Aminocaproic

Name: Aminocaproic

Aminocaproic Acid Tablets USP 500 mg, 1000 mg and Oral Solution 0.25 g/mL

Rx only

Aminocaproic - Clinical Pharmacology

The fibrinolysis-inhibitory effects of Aminocaproic acid appear to be exerted principally via inhibition of plasminogen activators and to a lesser degree through antiplasmin activity.

In adults, oral absorption appears to be a zero-order process with an absorption rate of 5.2 g/hr. The mean lag time in absorption is 10 minutes. After a single oral dose of 5 g, absorption was complete (F=1). Mean ± SD peak plasma concentrations (164 ± 28 mcg/mL) were reached within 1.2 ± 0.45 hours.

After oral administration, the apparent volume of distribution was estimated to be 23.1 ± 6.6 L (mean ± SD). Correspondingly, the volume of distribution after intravenous administration has been reported to be 30.0 ± 8.2 L. After prolonged administration, Aminocaproic acid has been found to distribute throughout extravascular and intravascular compartments of the body, penetrating human red blood cells as well as other tissue cells.

Renal excretion is the primary route of elimination. Sixty five percent of the dose is recovered in the urine as unchanged drug and 11% of the dose appears as the metabolite adipic acid. Renal clearance (116 mL/min) approximates endogenous creatinine clearance. The total body clearance is 169 mL/min. The terminal elimination half-life for Aminocaproic acid is approximately 2 hours.

Adverse Reactions

Aminocaproic acid is generally well tolerated. The following adverse experiences have been reported:

General: Edema, headache, malaise.

Hypersensitivity Reactions: Allergic and anaphylactoid reactions, anaphylaxis.

Cardiovascular: Bradycardia, hypotension, peripheral ischemia, thrombosis.

Gastrointestinal: Abdominal pain, diarrhea, nausea, vomiting.

Hematologic: Agranulocytosis, coagulation disorder, leukopenia, thrombocytopenia.

Musculoskeletal: CPK increased, muscle weakness, myalgia, myopathy (see WARNINGS), myositis, rhabdomyolysis.

Neurologic: Confusion, convulsions, delirium, dizziness, hallucinations, intracranial hypertension, stroke, syncope.

Respiratory: Dyspnea, nasal congestion, pulmonary embolism.

Skin: Pruritis, rash.

Special Senses: Tinnitus, vision decreased, watery eyes.

Urogenital: BUN increased, renal failure. There have been some reports of dry ejaculation during the period of Aminocaproic acid treatment. These have been reported to date only in hemophilia patients who received the drug after undergoing dental surgical procedures. However, this symptom resolved in all patients within 24 to 48 hours of completion of therapy.

OVERDOSAGE

A few cases of acute overdosage with Aminocaproic acid administered intravenously have been reported. The effects have ranged from no reaction to transient hypotension to severe acute renal failure leading to death. One patient with a history of brain tumor and seizures experienced seizures after receiving an 8 gram bolus injection of Aminocaproic acid. The single dose of Aminocaproic acid causing symptoms of overdosage or considered to be life-threatening is unknown. Patients have tolerated doses as high as 100 grams while acute renal failure has been reported following a dose of 12 grams.

The intravenous and oral LD50 of Aminocaproic acid were 3.0 and 12.0 g/kg respectively in the mouse and 3.2 and 16.4 g/kg respectively in the rat. An intravenous infusion dose of 2.3 g/kg was lethal in the dog. On intravenous administration, tonic-clonic convulsions were observed in dogs and mice.

No treatment for overdosage is known, although evidence exists that Aminocaproic acid is removed by hemodialysis and may be removed by peritoneal dialysis. Pharmacokinetic studies have shown that total body clearance of Aminocaproic acid is markedly decreased in patients with severe renal failure.

Aminocaproic Dosage and Administration

An identical dosage regimen may be followed by administering Aminocaproic acid tablets or Aminocaproic acid oral solution as follows:

For the treatment of acute bleeding syndromes due to elevated fibrinolytic activity, it is suggested that 5 Aminocaproic acid 1000 mg tablets or 10 Aminocaproic acid 500 mg tablets (5 g) or 20 milliliters of Aminocaproic acid oral solution (5 g) be administered during the first hour of treatment, followed by a continuing rate of 1 Aminocaproic acid 1000 mg tablet or 2 Aminocaproic acid 500 mg tablets (1 g) or 5 milliliters of Aminocaproic acid oral solution (1.25 g) per hour. This method of treatment would ordinarily be continued for about 8 hours or until the bleeding has been controlled.

