Aminocaproic Acid 1000mg Tablets
It is used to treat or prevent bleeding.
Drug Class
Antifibrinolytic agent
Pharmacologic Class
Lysine analogue
Pregnancy Category
C
FDA Approved
Aug 1964
DEA Schedule
Not Controlled
Overview
What is this medicine?
Aminocaproic acid is a medication used to help stop or prevent excessive bleeding. It works by helping your body form stable blood clots, which can be helpful in conditions where your body breaks down clots too quickly.
How to Use This Medicine
To use this medication correctly, follow your doctor's instructions and carefully read all accompanying information. 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 immediately.
- Report any signs of blood clots, such as chest pain, shortness of breath, swelling or pain in your legs, or sudden numbness/weakness.
- Report any muscle pain, weakness, or dark urine, as these could be signs of a serious side effect (rhabdomyolysis).
- Avoid activities that could increase your risk of injury or bleeding while on this medication, unless advised by your doctor.
- Maintain good hydration.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Initial dose: 5 g (five 1000 mg tablets) orally, followed by 1 to 1.25 g (one or one and a quarter 1000 mg tablets) orally every hour thereafter, or 6 g (six 1000 mg tablets) orally every 6 hours. Max daily dose: 30 g.
Dose Range:
1000 - 30000 mg
Condition-Specific Dosing:
Acute hemorrhage:
Initial dose: 5 g orally, then 1-1.25 g/hour for 8 hours or until bleeding is controlled. Max 30 g/24 hours.
Prophylaxis of rebleeding (e.g., subarachnoid hemorrhage):
1-1.25 g orally every hour for 7-10 days, or 6 g orally every 6 hours. Max 30 g/24 hours.
Dental procedures in hemophiliacs:
2.5-3 g orally 1 hour before procedure, then 1.25 g every 6 hours for 7-10 days.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Initial dose: 100 mg/kg or 3 g/m² orally, followed by 33.3 mg/kg/hour or 1 g/m²/hour. Max 18 g/m²/24 hours.
Adolescent:
Initial dose: 5 g orally, followed by 1-1.25 g/hour. Max 30 g/24 hours.
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment recommended, but monitor for accumulation.
Moderate:
Reduce dose by 50% or extend dosing interval. Monitor plasma levels if possible.
Severe:
Contraindicated in anuria. Significant dose reduction required (e.g., 1.25 g every 8-12 hours). Use with extreme caution and monitor closely.
Dialysis:
Aminocaproic acid is dialyzable. Administer dose after dialysis. Specific dosing recommendations vary; generally, a reduced dose (e.g., 1.25 g every 12-24 hours) is used with 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, a proteolytic enzyme that degrades fibrin clots, fibrinogen, and other plasma proteins. By binding to the lysine-binding sites on plasminogen and plasmin, it prevents plasmin from binding to and degrading fibrin, thereby stabilizing the clot and promoting hemostasis.
Pharmacokinetics
Absorption:
Bioavailability:
Not available (well-absorbed orally)
Tmax:
1.2 hours (oral)
FoodEffect:
Food may delay absorption but does not significantly affect total bioavailability.
Distribution:
Vd:
0.24 L/kg
ProteinBinding:
Not significantly protein bound
CnssPenetration:
Limited (crosses blood-brain barrier poorly)
Elimination:
HalfLife:
1-2 hours
Clearance:
Not available (primarily renal)
ExcretionRoute:
Renal (primarily unchanged)
Unchanged:
Approximately 80% within 12 hours
Pharmacodynamics
OnsetOfAction:
Rapid (within 1-2 hours orally)
PeakEffect:
Within 2-3 hours (oral)
DurationOfAction:
Dose-dependent, typically requires frequent dosing 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 notice 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 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. 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, 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 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 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. 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, 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:
- Unusual bleeding or bruising (e.g., nosebleeds, gum bleeding, blood in urine or stool)
- Signs of blood clots (e.g., sudden chest pain, shortness of breath, pain/swelling/warmth in a leg, sudden vision changes, slurred speech, weakness on one side of the body)
- Severe muscle pain, tenderness, or weakness
- Dark, reddish, or cola-colored urine
- Fever
- Chills
- Rash
- Dizziness or lightheadedness
- Nausea, vomiting, or diarrhea
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 currently 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 dosage 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 currently 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 dosage 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 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 your doctor to discuss 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 your doctor to discuss the potential benefits and risks of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- Hypotension (low blood pressure)
- Bradycardia (slow heart rate)
- Rhabdomyolysis (muscle breakdown leading to kidney damage)
- Acute renal failure
- Thrombosis (blood clot formation)
- Nausea, vomiting, diarrhea
- Dizziness
What to Do:
Seek immediate medical attention or call Poison Control at 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 (increased risk of thrombosis)
- Oral contraceptives/Estrogens (theoretical increased risk of thrombosis, especially with prolonged use)
Major Interactions
- Anticoagulants (e.g., warfarin, heparin, direct oral anticoagulants): May antagonize their effects, increasing risk of thrombosis.
