Active substanceAcetylsalicylic acidAcetylsalicylic acid
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  • Dosage form: & nbspenteric coated tablets
    Composition:

    One tablet contains:

    active substance: acetylsalicylic acid - 50 mg;

    Excipients: cellulose microcrystalline - 28.8 mg, pregelatinized starch - 8.5 mg, silicon dioxide colloid (aerosil) - 1.8 mg, stearic acid - 0.9 mg;

    composition of the shell: giprolase (hydroxypropylcellulose) 0.57 mg, copovidone 0.25 mg, triethyl citrate 0.918 mg, ACRYL-IZ 8.262 mg methacrylic acid and ethyl acrylate copolymer [1: 1] 66.0%, titanium dioxide E 171 - 15.0%, talc - 16.5%, silicon colloidal dioxide 1.0%, sodium bicarbonate 1.0%, sodium lauryl sulfate 0.5%.

    Description:Round, biconcave, enteric-coated tablets, with a faint smell of acetic acid; Two layers are visible on the transverse section: the shell is white or white with a yellowish tint and the core is white or almost white.
    Pharmacotherapeutic group:Antiaggregant agent
    ATX: & nbsp

    N.02.B.A   Salicylic acid and its derivatives

    Pharmacodynamics:

    Reduces aggregation, platelet adhesion and thrombus formation by suppressing the synthesis of thromboxane A2 in platelets. Antiaggregant effect persists for 7 days after a single dose (more pronounced in men than in women). Reduces the mortality and risk of myocardial infarction with unstable angina. Effective in the primary prevention of diseases of the cardiovascular system, especially myocardial infarction in men over 40, and with secondary prevention of myocardial infarction. Suppresses the synthesis of prothrombin in the liver and increases prothrombin time. Increases the fibrinolytic activity of blood plasma and reduces the concentration of vitamin-K-dependent clotting factors (II, VII, IX, X). Increases the risk of hemorrhagic complications during surgical interventions, increases the risk of bleeding during anticoagulant therapy.

    Acetylsalicylic acid in high doses can have anti-inflammatory, analgesic and antipyretic effects.

    The blockade of cyclooxygenase-1 (COX1) in the gastric mucosa leads to inhibition of gastroprotective Pg, which can cause ulceration of the mucosa and subsequent bleeding. The presence of enteric coating provides less irritant effect on the mucous membrane of the gastrointestinal tract (GIT).

    In high doses acetylsalicylic acid stimulates the excretion of uric acid (disrupts its reabsorption in the renal tubules).

    Pharmacokinetics:

    After oral administration acetylsalicylic acid absorbed in the upper part of the small intestine. The maximum concentration in blood plasma is observed on average 3 hours after taking the drug inside. Acetylsalicylic acid is partially metabolized in the liver with the formation of less active metabolites. It is excreted by the kidneys, both in unchanged form and in the form of metabolites; the half-life for acetylsalicylic acid is about 15 minutes, for metabolites - about 3 hours.

    Indications:

    Prevention of acute myocardial infarction in the presence of risk factors (eg, diabetes mellitus, hyperlipidemia, hypertension, obesity, smoking, elderly age) and repeated myocardial infarction.

    Unstable angina (including suspected development of acute myocardial infarction) and stable angina.

    Prevention of stroke (including in patients with transient impairment of cerebral circulation).

    Prevention of transient impairment of cerebral circulation.

    Prevention of thromboembolism after surgery and invasive vascular interventions (eg, coronary artery bypass grafting, carotid endarterectomy, arteriovenous shunting, carotid angioplasty).

    Prevention of deep vein thrombosis and thromboembolism of the pulmonary artery and its branches (for example, with prolonged immobilization as a result of surgical intervention).

    Contraindications:

    - Hypersensitivity to acetylsalicylic acid, excipients in the formulation, and other non-steroidal anti-inflammatory drugs (NSAIDs);

    - erosive and ulcerative lesions of the gastrointestinal tract (in the phase of exacerbation);

    - gastrointestinal bleeding;

    - hemorrhagic diathesis;

    - The bronchial asthma, induced by the intake of salicylates and other NSAIDs;

    - a combination of bronchial asthma,recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid;

    - simultaneous reception of methotrexate in a dose of 15 mg per week or more;

    - pregnancy (I and III trimester);

    - lactation period;

    - severe renal failure (creatinine clearance (CK) less than 30 ml / min);

    - severe hepatic insufficiency (class B and higher on the Child-Pugh scale);

    - chronic heart failure III-IV functional class by classification NYHA;

    - age to 18 years.

