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Drug Reference

tranexamic acid

antifibrinolytic agent· Brands: Cyklokapron, Lysteda, TransaminIVPO

Mechanism of action
Tranexamic acid is a synthetic lysine analogue that reversibly binds to the lysine-binding sites on plasminogen and plasmin. This prevents plasminogen and plasmin from binding to fibrin, thereby inhibiting plasmin-mediated fibrinolysis and stabilising formed clots. It is not a procoagulant and does not initiate clot formation; its action depends on the presence of a fibrin clot. At higher concentrations it may also directly inhibit plasmin activity. The result is reduced bleeding in states of excessive fibrinolysis.
Pharmacokinetics
Oral bioavailability is around 30 to 50 per cent, with peak plasma concentrations about 2 to 3 hours after an oral dose; intravenous administration produces immediate high plasma levels. It distributes into extracellular fluid, crosses the placenta and appears in breast milk in small amounts. Plasma protein binding is low. Elimination is mainly renal as unchanged drug by glomerular filtration, with a terminal half-life of about 2 to 3 hours in normal renal function. The half-life is prolonged in renal impairment, and dose reduction is required; it is removed by haemodialysis.
Indications & dosing

Major trauma with significant haemorrhage

Give within 3 hours of injury as a bolus over 10 minutes, then 1 g infused over 8 hours. Benefit falls sharply when given later than 3 hours, so do not delay resuscitation to give it.

  • adult · IV: 1000 mg single dose · Give within 3 hours of injury as a bolus over 10 minutes, then 1 g infused over 8 hours. Benefit falls sharply when given later than 3 hours, so do not delay resuscitation to give it.

Major trauma with significant haemorrhage

Weight-based dosing, maximum single dose 1 g, then a maintenance infusion as per local paediatric protocol. The 3-hour window applies as in adults.

  • pediatric · IV: 15 mg/kg single dose · Weight-based dosing, maximum single dose 1 g, then a maintenance infusion as per local paediatric protocol. The 3-hour window applies as in adults.

Postpartum haemorrhage

Give within 3 hours of birth alongside uterotonics. A second 1 g dose is given if bleeding continues after 30 minutes or restarts within 24 hours. Inject slowly, rapid injection can cause hypotension.

  • adult · IV: 1000 mg repeat once · Give within 3 hours of birth alongside uterotonics. A second 1 g dose is given if bleeding continues after 30 minutes or restarts within 24 hours. Inject slowly, rapid injection can cause hypotension.

Blood conservation in cardiac surgery with cardiopulmonary bypass

Given before skin incision. Some units add a dose to the bypass prime and a postoperative infusion. Regimens vary widely, so follow the local cardiac surgery protocol.

  • adult · IV: 15 mg/kg single dose · Given before skin incision. Some units add a dose to the bypass prime and a postoperative infusion. Regimens vary widely, so follow the local cardiac surgery protocol.

Heavy menstrual bleeding

Taken on the days of heaviest bleeding, usually the first 3 to 4 days of the cycle. Some formularies use 500 mg three or four times daily. Avoid in active thromboembolic disease.

  • adult · PO: 1000 mg TDS · Taken on the days of heaviest bleeding, usually the first 3 to 4 days of the cycle. Some formularies use 500 mg three or four times daily. Avoid in active thromboembolic disease.

Epistaxis

Short courses only, used with nasal packing or cautery. Topical gauze soaked in tranexamic acid solution is an alternative in some protocols. Investigate recurrent bleeding.

  • adult · PO: 1000 mg TDS · Short courses only, used with nasal packing or cautery. Topical gauze soaked in tranexamic acid solution is an alternative in some protocols. Investigate recurrent bleeding.

Prevention of bleeding after dental extraction in inherited bleeding disorders or in patients on anticoagulants

Usually continued for 5 to 7 days after extraction. Used with local haemostatic measures and with clotting factor replacement where indicated. Follow the haemophilia centre protocol.

  • adult · PO: 25 mg/kg TDS · Usually continued for 5 to 7 days after extraction. Used with local haemostatic measures and with clotting factor replacement where indicated. Follow the haemophilia centre protocol.

Prophylaxis of hereditary angioedema attacksoff-label

Off-label use in some centres for short-term prophylaxis before dental or surgical procedures, and occasionally for long-term prophylaxis. Specialist supervision only.

