Aminocaproic acid how to dilute the powder. Aminocaproic acid - instructions for use

Gross formula

C 6 H 13 NO 2

Pharmacological group of the substance Aminocaproic acid

Nosological classification (ICD-10)

CAS code

60-32-2

Characteristics of the substance Aminocaproic acid

fibrinolysis inhibitor.

Colorless crystals or white crystalline powder, odorless and tasteless. Easily soluble in water, very little in methanol, practically insoluble in ethanol and chloroform. Molecular weight 131.7.

Pharmacology

pharmachologic effect- hemostatic.

Inhibits activators of profibrinolysin and inhibits its transformation into fibrinolysin. To a lesser extent, it has a direct inhibitory effect on fibrinolysin. It inhibits the activating effect of streptokinase, urokinase and tissue kinases on fibrinolysis. Neutralizes the effects of kallikrein, trypsin and hyaluronidase, reduces capillary permeability. Stimulates the formation of platelets, sensitizes platelet receptors to thrombin, thromboxane A 2 and other endogenous aggregants. It has a systemic hemostatic effect in bleeding due to increased plasma fibrinolytic activity. It has antiallergic activity, improves the antitoxic function of the liver.

It is well absorbed when taken orally, Cmax in blood plasma is determined after 1-2 hours. It is excreted by the kidneys, mainly unchanged, approximately 40-60% is excreted within 4 hours. If the excretory function of the kidneys is impaired, the excretion slows down and the concentration of aminocaproic acids in the blood. With a / in the introduction is eliminated faster: T 1/2 - 77 minutes, more than 89% is excreted in 12 hours.

Application of the substance Aminocaproic acid

Bleeding (hyperfibrinolysis, hypo- and afibrinogenemia). Bleeding surgical interventions on organs rich in fibrinolysis activators (lungs, thyroid stomach, cervix, prostate). Diseases internal organs with hemorrhagic syndrome; placental abruption, complicated abortion. To prevent secondary hypofibrinogenemia during massive transfusions of canned blood.

Contraindications

Hypersensitivity, hypercoagulable states with a tendency to thrombosis and embolism, chronic renal failure, impaired cerebral circulation, DIC, pregnancy.

Application restrictions

Arterial hypotension, valvular heart disease, hematuria, bleeding from the upper urinary tract of unknown etiology, liver failure, impaired renal function.

Use during pregnancy and lactation

Side effects of the substance Aminocaproic acid

Rhabdomyolysis, myoglobinuria, acute renal failure, subendocardial hemorrhage, nausea, diarrhea, convulsions, decreased blood pressure, orthostatic hypotension, headache, dizziness, tinnitus, nasal congestion, skin rashes.

Interaction

The effect is reduced by anticoagulants (direct, indirect), antiaggregants.

Routes of administration

I/V(drip) , inside, locally.

Substance precautions Aminocaproic acid

When prescribing aminocaproic acid, it is necessary to control the fibrinolytic activity of the blood and the content of fibrinogen.

There are reports of the inappropriate use in women to prevent increased blood loss during childbirth due to the possibility of thromboembolic complications in the postpartum period.

Aminocaproic acid

International non-proprietary name

Aminocaproic acid

Dosage form

Solution for infusion 5%

Compound

100 ml of the drug contains

active substance - aminocaproic acid 5 g,

auxiliaryse substancesa: sodium chloride 0.9 g, water for injection.

Theoretical osmolarity 689 mOsm/l

Description

Colorless transparent liquid

Pharmacotherapeutic group

Drugs that affect hematopoiesis and blood. Hemostatics. Amino acids. Aminocaproic acid

Code ATXB02AA01

Pharmacological properties

Pharmacokinetics

With intravenous administration, the action of aminocaproic acid appears after 15-20 minutes. The drug is rapidly excreted from the body mainly unchanged (about 10-15% of the administered dose is metabolized). medicinal product). With normal kidney function, 40-60% of the administered amount is excreted by the kidneys in 4 hours.

In violation of the excretory function of the kidneys, the concentration of aminocaproic acid in the blood increases significantly.