    Carefully:

    - With gout, hyperuricemia, since acetylsalicylic acid in low doses reduces the excretion of uric acid; it should be borne in mind that acetylsalicylic acid in low doses can provoke the development of gout in predisposed patients (having decreased uric acid excretion).

    - If there is an anamnesis of ulcerative gastrointestinal lesions or gastrointestinal bleeding.

    - If the liver function is impaired (below class B on the Child-Pugh scale).

    - If the kidney function is impaired (QC more than 30 ml / min).

    - With bronchial asthma, chronic diseases of the respiratory system, hay fever, polyposis of the nose, drug allergy, including other NSAIDs (analgesics, anti-inflammatory, antirheumatic drugs).

    - In the second trimester of pregnancy.

    - With the proposed surgical intervention (including minor, for example, tooth extraction), since acetylsalicylic acid may cause a tendency to develop bleeding within a few days after taking the drug.

    - In severe forms of deficiency of glucose-6-phosphate dehydrogenase (risk of hemolysis and hemolytic anemia).

    - With simultaneous use with the following medicines (see section "Interaction with other drugs"):

    - with methotrexate in a dose of less than 15 mg per week;

    - with anticoagulant, thrombolytic or antiplatelet agents;

    - with NSAIDs and salicylic acid derivatives in large doses;

    - with digoxin;

    - with hypoglycemic agents for oral administration (derivatives of sulfonylureas) and insulin;

    - with valproic acid;

    - with alcohol (alcoholic beverages in particular);

    - with selective serotonin reuptake inhibitors;

    - with ibuprofen.

    Pregnancy and lactation:

    The drug Aspinat® Cardio is contraindicated for use in the I and III trimesters of pregnancy, as it has a teratogenic effect: when applied in the first trimester of pregnancy, the fetus originates in the cleavage of the upper palate,in the third trimester - causes inhibition of labor (suppression of the synthesis of prostaglandins), premature closure of the arterial duct in the fetus, hyperplasia of the pulmonary vessels and hypertension in the small circulation. Reception of the drug in the II trimester is possible if the potential benefit to the mother exceeds the risk to the fetus.

    Salicylates and their metabolites penetrate into breast milk. For the duration of treatment, breast-feeding should be discontinued.

    Dosing and Administration:

    Inside, before eating, squeezed a lot of liquid.

    The drug is intended for long-term use. The duration of therapy is determined by the attending physician.

    Unstable angina in case of suspected development of acute myocardial infarction - 100-200 mg / day (the first tablet must be chewed for faster absorption). Prevention of the first acute acute myocardial infarction in the presence of risk factors - 50-100 mg / day.

    Prevention of repeated myocardial infarction, stable and unstable angina is 100 mg / day.

    Preventive maintenance of a stroke and transient disturbance of a cerebral circulation - 50 mg / day.

    Prevention of thromboembolic complications after surgery or invasive vascular interventions - 100 mg / day.

    Prevention of deep vein thrombosis and thromboembolism of the pulmonary artery and its branches - 100-200 mg / day.

    Side effects:

    From the digestive system: nausea, decreased appetite, heartburn, vomiting, abdominal pain, diarrhea; ulcers of the mucous membrane of the stomach and duodenum; perforated ulcers of the stomach and duodenum, gastrointestinal bleeding, transient liver dysfunction with increased activity of "liver" transaminases.

    On the part of the hematopoiesis system: thrombocytopenia, anemia, and leukopenia; increased frequency of perioperative (intra- and post-operative) bleeding, hematomas, nasal bleeding, bleeding gums, bleeding from the urogenital tract. There are reports of serious bleeding events, which include gastrointestinal bleeding and cerebral hemorrhage (especially in patients with hypertension who have not reached the target figures for blood pressure and / or are receiving concomitant therapy with anticoagulant drugs), which in some cases may be life threatening character.Bleeding can lead to the development of acute or chronic posthemorrhagic / iron deficiency anemia (for example, due to latent bleeding) with appropriate clinical and laboratory signs and symptoms (asthenia, pallor, hypoperfusion). There are reports of hemolysis and hemolytic anemia in patients with severe forms of glucose-6-phosphate dehydrogenase deficiency.

    Allergic reactions: skin rash, skin itch, urticaria, angioedema, bronchospasm, rhinitis, swelling of the nasal mucosa, cardio-respiratory distress syndrome, as well as severe reactions, including anaphylactic shock.

