Amicar 0.25gm/ml Solution
It is used to treat or prevent bleeding.
Drug Class
Antifibrinolytic Agent
Pharmacologic Class
Lysine Analogue; Plasminogen Activation Inhibitor
Pregnancy Category
Category C
FDA Approved
Aug 1964
DEA Schedule
Not Controlled
Overview
What is this medicine?
Aminocaproic acid is a medicine used to stop or reduce bleeding. It works by helping your body form and keep blood clots, which are essential to stop bleeding. It's often used after surgery, for certain bleeding disorders, or to manage heavy menstrual bleeding.
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. When taking the liquid form, measure your dose accurately using the measuring device provided with the medication. If a measuring device is not included, consult your pharmacist for a suitable alternative.
To store this medication, keep it at room temperature and avoid freezing. If you miss a dose, contact your doctor for guidance on the best course of action.
To store this medication, keep it at room temperature and avoid freezing. If you miss a dose, contact your doctor for guidance on the best course of action.
Lifestyle & Tips
- Take exactly as prescribed by your doctor. Do not stop taking it without consulting your doctor.
- Measure the liquid medicine carefully using the provided measuring device, not a household spoon.
- Report any unusual bleeding or bruising, or signs of blood clots (e.g., chest pain, shortness of breath, leg swelling) to your doctor immediately.
- Avoid activities that may increase your risk of bleeding or injury while on this medication, unless advised by your doctor.
- Inform all healthcare providers, including dentists, that you are taking this medication.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
Initial loading dose of 5 grams (20 mL of 0.25 gm/mL solution) orally, followed by 1.25 grams (5 mL) orally every hour thereafter. Continue for approximately 8 hours or until bleeding has been controlled. Maximum daily dose: 30 grams (120 mL).
Dose Range:
1.25 - 30 mg
Condition-Specific Dosing:
prophylaxis_dental_procedures:
2-3 grams orally 1 hour prior to procedure, then 1-1.5 grams every 6 hours for 5-7 days.
menorrhagia:
1-1.5 grams orally 3-4 times daily during menstruation, not to exceed 5 days.
Pediatric Dosing
Neonatal:
Not established
Infant:
Initial loading dose of 100 mg/kg or 3 grams/m² orally, followed by 33.3 mg/kg/hour or 1 gram/m²/hour orally. Maximum daily dose: 18 grams/m².
Child:
Initial loading dose of 100 mg/kg or 3 grams/m² orally, followed by 33.3 mg/kg/hour or 1 gram/m²/hour orally. Maximum daily dose: 18 grams/m².
Adolescent:
Initial loading dose of 100 mg/kg or 3 grams/m² orally, followed by 33.3 mg/kg/hour or 1 gram/m²/hour orally. Maximum daily dose: 18 grams/m².
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment recommended, but monitor for accumulation.
Moderate:
Reduce dose by 50% or extend dosing interval. Monitor for accumulation.
Severe:
Reduce dose significantly (e.g., 75% reduction) or extend dosing interval. Avoid if possible. Monitor for accumulation.
Dialysis:
Aminocaproic acid is dialyzable. Administer dose after dialysis. Specific dosing recommendations vary, often requiring significant dose reduction and close monitoring.
Hepatic Impairment:
Mild:
No specific adjustment recommended.
Moderate:
No specific adjustment recommended, as hepatic metabolism is minimal. Monitor for adverse effects.
Severe:
No specific adjustment recommended, as hepatic metabolism is minimal. Monitor for adverse effects.
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 that degrades fibrin clots, fibrinogen, and other plasma proteins. By inhibiting plasmin formation and activity, it stabilizes blood clots and prevents their premature lysis, thereby promoting hemostasis.
Pharmacokinetics
Absorption:
Bioavailability:
High (well absorbed orally)
Tmax:
Approximately 1.2 hours (oral solution)
FoodEffect:
Not significantly affected by food.
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 (urine)
Unchanged:
Approximately 65% excreted unchanged within 12 hours
Pharmacodynamics
OnsetOfAction:
Rapid (within 1-2 hours after oral administration)
PeakEffect:
Correlates with peak plasma concentrations (Tmax)
DurationOfAction:
Dependent on continued dosing and plasma levels; effects persist as long as therapeutic concentrations are maintained.
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 change, or pain in a leg or arm
+ Trouble speaking or swallowing
This medication can also 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 may cause side effects in some people. Many individuals may not experience any side effects or only minor ones. If you notice any of the following side effects or any other symptoms that concern you or do not go away, 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 change, or pain in a leg or arm
+ Trouble speaking or swallowing
This medication can also 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 may cause side effects in some people. Many individuals may not experience any side effects or only minor ones. If you notice any of the following side effects or any other symptoms that concern you or do not go away, 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:
- Signs of a blood clot: sudden chest pain, shortness of breath, coughing up blood, sudden vision changes, sudden numbness or weakness, pain/swelling/warmth in an arm or leg.
