Amicar 500mg 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?
Aminocaproic acid is a medicine used to help stop or prevent excessive bleeding. It works by helping your body form and maintain blood clots, which are essential to stop bleeding. It's often used in situations where the body breaks down blood clots too quickly.
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
- Avoid activities that increase the risk of bleeding or injury while on this medication.
- Report any unusual bleeding or bruising immediately.
- Stay well-hydrated, especially if experiencing gastrointestinal side effects.
- Avoid alcohol if it exacerbates dizziness or other side effects.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
Initial 5 g orally, followed by 1 to 1.25 g every hour for 8 hours or until bleeding is controlled. Total daily dose should not exceed 30 g.
Dose Range:
1 - 30 mg
Condition-Specific Dosing:
Acute Bleeding:
Initial 5 g orally, then 1 to 1.25 g every hour for 8 hours or until bleeding is controlled. Max 30 g/24 hours.
Prophylaxis of Rebleeding:
Individualized based on clinical need and coagulation parameters.
Pediatric Dosing
Neonatal:
Not established (limited data, use with extreme caution and individualized dosing if necessary).
Infant:
Not established (limited data, use with extreme caution and individualized dosing if necessary).
Child:
Initial 100 mg/kg or 3 g/m² orally, then 33.3 mg/kg/hr or 1 g/m²/hr for 8 hours or until bleeding is controlled. Max 18 g/m²/24 hours or 30 g/24 hours, whichever is less.
Adolescent:
Same as adult dosing.
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment recommended, but monitor for accumulation.
Moderate:
Reduce dose by 50% or extend dosing interval. Monitor renal function and clinical response.
Severe:
Contraindicated in anuric patients. Significant dose reduction (e.g., 75% or more) and extended intervals are necessary. Monitor closely for accumulation and toxicity.
Dialysis:
Aminocaproic acid is dialyzable. Administer dose after dialysis session. Specific dosing recommendations vary, often requiring significant reduction and close monitoring.
Hepatic Impairment:
Mild:
No specific adjustment recommended.
Moderate:
No specific adjustment recommended, as hepatic metabolism is minimal.
Severe:
No specific adjustment recommended, as hepatic metabolism is minimal.
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, and to a lesser degree, directly inhibits plasmin activity. By binding to the lysine-binding sites on plasminogen and plasmin, it prevents their interaction with fibrin, thereby stabilizing the fibrin clot and preventing its premature degradation.
Pharmacokinetics
Absorption:
Bioavailability:
Nearly 100% (oral)
Tmax:
Approximately 1.2 hours (oral)
FoodEffect:
Food does not significantly affect absorption.
Distribution:
Vd:
Approximately 23 L (in adults)
ProteinBinding:
Not protein bound
CnssPenetration:
Limited (crosses blood-brain barrier to a small extent)
Elimination:
HalfLife:
Approximately 1 to 2 hours
Clearance:
Approximately 11.6 L/hr (renal clearance is primary)
ExcretionRoute:
Renal (primarily unchanged)
Unchanged:
Approximately 80% (within 12 hours)
Pharmacodynamics
OnsetOfAction:
Rapid (within minutes for IV, within 1-2 hours for oral)
PeakEffect:
Within 1-2 hours (oral)
DurationOfAction:
Approximately 3 hours (related to half-life and plasma concentration)
Safety & Warnings
Side Effects
Serious Side Effects: Seek Medical Attention Immediately
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 or seek medical help right away:
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
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
This medication can also cause severe muscle problems, which may lead to kidney problems. Inform your doctor if you experience:
Muscle pain or weakness, especially if you feel extremely tired or weak, or have a fever
Difficulty urinating or changes in urine output
Other Possible Side Effects
Like all medications, this drug can cause side effects. Many people may not experience any side effects or only minor ones. If you notice any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor or seek medical help:
Headache
Upset stomach or vomiting
Stomach pain or diarrhea
Dizziness, tiredness, or weakness
* Nasal congestion
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact 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 or seek medical help right away:
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
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
This medication can also cause severe muscle problems, which may lead to kidney problems. Inform your doctor if you experience:
Muscle pain or weakness, especially if you feel extremely tired or weak, or have a fever
Difficulty urinating or changes in urine output
Other Possible Side Effects
Like all medications, this drug can cause side effects. Many people may not experience any side effects or only minor ones. If you notice any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor or seek medical help:
Headache
Upset stomach or vomiting
Stomach pain or diarrhea
Dizziness, tiredness, or weakness
* Nasal congestion
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact 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:
- Signs of blood clots: sudden chest pain, shortness of breath, pain/swelling in a leg or arm, sudden severe headache, vision changes, slurred speech.
