Usage
Epsilon Aminocaproic Acid (EACA) is prescribed for the management of bleeding conditions caused by an increase in fibrinolytic activity (the breakdown of blood clots). It is classified as an antifibrinolytic. EACA works by inhibiting the breakdown of fibrin, a protein essential for blood clot formation, thereby promoting hemostasis (stopping bleeding).
Alternate Names
- Generic Name: Aminocaproic acid
- Brand Name: Amicar
How It Works
Pharmacodynamics: EACA primarily inhibits fibrinolysis by blocking the activation of plasminogen, the precursor to plasmin (the enzyme responsible for breaking down fibrin). It achieves this by competing with plasminogen for binding sites on fibrin. EACA also has a weaker direct antiplasmin effect. It does not affect clotting factor levels.
Pharmacokinetics:
- Absorption: Well-absorbed orally. Peak plasma concentrations are reached in about 1-2 hours after oral administration. Bioavailability is close to 100%.
- Distribution: Distributes widely throughout the body, including into red blood cells and other tissues. The apparent volume of distribution is approximately 20-30 L.
- Metabolism: A small portion is metabolized to adipic acid.
- Elimination: Primarily eliminated unchanged by the kidneys, with a half-life of about 2 hours. Renal clearance is close to creatinine clearance.
Dosage
Standard Dosage
Adults:
- IV: Initial dose of 4-5 g infused over 1 hour, followed by a continuous infusion of 1 g/hour. The maximum daily dose is 30g.
- Oral: Initial dose of 5 g followed by 1 g every hour (tablets) or 1.25 g every hour (oral solution). The maximum daily dose is 30g.
Children:
- IV: 100 mg/kg or 3 g/m² infused over 1 hour, followed by continuous infusion at 33.3 mg/kg/hour or 1 g/m²/hour. Maximum daily dose is 18 g/m² or 600mg/kg. Safety and efficacy in children have not been fully established.
Special Cases:
- Elderly Patients: Dose adjustment is generally not necessary but caution is advised due to potential age-related decline in renal function.
- Patients with Renal Impairment: Reduce the dose based on the degree of impairment. Close monitoring is essential.
- Patients with Hepatic Dysfunction: No specific dose adjustment is typically required.
- Patients with Comorbid Conditions: Use with caution in patients with a history of thromboembolic events.
Clinical Use Cases
Dosage recommendations are similar across various clinical settings and align with the standard dosage guidelines. The duration of treatment depends on the specific situation and is continued until bleeding is controlled. Clinical use cases include:
- Intubation: Standard dosage.
- Surgical Procedures: Standard dosage.
- Mechanical Ventilation: Standard dosage.
- Intensive Care Unit (ICU) Use: Standard dosage.
- Emergency Situations: Standard dosage.
Dosage Adjustments
Dose adjustments are primarily necessary for patients with renal impairment. The dose should be reduced based on creatinine clearance.
Side Effects
Common Side Effects:
- Nausea, vomiting, diarrhea
- Headache, dizziness
- Nasal congestion, watery eyes
- Skin rash, itching
- Hypotension (especially with rapid IV infusion)
- Muscle weakness
Rare but Serious Side Effects:
- Myopathy, rhabdomyolysis
- Thromboembolic events (e.g., deep vein thrombosis, pulmonary embolism)
- Seizures
- Acute renal failure
- Bradycardia, arrhythmias
Long-Term Effects:
Chronic complications from prolonged use are rare, but myopathy and muscle weakness are potential concerns.
Adverse Drug Reactions (ADR):
Severe hypotension, bradycardia, arrhythmias, and seizures require immediate medical attention.
Contraindications
- Active intravascular clotting (DIC) unless used concurrently with heparin
- Hypersensitivity to aminocaproic acid
Drug Interactions
- Factor IX complex, anti-inhibitor coagulant complex: Increased risk of thrombosis. Avoid concomitant use.
- Estrogens, oral contraceptives: May increase the risk of thromboembolic events.
- Thrombolytic agents (e.g., alteplase, streptokinase): Antagonistic effects. Avoid concomitant use.
Pregnancy and Breastfeeding
- Pregnancy: Not recommended unless clearly needed. Animal studies have shown adverse effects on reproduction. Pregnancy Safety Category C.
- Breastfeeding: Excretion in human milk is unknown. Use with caution.
Drug Profile Summary
- Mechanism of Action: Inhibits fibrinolysis by blocking plasminogen activation and having a weaker direct antiplasmin effect.
- Side Effects: Nausea, vomiting, headache, dizziness, hypotension, rash, myopathy, thromboembolic events.
- Contraindications: Active intravascular clotting, hypersensitivity.
- Drug Interactions: Factor IX complex, anti-inhibitor coagulant complex, estrogens, thrombolytics.
- Pregnancy & Breastfeeding: Not recommended unless clearly needed. Caution advised.
- Dosage: See detailed dosage guidelines above.
- Monitoring Parameters: Creatine phosphokinase (CPK) levels (for long-term use), signs of bleeding, blood pressure, heart rate.
Popular Combinations
- Desmopressin (DDAVP): May be used in combination with EACA for certain bleeding disorders.
Precautions
- General Precautions: Assess renal function before and during treatment, especially with prolonged use. Monitor for signs of thromboembolic events.
- Specific Populations: See “Special Cases” under Dosage.
- Lifestyle Considerations: No specific lifestyle restrictions are usually necessary.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Epsilon Aminocaproic Acid?
A: Refer to the detailed dosage section above.
Q2: How does EACA differ from Tranexamic Acid?
A: Both are antifibrinolytics, but Tranexamic Acid is considered more potent.
Q3: What are the signs of EACA overdose?
A: Acute renal failure, hypotension, seizures, bradycardia, arrhythmias.
Q4: Can EACA be used in patients with DIC?
A: Generally contraindicated unless administered concurrently with heparin.
Q5: What laboratory tests should be monitored during EACA therapy?
A: CPK (for long-term use), coagulation tests, renal function tests.
Q6: Can EACA be administered intramuscularly?
A: No, it should be administered intravenously or orally.
Q7: What are the key considerations for using EACA in pregnant or breastfeeding women?
A: Not recommended unless clearly needed. Potential fetal risks exist. Excretion in breast milk is unknown.
Q8: How should EACA be administered intravenously?
A: The initial dose should be diluted and infused slowly over 1 hour. Rapid IV push is not recommended as it can cause hypotension.
Q9: What are the common side effects of oral EACA?
A: Nausea, vomiting, diarrhea, headache, dizziness.
