{Hemostatics}

TRANEXAMIC ACID

Adult Dosing

• Menorrhagia
  • 1300 mg PO TID x 5 days during menstruation
• Dental Extraction
  • 25 mg/kg PO 2 hrs prior to procedure, THEN 25 mg/kg TID/QID up to 10 days post-procedure
  • 10 mg/kg IV 2 hrs prior to procedure, THEN 10 mg/kg TID/QID x 2-8 days post-procedure
• Surgery
  • Cardiac
    • Load 2.5–100 mg/kg IV, THEN 0.25–4 mg/kg/hr over 1–12 hrs
    • NMT 30–50 mg/kg generally recommended (increased seizure risk)
  • Orthopedic
    • Load 10–30 mg/kg IV with/without maintenance infusion of 1 mg/kg/hr
• Epistaxis
  • 1500 mg PO BID up to 10 days
• Hereditary angioedema
  • Initial 500-650 mg PO BID/TID
  • May titrate up to 3000 mg/day
• Intracranial hemorrhage (post thrombolytic Tx)
  • 1000 mg or 10-15 mg/kg IV x1
• Postpartum hemorrhage
  • 1000 mg IV over 10-20 min given within 3 hrs of delivery
  • If continued bleeding after 30 min, may repeat
• TBI
  • Load 1000 mg IV over 10 min within 3 hrs of injury, THEN
  • 1000 mg over next 8 hrs as continuous infusion
• Administration
  • PO: take with/without food
    • Swallow tabs whole; do not chew or break
  • IV: see IV information

Pediatric Dosing

• Menorrhagia (postmenarche)
  • As adult
• Dental Extraction
  • 10 mg/kg IV just prior to procedure, THEN 10 mg/kg TID/QID x 2-8 days post-procedure
• Trauma
  • <12 yo: load 15 mg/kg (NMT 1000 mg) IV over 10 min within 3 hrs of injury, THEN
    • 2 mg/kg/hr x ≥8 hrs
  • ≥12 yo: load 1000 mg IV over 10 min given within 3 hrs of injury, THEN
    • 1000 mg over 8 hrs

Renal and Hepatic Dosing

• Renal
  • Menorrhagia
    • SCr 1.4-2.8 mg/dL: 1300 mg PO BID
    • SCr 2.8-5.7 mg/dL: 1300 mg PO qD
    • SCr > 5.7 mg/dL: 650 mg PO qD
  • Dental Extraction
    • SCr 1.36-2.83 mg/dL (120-250 umol/L): 10 mg/kg IV BID
    • SCr 2.83-5.66 mg/dL (250-500 umol/L): 10 mg/kg IV qD
    • SCr >5.66 mg/dL (>500 umol/L): 10 mg/kg IV q48hr OR 5 mg/kg IV qD
• Hepatic
  • No dosage adjustment necessary

Contraindications & Cautions

• Contraindications
  • Hypersensitivity
  • Females of reproductive potential known to have:
    • Active thromboembolic disease
    • Hx of thrombosis or thromboembolism, including retinal vein or artery occlusion
    • An intrinsic risk of thrombosis or thromboembolism
    • Using combined hormonal contraception
  • Subarachnoid hemorrhage
  • Active intravascular clotting
• Cautions
  • Renal impairment
  • DIC
  • Thromboembolic history
  • Concomitant Factor IX complex, anti-inhibitor concentrates, oral tretinoin may incr thrombosis risk
  • D/C if visual or ocular symptoms occur
  • May cause cerebral edema and cerebral infarction in women with subarachnoid hemorrhage
  • Ligneous conjunctivitis reported

Indications & Uses

• Short-term use in prevention of hemorrhage d/t dental procedures in hemophiliacs
• Menorrhagia
• Off label: trauma, surgery, epistaxis, hereditary angioedema, hemorrhage

Mechanism of Action

• Inhibits fibrinolysis through inhibition of plasminogen activator substances; also exhibits antiplasmin activity (10x more potent in vitro than aminocaproic acid)

Adverse Drug Reactions

• Frequency not defined
  • diarrhea, hypotension (if inj too rapid), nausea/vomiting, visual abnormalities

Pregnancy and Lactation

• Pregnancy
  • Risk Summary: data insufficient to establish potential fetal risk
    • 2 observed cases with structural abnormalities resulting in death with 1st trimester exposure
    • However, causation not established
  • Human Data: known to pass the placenta
    • Appears in cord blood at concentrations equal to maternal concentration
  • Animal Data: no adverse fetal outcomes observed at 3x MRHD
• Lactation
  • Risk Summary: known to be present in human milk
  • Effect on production: unknown
  • Minimizing exposure: weigh risk/benefit of breastfeeding with Tx
• Reproductive Risk
  • Contraception: hormonal contraceptives may increase risk for thromboembolic ADRs
    • Use an effective alternative (nonhormonal) contraceptive method
  • Fertility: no effect on fertility or reproductive function in animal studies at 4-5x MRHD

