Aminocaproic Acid 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 medication used to help stop bleeding. It works by preventing the breakdown of blood clots, which are essential for stopping bleeding. It's often used for conditions where there's excessive bleeding due to problems with clot breakdown, such as 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 quality and effectiveness of this medication, 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 quality and effectiveness of this medication, 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 risk of injury or bleeding.
- Report any unusual bleeding or bruising immediately.
- Stay well-hydrated to support kidney function.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Initial loading dose of 5 grams orally, followed by 1 to 1.25 grams orally every hour thereafter, or 1.25 grams orally every 6 hours, for a total daily dose of 5 to 30 grams.
Dose Range:
5 - 30 mg
Condition-Specific Dosing:
Acute hemorrhage:
Initial 5g, then 1-1.25g/hr (max 30g/24hr) for 8 hours or until bleeding is controlled.
Prophylaxis for dental procedures in hemophilia:
2.5g every 6 hours starting 1 day prior to procedure and continuing for 7-10 days post-procedure.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Initial loading dose of 100 mg/kg or 3 grams/m² orally, followed by 33.3 mg/kg or 1 gram/m² orally every hour, up to a maximum of 18 grams/m²/24 hours. Total daily dose should not exceed 24 grams.
Adolescent:
Initial loading dose of 5 grams orally, followed by 1 to 1.25 grams orally every hour thereafter, or 1.25 grams orally every 6 hours, for a total daily dose of 5 to 30 grams.
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment recommended, but monitor closely.
Moderate:
Reduce dose by 50% or extend dosing interval. Monitor renal function and clinical response.
Severe:
Contraindicated in severe renal impairment due to risk of accumulation and toxicity (e.g., rhabdomyolysis, acute renal failure).
Dialysis:
Aminocaproic acid is dialyzable. Dosing post-dialysis may be required, but use with extreme caution and monitor closely.
Hepatic Impairment:
Mild:
No specific adjustment recommended.
Moderate:
No specific adjustment recommended, but monitor for adverse effects.
Severe:
No specific adjustment recommended, but use with caution as hepatic dysfunction may affect coagulation parameters.
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. Plasmin is an enzyme that degrades fibrin clots, fibrinogen, and other plasma proteins. By inhibiting plasmin, aminocaproic acid stabilizes clots and prevents their premature lysis, thereby promoting hemostasis.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 80-100%
Tmax:
Approximately 1.2 hours
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:
Approximately 116 mL/min (renal clearance)
ExcretionRoute:
Renal (primarily unchanged)
Unchanged:
Approximately 65% (within 12 hours)
Pharmacodynamics
OnsetOfAction:
Rapid (within minutes to hours depending on route and dose)
PeakEffect:
Within 1-2 hours
DurationOfAction:
Dose-dependent, typically 3-4 hours after last dose due to short half-life.
Safety & Warnings
Side Effects
Serious Side Effects: Seek Medical Help Immediately
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you experience any of the following symptoms, contact your doctor or seek medical attention 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 change, or pain in a leg or arm
+ Trouble speaking or swallowing
Muscle Problems and Kidney Damage
This medication can cause severe muscle problems, which may lead to kidney damage. 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 Side Effects
Like all medications, this drug can cause side effects. Many people experience no side effects or only mild ones. If you experience any of the following side effects, or if they bother you or persist, contact your doctor:
Headache
Upset stomach or vomiting
Stomach pain or diarrhea
Dizziness, fatigue, or weakness
* Nasal congestion
Reporting Side Effects
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 experience any of the following symptoms, contact your doctor or seek medical attention 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 change, or pain in a leg or arm
+ Trouble speaking or swallowing
Muscle Problems and Kidney Damage
This medication can cause severe muscle problems, which may lead to kidney damage. 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 Side Effects
Like all medications, this drug can cause side effects. Many people experience no side effects or only mild ones. If you experience any of the following side effects, or if they bother you or persist, contact your doctor:
Headache
Upset stomach or vomiting
Stomach pain or diarrhea
Dizziness, fatigue, or weakness
* Nasal congestion
Reporting Side Effects
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 a blood clot: sudden chest pain, shortness of breath, pain/swelling in leg or arm, sudden vision changes, slurred speech.
- Muscle pain, tenderness, or weakness, especially if accompanied by fever or dark urine (signs of rhabdomyolysis).
- Severe headache, dizziness, or confusion.
- Allergic reaction: rash, itching, swelling of face/tongue/throat, severe dizziness, trouble breathing.
- Unusual bleeding or bruising that worsens.
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 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 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. A discussion about the potential benefits and risks of this medication to both you and your baby will be necessary to ensure your safety and the safety of your child.
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. A discussion about the potential benefits and risks of this medication to both you and your baby will be necessary to ensure your safety and the safety of your child.