Pharmacodynamics

Aminocaproic acid inhibits the activity of proteolytic enzymes. It inhibits the activating effect of endogenous kinases on the process of fibrinolysis and disrupts the transition of plasminogen to plasmin. Partially inactivates the action of plasmin itself. It has a specific hemostatic effect in bleeding due to the activation of the fibrinolysis process. Other mechanisms are also involved in the implementation of the hemostatic effect of aminocaproic acid. So, it lowers the activity of hyaluronidase and reduces capillary permeability. Increases the adhesive activity of platelets, increases the synthetic and detoxifying functions of the liver. Inhibiting the activity of proteolytic enzymes (kallikrein, trypsin, chymotrypsin, plasmin, etc.) inhibits the formation of kinins (bradykinin and kallidin).

Aminocaproic acid is used for pathological conditions when there is an increased activity of the kinin system (acute pancreatitis, extensive burns, shock, traumatic operations on parenchymal organs, etc.).

Aminocaproic acid inhibits the formation of antibodies and prevents the activation of the complement system, so it is used in severe allergies to eliminate or prevent the phenomena of cytolysis and the formation of immune complexes.

The drug has low toxicity.

Indications for use

Bleeding (hyperfibrinolysis, hypo- and afibrinogenemia): bleeding during surgical interventions and pathological conditions, accompanied by an increase in fibrinolytic activity of the blood (during neurosurgical, intracavitary, thoracic, gynecological and urological operations, including those on the pancreas and prostate gland, lungs; tonsillectomy , after dental interventions, during operations using a heart-lung machine)

Diseases of the internal organs with hemorrhagic syndrome - premature detachment of the placenta, complicated abortion

hypoplastic anemia

Prevention of secondary hypofibrinogenemia in massive transfusions of canned blood

burn disease

Dosage and administration

Intravenously, drip.

Adults the drug is administered intravenously at a rate of 50-60 drops per minute, at the rate of 1 ml of a 5% solution of aminocaproic acid per 1 kg of the patient's weight. During the first hour, it is recommended to inject 80-100 ml (4-5 g), then, if necessary, 20 ml (1 g) every hour until the bleeding stops completely, but not more than 8 hours. In case of ongoing or repeated bleeding, the infusion of a 5% solution of aminocaproic acid is repeated after 4 hours. The maximum daily dose for adults is 600 ml (30 g).

children older than 1 year a solution of aminocaproic acid 5% is administered intravenously in a dose of 100 mg/kg in the first hour, then 33 mg/kg/hour, the maximum daily dose is 18 g/m2.

With a moderate increase in fibrinolytic activity:

Children's age

Daily dose

1 to 2 years

60 ml (3.0 g)

60 - 120 ml (3-6 g)

120-180 ml (6-9 g)

At acute blood loss:

Children's age

Daily dose

1 to 2 years

120-180 ml (6-9 g)

180-240 ml (9-12 g)

360 ml (18 g)

In acute fibrinolysis, it is additionally necessary to introduce fibrinogen in an average daily dose of 2-4 g (maximum dose 8 g).

The duration of the use of aminocaproic acid depends on clinical picture diseases.

Side effects

- general: headache, weakness

- allergic reactions : allergic and anaphylactoid reactions, anaphylactic shock

- local reactions: injection site reactions, pain and necrosis

- from the side of cardio-vascular system: bradycardia, arterial hypotension, orthostatic hypotension, peripheral ischemia, thrombosis, arrhythmias

- from the gastrointestinal tract: stomach ache, diarrhea, nausea, vomiting

- hematological: agranulocytosis, coagulation disorders, leukopenia, thrombocytopenia

- from the musculoskeletal system: an increase in creatine phosphokinase,

muscle weakness, myalgia, myopathy, myositis, rhabdomyolysis, convulsions

- from the nervous system: confusion, delirium, dizziness, hallucinations, intracranial hypertension, stroke, fainting

- from the side respiratory system: dyspnea, nasal congestion, thromboembolism pulmonary artery, catarrhal phenomena of the upper respiratory tract

- from the side of the skin: itching, rash

- from the sense organs: tinnitus, hearing loss, vision loss, lacrimation

- from the genitourinary system: an increase in the level of urea in the blood serum, renal failure.

