ASA cardio - instructions for use, dose, side effects, contraindications

shell: methacrylic acid and ethacrylate copolymer [1: 1] (colicoate MAE 100) 4.186 mg; Macrogol-6000 (high molecular weight polyethylene glycol) 0.558 mg; talc 1,117 mg; titanium dioxide 0.139 mg.

Description:

Round biconvex tablets, coated with a white coating. On the cross-section the nucleus is white.

Pharmacotherapeutic group:Antiaggregant agent

ATX: & nbsp

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

Pharmacodynamics:

Acetylsalicylic acid (ASA) is an ester of salicylic acid, belongs to the group of non-steroidal anti-inflammatory drugs (NSAIDs).The mechanism of action is based on the irreversible inactivation of the enzyme cyclooxygenase (COX-1), which blocks the synthesis of prostaglandins, prostacyclin and thromboxane. Reduces aggregation, platelet adhesion and thrombus formation by suppressing the synthesis of thromboxane A2 in platelets. Increases fibrinolytic activity of blood plasma and reduces the concentration of vitamin K-dependent coagulation factors (II, VII, IX, X). Antiaggregant effect develops after the application of small doses of the drug and persists for 7 days after a single dose. These properties of ASA are used in the prevention and treatment of myocardial infarction, ischemic heart disease, complications of varicose veins. ASA in high doses (more than 300 mg) has anti-inflammatory, antipyretic and analgesic effects.

Pharmacokinetics:

After oral administration ASA is quickly and completely absorbed from the gastrointestinal tract (GIT). ASA is partially metabolized during absorption. During and after absorption, ASA is converted to a major metabolite, salicylic acid, which is metabolized mainly in the liver under the influence of enzymes to form metabolites such as phenyl salicylate, glucuronide salicylate and salicyluric acid, found in many tissues and in urine. In women, the metabolic process is slower (less enzyme activity in the blood serum). The maximum concentration of ASA in the blood plasma is reached in 10-20 minutes after ingestion, salicylic acid - after 0.3-2 hours. Due to the fact that the tablets are covered with an acid-resistant coating, ASA is not released in the stomach (the membrane effectively blocks the dissolution of the drug in the stomach), but in the alkaline medium of the duodenum. Thus, the absorption of ASA in the dosage form of the tablet is enteric, film-coated. slowed down for 3-6 hours compared to conventional (without such a shell) tablets. ASA and salicylic acid strongly bind to blood plasma proteins (from 66% to 98% depending on the dose) and are quickly distributed in the body. Salicylic acid penetrates the placenta and is secreted with breast milk.

Elimination of salicylic acid is dose-dependent, since its metabolism is limited by the possibilities of the enzymatic system. Half-life is from 2-3 hours when appliedASA in low doses and up to 15 hours when the drug is used in high doses (usual doses of acetylsalicylic acid as an analgesic agent). Unlike other salicylates, with repeated administration of the drug, unhydrolyzed ASA does not accumulate in the blood serum. Salicylic acid and its metabolites are excreted by the kidneys. In patients with normal renal function 80-100% of a single dose of the drug is excreted by the kidneys within 24-72 hours.

Indications:

- Unstable angina;

- stable angina;

- primary prevention of acute myocardial infarction in the presence of risk factors (eg, diabetes mellitus, hyperlipidemia, hypertension, obesity, smoking, old age) and repeated myocardial infarction;

- prevention of ischemic stroke (including in patients with transient impairment of cerebral circulation);

- prophylaxis of transient disorders 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 pulmonary arteries and its branches (for example, with prolonged immobilization as a result of extensive surgical intervention).

Contraindications:

- Hypersensitivity to acetylsalicylic acid (ASA), to excipients of the drug and other non-steroidal anti-inflammatory drugs (NSAIDs);

- erosive and ulcerative lesions of the gastrointestinal tract in the stage of exacerbation; gastrointestinal bleeding;

- The bronchial asthma, induced by the intake of salicylates and NSAIDs; complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance of ASA or other NSAIDs, including in history;

- hemorrhagic diathesis (hemophilia, von Willebrand's disease, telangiectasia, hypoproteinemia, thrombocytopenia, thrombocytopenic purpura);

- combined use with methotrexate at a dose of 15 mg per week or more;

- pregnancy (I and III trimester) and the period of breastfeeding;

- age to 18 years;

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

- severe hepatic insufficiency (class B and higher according to the Child-Pugh classification);

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

- lactose intolerance, lactase deficiency and glucose-galactose malabsorption.

