Aminocaproic acid, also known as ε-aminocaproic acid (EACA), is a medication primarily used to treat excessive bleeding. It works by inhibiting the activity of plasminogen activators, enzymes that are involved in the breakdown of blood clots. By inhibiting these enzymes, aminocaproic acid helps to stabilize blood clots and reduce bleeding.

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:

• Give the aminocaproic acid through the mouth or into their veins.
• At first, they might get a big dose of 4 to 5 grams in the first hour, and then a smaller dose of 1 gram every hour for 8 hours.
• If needed, they might get more until the bleeding stops, but not more than 30 grams in one day.

Aminocaproic acid dose in bleeding patients with severe thrombocytopenia

• Give aminocaproic acid through the veins initially, with a dose of up to 100 milligrams per kilogram of body weight, but not more than 5 grams, over 30 to 60 minutes.
• After that, they might continue with oral or intravenous doses of 1 to 4 grams every 4 to 8 hours, or at a rate of 1 gram per hour.
• However, the total amount in a day should not exceed 24 grams.
• More research is needed to fully understand how aminocaproic acid works for this condition.

Aminocaproic acid dose in patients with uncontrolled bleeding and a congenital or acquired coagulation disorder.

• Aminocaproic acid can be given orally at a dose of 50 to 60 milligrams per kilogram of body weight every 4 hours.
• This medication might help control the bleeding, but more information is needed to fully understand how well it works for this condition.

Aminocaproic acid Patients with refractory bleeding associated with extracorporeal membrane oxygenation:

• Aminocaproic acid can be given intravenously.
• Initially, a loading dose of 4 to 5 grams is administered, followed by a continuous infusion of 1 to 1.25 grams per hour until the bleeding is under control.
• However, it's important to note that using aminocaproic acid for this purpose is not officially approved, so more research is needed to fully understand its effectiveness and safety in this specific situation.

Aminocaproic acid Patients who use thrombolytics in conjunction with iatrogenic intracranial haemorrhage (plasminogen-activator, alteplase, reteplase, tenecteplase)

• Aminocaproic acid can be given intravenously at a dose of 4 to 5 grams.
• This is used as an alternative to cryoprecipitate.
• After giving aminocaproic acid, doctors should check fibrinogen levels.
• If fibrinogen levels drop below 150 milligrams per deciliter, it's recommended to use cryoprecipitate instead.
• It's important to remember that this use of aminocaproic acid isn't officially approved, so further research is needed to confirm its effectiveness and safety in this situation.

Aminocaproic acid in order to stop bleeding during dental procedures in individuals receiving anticoagulant therapy:

• It's administered as an oral rinse, holding 4 grams of aminocaproic acid mixed with 10 milliliters of water in the mouth for 2 minutes, then spitting it out.
• This process is repeated every 6 hours for 2 days following the procedure.
• It's worth noting that the concentration and frequency of administration might differ depending on the institution and product availability.
• Further research is necessary to fully understand the effectiveness and safety of aminocaproic acid for this purpose.

Aminocaproic acid for the purpose of preventing post-cardiac surgery perioperative bleeding:

• Loading Dose: Typically ranges from 75 to 150 milligrams per kilogram of body weight (approximately 5 to 10 grams), administered intravenously. Alternatively, a loading dose of 10 grams may be given prior to surgery.
• Maintenance Dose: After the loading dose, a maintenance infusion is often started at a rate of 10 to 15 milligrams per kilogram per hour (approximately 1 gram per hour).
• Additional Administration: In some cases, aminocaproic acid may be added to the cardiopulmonary bypass circuit priming solution, usually at a concentration of 2 to 2.5 grams per liter. Alternatively, it may be given as additional doses during surgery or at specific times during the procedure, such as before skin incision, after heparin administration, or at discontinuation of cardiopulmonary bypass.

These dosing regimens are aimed at reducing perioperative bleeding associated with cardiac surgery. However, it's important to note that these uses of aminocaproic acid are off-label, meaning they are not officially approved by regulatory agencies for this specific purpose.

Aminocaproic acid Subarachnoid hemorrhage:

• The typical dosing regimen involves an initial intravenous (IV) loading dose of 4 grams, followed by a continuous infusion of 1 gram per hour for up to 72 hours after the onset of SAH.
• However, it's important to discontinue the infusion 4 hours before angiography or 2 hours before endovascular treatment of an aneurysm to minimize the risk of complications.
• It's crucial to note that further research is needed to fully understand the effectiveness and safety of aminocaproic acid in treating SAH.

