Aminocaproic AC 0.25gm/ml Solution
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 bleeding. It works by preventing the breakdown of blood clots that your body forms to stop bleeding. It's often used after surgery, injuries, 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. If you are using the liquid form, measure your dose accurately using the measuring device provided with the medication. If no device is included, consult your pharmacist for a suitable measuring tool.
To store this medication properly, keep it at room temperature and avoid freezing. If you miss a dose, contact your doctor for guidance on what to do next.
To store this medication properly, keep it at room temperature and avoid freezing. If you miss a dose, contact your doctor for guidance on what to do next.
Lifestyle & Tips
- Avoid activities that increase risk of injury or bleeding while on this medication.
- Report any unusual bleeding or bruising immediately.
- Maintain good hydration.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Loading dose: 5 grams (20 mL) orally, followed by 1 to 1.25 grams (4 to 5 mL) orally every hour for 8 hours or until bleeding is controlled. Max daily dose: 30 grams.
Dose Range:
1 - 30 mg
Condition-Specific Dosing:
Acute Hemorrhage:
Loading: 5 g (20 mL) once, then 1-1.25 g (4-5 mL) every hour for 8 hours or until bleeding control. Max 30 g/24 hr.
Prophylaxis (e.g., dental procedures in hemophilia):
Typically 50-100 mg/kg every 6-8 hours, adjusted based on procedure and patient factors.
Pediatric Dosing
Neonatal:
Not established
Infant:
Loading: 100 mg/kg or 3 g/m² (max 5 g) orally. Maintenance: 33.3 mg/kg/hr or 1 g/m²/hr (max 1.25 g/hr) for 8 hours or until bleeding controlled.
Child:
Loading: 100 mg/kg or 3 g/m² (max 5 g) orally. Maintenance: 33.3 mg/kg/hr or 1 g/m²/hr (max 1.25 g/hr) for 8 hours or until bleeding controlled.
Adolescent:
Loading: 100 mg/kg or 3 g/m² (max 5 g) orally. Maintenance: 33.3 mg/kg/hr or 1 g/m²/hr (max 1.25 g/hr) for 8 hours or until bleeding controlled. Adult dosing may be used for older adolescents.
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment, but monitor for accumulation.
Moderate:
Reduce dose by 50% or extend dosing interval. e.g., CrCl 20-50 mL/min: 1.25 g every 2-3 hours or 2.5 g every 6 hours.
Severe:
Contraindicated or significantly reduce dose (e.g., CrCl < 20 mL/min: 1.25 g every 6-12 hours) and monitor closely. Risk of accumulation and toxicity.
Dialysis:
Aminocaproic acid is dialyzable. Administer dose after dialysis. Specific dosing recommendations vary, often 1.25 g every 12-24 hours or as needed based on clinical response and monitoring.
Hepatic Impairment:
Mild:
No specific adjustment.
Moderate:
No specific adjustment, but use with caution due to potential for altered coagulation status in severe liver disease.
Severe:
No specific adjustment, but use with caution due to potential for altered coagulation status in severe liver disease.
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, an enzyme responsible for fibrinolysis (the breakdown of blood clots). It also, to a lesser extent, directly inhibits plasmin activity. By preventing the dissolution of fibrin clots, it helps to stabilize hemostasis and reduce bleeding.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 100%
Tmax:
Approximately 1.2 hours (oral)
FoodEffect:
Food does not significantly affect absorption.
Distribution:
Vd:
Approximately 23.1 L (in adults)
ProteinBinding:
Not protein bound
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 1-2 hours
Clearance:
Approximately 11.6 L/hr
ExcretionRoute:
Renal (primarily unchanged)
Unchanged:
Approximately 65% within 12 hours
Pharmacodynamics
OnsetOfAction:
Rapid (within 1-2 hours orally)
PeakEffect:
Correlates with peak plasma concentrations (around 1.2 hours)
DurationOfAction:
Dependent on dose and renal function, typically 3-4 hours after a single dose, but effects can persist longer with continuous dosing.
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, change in balance, drooping on one side of the face, or blurred vision
Fever, chills, or sore throat
Changes in vision
Ringing in the ears
If you experience any of the following symptoms, which may be signs of a blood clot, seek medical help immediately:
Chest pain or pressure
Coughing up blood
Shortness of breath
Swelling, warmth, numbness, change of color, or pain in a leg or arm
Trouble speaking or swallowing
Additionally, this medication can cause severe muscle problems, which may lead to kidney problems. Contact 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 may only have mild side effects. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:
Headache
Upset stomach or vomiting
Stomach pain or diarrhea
Dizziness, tiredness, or weakness
* Nasal congestion
This is not a comprehensive list of all 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, change in balance, drooping on one side of the face, or blurred vision
Fever, chills, or sore throat
Changes in vision
Ringing in the ears
If you experience any of the following symptoms, which may be signs of a blood clot, seek medical help immediately:
Chest pain or pressure
Coughing up blood
Shortness of breath
Swelling, warmth, numbness, change of color, or pain in a leg or arm
Trouble speaking or swallowing
Additionally, this medication can cause severe muscle problems, which may lead to kidney problems. Contact 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 may only have mild side effects. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:
Headache
Upset stomach or vomiting
Stomach pain or diarrhea
Dizziness, tiredness, or weakness
* Nasal congestion
This is not a comprehensive list of all 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:
- Severe muscle pain or weakness
- Dark or reddish-brown urine
- Chest pain, shortness of breath, or difficulty breathing
- Swelling, pain, or redness in an arm or leg (signs of a blood clot)
- Sudden severe headache or vision changes
- Severe dizziness or fainting
- Unusual or excessive bleeding that doesn't stop
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 your medications, including:
Prescription and over-the-counter (OTC) medications
Natural products
Vitamins
Additionally, inform them about any existing health problems. 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 your medications, including:
Prescription and over-the-counter (OTC) medications
Natural products
Vitamins
Additionally, inform them about any existing health problems. 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 potential 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 potential benefits and risks of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- Nausea
- Diarrhea
- Dizziness
- Confusion
- Bradycardia (slow heart rate)
- Hypotension (low blood pressure)
- Acute renal failure
- Myopathy/rhabdomyolysis (muscle pain, weakness, dark urine)
What to Do:
Seek immediate medical attention. Call 911 or Poison Control at 1-800-222-1222. Treatment is supportive and symptomatic, including gastric lavage, activated charcoal if recent ingestion, and monitoring of vital signs, renal function, and CK levels.