- Signs of bleeding: unusual bruising, prolonged bleeding from cuts, nosebleeds, blood in urine (pink or red urine), black or tarry stools, vomiting blood or material that looks like coffee grounds.
- Muscle pain, tenderness, or weakness, especially if accompanied by fever or dark urine (signs of rhabdomyolysis).
- Allergic reaction: 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 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 interact with this drug (your doctor or pharmacist can help you determine if any of your medications fall into this category)
To ensure your safety, it is crucial 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 if 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 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 interact with this drug (your doctor or pharmacist can help you determine if any of your medications fall into this category)
To ensure your safety, it is crucial 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 if 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. 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. Please note that 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 your doctor to carefully weigh the 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
- Thrombosis (blood clot formation)
What to Do:
Seek immediate medical attention or call a poison control center (e.g., 1-800-222-1222). Treatment is supportive and symptomatic. Gastric lavage may be considered if ingestion is recent. Hemodialysis may be effective in removing the drug.
Drug Interactions
Contraindicated Interactions
- Factor IX complex concentrates
- Activated prothrombin complex concentrates (e.g., FEIBA)
Major Interactions
- Oral contraceptives (estrogen-containing)
- Estrogens (systemic)
Moderate Interactions
- Thrombolytic agents (e.g., alteplase, streptokinase, urokinase)
- Tretinoin (oral)
Monitoring
Baseline Monitoring
Renal function (BUN, creatinine)
Rationale: Aminocaproic acid is primarily renally eliminated; impairment can lead to 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: Periodically, especially in patients with renal impairment or prolonged therapy.
Target: Within normal limits or stable for patient's baseline.
Action Threshold: Significant increase in BUN/creatinine may warrant dose adjustment or discontinuation.
Coagulation parameters (PT, aPTT, fibrinogen)
Frequency: Periodically, as clinically indicated.
Target: Dependent on underlying condition and therapeutic goal.
Action Threshold: Evidence of hypercoagulability or inadequate hemostasis may require intervention.
Creatine Phosphokinase (CPK)
Frequency: If muscle pain or weakness develops.
Target: Within normal limits.
Action Threshold: Elevated CPK may indicate myopathy/rhabdomyolysis, requiring discontinuation.
Urinalysis
Frequency: Periodically, especially with prolonged use.
Target: Absence of hematuria or signs of renal damage.
Action Threshold: Presence of hematuria or red cell casts may indicate glomerular capillary thrombosis.
Symptom Monitoring
- Signs and symptoms of thrombosis (e.g., chest pain, shortness of breath, sudden leg pain/swelling, vision changes, slurred speech)
- Signs and symptoms of bleeding (e.g., excessive bruising, prolonged bleeding from cuts, nosebleeds, blood in urine/stools, black/tarry stools, vomiting blood)
- Muscle pain, weakness, or tenderness (signs of myopathy/rhabdomyolysis)
- Dizziness, lightheadedness
- Nausea, vomiting, diarrhea
- Headache
Special Patient Groups
Pregnancy
Category C. Aminocaproic acid 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; use only if clearly needed.
Second Trimester:
Potential for fetal harm based on animal data; use only if clearly needed.
Third Trimester:
Potential for fetal harm based on animal data; use only if clearly needed.
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:
Not available; use with caution or consider alternative.
Pediatric Use
Dosing is established for pediatric patients, but careful weight-based or body surface area-based calculations are crucial. Close monitoring for adverse effects and efficacy is essential.
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 of concomitant disease or other drug therapy. Renal function should be monitored closely.
Clinical Information
Clinical Pearls
- Aminocaproic acid is primarily used for excessive bleeding due to enhanced fibrinolysis, such as in cardiac surgery, prostatectomy, or certain hematologic disorders.
- It is contraindicated in patients with disseminated intravascular coagulation (DIC) without concomitant heparin, due to the risk of promoting thrombosis.
- Monitor for signs of thrombosis (e.g., DVT, PE, arterial thrombosis) as this is a significant potential adverse effect, especially when used with procoagulant factors.
- Myopathy and rhabdomyolysis have been reported, particularly with prolonged use. Monitor for muscle pain, weakness, and elevated CPK.
- Renal impairment necessitates significant dose adjustment due to renal excretion of the drug.
- Oral solution is useful for patients who cannot swallow tablets or for precise dose adjustments.
Alternative Therapies
- Tranexamic acid (another antifibrinolytic agent, often preferred due to higher potency and longer half-life)
Cost & Coverage
Average Cost:
Varies widely by pharmacy and quantity per 120 mL bottle
Generic Available:
Yes
Insurance Coverage:
Generally covered by most insurance plans, often as a Tier 1 or Tier 2 generic. Prior authorization may be required for certain indications or quantities.
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 medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it occurred.