Usage
- Medical Conditions: This combination medication is primarily prescribed to prevent and treat excessive bleeding. Common uses include managing heavy menstrual bleeding (menorrhagia), controlling bleeding during and after surgical procedures (especially dental, orthopedic, and gynecological), and treating bleeding in trauma or postpartum situations. It can also be used for specific conditions like nosebleeds or gastrointestinal bleeding.
- Pharmacological Classification: Hemostatic agent, antifibrinolytic agent.
- Mechanism of Action: Ethamsylate works by enhancing platelet adhesion and aggregation, promoting clot formation. Tranexamic acid is an antifibrinolytic that inhibits the breakdown of blood clots by blocking the activity of plasmin, a protein involved in dissolving fibrin. This combined action effectively reduces bleeding.
Alternate Names
- No widely recognized alternate names exist for the combination itself. Individual components are sometimes referred to as:
- Ethamsylate: Cyclonamine, Dicynene
- Tranexamic acid: Cyklokapron, Lysteda
- Brand Names: Several brand names exist depending on the manufacturer and region (e.g., Cosklot Plus, Temsy-E, Menostat, Nexic-E, Travic ET, Osemic ET).
How It Works
- Pharmacodynamics: Ethamsylate increases platelet adhesiveness and capillary resistance, promoting primary hemostasis. Tranexamic acid inhibits plasminogen activation, preventing fibrinolysis and stabilizing clot formation.
- Pharmacokinetics:
- Absorption: Both drugs are readily absorbed orally. Tranexamic acid has good bioavailability, while ethamsylate’s bioavailability is somewhat lower.
- Metabolism: Both drugs undergo minimal hepatic metabolism.
- Elimination: Primarily renal excretion for both drugs. Dose adjustment is necessary in patients with renal impairment.
Dosage
Standard Dosage
Adults:
- Oral: The typical adult dose is 500-1000 mg of tranexamic acid combined with 250-500 mg of ethamsylate, two to three times daily. The dose may be adjusted depending on the severity of bleeding. The maximum daily dose should not exceed 4g of tranexamic acid.
- Intravenous: Tranexamic acid can be administered IV, usually as a 1 g bolus followed by a continuous infusion. The dose is determined by the specific clinical context (e.g., surgery, trauma). Ethamsylate can also be administered intravenously at a dose of 12.5 mg/kg every 6 hours.
Children:
- Dosage is weight-based, typically 25 mg/kg for both components, given two to three times daily. Pediatric safety considerations should be taken into account, and the dose adjusted based on the child’s age and clinical condition.
Special Cases:
- Elderly Patients and Patients with Renal/Hepatic Impairment: Dose adjustment is necessary based on renal function. Close monitoring is essential.
- Patients with Comorbid Conditions: Careful evaluation is needed for patients with a history of thromboembolic events, seizures, or other relevant medical conditions.
Clinical Use Cases
- Surgical Procedures: Dosage varies depending on the procedure and risk of bleeding. Preoperative, intraoperative, or postoperative administration may be used.
- Postpartum Hemorrhage: Intravenous administration of tranexamic acid and ethamsylate is often preferred to control bleeding rapidly.
- Emergency Situations: Intravenous administration for rapid control of bleeding in trauma or other emergencies.
Dosage Adjustments:
- Dose modification based on renal/hepatic function, age, and coexisting medical conditions is crucial for optimizing efficacy and minimizing adverse events.
Side Effects
Common Side Effects
- Nausea, vomiting, diarrhea, stomach pain, headache, dizziness, rash, muscle aches, joint pain.
Rare but Serious Side Effects
- Thromboembolic events (deep vein thrombosis, pulmonary embolism), allergic reactions (angioedema, anaphylaxis), seizures, visual disturbances.
Long-Term Effects
- Chronic use can potentially increase the risk of thrombotic events.
Contraindications
- Active thromboembolic disease, history of thrombosis or thromboembolism, severe renal impairment, hypersensitivity to either component, subarachnoid hemorrhage, active intravascular clotting.
Drug Interactions
- Hormonal contraceptives, estrogens, retinoids, prothrombotic agents, anticoagulants (warfarin, heparin), some antipsychotics (chlorpromazine). Concomitant use of alcohol may increase the risk of side effects.
Pregnancy and Breastfeeding
- Pregnancy: Tranexamic acid and ethamsylate should be used with caution during pregnancy, only if the potential benefit outweighs the risk to the fetus. Limited data are available regarding fetal risks.
- Breastfeeding: Both drugs are excreted in breast milk in small amounts. Use cautiously while breastfeeding and consider potential neonatal side effects.
Drug Profile Summary
- Mechanism of Action: Ethamsylate enhances platelet function and capillary resistance. Tranexamic acid inhibits fibrinolysis.
- Side Effects: Nausea, vomiting, diarrhea, headache, dizziness, rash, thromboembolic events (rare).
- Contraindications: Active thromboembolic disease, severe renal impairment, hypersensitivity.
- Drug Interactions: Hormonal contraceptives, estrogens, anticoagulants.
- Pregnancy & Breastfeeding: Use with caution, potential risks.
- Dosage: Varies depending on indication and patient factors.
- Monitoring Parameters: Bleeding status, renal function, signs of thromboembolic events.
Popular Combinations
- The combination of ethamsylate and tranexamic acid is itself a popular combination due to their synergistic hemostatic effects.
Precautions
- Assess for allergies, renal/hepatic impairment, history of thromboembolic events, bleeding disorders. Monitor for signs of allergic reactions or thromboembolism. Avoid driving or operating machinery if experiencing dizziness or visual disturbances.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Ethamsylate + Tranexamic Acid?
A: Dosage varies based on indication and patient factors. The typical adult oral dose is 500-1000 mg tranexamic acid and 250-500 mg ethamsylate, 2-3 times daily. Intravenous and pediatric dosing differ.
Q2: What are the primary uses of this combination?
A: Managing heavy menstrual bleeding, controlling surgical bleeding, treating postpartum hemorrhage, and managing bleeding in certain other conditions (nosebleeds, gastrointestinal bleeding).
Q3: What are the common side effects?
A: Nausea, vomiting, diarrhea, stomach pain, headache, dizziness, and rash.
Q4: Are there any serious side effects?
A: Although rare, serious side effects can include blood clots (thromboembolism), severe allergic reactions, and seizures.
Q5: Who should not take this medication?
A: Individuals with active thromboembolic disease, a history of thrombosis, severe renal impairment, and hypersensitivity to the components should avoid this medication.
Q6: Does it interact with other medications?
A: Yes, clinically significant interactions exist with hormonal contraceptives, estrogens, certain retinoids, some antipsychotics, and anticoagulants.
Q7: Can it be used during pregnancy and breastfeeding?
A: It should be used cautiously in pregnancy and breastfeeding, only if the potential benefits outweigh the risks. Consult a specialist for guidance.
Q8: How does renal impairment affect dosage?
A: Dose reduction is necessary for patients with renal impairment due to altered drug elimination.
Q9: What should I monitor in patients taking this medication?
A: Closely monitor bleeding, renal function, and any signs or symptoms suggesting thromboembolic complications or allergic reactions.
Q10: Are there any specific lifestyle considerations while on this medication?
A: Patients should avoid alcohol as it might exacerbate side effects. Caution should be exercised when driving or operating machinery if dizziness or visual disturbances occur.