Aminocaproic acid Traumatic hyphema (off-label use):

• The typical dose is oral administration of 50 milligrams per kilogram of body weight every 4 hours.
• The maximum daily dose should not exceed 30 grams.
• This regimen is usually continued for a duration of 5 days.

Aminocaproic acid Dose in Children

Aminocaproic acid Control of bleeding in hemophilic patients:

In infants, children, and adolescents:

• The typical oral dose ranges from 50 to 100 milligrams per kilogram of body weight per dose, given every 6 hours.
• The maximum daily dose should not exceed 24 grams.

Aminocaproic acid Control of bleeding in patients with a platelets disorder:

In infants, children, and adolescents, aminocaproic acid can be used with caution.

• The typical dose, based on limited data available, is 50 to 100 milligrams per kilogram of body weight per dose, administered orally or intravenously every 6 hours.
• The maximum daily dose should not exceed 24 grams.

Aminocaproic acid Refractory gross hematuria:

In children aged 11 years and older and adolescents, aminocaproic acid can be considered based on limited data available.

• The recommended dose is 100 milligrams per kilogram of body weight per dose, given orally every 6 hours.
• Treatment should be continued for 2 days beyond the resolution of hematuria.
• This dosing regimen is based on a small case series involving four patients, which showed resolution of hematuria within 2 to 7 days.

Aminocaproic acid Preventing bleeding in persons with haemophilia (related to dental procedures): 

In infants, children, and adolescents:

• The dose typically ranges from 50 to 100 milligrams per kilogram of body weight per dose, given orally every 6 hours.
• The maximum daily dose should not exceed 24 grams.
• This medication is usually used alongside desmopressin (DDAVP) or factor replacement therapy.
• Treatment can be continued for up to 7 days or until mucosal healing is complete.

Aminocaproic acid Extracorporeal membrane oxygenation (ECMO)-associated high-risk patients' bleeding control: 

In infants, children, and adolescents:

• The typical intravenous dose is 100 milligrams per kilogram prior to or immediately after cannulation, followed by a continuous infusion of 25 to 30 milligrams per kilogram per hour for up to 72 hours.
• During therapy, a target activated clotting time (ACT) range of 180 to 200 seconds has been used.
• However, it's important to note that results may vary, and the most benefit seems to be observed in patients requiring surgery just prior to or while on ECMO.

Aminocaproic acid dose in Prevention of perioperative bleeding associated with cardiac surgery: Limited data available:

For infants and children under 2 years old:

• IV administration with variable dosing regimens.
• In one trial, a dose of 75 milligrams per kilogram was given at the beginning and end of cardiopulmonary bypass (CPB), and 75 milligrams per 100 milliliters was added to the CPB priming fluid.
• In another trial, a dose of 100 milligrams per kilogram was administered after induction, during CPB pump priming, and when weaning CPB, given over 3 hours for a total of three doses.

For children 2 years old and older, as well as adolescents:

• IV administration with a consistent regimen used in two separate trials involving a total of 110 participants aged 2 months to 14 years.
• A dose of 100 milligrams per kilogram was given after induction, during CPB pump priming, and when weaning CPB, administered over 3 hours for a total of three doses.

These dosing regimens aim to reduce perioperative bleeding during cardiac surgery, but since data is limited, caution should be exercised.

Aminocaproic acid dose in Prevention of perioperative bleeding associated with spinal surgery (eg, idiopathic scoliosis): Limited data available:

For children aged 11 years and older, as well as adolescents:

• IV administration: A loading dose of 100 milligrams per kilogram (with a maximum dose of 5 grams) is administered over 15-20 minutes after induction of anesthesia.
• This is followed by a continuous IV infusion of 10 milligrams per kilogram per hour for the remainder of the surgery.
• The infusion is discontinued at the time of wound closure.

This dosing regimen aims to reduce perioperative bleeding during spinal surgery, but since data is limited, caution should be exercised.

Aminocaproic acid dose in Traumatic hyphema: Limited data available:

In infants, children, and adolescents:

• The typical oral dose ranges from 50 to 100 milligrams per kilogram of body weight per dose, administered every 4 hours for a duration of 5 days.
• The maximum daily dose should not exceed 30 grams.

Pregnancy Risk Factor C

• There haven't been any studies done on animals to see how this medicine might affect pregnancy.
•  So, it's hard to know if it's safe to use when someone is pregnant.

