Amicar 1000mg Tablets
It is used to treat or prevent bleeding.
Drug Class
Antifibrinolytic Agent
Pharmacologic Class
Lysine Analog
Pregnancy Category
Category C
FDA Approved
Aug 1964
DEA Schedule
Not Controlled
Overview
What is this medicine?
Amicar is a medicine that helps your blood clot. It works by stopping the body from breaking down blood clots too quickly. This can help reduce or stop bleeding, especially after surgery or in certain bleeding disorders.
How to Use This Medicine
To use this medication correctly, follow your doctor's instructions and read all accompanying information carefully. You can take this medication with or without food.
To maintain the medication's effectiveness, store it at room temperature and avoid freezing.
If you miss a dose, contact your doctor for guidance on the best course of action to take.
To maintain the medication's effectiveness, store it at room temperature and avoid freezing.
If you miss a dose, contact your doctor for guidance on the best course of action to take.
Lifestyle & Tips
- Take exactly as prescribed by your doctor. Do not stop taking it without consulting your doctor.
- Report any unusual bleeding or bruising, or signs of new blood clots (like pain/swelling in legs, chest pain, shortness of breath) immediately.
- Report any muscle pain, weakness, or dark urine, as these could be signs of a serious muscle problem.
- Avoid activities that could lead to injury or bleeding while on this medication, especially if you have an underlying bleeding disorder.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
Initial 5 g orally or IV, then 1 to 1.25 g/hour orally or IV for 8 hours or until bleeding is controlled.
Dose Range:
1 - 30 mg
Condition-Specific Dosing:
Acute Bleeding:
Initial 5 g (oral or IV), followed by 1 to 1.25 g/hour (oral or IV) for 8 hours or until bleeding is controlled. Maximum 30 g in 24 hours.
Prophylaxis for Dental Extractions in Hemophiliacs:
2.5 g orally every 6 hours for 5-7 days, starting 1 day prior to surgery.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Limited data; often 100 mg/kg or 3 g/m2 orally or IV initially, then 33.3 mg/kg/hour or 1 g/m2/hour. Max 18 g/m2/24 hours.
Adolescent:
Same as adult dosing, or weight-based if appropriate for smaller adolescents.
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment, but monitor for accumulation.
Moderate:
Reduce dose by 50% or extend dosing interval. Monitor plasma levels if possible.
Severe:
Reduce dose significantly (e.g., 75% reduction or extend interval to 12-24 hours). Avoid if possible.
Dialysis:
Aminocaproic acid is dialyzable. Administer dose after dialysis. Specific dosing recommendations vary, often 25% of normal dose or based on plasma levels.
Hepatic Impairment:
Mild:
No adjustment
Moderate:
No adjustment
Severe:
No specific adjustment, but use with caution due to potential for impaired elimination in severe cases.
Pharmacology
Mechanism of Action
Aminocaproic acid is a synthetic amino acid that acts as an antifibrinolytic agent. It competitively inhibits the activation of plasminogen to plasmin, a proteolytic enzyme responsible for the breakdown of fibrin clots (fibrinolysis). It also, to a lesser extent, directly inhibits plasmin activity. By preventing fibrinolysis, it helps stabilize clots and reduce bleeding.
Pharmacokinetics
Absorption:
Bioavailability:
High (nearly complete)
Tmax:
Approximately 1.2 hours (oral)
FoodEffect:
Food does not significantly affect absorption.
Distribution:
Vd:
Approximately 0.2 L/kg
ProteinBinding:
Not significantly protein bound
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 1-2 hours
Clearance:
Primarily renal clearance
ExcretionRoute:
Renal (glomerular filtration)
Unchanged:
Approximately 80% unchanged
Pharmacodynamics
OnsetOfAction:
Rapid (within minutes for IV, within 1-2 hours for oral)
PeakEffect:
Within 2-3 hours (oral)
DurationOfAction:
Dose-dependent, typically requires continuous infusion or frequent dosing to maintain effect.
