Aminocaproic acid is an antifibrinolytic agent that acts by inhibiting plasminogen activators which have fibrinolytic properties. Aminocaproic Acid is a synthetic lysine derivative with antifibrinolytic activity. Aminocaproic acid competitively inhibits activation of plasminogen, thereby reducing conversion of plasminogen to plasmin (fibrinolysin), an enzyme that degrades fibrin clots as well as fibrinogen and other plasma proteins including the procoagulant factors V and VIII. Aminocaproic acid competitively reduces the conversion of plasminogen to plasmin by plasminogen activators. It directly inhibits proteolytic activity of plasmin, but higher doses are required than are needed to reduce plasmin formation. Aminocaproic acid is used in the treatment of hemorrhage and prophylactically against hemorrhage, including hyperfibrinolysis-induced hemorrhage and postsurgical hemorrhage.
Aminocaproic acid is a derivative and analog of the amino acid lysine, which makes it an effective inhibitor for enzymes that bind that particular residue. Such enzymes include proteolytic enzymes like plasmin, the enzyme responsible for fibrinolysis. For this reason, it is effective in the treatment of certain bleeding disorders. An antifibrinolytic agent that acts by inhibiting plasminogen activators which have fibrinolytic properties.
Mechanism of Action
Aminocaproic acid binds reversibly to the kringle domain of plasminogen and blocks the binding of plasminogen to fibrin and its activation to plasmin. With NO activation of plasmin, there is a reduction in fibrinolysis. This consequently will reduce the amount of bleeding post surgery. Elevated plasma levels of lipoprotein(a) have been shown to increase the risk of vascular disease. Lipoprotein 9a)a has two components, apolipoprotein B-100, linked to apolipoprotein (a). Aminocaproic acid may change the conformation of apoliprotein (a), changing its binding properties and potentially preventing the formation of lipoprotein (a).
Indications
- excessive postoperative bleeding.
- Fibrinolytic Bleeding
- Bleeding caused by thrombocytopenia
- Bleeding of the oral
- Hemorrhage
- Secondary subarachnoid hemorrhage
Dosage
Strengths: 500 mg; 1000 mg, 1.25 g/5 mL; 250 mg/mL;
Fibrinolytic Bleeding
- IV: 4 to 5 g IV infusion during the first hour of treatment, followed by a continuous infusion of 1 g/hr.
- Oral: 5 g orally during the first hour of treatment, followed by a continuous rate of 1 g/hr (tablets) or 1.25 g/hr (oral solution).
Side Effects
The most common
- nausea ,vomiting
- stomach pain or cramping
- diarrhea
- a headache
- dizziness
- confusion
- stomach pain;
- tired feeling;
- eye redness; or
- back pain, joint or muscle pain.
- problems with your vision (including color vision);
- sudden numbness or weakness, especially on one side of the body;
- a sudden headache, confusion, problems with vision, speech, or balance;
- sudden chest pain or trouble breathing;
- pain or swelling in one or both legs;
- migraine headache;
- pale skin, feeling light-headed or short of breath, rapid heart rate, trouble concentrating; or
- feeling like you might pass out.
More common
- Abdominal or stomach pain, discomfort, or tenderness
- chills or fever
- difficulty with moving
- headache, severe and throbbing
- joint or back pain
- muscle aching or cramping
- muscle pains or stiffness
- chest pressure or squeezing pain in chest
- discomfort in arms, shoulders, neck or upper back
- excessive sweating
- feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
- sudden tingling or coldness in an arm or leg
- sudden slow or difficult speech
- sudden drowsiness or need to sleep
- sudden weakness or numbness of an arm or leg
- fast breathing
- sharp pain when taking a deep breath
- fast or slow heartbeat
- coughing up blood
- rust colored urine
- decreased amount of urine
Incidence not known
- Anxiety
- change in vision
- chest pain or tightness
- confusion
- cough
- difficulty with swallowing
- dizziness or lightheadedness
- fainting
- fast heartbeat
- numbness of the hands
- pain, redness, or swelling in the arm or leg
- puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue
Drug Interactions
There may be an interaction between tranexamic acid and any of the following:
- fibrinogen
- hormonal birth control (estrogens and progesterones)
- tretinoin
Some products that may interact with this drug include: “blood thinners” (anticoagulants such as warfarin, heparin), drugs that prevent bleeding (including factor IX complex, anti-inhibitor coagulant concentrates), tretinoin, estrogens, hormonal birth control (such as pills, patch, ring).
Check all prescription and nonprescription medicine labels carefully since many medications contain pain relievers/fever reducers (NSAIDs such as aspirin, ibuprofen, naproxen) that may increase your risk of bleeding. Low-dose aspirin should be continued if prescribed by your doctor for specific medical reasons such as heart attack or stroke prevention.
Pregnancy Catagory
FDA Pregnancy Category C
Pregnancy
Animal reproduction studies have not been conducted with (aminocaproic acid) . It is also not known whether (aminocaproic acid) can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. (aminocaproic acid) should be given to a pregnant woman only if clearly needed.
Lactation
It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when AMICAR (aminocaproic acid) is administered to a nursing woman.Safety and effectiveness in pediatric patients have not been established.
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