Carefully:

FROM caution prescribe to patients with gout, hyperuricemia; if there is an anamnesis of ulcerative lesions of the gastrointestinal tract or gastrointestinal bleeding; renal failure (QC more than 30 ml / min); Hepatic insufficiency (below class B according to Child-Pugh classification); bronchial asthma, chronic respiratory diseases, hay fever, nasal polyposis, drug allergy, including the group of NSAIDs (analgesics, anti-inflammatory, antirheumatic drugs); in the second trimester of pregnancy; vitamin K deficiency; with severe forms of glucose-6-phosphate dehydrogenase deficiency; with the proposed surgical intervention (including minor, for example, tooth extraction); with simultaneous use with the following medicines (with methotrexate in a dose of less than 15 mg per week, with anticoagulant, thrombolytic or antiplatelet agents; NSAIDs, ibuprofen, salicylic acid derivatives in large doses, with digoxin; with hypoglycemic agents for ingestion (sulfonylurea derivatives) and insulin, with valproic acid, with alcohol,with selective serotonin reuptake inhibitors), with uricosuric drugs, ACE inhibitors, diuretics, glucocorticosteroids.

Pregnancy and lactation:

The use of the drug is contraindicated in pregnancy (I and III trimesters) and during breastfeeding. The use of large doses of salicylates in the first 3 months of pregnancy is associated with an increased frequency of fetal development defects (split sky, heart defects). In the second trimester of pregnancy, salicylates can be administered only in the light of a strict assessment of the risk and benefit.

In the last trimester of pregnancy, high-dose salicylates (more than 300 mg / day) cause weakening of labor, premature closure of the arterial duct in the fetus, increased bleeding in the mother and fetus, and the appointment immediately before childbirth can cause intracranial hemorrhage, especially in premature infants. The appointment of salicylates in the last trimester is contraindicated. Salicylates and their metabolites penetrate into breast milk in small amounts. The accidental intake of salicylates during breastfeeding is not accompanied by the development of adverse reactions in the child and does not require the cessation of breastfeeding.However, with prolonged use of the drug or its administration in a high dose, breast-feeding should be stopped immediately.

Dosing and Administration:

ASA cardio should be taken orally, preferably before eating, without chewing, with plenty of water.

ASA-cardio is intended for long-term use. The duration of therapy is determined by the attending physician. In the absence of other prescriptions, the following dosing regimen is recommended:

Unstable angina (with suspected acute myocardial infarction) the initial dose of 100-300 mg (the first tablet must be chewed for faster absorption) should be accepted by the patient as soon as possible after the suspicion of developing an acute myocardial infarction has arisen. In the next 30 days after the development of myocardial infarction, a dose of 200-300 mg per day should be maintained.

Primary prevention of acute myocardial infarction in the presence of risk factors 100 mg per day or 300 mg every other day.

Prevention of repeated myocardial infarction. Unstable and stable angina. Prophylaxis of ischemic stroke and transient disturbance of cerebral circulation.Prevention of thromboembolism after surgery and invasive vascular interventions 100-300 mg per day.

Prevention of deep vein thrombosis and thromboembolism of the pulmonary artery and its branches 100-200 mg per day or 300 mg every other day.

Side effects:

Disorders from the gastrointestinal tract: the most frequently observed nausea, heartburn, vomiting, pain in the abdomen; rarely - gastric and duodenal ulcers, including perforating, gastrointestinal bleeding; transient violations of liver function with increased activity of "liver" transaminases.

Heart Disease in rare cases - increased symptoms of chronic heart failure.

Vascular disorders: in rare cases - swelling of the lower extremities.

Violations of the blood and lymphatic system increased frequency of perioperative (intra- and post-operative) bleeding, hematomas, nasal bleeding, bleeding gums, bleeding from the urogenital tract. There are reports of serious cases of bleeding, which include gastrointestinal bleeding and hemorrhage in the brain (especially in patients with hypertension,who did not reach the target of blood pressure (BP) and / or who received concomitant therapy with anticoagulant drugs), which in some cases may be life-threatening. Bleeding can lead to the development of acute or chronic posthemorrhagic / iron deficiency anemia (eg, due to latent bleeding) with appropriate clinical and laboratory symptoms (asthenia, pallor, hypoperfusion).

There are reports of hemolysis and hemolytic anemia in patients with severe forms of glucose-6-phosphate dehydrogenase deficiency.

Disorders from the urinary system: there are reports of cases of development of renal dysfunction and acute renal failure.

Impaired nervous system: dizziness, hearing loss, tinnitus, which may be a sign of drug overdose (see Overdose section).

Immune system disorders: reactions of hypersensitivity with appropriate laboratory and clinical manifestations, such as asthmatic syndrome (bronchospasm), light and moderate reactions from the skin skin, itching, urticaria, Quincke's edema, rhinitis, edema of the nasal mucosa, cardio-respiratory distress syndrome, as well as severe reactions, including anaphylactic shock.

Overdose:It can have serious consequences, especially in elderly patients and children. The syndrome of salicylism develops when taking ASA at a dose of more than 100 mg / kg / day for more than 2 days due to the use of toxic doses of the drug in the context of improper therapeutic use (chronic poisoning) or a single accidental or intentional intake of a toxic dose of the drug by an adult or child (acute poisoning) .

Symptoms of overdose:

-For light and moderate severity (single dose less than 150 mg / kg):

Dizziness, noise in the ears, hearing loss, increased sweating, nausea and vomiting, headache, confusion, tachypnea, hyperventilation, respiratory alkalosis.