Overdose Information
Overdose Symptoms:
- Nausea
- Diarrhea
- Dizziness
- Confusion
- Hypotension (low blood pressure)
- Acute renal failure
- Thrombosis (blood clot formation)
What to Do:
Seek immediate medical attention or call a poison control center (1-800-222-1222). Treatment is supportive and symptomatic. Hemodialysis may be considered as aminocaproic acid is dialyzable.
Drug Interactions
Contraindicated Interactions
- Factor IX Complex Concentrates (e.g., Konyne 80, Profilnine SD, Bebulin VH, Alphanine SD) - due to increased risk of thrombosis.
- Anti-inhibitor Coagulant Complex (e.g., FEIBA) - due to increased risk of thrombosis.
Major Interactions
- Oral Contraceptives/Estrogens (increased risk of thrombosis)
- Coagulation Factor VIIa (recombinant) (increased risk of thrombosis)
- Tretinoin (oral) (increased risk of thrombosis)
Moderate Interactions
- Anticoagulants (e.g., Warfarin, Heparin) - may antagonize effects of anticoagulants, increasing risk of thrombosis.
- Thrombolytic agents (e.g., Alteplase, Reteplase, Tenecteplase) - concurrent use is contraindicated as aminocaproic acid inhibits fibrinolysis.
Monitoring
Baseline Monitoring
Renal function (BUN, creatinine)
Rationale: Aminocaproic acid is primarily renally excreted; impairment increases risk of accumulation and toxicity.
Timing: Prior to initiation of therapy.
Coagulation parameters (PT, aPTT, fibrinogen, platelet count)
Rationale: To assess baseline hemostatic status and guide therapy.
Timing: Prior to initiation of therapy.
Routine Monitoring
Renal function (BUN, creatinine)
Frequency: Daily or every other day, especially in prolonged therapy or renal impairment.
Target: Within normal limits or stable 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 time, stable fibrinogen levels).
Action Threshold: Evidence of hypercoagulability or inadequate hemostasis; adjust dose or consider alternative therapy.
Creatine Kinase (CK) levels
Frequency: If muscle pain or weakness develops.
Target: Within normal limits.
Action Threshold: Significant elevation (suggestive of rhabdomyolysis); discontinue drug immediately.
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 rhabdomyolysis)
- Signs of allergic reaction (e.g., rash, itching, swelling, dizziness, trouble breathing)
- Gastrointestinal upset (nausea, vomiting, diarrhea, abdominal cramps)
- Dizziness, lightheadedness
- Headache
Special Patient Groups
Pregnancy
Category C. Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks. Use only if clearly needed and the potential benefits outweigh the potential risks to the fetus.
Trimester-Specific Risks:
First Trimester:
Potential for fetal harm based on animal data; human data lacking.
Second Trimester:
Potential for fetal harm based on animal data; human data lacking.
Third Trimester:
Potential for fetal harm based on animal data; human data lacking. 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, caution should be exercised when aminocaproic acid is administered to a nursing woman. 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:
Not available; potential for unknown risk.
Pediatric Use
Dosing is weight-based for children. Safety and efficacy in neonates and infants are not established. Use with caution and close monitoring due to potential for increased risk of adverse effects, especially in younger children.
Geriatric Use
No specific dose adjustment is generally required based on age alone, but elderly patients are more likely to have decreased renal function, which necessitates dose adjustment. Monitor renal function closely. Increased susceptibility to adverse effects, particularly thrombosis, may occur.
Clinical Information
Clinical Pearls
- Aminocaproic acid is primarily used for excessive bleeding due to enhanced fibrinolysis, not for general bleeding disorders.
- Oral administration is preferred for chronic or prophylactic use, while IV is used for acute, severe bleeding.
- Monitor for signs of thrombosis (e.g., DVT, PE) as this is a serious potential side effect, especially with concomitant procoagulant factors.
- Educate patients on symptoms of rhabdomyolysis (muscle pain, weakness, dark urine) and to seek immediate medical attention if they occur.
- Contraindicated in disseminated intravascular coagulation (DIC) with active intravascular clotting, unless the primary problem is fibrinolysis.
Alternative Therapies
- Tranexamic Acid (another lysine analog antifibrinolytic)
- Desmopressin (for certain bleeding disorders like hemophilia A, von Willebrand disease)
- Factor replacement therapies (e.g., Factor VIII, Factor IX concentrates)
- Topical hemostatic agents (for localized bleeding)
Cost & Coverage
Average Cost:
Price range: $30 - $100 per 30 tablets
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (Generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it is 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 it's a good idea 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 seeking help, be prepared to provide details about the medication, including the amount taken and the time it happened, to facilitate prompt and effective treatment.