- Muscle pain, tenderness, or weakness, especially if accompanied by dark urine (signs of myopathy/rhabdomyolysis).
- Severe dizziness or fainting.
- Unusual or excessive bleeding (e.g., nosebleeds, gum bleeding, blood in urine or stool) that is not related to the condition being treated.
- Allergic reaction symptoms: rash, itching, swelling (especially of face/tongue/throat), severe dizziness, trouble breathing.
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 allergic reaction you experienced, including any symptoms that occurred.
If you have a history of blood clots.
If you are currently taking any medications that may increase the risk of blood clots, such as factor IX complex, anti-inhibitor coagulant complex, or hormone-based birth control. There are many medications that can increase this risk, so it is crucial to ask your doctor or pharmacist if you are unsure.
To ensure your safety, it is vital to provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter medications you are taking
Any natural products or vitamins you are using
Your medical history, including any health problems you have
This information will help your doctor determine whether it is safe for you to take this medication with your other medications and health conditions. Never 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 allergic reaction you experienced, including any symptoms that occurred.
If you have a history of blood clots.
If you are currently taking any medications that may increase the risk of blood clots, such as factor IX complex, anti-inhibitor coagulant complex, or hormone-based birth control. There are many medications that can increase this risk, so it is crucial to ask your doctor or pharmacist if you are unsure.
To ensure your safety, it is vital to provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter medications you are taking
Any natural products or vitamins you are using
Your medical history, including any health problems you have
This information will help your doctor determine whether it is safe for you to take this medication with your other medications and health conditions. Never 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. Regular blood tests will be necessary, as directed by your doctor, to monitor your condition. Be sure to discuss any concerns or questions with your doctor.
Additionally, this medication may interfere with certain laboratory tests, so it is crucial to notify all your 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.
Additionally, this medication may interfere with certain laboratory tests, so it is crucial to notify all your 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:
- Severe nausea, vomiting, diarrhea
- Dizziness, lightheadedness
- Hypotension (low blood pressure)
- Bradycardia (slow heart rate)
- Acute renal failure
- Myopathy/rhabdomyolysis (muscle pain, weakness, dark urine)
- Thrombosis (blood clot formation)
What to Do:
Seek immediate medical attention or call 911. For poison control, call 1-800-222-1222. Treatment is supportive and symptomatic, including gastric lavage, activated charcoal, and close monitoring of vital signs, renal function, and coagulation parameters. Hemodialysis may be considered as aminocaproic acid is dialyzable.
Drug Interactions
Contraindicated Interactions
- Factor IX Complex Concentrates (increased risk of thrombosis)
- Anti-inhibitor Coagulant Complex (increased risk of thrombosis)
Major Interactions
- Estrogens (increased risk of thrombosis, especially with concomitant use for prolonged periods)
- Oral Contraceptives (increased risk of thrombosis, especially with concomitant use for prolonged periods)
- Thrombolytic Agents (antagonistic effect, may reduce efficacy of thrombolytics)
Moderate Interactions
- Chlorpromazine (potential for increased risk of myopathy/rhabdomyolysis, though rare)
- Corticosteroids (potential for increased risk of myopathy/rhabdomyolysis, though rare)
Monitoring
Baseline Monitoring
Complete Blood Count (CBC)
Rationale: To assess baseline hemoglobin, hematocrit, and platelet count, which are relevant for bleeding disorders.
Timing: Prior to initiation of therapy.
Renal Function (BUN, Creatinine)
Rationale: Aminocaproic acid is primarily renally excreted; impaired renal function requires dose adjustment.
Timing: Prior to initiation of therapy.
