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# Tranexamic acid
## Overview
Tranexamic acid is a synthetic derivative of the amino acid lysine. It is an antifibrinolytic agent that competitively inhibits the activation of plasminogen to plasmin, a key enzyme responsible for fibrinolysis. This action helps to stabilize blood clots and reduce bleeding.
## Primary Indications
* Hemorrhagic stroke (intracerebral hemorrhage)
* Epistaxis (nosebleeds)
* Menorrhagia (heavy menstrual bleeding)
* Surgical bleeding (e.g., post-tonsillectomy, cardiac surgery, orthopedic surgery)
* Traumatic bleeding
## Adult Dosing
* **Hemorrhagic stroke:**
* Loading dose: 1 g IV every 8 hours.
* Maintenance dose: 1 g IV every 8 hours for up to 7 days.
* *Note:* Dosing may vary based on local protocols and specific clinical scenarios.
* **Bleeding prevention/management (general surgical/trauma):**
* Loading dose: 1 g to 2 g IV.
* Maintenance dose: 1 g IV every 8 hours.
* *Note:* Specific dosing and duration depend heavily on the surgical procedure or type of bleeding and should follow institutional guidelines or surgeon/hematologist recommendations.
* **Menorrhagia:**
* Oral: 1 g to 1.5 g PO three times daily for up to 4 days during menstruation. Maximum daily dose is 4 g.
* **Epistaxis (recurrent severe):**
* Oral: 1 g to 2 g PO three times daily.
* Topical: Can be applied locally as a soaked gauze or nasal spray.
## Pediatric Dosing
Pediatric dosing is not well-established and should be guided by specialist consultation (e.g., pediatric hematology, critical care) and institutional protocols. Extrapolation from adult data is generally not recommended.
## Dose Adjustments
* **Renal impairment:** Dose adjustment is necessary.
* Creatinine clearance (CrCl) 50-80 mL/min: 50% of the usual dose every 12 hours.
* CrCl 10-50 mL/min: 25% of the usual dose every 12 hours or 50% of the usual dose every 24 hours.
* CrCl <10 mL/min: 12.5% of the usual dose every 12 hours or 25% of the usual dose every 24 hours.
* *Note:* Calculation of CrCl is essential. Dose adjustments should be confirmed with institutional guidelines.
## Contraindications
* Active intravascular clotting or thromboembolic disease (e.g., deep vein thrombosis, pulmonary embolism, arterial thrombosis).
* Acquired defects in color vision.
* Hypersensitivity to tranexamic acid.
* Subarachnoid hemorrhage (controversial, potential for cerebral edema and ischemia).
## Adverse Effects
* **Common:** Nausea, vomiting, diarrhea, abdominal pain, dizziness.
* **Serious:**
* Thromboembolic events (e.g., deep vein thrombosis, pulmonary embolism, myocardial infarction, stroke). Risk is increased in patients with risk factors for thrombosis.
* Hypersensitivity reactions.
* Visual disturbances (especially with prolonged use or high doses).
* Seizures (rare, more associated with rapid IV infusion).
* Anaphylaxis.
## Key Drug Interactions
* **Hormonal contraceptives (oral, transdermal, vaginal, injectable):** Increased risk of thromboembolic events. Concurrent use should be carefully considered.
* **Factoring VIII concentrates (e.g., anti-inhibitor coagulant complex, activated prothrombin complex concentrate):** Increased risk of thrombosis.
* **Retinoic acid (ATRA):** Case reports suggest increased risk of thrombosis.
* **Antifibrinolytics (e.g., aminocaproic acid, epsilon-aminocaproic acid):** Concurrent use is generally not recommended due to additive thrombotic risk.
## Monitoring
* **Clinical:** Assess for signs and symptoms of bleeding and thrombosis. Monitor urine output and signs of renal dysfunction.
* **Laboratory:** Generally no routine laboratory monitoring is required unless investigating potential causes of bleeding or thrombosis. Coagulation parameters are not typically altered by therapeutic doses of tranexamic acid.
* **Ophthalmologic:** Periodic ophthalmologic examinations may be considered for patients on long-term therapy, particularly at higher doses, to screen for visual disturbances.
## Clinical Pearls
* Tranexamic acid is a lysine analogue that competitively inhibits plasminogen activation.
* It is crucial to rule out active thromboembolic disease before initiating tranexamic acid.
* Rapid IV infusion (e.g., >100 mg/min) has been associated with a risk of hypotension and seizures; dilute and infuse slowly.
* Oral administration is effective for heavy menstrual bleeding and can be used for other indications where IV access is not required.
* Topical application can be effective for localized bleeding, such as epistaxis.
* Caution is advised in patients with a history of seizures.
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*Disclaimer: This information is intended for healthcare professionals and is not a substitute for professional medical advice. Always consult the most current prescribing information and relevant clinical guidelines before making any treatment decisions. Dosing and indications may vary based on individual patient factors and local protocols.*
