Aminocaproic acid - Dosage, side effects, MOA ...

Aminocaproic acid stops fibrinolysis by preventing plasminogen from being converted into plasmin. In the following circumstances, it is utilised to ensure hemostasis:

  • Urinary fibrinolysis
  • Patients with uncontrolled bleeding following surgical procedures especially cardiac surgery
  • Neoplastic disorders
  • Abruptio placentae,
  • Hematologic disorders like patients with hemophilia
  • Hepatic cirrhosis, and

It may also be used (off-label) in the following conditions:

  • Patients who are on anticoagulants and bleeding due to dental procedures
  • Uncontrolled bleeding due to severe thrombocytopenia
  • Refractory bleeding associated with extracorporeal membrane oxygenation
  • Thrombolytic associated intracranial hemorrhage

Aminocaproic acid Dose in Adults

  • Aminocaproic acid dose in acute bleeding:
    • During the first hour, provide a loading dosage of 4 to 5 gms orally or intravenously, followed by a maintenance dose of 1 gm/hour for the next 8 hours (or 1.25 g/hour for oral solution), or until bleeding is under control. The highest dose that is suggested per day is 30 gms.
  • Aminocaproic acid dose in bleeding patients with severe thrombocytopenia
    • Up to 5 gms of 100 mg/kg administered intravenously during a 30- to 60-minute period. The next step is an oral or intravenous infusion of 1 to 4 gms every 4 to 8 hours, or 1 g/hour up to a daily dosage cap of 24 gms.
  • Aminocaproic acid dose in patients with uncontrolled bleeding and a congenital or acquired coagulation disorder.
    • Every four hours, 50–60 mg/kg.
  • Patients with refractory bleeding associated with extracorporeal membrane oxygenation:
    • 4 to 5 g intravenous loading dose followed by an infusion rate of 1 to 1.25 g/hour until bleeding is controlled.
  • Patients who use thrombolytics in conjunction with iatrogenic intracranial haemorrhage (plasminogen-activator, alteplase, reteplase, tenecteplase)
    • As an alternative to cryoprecipitate, provide 4 to 5 g intravenously. After administration, the fibrinogen levels should be assessed. In cases when fibrinogen levels are fewer than 150 mg/dL, cryoprecipitate should be administered.
  • In order to stop bleeding during dental procedures in individuals receiving anticoagulant therapy:
    • Oral rinse: Spit out the solution after holding 4 g/10 mL of it in your mouth for 2 minutes. After the operation, repeat every six hours for two days.
  • For the purpose of preventing post-cardiac surgery perioperative bleeding:
    • a loading dose of 75 to 150 mg/kg intravenously, followed by an intravenous infusion of 10 to 15 mg/kg/hour Or
    • A loading dosage of 10 grammes followed by 2 grammes every hour throughout surgery, or a loading dose of 10 grammes spread out over 20 to 30 minutes before to the incision, 10 grammes following heparin administration, and finally 10 grammes after cardiopulmonary bypass is stopped.
  • Subarachnoid hemorrhage:
    • A Loading dose of 4 gms intravenous followed by 1 gm/hour infusion for up to 72 hours after the onset of subarachnoid hemorrhage.

Aminocaproic acid Dose in Childrens

  • Control of bleeding in hemophilic patients:
    • 50-100 mg/kg/dose four times a day to a maximum of 24 gms per day.
  • Control of bleeding in patients with a platelets disorder:
    • 50-100 mg/kg/dose four times a day orally or intravenous to a maximum of 24 gms/day.
  • Refractory gross hematuria:
    • 100 mg/kg/dose four times a day for 2 days beyond the resolution of hematuria in children aged 11 years or more.
  • Preventing bleeding in persons with haemophilia (related to dental procedures): 
    • In conjunction with desmopressin or factor VIII replacement therapy for up to seven days or until recovery is complete, 50-100 mg/kg/dose orally four times a day.
  • Extracorporeal membrane oxygenation (ECMO)-associated high-risk patients' bleeding control: 
    • Prior to cannulation, 100 mg/kg intravenously followed by 25–30 mg/kg/hour for a maximum of 72 hours. During aminocaproic acid treatment, the goal active clotting time (ACT) should fall between 180 and 200 seconds.

Pregnancy Risk Factor C

  • Aminocaproic acids have not been used in pregnancy.

Aminocaproic acid use during breastfeeding:

  • It is unknown if the drug can be absorbed into breastmilk. It should not be used by nursing women.  