- Thrombolytic agents (e.g., alteplase, streptokinase): Antagonizes their effects, potentially leading to re-thrombosis.
Moderate Interactions
- Chlorpromazine: May increase risk of rhabdomyolysis when co-administered with aminocaproic acid.
- Corticosteroids: May increase risk of myopathy/rhabdomyolysis when co-administered with aminocaproic acid.
Monitoring
Baseline Monitoring
Renal function (BUN, creatinine)
Rationale: Aminocaproic acid is primarily renally excreted; impairment requires dose adjustment.
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
Coagulation parameters (PT, aPTT, fibrinogen)
Frequency: Daily or as clinically indicated, especially during acute bleeding episodes.
Target: Maintain within therapeutic goals for hemostasis.
Action Threshold: Significant prolongation or shortening may require dose adjustment or investigation of underlying cause.
Renal function (BUN, creatinine)
Frequency: Every 2-3 days, or more frequently in patients with pre-existing renal impairment or prolonged therapy.
Target: Maintain within normal limits or patient's baseline.
Action Threshold: Rising creatinine or BUN may indicate drug accumulation or renal toxicity, requiring dose adjustment or discontinuation.
Signs and symptoms of thrombosis
Frequency: Continuously
Target: Absence of new thrombotic events.
Action Threshold: Development of chest pain, shortness of breath, limb swelling, or neurological deficits requires immediate investigation and discontinuation.
Signs and symptoms of myopathy/rhabdomyolysis (e.g., muscle pain, weakness, dark urine)
Frequency: Continuously
Target: Absence of muscle symptoms.
Action Threshold: Presence of symptoms, especially with elevated CK, requires discontinuation.
Symptom Monitoring
- Bleeding (cessation or reduction)
- Signs of thrombosis (e.g., chest pain, dyspnea, limb swelling, neurological changes)
- Muscle pain, weakness, tenderness
- Dark or reddish-brown urine (suggestive of rhabdomyolysis)
- Hypotension
- Bradycardia
- Nausea, vomiting, diarrhea
Special Patient Groups
Pregnancy
Category C. Use 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, but data are limited.
Second Trimester:
Potential for fetal harm, but data are limited.
Third Trimester:
Potential for fetal harm, but data are limited. Risk of thrombosis in mother and fetus.
Lactation
L3 (Moderately Safe). Aminocaproic acid is excreted into breast milk. Caution should be exercised when administered to a nursing mother. Monitor infant for adverse effects (e.g., gastrointestinal upset, signs of thrombosis). Weigh benefits of breastfeeding against potential risks.
Infant Risk:
Low to moderate. Potential for gastrointestinal upset or theoretical risk of thrombosis in the infant, though systemic absorption by the infant is likely low.
Pediatric Use
Dosing is weight-based or body surface area-based. Safety and efficacy have been established in pediatric patients for certain indications (e.g., prevention of bleeding in hemophilia). Close monitoring for adverse effects, especially thrombosis and rhabdomyolysis, is crucial.
Geriatric Use
Use with caution, especially in elderly patients with pre-existing renal impairment, as aminocaproic acid is primarily renally excreted. Start with lower doses and monitor renal function closely to avoid accumulation and toxicity. Increased risk of age-related comorbidities that may predispose to thrombosis.
Clinical Information
Clinical Pearls
- Aminocaproic acid is a potent antifibrinolytic; careful patient selection is crucial to avoid thrombotic complications.
- Renal function must be closely monitored, and dose adjusted in patients with kidney impairment, as the drug is primarily renally excreted.
- Patients should be advised to report any muscle pain, weakness, or dark urine immediately, as these can be signs of rhabdomyolysis, a rare but serious side effect.
- Concurrent use with Factor IX complex concentrates is generally contraindicated due to increased risk of thrombosis.
- Oral administration is preferred for chronic or prophylactic use due to convenience, but IV formulation is available for acute, severe bleeding.
- Not effective for bleeding due to thrombocytopenia or platelet dysfunction.
Alternative Therapies
- Tranexamic acid (another lysine analogue, often preferred due to higher potency and longer half-life)
- Desmopressin (for certain bleeding disorders like hemophilia A or von Willebrand disease)
- Topical hemostatic agents (e.g., thrombin, fibrin sealants) for localized bleeding
- Blood products (e.g., fresh frozen plasma, cryoprecipitate) for specific coagulation factor deficiencies
Cost & Coverage
Average Cost:
$50 - $150 per 30 tablets (1000mg)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (Generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor promptly. 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 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 details about the medication taken, the amount, and the time it happened.