Contraindications

Individual intolerance

Hypercoagulability (thrombosis, thromboembolism)

Tendency to thrombosis and thromboembolic diseases

Coagulopathy due to diffuse intravascular coagulation

Acute disorders of the coronary circulation

DIC

Kidney disease with impaired excretory function

Hematuria

Cerebral circulation disorders

Bleeding from the upper urinary system of unknown etiology

Pregnancy, lactation

Children's age up to 1 year

Drug Interactions

It can be combined with the introduction of hydrolysates, glucose solutions, anti-shock solutions.

Anticoagulants of direct and indirect action, antiplatelet agents reduce the effectiveness of aminocaproic acid.

special instructions

The drug should not be prescribed without a definite diagnosis and / or laboratory confirmation of hyperfibrinolysis.

When used, it is necessary to control the content of fibrinogen, fibrinolytic activity and blood clotting time. It is necessary to control the coagulogram, especially when coronary disease heart, after myocardial infarction, with pathological processes in the liver.

During long-term therapy, the level of serum creatine phosphokinase (CPK) should be monitored; if an increase in CPK is detected, the use of the drug should be discontinued.

Use with caution in diseases of the heart and kidneys (due to the risk of developing acute renal failure).

Use with caution in arterial hypotension, valvular heart disease, liver failure, chronic renal failure, children and adolescence up to 18 years old.

Do not use for bleeding from the upper urinary system due to the risk of intrarenal obstruction in the form of glomerular capillary thrombosis.

Avoid fast intravenous administration drug, as it may cause hypotension, bradycardia, and/or arrhythmia.

Pregnancy and lactation

Use during pregnancy is contraindicated. For the period of use of the drug should stop breastfeeding.

28.03.2019

A solution of aminocaproic acid is classified as a hemostatic and antihemorrhagic agent. The use of aminocaproic acid is recommended to stop bleeding, with an increase in fibrolysis (the process of thinning blood clots).

How to use this solution, can a child drink it? The instructions below will help you figure this out.

Pharmacological actions

The instruction says that a solution of aminocaproic acid can reduce capillary permeability, in addition, its use can increase the antitoxic ability of the liver. If you use the remedy inside, then it shows anti-allergic and anti-shock activity.

The use of the tool provides an improvement in a number of indicators that are responsible for non-specific and specific protection in ARVI.

The limiting value of the concentration of such a solution can be observed approximately three hours after its ingestion. In most cases, the excretion of aminocaproic acid is carried out through the kidneys without any changes, only 10-15% undergoes biotransformation in the liver. Accumulation in the body of the drug occurs in case of dysfunction of the excretory system.

Indications for use

A solution of aminocaproic acid is used as a means to prevent various bleeding:
Hypo- and afibrinogenemia (blood clotting problems);
Bleeding resulting from surgical operations on organs in which there is an increased amount of fibrinolysis activators (lungs, thyroid gland, cervix, stomach, prostate gland).

Such an oral solution is used to treat many who have general symptoms, namely an increased tendency to bleed. In gynecology, aminocaproic acid solution is recommended for use in case of placental abruption or during abortions that have complications.

Method of application and dosage

Aminocaproic acid is used in the nose (for irrigation) or inside (via a dropper). In some cases, the solution can be drunk. The dosage of the drug for adults depends on the specific situation. In acute bleeding, intravenous administration of the drug 4-5 grams (previously diluted in 250 milliliters of 0.9% sodium chloride solution) is necessary drip for one hour.

During maintenance therapy, 1 gram of the agent, dissolved in 50 milliliters of sodium chloride solution, should be administered every 60 minutes until the bleeding can be stopped.

The instructions for this drug say that when taken orally, the remedy should be washed down with sweet water. With this method of use, the dosage should be as follows: the first dose is five grams, then for eight hours (until there is a complete cessation of bleeding) 1 gram every hour. The maximum daily dose of the drug is 24 grams.