  • adult · PO: 1000 mg BD-TDS · Off-label use in some centres for short-term prophylaxis before dental or surgical procedures, and occasionally for long-term prophylaxis. Specialist supervision only.
Contraindications & precautions
  • Active thromboembolic disease (e.g. deep vein thrombosis, pulmonary embolism) · Risk of exacerbating thrombosis. Avoid unless required for life-threatening haemorrhage with fibrinolysis; specialist advice needed.
  • History of arterial or venous thromboembolism · Includes previous stroke, myocardial infarction, or venous thrombosis. Risk of recurrence.
  • Severe renal impairment (e.g. eGFR <30 mL/min/1.73 m2) · Dose reduction required; risk of accumulation and toxicity. Practice varies; some formularies contraindicate. Seek specialist advice.
  • Known hypersensitivity to tranexamic acid · Discontinue immediately if allergic reaction occurs.
  • Disseminated intravascular coagulation (DIC) · Contraindicated unless there is predominant fibrinolysis. Specialist use only; risk of worsening thrombosis.
  • Dose adjust in renal impairment: reduce dose or increase interval. Monitor renal function and consider specialist advice.
  • Avoid use in upper urinary tract haematuria unless benefit outweighs risk of clot obstruction.
  • Administer IV slowly to reduce risk of hypotension and injection site reactions.
  • Use with caution in patients with a history of seizures or risk factors for seizures; avoid high doses in cardiac surgery.
  • Avoid concomitant use with procoagulant agents (e.g. factor IX complex concentrates, anti-inhibitor coagulant concentrates) due to increased risk of thrombosis.
  • Assess thrombotic risk before use, especially in patients on hormonal contraception or hormone replacement therapy; monitor for signs of thrombosis.
Adverse effects
  • Nausea
  • Diarrhoea
  • Vomiting
  • Hypotension (especially with rapid IV injection)serious
  • Thromboembolic events (e.g. deep vein thrombosis, pulmonary embolism, stroke, myocardial infarction)serious
  • Seizuresserious
  • Visual disturbance (e.g. blurred vision, colour vision changes)serious
Renal & hepatic adjustment
  • eGFR 50+: No dose adjustment required for eGFR 50 mL/min/1.73 m2 or above. Use standard dosing for the indication.
  • eGFR 30–49: Reduce dose. A common teaching example is 15 mg/kg once daily (IV or PO) instead of two or three times daily. Follow local formulary.
  • eGFR 10–29: Reduce dose further. A common teaching example is 10 mg/kg once daily, or 15 mg/kg every 48 hours. Monitor closely for seizures.
  • eGFR 0–9: Specialist use only. A common teaching example is 10 mg/kg after each dialysis session, or 15 mg/kg every 48 hours. Risk of accumulation and seizures is increased.
Monitoring, pregnancy & toxicity
  • Haemoglobin and haematocrit · Baseline and as clinically indicated to assess bleeding control.
  • Renal function (eGFR, serum creatinine) · Baseline and periodically in renal impairment or during prolonged therapy.
  • Seizures or myoclonus · During and after high-dose or IV therapy, especially in renal impairment.
  • Thromboembolic events (DVT, PE, MI, stroke) · Throughout therapy and after discharge; advise patient to report symptoms.
  • Visual acuity and colour vision · For long-term oral therapy or if visual symptoms occur.
  • Bleeding from surgical site, drains, or other sites · Continuous during acute use.
  • Pregnancy: Tranexamic acid can be used in pregnancy when clinically indicated, such as for postpartum haemorrhage or major trauma, where evidence supports benefit. It crosses the placenta, but available data do not show an increased risk of congenital malformations. Use the lowest effective dose for the shortest duration. Practice may vary by region and formulary; follow local guidance.
  • Toxicity: Seizures, myoclonus, or altered consciousness, especially with high doses or renal impairment. · Stop the drug. Provide supportive care; treat seizures with benzodiazepines or other standard anticonvulsants. Consider ICU admission and specialist advice.
  • Toxicity: Thromboembolic events such as deep vein thrombosis, pulmonary embolism, myocardial infarction, or stroke. · Stop the drug. Assess and treat thrombosis as clinically indicated, with anticoagulation if appropriate. Seek specialist haematology or vascular advice.
  • Toxicity: Hypotension, bradycardia, or arrhythmias. · Stop the drug. Provide supportive care with IV fluids and vasopressors if needed. Monitor continuously.
  • Toxicity: Visual disturbances or retinal changes. · Stop the drug. Refer for ophthalmological assessment. Avoid further exposure until reviewed.
Clinical notes
Tranexamic acid is used to reduce bleeding in hyperfibrinolytic states. Common indications include major trauma with suspected bleeding, postpartum haemorrhage, cardiac and orthopaedic surgery, dental procedures in patients with bleeding disorders, heavy menstrual bleeding and epistaxis. Benefit in trauma and postpartum haemorrhage is time-dependent: early administration, generally within 3 hours of injury or birth, is recommended, whereas late administration may be less effective or harmful. Doses are teaching examples only. A typical adult intravenous regimen for trauma is 1 g over 10 minutes followed by 1 g over 8 hours; oral regimens for heavy menstrual bleeding often use 1 g three times daily during bleeding. Contraindications include active thromboembolic disease, a history of venous or arterial thrombosis, and disseminated intravascular coagulation, except in the context of major haemorrhage where the balance of risk may favour use under specialist guidance. Caution is needed in severe renal impairment and in patients with haematuria from the upper urinary tract because of the risk of clot obstruction. High doses, particularly in cardiac surgery, have been associated with seizures. Monitor renal function and clinical response; follow local protocols for trauma, obstetric and surgical use.

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BNF; local formulary; product SPC; local protocols for trauma, obstetric haemorrhage and surgery.