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor immediately or seek emergency medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Abnormal heartbeat or slow heartbeat
Unexplained bruising or bleeding
Swelling
Seizures
Severe dizziness or fainting
Hallucinations (seeing or hearing things that are not there)
Confusion
Weakness on one side of the body, trouble speaking or thinking, balance changes, drooping on one side of the face, or blurred vision
Fever, chills, or sore throat
Changes in vision
Ringing in the ears
Signs of a blood clot, such as:
+ Chest pain or pressure
+ Coughing up blood
+ Shortness of breath
+ Swelling, warmth, numbness, color changes, or pain in a leg or arm
+ Trouble speaking or swallowing
Additionally, this medication can cause severe muscle problems, which may lead to kidney issues. Inform your doctor if you experience:
Muscle pain or weakness, especially if accompanied by fatigue, weakness, or fever
Difficulty urinating or changes in urine output
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or persist, contact your doctor:
Headache
Upset stomach or vomiting
Stomach pain or diarrhea
Dizziness, fatigue, or weakness
Nasal congestion
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor immediately or seek emergency medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Abnormal heartbeat or slow heartbeat
Unexplained bruising or bleeding
Swelling
Seizures
Severe dizziness or fainting
Hallucinations (seeing or hearing things that are not there)
Confusion
Weakness on one side of the body, trouble speaking or thinking, balance changes, drooping on one side of the face, or blurred vision
Fever, chills, or sore throat
Changes in vision
Ringing in the ears
Signs of a blood clot, such as:
+ Chest pain or pressure
+ Coughing up blood
+ Shortness of breath
+ Swelling, warmth, numbness, color changes, or pain in a leg or arm
+ Trouble speaking or swallowing
Additionally, this medication can cause severe muscle problems, which may lead to kidney issues. Inform your doctor if you experience:
Muscle pain or weakness, especially if accompanied by fatigue, weakness, or fever
Difficulty urinating or changes in urine output
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or persist, contact your doctor:
Headache
Upset stomach or vomiting
Stomach pain or diarrhea
Dizziness, fatigue, or weakness
Nasal congestion
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe muscle pain or weakness
- Dark or reddish-brown urine
- Swelling, pain, or tenderness in a leg (signs of DVT)
- Sudden shortness of breath or chest pain (signs of PE)
- Sudden numbness or weakness, especially on one side of the body
- Severe headache, confusion, or problems with vision or speech
- Unusual bleeding or bruising that is worse than expected
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have a history of blood clots.
If you are taking any medications that may increase the risk of blood clots, including:
+ Factor IX complex
+ Anti-inhibitor coagulant complex
+ Hormone-based birth control methods
+ Other medications that may have this effect (consult your doctor or pharmacist if you are unsure)
Please note that this is not an exhaustive list of all potential interactions. To ensure your safety, it is crucial to:
Inform your doctor and pharmacist about all medications you are taking, including:
+ Prescription and over-the-counter (OTC) medications
+ Natural products
+ Vitamins
Share information about your health problems.
Verify that it is safe to take this medication with all your other medications and health conditions.
* Do not start, stop, or change the dose of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have a history of blood clots.
If you are taking any medications that may increase the risk of blood clots, including:
+ Factor IX complex
+ Anti-inhibitor coagulant complex
+ Hormone-based birth control methods
+ Other medications that may have this effect (consult your doctor or pharmacist if you are unsure)
Please note that this is not an exhaustive list of all potential interactions. To ensure your safety, it is crucial to:
Inform your doctor and pharmacist about all medications you are taking, including:
+ Prescription and over-the-counter (OTC) medications
+ Natural products
+ Vitamins
Share information about your health problems.
Verify that it is safe to take this medication with all your other medications and health conditions.
* Do not start, stop, or change the dose of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. As directed by your doctor, regular blood tests will be necessary to monitor your condition, and you should discuss any concerns or questions with your doctor. Additionally, this medication may interfere with certain laboratory tests, so it is crucial to notify all healthcare providers and laboratory personnel that you are taking this drug. If you are pregnant, planning to become pregnant, or are breastfeeding, you must consult with your doctor to weigh the benefits and risks of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- Nausea
- Diarrhea
- Dizziness
- Hypotension (low blood pressure)
- Bradycardia (slow heart rate)
- Acute renal failure
- Thrombosis (blood clot formation)
What to Do:
Seek immediate medical attention. Call 911 or your local emergency number. For poison control, call 1-800-222-1222. Treatment is supportive and symptomatic. Hemodialysis may be effective in removing the drug.
Drug Interactions
Major Interactions
- Factor IX Complex Concentrates (e.g., Konyne 80, Profilnine SD)
- Anti-inhibitor Coagulant Complex (e.g., FEIBA NF)
- Estrogens (e.g., oral contraceptives, hormone replacement therapy)
- Thrombolytic agents (e.g., alteplase, streptokinase, urokinase)
Moderate Interactions
- Chlorpromazine (may increase risk of myopathy)
- Corticosteroids (may increase risk of myopathy)
Monitoring
Baseline Monitoring
Renal Function (BUN, Creatinine)
Rationale: Aminocaproic acid is primarily renally excreted; impaired renal function requires dose adjustment.
