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Aminocaproic Acid; Use, Dosage, Side effects, Interactions

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

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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

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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.

References