If aminocaproic liquid is used or for other cases, it is recommended to pre-cool it. With its help, either the bleeding area is irrigated, or a bandage (napkin) moistened with a solution is applied over it. It is recommended to take a 5% solution. If the next reception is missed, then it must be carried out as soon as you remember. A new reception is carried out after a while.

With extreme caution, aminocaproic acid is recommended for use in violation of the circulatory process in the brain. As a preventive measure for increased blood loss during childbirth, such a drug cannot be used; thromboembolic complications may occur in the postpartum period.

Aminocaproic acid for nose

Aminocaproic acid in the nose is used as a preventive measure for influenza. This is primarily due to the ability of the drug to strengthen blood vessels in the sinuses, reduce the likelihood of bleeding and increase blood clotting. The appointment of instillation of such a drug into the nose is based on its antiallergic effect, inhalations with aminocaproic acid can be used.

This method of application allows you to reduce the number of discharges from the nose, breaking any connection of the body with viruses. In this case, the dosage should be as follows: 2-4 drops of aminocaproic acid should be instilled into each sinus once a day for preventive purposes and every 3 hours (for treatment purposes).

The use of aminocaproic acid in the nose during the period of bearing a child is not contraindicated, but in this case it is recommended to consult a doctor first.

Aminocaproic acid for children

Aminocaproic acid for children can effectively cope with swelling of the nasal sinuses and mucous membranes, which distinguishes it from many drugs that have a vasoconstrictive effect.

Experts recommend using aminocaproic acid for children with a runny nose. This drug has an antiviral effect, its use is quite effective in the treatment of adenoviruses, SARS and influenza.

It can prevent the reproduction of harmful organisms, while preventing others from entering through the upper respiratory tract.

As a preventive measure viral diseases, write out instillation of aminocaproic acid into the nose of children 3-5 times a day. In this case, the duration of the course is a week. In the case of a moderate increase in fibrinolytic activity - an unexpected dissolution of blood clots in children, aminocaproic acid (5%) is recommended to be taken orally.

Contraindications for use

In some cases, the use of such medicinal product is invalid. Aminocaproic acid can not be used in such diseases:

Pregnancy and while breastfeeding;
Violation of the blood circulation of the brain;
The presence of a predisposition to embolism (blockage of blood vessels) and the formation of blood clots;
chronic;
Gross hematuria (manifestation in the urine of blood);
Syndrome of disseminated coagulation within the vessels.

It is necessary to limit the use of such a drug for diseases such as:
Liver failure;
Arterial hypotension (prolonged decrease blood pressure);
valvular heart defects;
Bleeding from the upper parts of the excretory system, the causes of which could not be established.

Side effects

Aminocaproic acid can cause a number of side effects. Among the most frequently encountered are:

convulsions;
and arrhythmia;
subendocardial hemorrhage;
Rash on skin;
Pain in the head, accompanied by dizziness, tinnitus;
Disorder of the functions of the gastrointestinal tract (diarrhea);
Inflammatory processes mucous membrane of the upper respiratory tract;
Orthostatic (sudden decrease in pressure leading to a decrease in cerebral blood supply and fainting).

To reduce the action of aminocaproic acid, antiplatelet agents or anticoagulants are used. The former are responsible for reducing the occurrence of blood clots, which occurs due to inhibition of platelet aggregation.

The latter prevent the formation of fibrin, preventing the appearance of blood clots.

Aminocaproic acid is an excellent tool that eliminates all kinds of bleeding in children and adults. It can be used for both outdoor and internal use. It is especially effective for children in the treatment of diseases of the upper respiratory tract.

Before starting the use of aminocaproic acid, it is recommended to consult with your doctor.

Aminocaproic acid is a drug that belongs to the group of hemostatics.

In other words, the use of this pharmacological drug increases blood clotting. That is, aminocaproic acid remarkably stops bleeding.

