Introduction

Tranexamic acid (TXA) is a synthetic lysine derivative that inhibits fibrinolysis by blocking the lysine binding sites on plasminogen. Plasminogen is an inactive form of plasmin which acts to dissolve fibrin clots.

Key Points

  • Tranexamic acid is a synthetic lysine derivative that inhibits fibrinolysis by blocking lysine binding sites on plasminogen, stabilizing fibrin clots.
  • TXA offers a route-flexible option for several minor bleeding presentations — including topical/soaked gauze for anterior epistaxis and dental bleeding.
  • Across the cited studies, TXA was associated with stopped or reduced bleeding compared with its respective comparators.
  • Rapid IV administration may cause hypotension; use caution in patients on oral contraceptives and those with clotting disorders.

Clinical Detail

PropertiesTranexamic Acid (TXA)
DoseEpistaxis: 500–1000 mg via topical nasal gauze
Heavy Menstrual Bleeding: 1.3 g PO TID
Hemoptysis: 500 mg via nebulizer
FormulationIV 1000 mg/10 ml vial
650 mg tablets
PK/PDOnset IV: 1–5 hours
Time to Peak Concentration PO: 2.5–3 hours; IV: 5 minutes
Duration PO: 24 hours; IV: 17 hours
Excretion: Urine (>95% as unchanged drug)
Adverse EffectsRapid administration could cause hypotension
Drug Interactions and WarningsCaution in women taking oral contraceptives, patients with clotting disorders, and those taking chlorpromazine
CompatibilityCompatible with Normal Saline and Dextrose solutions

Directions for Administration by Indication

IndicationDirections
Anterior EpistaxisConsider using 500–1,000 mg of TXA (5–10 ml) to soak gauze/pledget and insert it into the nasal cavity for ~30 min
Heavy Menstrual BleedingConsider administering 1300 mg of oral TXA tablets TID x 7 days
HemoptysisConsider mixing 500–1000 mg of TXA (5–10 ml) with 5–10 ml of NS then administer via nebulizer
Dental BleedingConsider dissolving 1–2 650 mg TXA tablets in 10 mL distilled water, then swish for two minutes followed by expectoration

Evidence

Author, yearIndicationIntervention & ComparisonOutcome
Bryant-Smith (Cochrane), 2018Heavy menstrual bleedingTXA*TXA associated with a reduced blood loss of −53.20 to −73 ml per cycle and ↑ likelihood of improvement.

Effective for treating HMB compared to placebo, NSAIDs, oral luteal progestogens
Lukes, 2010Heavy menstrual bleedingTXA 1300 mg PO TID x 7 daysTXA had greater ↓ in menstrual blood loss, ↓ menstrual blood loss exceeding 50 mL, and ↑ QOL compared with women receiving placebo
Zirk, 2018Dental BleedingTXA soaked gauze*TXA provided ↑ chance to stop oral bleeding event by a factor of 1.6 over gauze alone
Nuvvula, 2014Dental BleedingDissolved 500 mg TXA tablets in 10 mL distilled waterTopical TXA was non-inferior and an effective alternative to factor therapy in controlling gingival hemorrhage.
Zahed, 2018Anterior EpistaxisTopical TXA 500 mg soaked gauzeBleeding was stopped in 73% of the patients in the TXA group, compared with 29% in the ANP group.

At 1 week, rebleeding was 5% vs 21% in TXA and nasal packing respectively
Zahed, 2013Anterior EpistaxisTopical TXA 500 mg soaked gauzeWithin 10 minutes of treatment, bleeding stopped in 71% of the patients in the tranexamic acid group, compared with 31.2% in the anterior nasal packing group
Wand, 2018HemoptysisNebulized TXA 500 mg/5 ml↑ Rate of complete resolution of hemoptysis during first 5 days, ↓ LOS, and ↓ daily volume of expectorated blood
Solomonov, 2009HemoptysisNebulized TXA 500 mg/5 mlIn all cases, the bleeding stopped with the first dose of TXA and was well tolerated without adverse events

* Dose not recorded

Conclusions

  • Tranexamic acid (TXA) is a synthetic lysine derivative that inhibits fibrinolysis by blocking lysine binding sites on plasminogen, stabilizing the fibrin clot.
  • TXA offers a route-flexible option for several minor bleeding presentations on this page — topical/soaked gauze for anterior epistaxis and dental bleeding, oral dosing for heavy menstrual bleeding, and nebulized administration for hemoptysis.
  • Across the cited studies, TXA was associated with stopped or reduced bleeding compared with its respective comparators (e.g., anterior nasal packing, placebo, or gauze alone) and was generally well tolerated.
  • Rapid IV administration may cause hypotension, and caution is warranted in patients on oral contraceptives, those with clotting disorders, and those taking chlorpromazine.

References

Tranexamic acid. Micromedex [Electronic version].Greenwood Village, CO: Truven Health Analytics. Retrieved September 6, 2018, from http://www.micromedexsolutions.com/

Bryant-Smith AC et al. Antifibrinolytics for heavy menstrual bleeding. Cochrane Database Syst Rev. 2018 Apr 15;4. PMID: 29656433.

Lukes AS et al. Tranexamic acid treatment for heavy menstrual bleeding: a randomized controlled trial. Obstet Gynecol. 2010 Oct;116(4):865-75. PMID: 20859150

Zirk M et al. Supportive topical tranexamic acid application for hemostasis in oral bleeding events – Retrospective cohort study of 542 patients. J Craniomaxillofac Surg. 2018 Jun;46(6):932-936. PMID: 29627368

Nuvvula S et al. Efficacy of tranexamic acid mouthwash as an alternative for factor replacement in gingival bleeding during dental scaling in cases of hemophilia: A randomized clinical trial. Contemp Clin Dent. 2014 Jan-Mar; 5(1): 49-53. PMID: 24808695

Zahed R et al. A New and Rapid Method for Epistaxis Treatment Using Injectable arm of Tranexamic Acid Topically: A Randomized Controlled Trial Am J Emerg Med 2013. PMID: 23911102

Zahed R et al. Topical Tranexamic Acid Compared With Anterior Nasal Packing for Treatment of Epistaxis in Patients Taking Antiplatelet Drugs: Randomized Controlled Trial. Acad Emerg Med. 2018 Mar;25(3):261-266. PMID: 29125679

Wand O et al. Inhaled Tranexamic Acid for Hemoptysis Treatment: A Randomized Controlled Trial. CHEST 2018. PMID: 30321510

Solomonov A et al. Pulmonary hemorrhage: A novel mode of therapy. Respir Med. 2009 Aug;103(8):1196-200.

How To Place An Epistaxis TXA Pack. https://www.youtube.com/watch?v=ekGsM9CZSpY

Tags:tranexamic acid TXA minor bleeding topical