    From the central nervous system: dizziness, headache, hearing loss, tinnitus, which may be a sign of drug overdose (see "Overdose"),

    From the urinary system: impaired renal function and acute renal failure.

    Overdose:

    May occur after a single dose of a large dose or with prolonged use. If a single dose is less than 150 mg / kg, acute poisoning is considered easy, 150-300 mg / kg - moderate and with higher doses - heavy.

    Symptoms of an overdose from mild to moderate severity:

    dizziness, tinnitus, hearing impairment, visual impairment, increased sweating (including profuse), nausea, vomiting, headache, confusion, tachypnea, hyperventilation, respiratory alkalosis.

    Treatment: Provocation of vomiting, repeated intake of activated carbon, forced alkaline diuresis, restoration of water-electrolyte balance and acid-base state.

    Symptoms of an overdose from medium to severe:

    - respiratory alkalosis with compensatory metabolic acidosis;

    - hyperpyrexia (extremely high body temperature);

    - breathing disorders: hyperventilation, non-cardiogenic pulmonary edema, respiratory depression, asphyxia;

    - disorders of the cardiovascular system: heart rhythm disturbances, lowering of blood pressure, suppression of cardiac activity, collapse;

    - disturbance of water-electrolyte balance: dehydration, disturbance of kidney function from oliguria up to the development of renal failure, characterized by hypokalemia, hypernatremia, hyponatremia;

    - impaired glucose metabolism: hyperglycemia, hypoglycemia (especially in children), ketoacidosis;

    - noise in the ears, deafness;

    - gastrointestinal bleeding;

    - hematological disorders: from inhibition of platelet aggregation to coagulopathy, prolongation of prothrombin time, hypoprothrombinemia;

    - neurological disorders: toxic encephalopathy and depression of the central nervous system (drowsiness, confusion, coma, convulsions).

    Treatment: immediate hospitalization in specialized units for emergency therapy - gastric lavage, repeated administration of activated charcoal and laxatives alkalization urine (shown in the level of salicylates higher than 500 mg / l, provides an intravenous infusion of sodium carbonate - 88 mEq in 1 L of 5% glucose solution with rate of 10-15 ml / kg / h), the restoration of circulating blood volume and the induction of diuresis (achieved by the introduction of sodium hydrogen carbonate at the same dose and dilution was repeated 2-3 times); it should be borne in mind that intensive fluid infusion of the elderly can lead to pulmonary edema. It is not recommended to use acetosolamide for alkalinization of urine (can cause acidemia and enhance the toxic effect of salicylates). When carrying out alkaline diuresis, it is necessary to achieve pH values ​​between 7.5 and 8.Hemodialysis is indicated at a level of salicylates in the blood plasma of more than 1000 mg / l, and in patients with chronic poisoning it is 500 mg / l and lower in the presence of indications (refractory acidosis, progressive deterioration, severe central nervous system damage, pulmonary edema and kidney failure) . With pulmonary edema, artificial ventilation of the lungs with a mixture enriched with oxygen is shown in the positive pressure mode at the end of the exhalation; To treat edema of the brain, hyperventilation and osmotic diuresis are used.

    The greatest risk of developing chronic intoxication is observed in the elderly with more than 100 mg / kg / day for several days. In children and elderly patients, the initial signs of salicylism (nausea, vomiting, tinnitus, visual impairment, dizziness, headache, general malaise) are not always noticeable, so it is advisable to periodically determine the salicylate content in the blood plasma.

    Interaction:

    Acetylsalicylic acid with simultaneous application enhances the effect of the following drugs:

    - methotrexate by reducing renal clearance and displacing it from the bond with plasma proteins,also a combination of acetylsalicylic acid with methotrexate is accompanied by an increased incidence of side effects on the part of the hematopoiesis;

    - narcotic analgesics, other NSAIDs;

    - hypoglycemic agents for oral administration;

    - heparin and indirect anticoagulants due to disruption of platelet function and displacement of indirect anticoagulants from the connection with plasma proteins;

    - thrombolytic agents and antiplatelet agents;

    - selective serotonin reuptake inhibitors, which may lead to an increased risk of bleeding from the upper gastrointestinal tract (synergism with acetylsalicylic acid);

    - digoxin due to a decrease in its renal excretion;

    - hypoglycemic agents (insulin and sulfonylurea derivatives) due to the hypoglycemic properties of acetylsalicylic acid itself in high doses and the displacement of sulfonylurea derivatives from binding to plasma proteins;

    - Valproic acid due to its displacement from the connection with blood plasma proteins.