Scientifically speaking, this medicine makes the process of dissolving blood clots (fibrinolysis) much slower.

However, aminocaproic acid is pharmacological drug wide spectrum of activity. In addition to the hemostatic effect, when instilled into the nose, it has a decongestant and anti-allergic effect on human body. In addition, when instilled into the nose, this medicine significantly reduces the amount of mucous secretions in various rhinitis (runny nose), as well as flu and colds.

According to the instructions for use of Aminocaproic Acid, it should be stored in a place protected from direct sunlight and out of the reach of children. The proper storage temperature is between 2 and 25 degrees Celsius. Subject to these requirements, the manufacturer declared a guaranteed shelf life of the drug equal to 3 years from the date indicated on the package.

Price

Aminocaproic acid is a democratic and affordable drug for the widest segments of the population. Currently, its price ranges from 28 to 70 rubles per pack.

Indications for use

In accordance with the instructions for the use of aminocaproic acid, indications for its use are bleeding in pathological conditions and surgical interventions of various etiologies (origin). For example, it can be bleeding:

  • during abdominal operations;
  • in dental treatment;
  • with hemorrhagic syndrome;
  • with blood transfusions;
  • with complex abortions;
  • and others.
  • during the preventive measures during epidemics of acute respiratory viral infections and acute respiratory infections;
  • for use with complex treatment colds and flu;
  • in the treatment of adenoids in children and adults;
  • in the treatment of the common cold.

Aminocaproic acid with a cold and other cases listed above is instilled directly into the nose.

It can also be used in cases where the patient has observed.

Release forms

Aminocaproic acid is currently available in three forms:

  • solution for infusion (5%);
  • tablets;
  • powder.

Depending on the form of release of the drug and the existing problem, it can be taken in different ways:

  • intravenously (dropper);
  • orally (swallowed through the mouth);
  • intranasally (buried in the nose);
  • carrying out inhalations.

The tablet form of aminocaproic acid is taken with chronic diseases and pathological conditions that do not pose an immediate threat to the life of the patient. The medicine should be taken three times a day one hour before meals, 1 tablet.

Dosages for intravenous administration of the drug are determined by the attending physician, depending on the existing problematic pathological condition.

Use for instillation into the nose for a cold and flu

When taking prophylactic aminocaproic acid, 1-2 drops of medication should be instilled into each nostril of the nose 4-5 times a day.

When treating an existing disease, children under 16 years of age should instill 2-3 drops of medication into each nasal passage 3-4 times a day. For adults in a similar situation, instill 3-4 drops of the drug in each nasal passage 6-8 times a day.

Contraindications, overdose and side effects

In accordance with the instructions for the use of Aminocaproic acid, its intake is limited to the following contraindications:

  • individual intolerance;
  • hypercoagulation (increased blood clotting);
  • other problems with blood clotting;
  • violation of the blood circulation of the brain;
  • kidney disease.

An overdose of the drug is possible. As a rule, it manifests itself in the onset of side effects. At the first symptoms of an overdose of aminocaproic acid, it is necessary to stop taking it and consult a doctor.

Side effects are:

  • dizziness and headaches;
  • nasal congestion;
  • nausea, diarrhea and vomiting;
  • lowering blood pressure;
  • kidney failure;
  • skin rash;
  • convulsions;
  • myoglobinuria;
  • rhabdomyolysis.

Efficiency and reviews

Aminocaproic acid has good feedback doctors and their patients. This applies to both its main hemostatic properties and additional uses.

For example, in the treatment of adenoids in children, aminocaproic acid has proven itself well. The same applies to the prevention and treatment of the common cold and colds.

However, considering a large number of side effects from taking it, the choice of this drug should definitely be entrusted to the attending physician. It is not necessary to rely solely on comments read somewhere in such a serious matter.

If you have already used Aminocaproic Acid, please leave a review about the effectiveness of the drug.

During pregnancy and lactation

Aminocaproic acid is prohibited for women who are pregnant or breastfeeding.