Kinetics/Dynamics

• Half-Life: 2 hrs
• Duration: 3 hrs (after 1 dose)
• Peak Plasma (after 2 g PO)
  • Time: 3 hrs
  • Concentration: 15 mg/L
• Protein Bound: 3%
• Vd: 9-12 L
• Clearance: 110-116 mL/min
• Excretion: urine (95%)

Overdose Management

• Symptomatic Tx

Interactions

• Go to Drug Interactions [DI]

Trade Names

* = Discontinued

• United States: Cyklokapron; Lysteda
• Canada: Cyklokapron

IV Info

• IV Incompatibilities
  • Additive: blood, penicillin
• IV Compatibilities
  • Solution: compatible with most common solutions for infusion
  • Additive: heparin
• IV Preparation
  • Prepare solution same day it will be used
  • Dilute a single dose w/t 50 mL compatible fluid (eg, NS, Ringers, dextrose/water)
• IV Administration
  • 100 mg or fraction thereof over at least 1 minute, usually 5 min
  • Avoid rapid infusion
• Storage
  • Store at 25°C (77°F)

Other Information

• Class: Hemostatics
• Requires prescription
• ATC Code: B02AA02
• Cost Info: Generic ($$$) | Brand ($$$$)
• Medicare Part D: Coverage

References

1. ASHP Drug Compendium (Tranexamic Acid (Systemic); Hemostatics)
2. FDA Monograph (Lysteda) https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022430s009lbl.pdf (Accessed April 2024)
3. FDA Monograph (Cyklokapron) https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/019281Orig1s047lbl.pdf (Accessed April 2024)
4. Beno S, Ackery AD, Callum J, et al. Tranexamic acid in pediatric trauma: why not?. Crit Care. 2014;18(4):313.
5. Busse PJ, Christiansen SC, Riedl MA, et al. US HAEA Medical Advisory Board 2020 guidelines for the management of hereditary angioedema. J Allergy Clin Immunol Pract. 2021;9(1):132-150.e3.
6. Chimento GF, Huff T, Ochsner JL, Meyer M, Brandner L, Babin S. An evaluation of the use of topical tranexamic Acid in total knee arthroplasty. J Arthroplasty. 2013;28(8 Suppl):74-77.
7. CRASH-3 Trial Collaborators. Effects of tranexamic acid on death, disability, vascular occlusive events and other morbidities in patients with acute traumatic brain injury (CRASH-3): a randomised, placebo-controlled trial. Lancet. 2019;394(10210):1713-1723.
8. Faraoni D, Goobie SM. New insights about the use of tranexamic Acid in children undergoing cardiac surgery: from pharmacokinetics to pharmacodynamics. Anesth Analg. 2013;117(4):760-762.
9. Hourlier H, Fennema P. Single tranexamic acid dose to reduce perioperative morbidity in primary total hip replacement: a randomised clinical trial. Hip Int. 2013:0.
10. Huang F, Wu D, Ma G, Yin Z, Wang Q. The use of tranexamic acid to reduce blood loss and transfusion in major orthopedic surgery: a meta-analysis. J Surg Res. 2013.
11. Karam JA, Bloomfield MR, Diiorio TM, Irizarry AM, Sharkey PF. Evaluation of the Efficacy and Safety of Tranexamic Acid for Reducing Blood Loss in Bilateral Total Knee Arthroplasty. J Arthroplasty. 2013.
12. Lipsky AM, Abramovich A, Nadler R, et al. Tranexamic acid in the prehospital setting: Israel Defense Forces' initial experience. Injury. 2013.
13. Makhija N, Sarupria A, Kumar Choudhary S, Das S, Lakshmy R, Kiran U. Comparison of Epsilon Aminocaproic Acid and Tranexamic Acid in Thoracic Aortic Surgery: Clinical Efficacy and Safety. J Cardiothorac Vasc Anesth. 2013.
14. Morrison JJ, Ross JD. Is viscoelastic evidence of hyperfibrinolysis the ideal indicator for tranexamic acid administration in trauma? J Trauma Acute Care Surg. 2013;75(4):743.
15. Myles PS. Antifibrinolytics, aspirin and cardiac surgery: evidence, guidelines and implications for current research. Anaesth Intensive Care. 2014; 42:293-7.
16. Napolitano LM, Cohen MJ, Cotton BA, Schreiber MA, Moore EE. Re: Is viscoelastic evidence of hyperfibrinolysis the ideal indicator for tranexamic acid administration in trauma? J Trauma Acute Care Surg. 2013;75(4):743-744.
17. Powers WJ, Rabinstein AA, Ackerson T, et al. American Heart Association Stroke Council. 2018 guidelines for the early management of patients with acute ischemic stroke: a guideline for healthcare professionals from the American Heart Association/American Stroke Association. Stroke. 2018;49(3):e46-e110.
18. Remérand F, Cotten M, N'guessan YF, et al. Tranexamic acid decreases risk of haematomas but not pain after hip arthroplasty. Orthop Traumatol Surg Res. 2013.
19. 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 [published correction appears in Lancet. 2017;389(10084):2104]. Lancet. 2017;389(10084):2105-2116.

Contributor(s)

1. Reiner, Stefan, PharmD

Updated/Reviewed: April, 2024