    The combination of acetylsalicylic acid with anticoagulants, thrombolytic agents and antiplatelet agents is accompanied by an increased risk of bleeding.Simultaneous reception with acetylsalicylic acid increases the concentration of barbiturates and lithium salts in blood plasma.

    Glucocorticosteroids (GCS), ethanol and ethanol-containing drugs increase the negative effect on the mucosa of the gastrointestinal tract and increase the risk of developing gastrointestinal bleeding.

    At simultaneous reception of acetylsalicylic acid with ethanol, the toxic effect of ethanol on the central nervous system is increased, the risk of damage to the mucous membrane of the gastrointestinal tract increases and the time of bleeding prolongs.

    Acetylsalicylic acid reduces the effect of uricosuric drugs benzbromaron, probenicid (reduction urikozuricheskogo effect due to competitive suppressing renal tubular excretion of uric acid), angiotensin-converting enzyme (ACE) inhibitors (marked dose-dependent decrease in glomerular filtration rate by inhibiting prostaglandins possessing vasodilating action, and accordingly attenuation of the hypotensive actions), diuretics (when combined with acetylsal tsilovoy acid in high doses indicateddecrease in glomerular filtration rate as a result of decreased synthesis of prostaglandins in the kidneys).

    By enhancing the elimination of salicylates, systemic GCSs weaken their action.

    Antatsida containing magnesium and / or aluminum, slow down and worsen the absorption of acetylsalicylic acid.

    Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

    Special instructions:

    The drug should be used as directed by a doctor.

    Acetylsalicylic acid can provoke bronchospasm, as well as cause attacks of bronchial asthma and other reactions of hypersensitivity. Risk factors are history of bronchial asthma, hay fever, nasal polyposis, chronic diseases of the respiratory system, and allergic reactions to other drugs (for example: skin reactions, itching, urticaria).

    The inhibitory effect of acetylsalicylic acid on platelet aggregation persists for several days after ingestion, which may increase the risk of bleeding during surgery or in the postoperative period. Before surgical intervention to reduce bleeding during surgery and inpostoperative period should be canceled taking the drug for 5-7 days and inform the doctor.

    It should be borne in mind that in predisposed patients acetylsalicylic acid (even in small doses) reduces the excretion of uric acid from the body and can lead to the development of an acute attack of gout or exacerbation of the flow.

    With the simultaneous use of GCS and salicylates, it should be remembered that during treatment, the concentration of salicylates in the blood plasma is reduced, and after the cancellation of GCS, an overdose of salicylates is possible.

    The combination of acetylsalicylic acid with anticoagulants, thrombolytic agents and anti-platelet drugs is accompanied by an increased risk of bleeding.

    The combination of acetylsalicylic acid with methotrexate is accompanied by an increased incidence of side effects from the hematopoiesis.

    High doses of acetylsalicylic acid have a hypoglycemic effect, which should be borne in mind when prescribing it to patients with diabetes mellitus receiving hypoglycemic drugs.

    Excess dose of acetylsalicylic acid is associated with a risk of gastrointestinal bleeding.

    Overdose is especially dangerous in elderly patients.

    When combined with acetylsalicylic acid and alcohol, the risk of damage to the mucous membrane of the gastrointestinal tract and prolong the bleeding time.

    With prolonged use of the drug should periodically make a general blood test and analysis of feces for latent blood.

    With simultaneous use with ibuprofen, antagonism is noted with respect to irreversible platelet suppression caused by the action of acetylsalicylic acid, which leads to a decrease in the cardioprotective effects of acetylsalicylic acid. Therefore, the combination of acetylsalicylic acid with ibuprofen is not recommended in patients with an increased risk of cardiovascular disease.

    During treatment should refrain from drinking alcohol.

    Effect on the ability to drive transp. cf. and fur:During the administration of the drug, care should be taken when driving vehicles, mechanisms and other potentially hazardous activities that require a high concentration of attention and speed of psychomotor reactions.
    Form release / dosage:

    Tablets, coated with enteric coating, 50 mg.

    Packaging:

    For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

    3 contour mesh packages together with instructions for use are placed in a pack of cardboard.

    Storage conditions:

    In the dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years. Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:Without recipe
    Registration number:LS-001956
    Date of registration:22.12.2011 / 21.08.2017
    Expiration Date:Unlimited
    The owner of the registration certificate:VALENTA PHARM, PAO VALENTA PHARM, PAO Russia
    Manufacturer: & nbsp
    Information update date: & nbsp27.09.2017
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