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

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            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
                  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
                  aminocaproic acid intravenous
                  -
                  250 mg/mL vial
                  aminocaproic acid intravenous
                  -
                  250 mg/mL vial

                  Copyright © 2010 First DataBank, Inc.

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                  Patient Education
                  aminocaproic acid oral

                  AMINOCAPROIC ACID - ORAL

                  (a-MEE-noe-ka-PROE-ik-AS-id)

                  COMMON BRAND NAME(S): Amicar

                  USES: This medication is used to help control bleeding due to a condition where your blood does not clot the way it normally should (fibrinolysis). This may cause serious bleeding after certain surgeries or in certain conditions (such as bleeding disorders, liver disease, cancer). Aminocaproic acid works by helping your blood clot normally. It belongs to a class of drugs known as antifibrinolytics.

                  HOW TO USE: Take this medication by mouth as directed by your doctor. Follow your doctor's instructions carefully. The dosage and how often you take this medication are based on your medical condition and response to treatment.Your doctor should closely monitor you until your bleeding is controlled. See also Notes section.It is very important to take this medication as prescribed by your doctor to get the most benefit from it. Do not skip any doses. Do not increase your dose or use this drug more often or for longer than prescribed. Your condition will not improve any faster, and your risk of side effects will increase.If you are using the liquid form of this medication, carefully measure the dose using a special measuring device/spoon. Do not use a household spoon because you may not get the correct dose.Tell your doctor if your condition lasts or gets worse.

                  SIDE EFFECTS: Headache, stomach pain, loss of appetite, nausea, vomiting, diarrhea, unusual tiredness, dizziness, stuffy nose, or watery eyes may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: sore throat that doesn't go away, ringing in the ears, vision changes, muscle pain/weakness, signs of kidney problems (such as change in the amount of urine), confusion, slow heartbeat, unusual bleeding or bruising.Get medical help right away if you have any very serious side effects, including: chest pain, shortness of breath, seizures.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or 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: Before taking aminocaproic acid, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: heart disease, liver disease, kidney disease, other blood/bleeding disorders (such as hemophilia).This drug may make you dizzy. Alcohol or marijuana (cannabis) can make you more dizzy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.It is unknown if this drug passes into breast milk. Consult your doctor before breast-feeding.

                  DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug include: blood clotting factors (such as Factor IX complex, anti-inhibitor coagulant complex), tretinoin.This medication may interfere with certain lab tests, possibly causing false test results. Make sure lab personnel and all your doctors know you use this drug.

                  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: Do not share this medication with others.Lab and/or medical tests (such as platelet counts, blood clotting tests, CPK levels) should be done while you are taking this medication. Consult your doctor for more details.

                  MISSED DOSE: If you miss a dose, ask your doctor or pharmacist right away for a new dosing schedule. Do not double the dose to catch up.

                  STORAGE: Store in a tightly closed container at room temperature away from light and moisture. Do not freeze. Do not store in the bathroom. Keep all medications away from children and pets.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.

                  MEDICAL ALERT: Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-888-633-4298 (US) or 1-800-668-1507 (Canada).

                  Information last revised August 2021. 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

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                  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.
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                  NC NOT COVERED – Drugs that are not covered by the plan.
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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.