous thromboembolism, retinal vein occlusion
- arterial thromboembolism, retinal artery occlusion
- allergic reaction may occur at any time during treatment
- no relevant adverse cardiovascular events if used during noncardiac surgery*[14]
* non inferiority to placebo not shown[14]
Drug interactions
- use of the drug while taking hormonal contraceptives may increase the risk for thrombi, stroke, & myocardial infarction
- concurrent use of facotr IX complex concentrates may increase risk of thrombosis[4]
Mechanism of action
- inhibitor of fibrinolysis
- a derivative of the amino acid lysine
- blocks lysine-binding sites on plasminogen, thus blocking fibrinolysis
- effectiveness decreases 10% for every 15-minute delay is negligible at 3 hours[9]
More general terms
Component of
References
- ↑ Medical Knowledge Self Assessment Program (MKSAP) 11, American College of Physicians, Philadelphia 1998
- ↑ FDA NEWS RELEASE, Nov. 13, 2009 FDA Approves Lysteda to Treat Heavy Menstrual Bleeding http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm190551.htm
- ↑ 3.0 3.1 3.2 3.3 The NNT: Tranexamic Acid for Severe Trauma. http://www.thennt.com/nnt/tranexamic-acid-for-severe-trauma/
CRASH-2 trial collaborators. Effects of tranexamic acid on death, vascular occlusive events, and blood transfusion in trauma patients with significant haemorrhage (CRASH-2): A randomised, placebo-controlled trial. Lancet 2010 Jun 15; [e-pub ahead of print]. <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/20554319 <Internet> http://dx.doi.org/10.1016/S0140-6736(10)60835-5
Levy JH. Antifibrinolytic therapy: New data and new concepts. Lancet 2010 Jun 15; [e-pub ahead of print]. <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/20554318 <Internet> http://dx.doi.org/10.1016/S0140-6736(10)60939-7 - ↑ 4.0 4.1 4.2 Prescriber's Letter 17(8): 2010 COMMENTARY: New Drug: Lysteda (Tranexamic Acid) COMMENTARY: Stop the Bleeding: Tranexamic Acid in Trauma Patients Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=260827&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 5.0 5.1 Lukes AS et al. Tranexamic acid treatment for heavy menstrual bleeding: A randomized controlled trial. Obstet Gynecol 2010 Oct; 116:865 PMID: https://www.ncbi.nlm.nih.gov/pubmed/20859150
- ↑ McNeil DG A Cheap Drug Is Found to Save Bleeding Victims New York Times, March 20, 2012 http://www.nytimes.com/2012/03/21/health/tranexamic-acid-cheap-drug-is-found-to-staunch-bleeding.html
- ↑ 7.0 7.1 Roberts I et al Effect of tranexamic acid on mortality in patients with traumatic bleeding: prespecified analysis of data from randomised controlled trial BMJ 2012;345:e5839 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/22968527 <Internet> http://www.bmj.com/content/345/bmj.e5839
- ↑ 8.0 8.1 WOMAN Trial Collaborators. 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. Lancet 2017 Apr 26 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/28456509 Free Article <Internet> http://www.thelancet.com/journals/lancet/article/PIIS0140-6736(17)30638-4/fulltext
- ↑ 9.0 9.1 9.2 9.3 Gayet-Ageron A, Prieto-Merino D et al. Effect of treatment delay on the effectiveness and safety of antifibrinolytics in acute severe haemorrhage: A meta-analysis of individual patient-level data from 40 138 bleeding patients. Lancet 2017 Nov 7; [e-pub]. <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/29126600 <Internet> http://www.thelancet.com/journals/lancet/article/PIIS0140-6736(17)32455-8/fulltext
Dries DJ. Tranexamic acid: Is it about time? Lancet 2017 Nov 7 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/29126598 <Internet> http://www.thelancet.com/journals/lancet/article/PIIS0140-6736(17)32806-4/fulltext - ↑ 10.0 10.1 Wand O, Guber E, Guber A et al. Inhaled tranexamic acid for hemoptysis treatment. Chest 2018 Dec; 154:1379 PMID: https://www.ncbi.nlm.nih.gov/pubmed/30321510 https://journal.chestnet.org/article/S0012-3692(18)32572-8/fulltext
- ↑ HALT-IT Trial Collaborators. Effects of a high-dose 24-h infusion of tranexamic acid on death and thromboembolic events in patients with acute gastrointestinal bleeding (HALT-IT): An international randomised, double-blind, placebo-controlled trial. Lancet 2020 Jun 20; 395:1927 PMID: https://www.ncbi.nlm.nih.gov/pubmed/32563378 Free PMC article https://www.thelancet.com/pdfs/journals/lancet/PIIS0140-6736(20)30848-5.pdf
- ↑ 12.0 12.1 Bossers SM, Loer SA, Bloemers, FW et al Association Between Prehospital Tranexamic Acid Administration and Outcomes of Severe Traumatic Brain Injury. JAMA Neurol. Published online December 7, 2020 PMID: https://www.ncbi.nlm.nih.gov/pubmed/33284310 https://jamanetwork.com/journals/jamaneurology/article-abstract/2773529
- ↑ 13.0 13.1 Guyette FX, Brown JB, Zenati MS et al Tranexamic Acid During Prehospital Transport in Patients at Risk for Hemorrhage After Injury. A Double-blind, Placebo-Controlled, Randomized Clinical Trial. JAMA Surg. 2021;156(1):11-20 PMID: https://www.ncbi.nlm.nih.gov/pubmed/33016996 PMCID: PMC7536625 https://jamanetwork.com/journals/jamasurgery/fullarticle/2771225
- ↑ 14.0 14.1 14.2 14.3 Devereaux PJ et al. Tranexamic acid in patients undergoing noncardiac surgery. N Engl J Med 2022 Apr 2; [e-pub]. PMID: https://www.ncbi.nlm.nih.gov/pubmed/35363452 https://www.nejm.org/doi/10.1056/NEJMoa2201171
- ↑ 15.0 15.1 NEJM Knowledge+ Hematology