For the Consumer

Applies to aminocaproic acid: oral solution, oral syrup, oral tablet

Other dosage forms:

  • intravenous solution

Along with its needed effects, aminocaproic acid may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur while taking aminocaproic acid:

Incidence not known
  • Anxiety
  • black, tarry stools
  • bleeding gums
  • blood in the urine or stools
  • blurred vision
  • change in the ability to see colors, especially blue or yellow
  • chest pain or discomfort
  • chills
  • confusion
  • cough or hoarseness
  • dark-colored urine
  • decreased frequency or amount of urine
  • difficult or labored breathing
  • difficulty with moving
  • difficulty with speaking
  • difficulty with swallowing
  • dizziness or lightheadedness
  • dizziness, faintness, or lightheadedness when getting up from a lying or sitting position suddenly
  • double vision
  • fainting
  • fast heartbeat
  • fever with or without chills
  • general feeling of discomfort or illness
  • general feeling of tiredness or weakness
  • headache
  • hives
  • inability to move the arms, legs, or facial muscles
  • inability to speak
  • increased thirst
  • itching of the skin
  • joint pain
  • loss of appetite
  • lower back or side pain
  • muscle aching or cramping
  • muscle cramps or spasms
  • muscle pain or stiffness
  • muscular pain, tenderness, wasting, or weakness
  • nausea and vomiting
  • numbness and tingling of the face, fingers, or toes
  • pain in the arms, legs, or lower back, especially pain in the calves or heels upon exertion
  • painful or difficult urination
  • pale, bluish-colored, or cold hands or feet
  • pinpoint red spots on the skin
  • problems with bleeding or clotting
  • puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue
  • shortness of breath
  • skin rash
  • slow or irregular heartbeat
  • slow speech
  • sore throat
  • sores, ulcers, or white spots on the lips or in the mouth
  • sudden shortness of breath or troubled breathing sweating
  • swelling
  • swelling of the face, fingers, or lower legs
  • swollen glands
  • swollen joints
  • tenderness, pain, swelling, warmth, skin discoloration, and prominent superficial veins over the affected area
  • tightness in the chest
  • troubled breathing
  • unusual bleeding or bruising
  • unusual tiredness or weakness
  • vomiting
  • weak or absent pulses in the legs
  • weight gain
  • wheezing

Some side effects of aminocaproic acid may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

Incidence not known
  • Abdominal or stomach pain
  • confusion as to time, place, or person
  • continuing ringing or buzzing or other unexplained noise in the ears
  • decreased vision
  • diarrhea
  • ejaculation without semen
  • hearing loss
  • holding false beliefs that cannot be changed by fact
  • mood or mental changes
  • seeing, hearing, or feeling things that are not there
  • stuffy nose
  • unusual excitement, nervousness, or restlessness
  • watery eyes

For Healthcare Professionals

Applies to aminocaproic acid: compounding powder, intravenous solution, oral syrup, oral tablet

Nervous system

Frequency not reported: Headache, convulsions, dizziness, intracranial hypertension, stroke, syncope, tinnitus[Ref]

Musculoskeletal

Frequency not reported: Creatine phosphokinase increased, muscle weakness, myalgia, myopathy, myositis, rhabdomyolysis[Ref]

Cardiovascular

Frequency not reported: Bradycardia, hypotension, peripheral ischemia, thrombosis[Ref]

Gastrointestinal

Frequency not reported: Abdominal pain, diarrhea, nausea, vomiting[Ref]

Hematologic

Frequency not reported: Agranulocytosis, coagulation disorder, leukopenia, thrombocytopenia[Ref]

Local

Frequency not reported: Injection site reactions, injection site pain, injection site necrosis[Ref]

Psychiatric

Frequency not reported: Confusion, delirium, hallucinations[Ref]

Respiratory

Frequency not reported: Dyspnea, nasal congestion, pulmonary embolism[Ref]

Dermatologic

Frequency not reported: Pruritus, rash[Ref]

Immunologic

Frequency not reported: Allergic and anaphylactic reactions, anaphylaxis[Ref]

Ocular

Frequency not reported: Vision decreased, watery eyes[Ref]

Renal

Frequency not reported: BUN increased, renal failure[Ref]

Genitourinary

Frequency not reported: Dry ejaculation[Ref]

Metabolic

Frequency not reported: Edema[Ref]

Other

Frequency not reported: Malaise[Ref]

Some side effects of aminocaproic acid may not be reported. Always consult your doctor or healthcare specialist for medical advice. You may also report side effects to the FDA.

Usual Adult Dose for 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).

Duration of therapy: Usually continued for about 8 hours or until bleeding controlled.

Use: To enhance hemostasis when fibrinolysis contributes to bleeding.

Other Comments

Administration advice: Rapid injection of undiluted drug into a vein is not recommended.

IV compatibility: Usual compatible IV vehicles may be used (e.g., sterile water for injection, sodium chloride for Injection, 5% dextrose or Ringer's injection). The resultant solution with sterile water for injection is hypo-osmolar.

Monitoring:
-Hematologic: Tests to determine the amount of fibrinolysis present.
-Musculoskeletal: Creatine phosphokinase (CPK) levels in patients taking this drug long-term.

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