Aminocaproic acid Dose in Renal Disease:

  • Patients with decreased renal function may have aminocaproic acid accumulation.
  • It would make sense to start with a lower loading dosage and then continue at a maintenance continuous infusion rate of 5 mg/kg/hour. 2008, Gravlee

Aminocaproic acid Dose in Liver Disease:

  •  The manufacturer does not recommend any dose adjustment in liver disease.

Side Effects of Aminocaproic Acid:

  • Neuromuscular & skeletal:
    • Myalgia
    • Myositis
    • Rhabdomyolysis
  • Cardiovascular:
    • Bradycardia
    • Edema
    • Syncope
    • Low blood pressure
    • Raised intracranial pressure
    • Arrhythmias
    • Thrombosis
  • Genitourinary:
    • Dry ejaculation
  • Hematologic:
    • Agranulocytosis
    • Leukopenia
    • Thrombocytopenia.
  • Central nervous system:
    • Dizziness
    • Lethargy
    • Hallucinations
    • Seizures
    • Stroke.
    • Confusion
    • Delirium
    • Headache
  • Gastrointestinal:
    • Nausea
    • Abdominal pain & cramps
    • Diarrhea
    • Vomiting
  • Dermatologic:
    • Rash
    • Pruritus
  • Local:
    • Injection site pain & necrosis
  • Ophthalmic:
    • Watery eyes
    • Reduced vision.
  • Otic:
    • Tinnitus
  • Renal:
    • Increased BUN
    • Acute renal failure.
    • Myoglobinuria
  • Respiratory:
    • Shortness of breath
    • Pulmonary embolism.
    • Nasal congestion
  • Miscellaneous:
    • Allergic reactions
    • Anaphylaxis
  • Rare case reports include myocardial infarction and hyperkalemia

Contraindication to Aminocaproic Acid Include:

  • DIAC (Disseminated intravascular Cocoagulation)
  • Active intravascular thrombosis

Warnings and Precautions

  • Occlusion of the intrarenal:
    • There may be clot formation and glossular capillarythrombosis. Aminocaproic acid should not be recommended for patients with hematurias of the upper urinary tract.
  • Skeletal muscle weakness
    • It has been associated with myalgias and fatigue as well as myopathy in severe cases. If CPK levels rise after therapy is initiated, it should be stopped.
    • Do not use factor IX concentrates.
    • Patients with severe renal impairment should be cautious.

Aminocaproic acid: Drug Interaction

Note: Drug Interaction Categories:

  • Risk Factor C: Monitor When Using Combination
  • Risk Factor D: Consider Treatment Modification
  • Risk Factor X: Avoid Concomitant Use

Risk Factor C (Monitor therapy).

Tretinoin (Systemic) Antifibrinolytic agents may have a greater thrombogenic effect.

Risk Factor X (Avoid Combination)

 
Complex Anti-inhibitor Coagulant (Human). Antifibrinolytic agents may increase the thrombogenic effects of Anti-inhibitor Coagulant Complex Human.
Factor IX Complex (Human). [(Factors II. IX. X)] Aminocaproic acid may intensify Factor IX Complex Human's toxic/unfavorable impact (Factors II. IX. X). Your chance of getting thrombosis may be up as a result of this combination.

Monitoring Parameters:

  • Creatine phosphokinase with long-term therapy
  • BUN, and creatinine.
  • Monitor fibrinogen
  • Fibrin split products

How to Administer Aminocaproic acid:

  • Aminocaproic acid should be given as a slow intravenous infusion over 15 - 60 minutes to avoid hypotension, bradycardia, and arrhythmia.
  • The oral formulation may be taken without regard to meals.

Mechansim of Action of Aminocaproic acid:

Aminocaproic acids compete with plasminogen for binding, preventing it from attaching to fibrin. It prevents the breakdown of fibrin, which creates a meshwork close to the site of bleeding, as well as the conversion of plasminogen into plasmin.

  • The Onset of action varies from 1 to 72 hours
  • It is minimally metabolized by the liver.
  • Oral bioavailability is close to 100%
  • Half-life elimination is around 2 hours
  • The time to peak plasma concentration is around one hour.
  • Excretion is mainly via urine.

International Brands of Aminocaproic acid:

  • Acepramin
  • Acidum e-aminocapronicum
  • AKK
  • Amicar
  • Caproamin
  • Caprolest
  • Caprolex
  • Caprolisin
  • EAC
  • Epsamon
  • Epsicaprom
  • Epsikapron
  • Epsilon
  • Kai Nai Yin
  • Minocap
  • Hamostat
  • Hexalense
  • Ipsilon
  • Inselon
  • Ipron
  • Plaslloid
  • Resplamin
  • Syrop acidi e-aminocapronici

Aminocaproic acid Brands in Pakistan:

 No brands available in Pakistan.