Liver Function Tests (LFTs)
Rationale: To assess baseline hepatic function, although hepatic metabolism is minimal.
Timing: Prior to initiation of therapy.
Coagulation Parameters (PT, aPTT, Fibrinogen, D-dimer)
Rationale: To assess baseline coagulation status and identify underlying hyperfibrinolysis.
Timing: Prior to initiation of therapy.
Routine Monitoring
Renal Function (BUN, Creatinine)
Frequency: Periodically, especially in patients with pre-existing renal impairment or during prolonged therapy.
Target: Within normal limits or stable for patient's baseline.
Action Threshold: Significant increase in BUN/Creatinine may necessitate dose adjustment or discontinuation.
Coagulation Parameters (PT, aPTT, Fibrinogen)
Frequency: As clinically indicated, especially during acute bleeding episodes or prolonged therapy.
Target: Aimed at achieving hemostasis.
Action Threshold: Persistent bleeding or signs of thrombosis may require re-evaluation of therapy.
Creatine Kinase (CK)
Frequency: If muscle pain or weakness develops.
Target: Within normal limits.
Action Threshold: Significant elevation may indicate myopathy/rhabdomyolysis, requiring discontinuation.
Symptom Monitoring
- Signs of thrombosis (e.g., chest pain, shortness of breath, swelling/pain in extremities, sudden severe headache, vision changes)
- Muscle pain, weakness, or tenderness (signs of myopathy/rhabdomyolysis)
- Hypotension (especially with rapid IV infusion)
- Gastrointestinal upset (nausea, vomiting, diarrhea, abdominal cramps)
- Dizziness, lightheadedness
- Skin rash or allergic reactions
Special Patient Groups
Pregnancy
Aminocaproic acid is Pregnancy Category C. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Animal studies have shown adverse effects, but there are no adequate and well-controlled studies in pregnant women.
Trimester-Specific Risks:
First Trimester:
Potential for fetal harm based on animal data; avoid if possible.
Second Trimester:
Use only if clearly needed and benefits outweigh risks.
Third Trimester:
Use only if clearly needed and benefits outweigh risks; potential for increased risk of thrombosis in mother.
Lactation
It is not known whether aminocaproic acid is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Infant Risk:
L3 (Moderate Caution - No human data; molecular weight is low, but potential for accumulation in infant with impaired renal function or theoretical risk of thrombosis).
Pediatric Use
Dosing is weight-based and requires careful calculation. Safety and efficacy in neonates and infants are not well-established. Close monitoring for adverse effects, especially thrombosis and renal function, is crucial.
Geriatric Use
Use with caution in elderly patients, generally starting at the lower end of the dosing range, due to the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant disease or other drug therapy. Renal function should be monitored closely.
Clinical Information
Clinical Pearls
- Aminocaproic acid is primarily used for hyperfibrinolytic bleeding, not for general coagulopathies. Ensure proper diagnosis before use.
- Rapid IV infusion can cause hypotension, bradycardia, and arrhythmias; administer slowly.
- Monitor for signs of thrombosis, especially in patients with pre-existing thrombotic risk factors or those receiving concomitant procoagulant agents.
- Myopathy and rhabdomyolysis are rare but serious side effects; discontinue if muscle pain/weakness or elevated CK occurs.
- Dose adjustment is critical in renal impairment due to significant renal excretion and risk of accumulation.
- Oral formulation is generally well-tolerated but can cause GI upset; taking with food may help.
Alternative Therapies
- Tranexamic Acid (another antifibrinolytic agent, often preferred due to higher potency and longer half-life)
- Desmopressin (for certain bleeding disorders like hemophilia A or von Willebrand disease)
- Factor Concentrates (e.g., Factor VIII, Factor IX for specific deficiencies)
- Cryoprecipitate (source of fibrinogen, Factor VIII, vWF, Factor XIII)
- Fresh Frozen Plasma (FFP) (source of all coagulation factors)
Cost & Coverage
Average Cost:
$50 - $150 per 30 tablets (500mg)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 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 this 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 medical attention. When reporting the incident, be prepared to provide details about the medication taken, the amount, and the time it occurred.