aminocaproic acid (Rx)

Brand and Other Names:Amicar
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

injectable solution

  • 250mg/mL

syrup

  • 1.25g/5mL

tablet

  • 500mg
  • 1,000mg

Fibrinolytic Bleeding

Initial: 4-5 g IV/PO during 1st hr, THEN 1-1.25 g PO q1hr, OR

Continuous IV infusion at 1 g/hr

Continue for 8 hr or until bleeding controlled, not to exceed 30 g/day

Decrease dose in cardiac, renal, or hepatic disease

Control of Bleeding with Severe Thrombocytopenia (Off-label)

Initial: 100 mg/kg IV over 30-60 min; not to exceed 5 g

Maintenance: 1-4 g PO/IV q4-8hr for 1 g/hr; not to exceed 24 g/24hr

Hyphema (Orphan)

Topical gel (Caprogel) for treatment of traumatic hyphema of the eye

Administration: Topical

Orphan indication sponsor

  • Eastern Virginia Medical School Department of Ophthalmology; 880 Kempsville Road, Suite 2500; Norfolk, VA 23502-3990

Other Indications & Uses

Bleeding due to systemic hyperfibrinolysis

Off-label: prevent recurrence of subarachnoid hemorrhage; prevent hereditary angioneurotic edema attacks; reduce post-op bleeding

Dosage Forms & Strengths

injectable solution

  • 250mg/mL

syrup

  • 1.25g/5mL

tablet

  • 500mg

Prevention of Perioperative Bleeding Associated with Cardiac Surgery (Off-label)

100 mg/kg IV over 20-30 min after induction prior to incision

100 mg/kg IV over 20-30 min during cardiopulmonary bypass

100 mg/kg IV after heparin reversal

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Interactions

Interaction Checker

and aminocaproic acid

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    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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             activity indicator 

            Contraindicated (0)

              Serious - Use Alternative (0)

                Monitor Closely (3)

                • defibrotide

                  aminocaproic acid decreases effects of defibrotide by pharmacodynamic antagonism. Modify Therapy/Monitor Closely. Defibrotide may diminish effects of thrombolytic agents. Consider therapy modification.

                • ethinylestradiol

                  ethinylestradiol, aminocaproic acid. Other (see comment). Use Caution/Monitor. Comment: Concomitant use may lead to additive hypercoagulability. Estrogens increase clotting factor production and platelet aggregation; aminocaproic acid inhibits fibrinolysis and activity of plasminogen.

                • mestranol

                  mestranol decreases effects of aminocaproic acid by pharmacodynamic antagonism. Use Caution/Monitor. Risk of thromboembolic disorder.

                Minor (0)

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                  Adverse Effects

                  Frequency Not Defined

                  Confusion

                  Vision decrease

                  Vomiting

                  Headache

                  Convulsions

                  Malaise

                  Muscle weakness

                  Dizziness

                  Tinnitus

                  Nausea

                  Bradycardia

                  Thrombosis

                  Edema

                  Hypotension

                  Stroke

                  Syncope

                  Intracranial hypertension

                  Peripheral ischemia

                  Pulmonary embolism

                  Dyspnea

                  Congestion

                  Diarrhea

                  Abdominal pain

                  Leukopenia

                  Agranulocytosis

                  Coagulation disorder

                  Dry ejaculation

                  Injection site reactions (pain/necrosis)

                  Myopathy

                  Pruritus

                  Rash

                  Renal failure

                  Anaphylaxis

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                  Warnings

                  Contraindications

                  In presence of DIC without concomitant heparin

                  Evidence of active intravascular clotting process

                  Cautions

                  Use cautioni in renal/cardiac/hepatic impairment

                  Risk of myopathy

                  In patients with upper urinary tract bleeding, therapy has been known to cause intrarenal obstruction in form of glomerular capillary thrombosis or clots in renal pelvis and ureters; for this reason, drug should not be used in hematuria of upper urinary tract origin, unless possible benefits outweigh risks

                  Avoid rapid IV administration

                  Therapy inhibits both action of plasminogen activators and to a lesser degree, plasmin activity; drug should not be administered without a definite diagnosis and/or laboratory finding indicative of hyperfibrinolysis (hyperplasminemia)

                  Preservative benzyl alcohol linked to fatal "Gasping Syndrome" in premature neonates

                  Skeletal muscle weakness with necrosis of muscle fibers reported following prolonged administration (rare); Clinical presentation may range from mild myalgias with weakness and fatigue to severe proximal myopathy with rhabdomyolysis, myoglobinuria, and acute renal failure; muscle enzymes, especially creatine phosphokinase (CPK) are elevated; monitor CPK levels in patients on long-term therapy; stop therapy if rise in CPK noted; resolution follows discontinuation of therapy; however, syndrome may recur if therapy restarted

                  Inhibition of fibrinolysis may theoretically result in clotting or thrombosis; there is no definite evidence that therapy has been responsible for few reported cases of intravascular clotting which followed treatment; rather, it appears that intravascular clotting was most likely due to patient's preexisting clinical condition, eg, the presence of DIC; it has been postulated that extravascular clots formed in vivo may not undergo spontaneous Iysis as do normal clots