Analogues

Aminocaproic acid as a remedy for bleeding has the following analogues:

  • Traneksam;
  • Aprotinin;
  • Ingitril;
  • Trenax.
  • 1 ml 5% solution for infusion drugs Aminocaproic acid contains 50 mg active substance entitled ε(epsilon)-aminocaproic acid. Additional substances: water, sodium chloride.
  • 1 gram aminocaproic acid drug powder contains 1 gram of the active substance called ε(epsilon)-aminocaproic acid .

Release form

Clear liquid without color:

  • 100 ml of liquid in a bottle; 1, 10, 15, 24, 28, 30, 35, 48 or 36 bottles in a carton.
  • 200 ml of liquid in a bottle; 1 or 28 bottles in a carton.
  • 250 ml, 100 ml, 500 ml or 1000 ml of liquid in a polymer container; one container in a plastic bag.
  • 100 ml of liquid in a polymer container; 50 or 75 containers in a plastic bag.
  • 250 ml of liquid in a polymer container; 24 or 36 containers in a plastic bag.
  • 500 ml of liquid in a polymer container; 12 or 18 containers in a plastic bag.
  • 1000 ml of liquid in a polymer container; 6 or 9 containers in a plastic bag.

Odorless white powder:

  • 1 gram of powder in a bag, ten bags in a cardboard box.

pharmachologic effect

hemostatic action.

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

Hemostatic drug, fibrinolysis blocker .

The chemical formula is H2N(CH2)5COOH.

Blocks the effects of activators plasminogen , suppresses the action plasmin , does not completely inhibit kinins . It has anti-allergic activity and slightly enhances the anti-toxic function of the liver.

Pharmacokinetics

After oral administration, it is actively absorbed from the digestive tract. The highest concentration is reached after two hours. Rapidly excreted in the urine, mostly unchanged. The half-life is approximately 2 hours.

Indications for use

The use of the drug is justified in the following conditions and situations:

  • prevention of bleeding during interventions on the liver, pancreas, lungs;
  • prevention and treatment menorrhagia and bleeding from internal organs, mucous membranes, erosions of the stomach and intestines, as well as during menstruation;
  • hyperfibrinolysis various genesis, including those associated with the use thrombolytic drugs and transfusion of canned blood products in large volumes;
  • treatment and prevention and;
  • for the symptomatic treatment of bleeding caused by thrombocytopenia and inferiority of function.

Contraindications

  • Hypersensitivity to the components of the drug.
  • Hematuria.
  • Hypercoagulation, coagulopathy due to diffusion intravascular disseminated coagulation , predisposition to or thromboembolic diseases .
  • Kidney disease with impaired excretory function.
  • Cerebral circulation disorders.
  • or .

It is recommended to use the drug with caution in valvular heart disease, arterial hypotension, hematuria, cryptogenic bleeding from the upper urinary tract, liver failure, chronic insufficiency kidney function, less than a year old.

Side effects

Intranasal instillation of aminocaproic acid up to four times a day is advisable to carry out during the epidemic period for prevention.

The duration of therapy depends on the severity of the disease and is determined individually by the doctor.

Overdose

Signs of overdose: increased adverse events, the appearance blood clots . With prolonged use (over 6 days) of large doses (from 24 grams per day for adults), the development of hemorrhage .

Overdose treatment: drug withdrawal, symptomatic therapy.

Interaction

The drug can be combined with the use glucose solutions, hydrolysates, anti-shock solutions.

Other drugs should not be added to the solution of the drug.

Terms of sale

Without recipe.

Storage conditions

Store in a dark dry place at a temperature of 2-25°C. Keep away from children.

Best before date

special instructions

When using the drug, it is recommended to measure the indicators of fibrinolytic activity and the content fibrinogen in blood. With intravenous administration, it is recommended to carry out, especially after, with coronary disease and liver diseases.

Analogues

Coincidence in the ATX code of the 4th level:

Polycapran.

children

The use of the drug is allowed for children for inhalation, instillation, oral and intravenous administration in the above dosages.

During pregnancy and lactation

The drug is prohibited for use in pregnant and lactating women, as well as during childbirth.