Timing: Prior to initiation of therapy.
Complete Blood Count (CBC) with Platelets
Rationale: To assess baseline hematologic status and identify underlying causes of bleeding.
Timing: Prior to initiation of therapy.
Coagulation Parameters (PT, aPTT, Fibrinogen)
Rationale: To assess baseline coagulation status and guide therapy.
Timing: Prior to initiation of therapy.
Routine Monitoring
Renal Function (BUN, Creatinine)
Frequency: Daily or every 2-3 days, especially in patients with impaired renal function or prolonged therapy.
Target: Within normal limits or stable for patient's baseline.
Action Threshold: Significant increase in BUN/creatinine; consider dose adjustment or discontinuation.
Coagulation Parameters (PT, aPTT, Fibrinogen)
Frequency: Daily or as clinically indicated, especially during acute bleeding episodes.
Target: Dependent on clinical goal (e.g., normalization of bleeding, prevention of re-bleeding).
Action Threshold: Persistent bleeding despite therapy, or signs of hypercoagulability.
Signs and Symptoms of Thrombosis (e.g., DVT, PE, arterial thrombosis)
Frequency: Continuously
Target: Absence of thrombotic events.
Action Threshold: New onset of pain, swelling, redness in limbs; shortness of breath, chest pain; neurological deficits. Discontinue drug and initiate appropriate treatment.
Signs and Symptoms of Myopathy/Rhabdomyolysis (e.g., muscle pain, weakness, dark urine)
Frequency: Daily
Target: Absence of muscle symptoms.
Action Threshold: New onset of muscle pain, weakness, or dark urine. Discontinue drug and check CK levels.
Symptom Monitoring
- Bleeding (cessation or reduction)
- Signs of thrombosis (e.g., leg pain/swelling, chest pain, shortness of breath, sudden vision changes, slurred speech)
- Muscle pain or weakness
- Dark or reddish-brown urine (rhabdomyolysis)
- Nausea, vomiting, diarrhea
- Dizziness, headache
Special Patient Groups
Pregnancy
Use only if the potential benefit justifies the potential risk to the fetus. Animal studies have shown some evidence of teratogenicity at high doses.
Trimester-Specific Risks:
First Trimester:
Potential for fetal harm, especially during organogenesis. Use with caution.
Second Trimester:
Risk likely similar to first trimester, but less data. Monitor for fetal well-being.
Third Trimester:
Risk of fetal harm, potential for effects on fetal coagulation. Use with caution.
Lactation
Aminocaproic acid is excreted in breast milk. Caution should be exercised when administered to a nursing mother. Consider potential risks to the infant versus benefits to the mother.
Infant Risk:
Risk level L3 (Moderate risk). Potential for adverse effects on infant coagulation or other systemic effects. Monitor infant for signs of bleeding or clotting.
Pediatric Use
Safety and efficacy have not been fully established in pediatric patients. Use with caution and generally only when the potential benefits outweigh the risks. Dosing is often weight or body surface area-based, and close monitoring is required.
Geriatric Use
Use with caution in elderly patients, as they are more likely to have decreased renal function. Dose adjustment may be necessary based on renal creatinine clearance. Monitor closely for adverse effects, particularly thrombotic events.
Clinical Information
Clinical Pearls
- Aminocaproic acid should be administered promptly after the onset of bleeding or prior to procedures where excessive bleeding is anticipated due to fibrinolysis.
- Rapid IV infusion can cause hypotension, bradycardia, and arrhythmias; administer IV doses slowly (e.g., over 1 hour for initial dose).
- Monitor for signs of thrombosis (e.g., DVT, PE, arterial thrombosis) throughout therapy, especially in patients with pre-existing thrombotic risk factors.
- Patients should be advised to report any muscle pain, weakness, or dark urine immediately, as these may indicate myopathy or rhabdomyolysis.
- Not effective for bleeding due to thrombocytopenia or other coagulation factor deficiencies unless accompanied by hyperfibrinolysis.
- Consider tranexamic acid as an alternative, which may have a more favorable pharmacokinetic profile and potentially fewer side effects in some cases.
Alternative Therapies
- Tranexamic acid (another antifibrinolytic agent)
Cost & Coverage
Average Cost:
Varies widely, typically $50-$200 per 30 tablets
Generic Available:
Yes
Insurance Coverage:
Tier 1 or 2 (Generic), Tier 3 (Brand)
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.