                  Therapy should not be administered with Factor IX Complex concentrates or Anti-Inhibitor Coagulant concentrates, as risk of thrombosis may increase

                  Reports have appeared in literature of increased incidence of certain neurological deficits,j including hydrocephalus, cerebral ischemia, or cerebral vasospasm associated with use of antifibrinolytic agents in treatment of subarachnoid hemorrhage (SAH); all of these events have also been described as part of the natural course of SAH, or as a consequence of diagnostic procedures such as angiography; drug relatedness remains unclear

                  Differentiate primary fibrinolysis from disseminated intravascular coagulation (DIC)

                  • When there is uncertainty as to whether cause of bleeding is primary fibrinolysis or disseminated intravascular coagulation (DIC), distinction must be made before administering therapy
                  • The following tests can be applied to differentiate the two conditions:
                    • Platelet count is usually decreased in DIC but normal in primary fibrinolysis
                    • Protamine paracoagulation test is positive in DIC; a precipitate forms when protamine sulfate is dropped into citrated plasma; the test is negative in presence of primary fibrinolysis
                    • The euglobulin clot Iysis test is abnormal in primary fibrinolysis but normal in DIC

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                  Pregnancy & Lactation

                  Pregnancy Category: C

                  Lactation: Not known whether excreted in breast milk, use caution

                  Pregnancy Categories

                  A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

                  B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

                  C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

                  D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

                  X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

                  NA: Information not available.

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                  Pharmacology

                  Mechanism of Action

                  Inhibits fibrinolysis through inhibition of plasminogen binding to fibrin and subsequent conversion to plasmin, which in turn inhibits fibrinolysis

                  Exhibits antiplasmin activity

                  Pharmacokinetics

                  Onset: 1-72 hr

                  Duration: 3-4 hr (after 1 dose)

                  Half-Life: 2 hr

                  Vd: 23 L (PO), 30 L (IV)

                  Metabolism: Liver

                  Metabolites: Adipic acid

                  Clearance: 169 mL/min

                  Time to peak: Within 2 hr (PO)

                  Excretion: urine (65%)

                  Dialyzable: HD: yes

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                  Administration

                  IV Compatibilities

                  Solution: D5W, NS, Ringer's

                  Additive: netilmicin

                  Y-site: fenoldopam

                  IV Administration

                  Initial 5 g in 250 mL over 1 hr, each subsequent gram in 50-100 mL at 1 g/hr

                  Rapid injection undiluted into a vein is not recommended

                  Continue for about 8 hr or until bleeding has been controlled

                  Storage

                  Store between 15-30°C (59-86°F)

                  Do not freeze

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                  Images

                  BRAND FORM. UNIT PRICE PILL IMAGE
                  aminocaproic acid intravenous
                  -
                  250 mg/mL vial
                  aminocaproic acid intravenous
                  -
                  250 mg/mL vial
                  Amicar oral
                  -
                  500 mg tablet
                  Amicar oral
                  -
                  1,000 mg tablet
                  Amicar oral
                  -
                  250 mg/mL (25 %) solution
                  aminocaproic acid oral
                  -
                  250 mg/mL (25 %) solution
                  aminocaproic acid oral
                  -
                  500 mg tablet
                  aminocaproic acid oral
                  -
                  1,000 mg tablet
                  aminocaproic acid oral
                  -
                  500 mg tablet

                  Copyright © 2010 First DataBank, Inc.

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                  Patient Handout

                  Select a drug:
                  Patient Education
                  aminocaproic acid intravenous

                  NO MONOGRAPH AVAILABLE AT THIS TIME

                  USES: Consult your pharmacist.

                  HOW TO USE: Consult your pharmacist.

                  SIDE EFFECTS: Consult your pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

                  PRECAUTIONS: Consult your pharmacist.

                  DRUG INTERACTIONS: Consult your pharmacist.Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

                  OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

                  NOTES: No monograph available at this time.

                  MISSED DOSE: Consult your pharmacist.

                  STORAGE: Consult your pharmacist.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

                  Information last revised July 2016. Copyright(c) 2021 First Databank, Inc.

                  IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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                  Formulary

                  FormularyPatient Discounts

                  Adding plans allows you to compare formulary status to other drugs in the same class.

                  To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

                  Adding plans allows you to:

                  • View the formulary and any restrictions for each plan.
                  • Manage and view all your plans together – even plans in different states.
                  • Compare formulary status to other drugs in the same class.
                  • Access your plan list on any device – mobile or desktop.

                  The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

                  Tier Description
                  1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
                  2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
                  3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
                  4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                  5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                  6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                  NC NOT COVERED – Drugs that are not covered by the plan.
                  Code Definition
                  PA Prior Authorization
                  Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
                  QL Quantity Limits
                  Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
                  ST Step Therapy
                  Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
                  OR Other Restrictions
                  Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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                  Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.