Drug Interactions
Contraindicated Interactions
- Factor IX Complex Concentrates (e.g., Konyne 80, Profilnine SD)
- Anti-inhibitor Coagulant Complex (e.g., FEIBA NF)
Major Interactions
- Estrogens (e.g., ethinyl estradiol, conjugated estrogens) - increased risk of thrombosis
- Oral Contraceptives - increased risk of thrombosis
- Thrombolytic agents (e.g., alteplase, streptokinase, urokinase) - antagonistic effect, concurrent use is contraindicated in most cases.
Moderate Interactions
- Chlorpromazine - theoretical increased risk of myopathy/rhabdomyolysis (rare)
- Corticosteroids (systemic) - theoretical increased risk of myopathy/rhabdomyolysis (rare)
Monitoring
Baseline Monitoring
Renal function (BUN, Creatinine)
Rationale: Aminocaproic acid is primarily renally excreted; impairment can lead to accumulation and toxicity.
Timing: Prior to initiation
Coagulation parameters (PT, aPTT, Fibrinogen, Platelet count)
Rationale: To assess baseline hemostatic status and guide therapy.
Timing: Prior to initiation
Complete Blood Count (CBC)
Rationale: To assess baseline hematologic status.
Timing: Prior to initiation
Routine Monitoring
Renal function (BUN, Creatinine)
Frequency: Daily or every 2-3 days, especially in prolonged therapy or renal impairment.
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: As clinically indicated, especially during acute bleeding episodes.
Target: Dependent on underlying condition and therapeutic goal.
Action Threshold: Evidence of continued hyperfibrinolysis or signs of thrombosis.
Creatine Kinase (CK)
Frequency: If muscle pain or weakness develops.
Target: Within normal limits.
Action Threshold: Significant elevation; investigate for myopathy/rhabdomyolysis.
Symptom Monitoring
- Muscle pain or weakness
- Dark or reddish-brown urine (suggestive of rhabdomyolysis)
- Signs of thrombosis (e.g., chest pain, shortness of breath, swelling/pain in leg, sudden headache, vision changes)
- Nausea, vomiting, diarrhea
- Dizziness, lightheadedness
- Hypotension
Special Patient Groups
Pregnancy
Category C. Animal studies have shown adverse effects on the fetus. Use only if the potential benefit justifies the potential risk to the fetus. Limited human data, but generally avoided unless clearly indicated for life-threatening bleeding.
Trimester-Specific Risks:
First Trimester:
Potential for fetal harm, use only if essential.
Second Trimester:
Potential for fetal harm, use only if essential.
Third Trimester:
Potential for fetal harm, use only if essential. Risk of thrombosis in mother and fetus.
Lactation
Aminocaproic acid is excreted into breast milk. Due to the potential for serious adverse reactions in the nursing infant, 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. L3 (Moderate risk).
Infant Risk:
Potential for gastrointestinal upset, theoretical risk of thrombosis, or other unknown effects. Monitor infant for adverse effects.
Pediatric Use
Dosing is weight or body surface area-based. Close monitoring is essential due to potential for accumulation, especially in neonates and infants with immature renal function. Safety and efficacy in neonates are not well-established.
Geriatric Use
Use with caution due to the higher likelihood of decreased renal function in elderly patients, which can lead to drug accumulation and increased risk of adverse effects. Start with lower doses and monitor renal function closely.
Clinical Information
Clinical Pearls
- Aminocaproic acid is primarily used for hyperfibrinolytic bleeding, not for general coagulopathies.
- Contraindicated in active intravascular clotting (e.g., DIC without concomitant heparin) due to risk of promoting widespread thrombosis.
- Monitor for signs of myopathy/rhabdomyolysis (muscle pain, weakness, dark urine), especially with prolonged use or in patients with renal impairment.
- Oral solution can be mixed with water, fruit juices, or soft drinks for palatability.
- Ensure adequate hydration to prevent renal complications.
Alternative Therapies
- Tranexamic Acid (another antifibrinolytic agent, often preferred due to higher potency and longer half-life)
Cost & Coverage
Average Cost:
Varies, typically $50-$200 per 480 mL bottle (0.25 gm/mL)
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 evaluation and guidance. To ensure your safety and the effectiveness of your treatment, never share your medication with others or take someone else's medication. Some medications may come with additional patient information leaflets, so it is a good idea to consult with your pharmacist for more details. If you have any questions or concerns about your medication, do not hesitate to discuss them with 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 information about the medication taken, the amount, and the time it was taken, as this will aid in your treatment.