Aminocaproic acid use during breastfeeding:

• It's uncertain whether aminocaproic acid passes into breast milk.
• Because of this, the manufacturer advises caution when giving aminocaproic acid to breastfeeding mothers.
• This means doctors should be careful when deciding whether to prescribe it to nursing women.

Aminocaproic acid Dose in Renal Disease:

• In patients with decreased kidney function, aminocaproic acid may build up in the body over time.
• For individuals who don't have functioning kidneys (anephric patients) and are undergoing cardiopulmonary bypass, it's recommended to use a normal or slightly reduced initial dose, followed by a continuous infusion at a rate of 5 milligrams per kilogram per hour.
• This adjusted dosing strategy helps to minimize the risk of aminocaproic acid accumulating to harmful levels in the body.

Aminocaproic acid Dose in Liver Disease:

• The manufacturer's instructions do not specify any dosage adjustments for individuals with liver problems.

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:

• Disseminated intravascular coagulation (DIC) is when your blood starts to clot too much in your blood vessels.
• If you have DIC and you're not being treated with heparin, it means there's a lot of clotting happening in your blood vessels right now.
• This can be dangerous because it can lead to blockages in your blood flow and affect how your organs work.

Warnings and Precautions

Occlusion of the intrarenal:

• Sometimes, there can be blockages inside the kidneys, either because of tiny blood clots in the kidney filters (glomerular capillary thrombosis) or clots in the tubes that carry urine out of the kidneys (renal pelvis and ureters).
• In cases where there's blood in the urine coming from the upper urinary tract, like the kidneys or tubes, it's important to be cautious about using aminocaproic acid.
• It shouldn't be used unless the possible benefits are thought to be greater than the risks.
• This is because using the medication might not be safe in these situations and could potentially make things worse.

Skeletal muscle weakness

• Using aminocaproic acid for a long time can sometimes lead to weakness in your skeletal muscles.
• This can vary from feeling tired and having muscle aches to more severe muscle problems like rhabdomyolysis, where muscle breakdown can lead to kidney damage.
• To keep an eye on this, doctors will often check the levels of an enzyme called CPK in your blood.
• If these levels go up, it's a sign that your muscles might be getting damaged, and the treatment with aminocaproic acid should be stopped.

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:

• Fibrinogen and Fibrin Split Products:
  • These are substances related to blood clotting.
  • Monitoring helps understand how well blood is clotting and if there's any excessive breakdown of clots.
• Creatine Phosphokinase (CPK) with Long-Term Therapy:
  • CPK is an enzyme found in muscles.
  • Long-term use of aminocaproic acid might affect muscles.
  • Checking CPK levels helps watch for muscle damage.
• Blood Urea Nitrogen (BUN) and Creatinine:
  • These are markers of kidney function.
  • Monitoring these levels helps detect any potential kidney problems, especially with prolonged use of aminocaproic acid.

How to Administer Aminocaproic acid:

• Rapid IV Injection (IVP):
  • Avoid injecting the undiluted solution quickly into the veins.
  • Rapid injection may lead to low blood pressure, slow heart rate, and irregular heart rhythms.
• IV Administration:
  • The loading dose can be given over 15-60 minutes, depending on the specific medical condition being treated.
  • Continuous infusion might be needed for some situations where a steady level of the medication is required over time.

Mechansim of Action of Aminocaproic acid:

• Aminocaproic acid works by competing with plasminogen, a substance involved in breaking down blood clots.
• By blocking plasminogen from attaching to fibrin, a protein in blood clots, and stopping its conversion into plasmin, aminocaproic acid helps prevent the breakdown of fibrin (fibrinolysis).
• This inhibition of fibrin degradation helps stabilize blood clots and reduces bleeding.

Onset of Action:

• Begins working within approximately 1 to 72 hours after administration.

Distribution:

• Spreads widely throughout both the bloodstream and tissues.
• Volume of distribution:
  • Oral: 23 liters
  • IV: 30 liters

Metabolism:

• Mostly processed by the liver, but to a minimal extent.

Bioavailability:

• When taken orally, the entire dose is absorbed into the bloodstream (100% bioavailability).

Half-life Elimination:

• Takes about 1 to 2 hours for half of the drug to leave the body.

Time to Peak:

• After oral administration, reaches peak levels in the bloodstream in approximately 1.2 ± 0.45 hours.

Excretion:

• Primarily eliminated through the urine.
• About 65% is excreted unchanged, while around 11% is excreted as a metabolite.

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.