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

- With moderate to severe severity (single dose 150 mg / kg-300 mg / kg - moderate severity, more than 300 mg / kg - severe poisoning):

Respiratory alkalosis with compensatory metabolic acidosis, hyperpyrexia, hyperventilation, non-cardiogenic pulmonary edema, respiratory depression, asphyxia; cordially-cardiovascular system: heart rhythm disturbances, marked decrease in blood pressure, suppression of cardiac activity; from the side 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 departments for emergency therapy - gastric lavage, repeated intake of activated carbon, forced alkaline diuresis, hemodialysis, restoration of water-electrolyte balance and acid-base state, symptomatic therapy.

Interaction:

With the simultaneous use of ASA strengthens action of the following medicines; if it is necessary to simultaneously use ASA with the listed drugs, consider the need to reduce the dose of medicines:

- methotrexate, by reducing renal clearance and displacing it from the bond with proteins;

- with simultaneous use with anticoagulants, thrombolytic and antiplatelet agents (ticlopidine, clopidogrel) there is an increased risk of bleeding as a result of synergism of the main therapeutic effects of the drugs used;

- when used simultaneously with drugs that have anticoagulant, thrombolytic or antiplatelet effect, there is an increase in the damaging effect on the mucosa of the gastrointestinal tract;

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

- digoxin, due to a decrease in its renal excretion, which can lead to an overdose;

- hypoglycemic agents for oral administration (sulfonylurea derivatives) and insulin due to hypoglycemic properties of ASA itself at high doses and displacement of sulfonylurea derivatives from binding to plasma proteins;

- when used with valproic acid, its toxicity increases due to the displacement of its binding to blood plasma proteins;

- NSAIDs and salicylic acid derivatives in high doses (increased risk of ulcerogenic effect and bleeding from the gastrointestinal tract as a result of synergism of action); when used simultaneously with ibuprofen, antagonism is noted with respect to irreversible platelet suppression caused by the action of ASA, which leads to a decrease in the cardioprotective effects of ASA;

- Ethanol (increased risk of damage to the mucous membrane of the gastrointestinal tract and prolongation of the bleeding time due to the mutual enhancement of the effects of ASA and ethanol);

- With the simultaneous use of acetylsalicylic acid (as an antiplatelet agent) and blockers of "slow" calcium channels, the risk of bleeding increases;

- When used simultaneously with gold preparations acetylsalicylic acid can induce liver damage.

With the simultaneous use of ASA in high doses weakens action of the medicines listed below; if it is necessary to simultaneously prescribe ASA with the listed medicines, consideration should be given to the need for correction of the dose of the listed drugs:

- any diuretics (when combined with ASA in high doses, there is a decrease in the glomerular filtration rate (GFR) as a result of a decrease in the synthesis of prostaglandins in the kidneys);

- inhibitors of angiotensin-converting enzyme (ACE) (a dose-dependent decrease in GFR due to inhibition of prostaglandins with vasodilating action, respectively, weakening of hypotensive effect.) Clinical decline in GFR is observed with a daily dose of ACA greater than 160 mg.In addition, there is a decrease in the positive cardioprotective effect of ACE inhibitors assigned to patients for chronic heart failure therapy. This effect is also manifested when applied in conjunction with ASA in large doses);

- drugs with uricosuric action - benzbromarone, probenecid (reduction of uricosuric effect due to competitive suppression of renal tubular excretion of uric acid);

- when used simultaneously with systemic glucocorticosteroids (with the exception of hydrocortisone used for the replacement therapy of Addison's disease), the salicylate excretion is increased and, accordingly, their effect is weakened.

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

Special instructions:

The drug should be used after the appointment of a doctor.

ASA can provoke bronchospasm, as well as cause seizures of bronchial asthma and other reactions of hypersensitivity. Risk factors are the presence of bronchial asthma in history, hay fever, nasal polyposis, chronic diseases of the respiratory system, as well as allergic reactions to other drugs (eg, skin reactions, pruritus, urticaria).

ASA can cause bleeding of varying severity during and after surgical interventions, so if absolute elimination of bleeding is necessary in the course of surgery, it is necessary, if possible, to completely discontinue the use of ASA in the preoperative period.

The combination of ASA with anticoagulants, thrombolytic agents and antiaggregant drugs is accompanied by an increased risk of bleeding.

ASA in low doses can provoke the development of gout in predisposed individuals (having a decreased excretion of uric acid).

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

High doses of ASA have a hypoglycemic effect, which must be borne in mind when prescribing it to patients with diabetes mellitus receiving hypoglycemic drugs for ingestion and insulin.

When combined glucocorticosteroids (GCS) and salicylates should be remembered that during treatment, the level of salicylates in the blood is reduced, and after the abolition of SCS, an overdose of salicylates is possible.

The combination of ASA with ibuprofen in patients with an increased risk of cardiovascular disease is not recommended, as the latter reduces the positive effect of ASA on life expectancy (reduces the cardioprotective effect of ASA). Excess dose of ASA is associated with a risk of gastrointestinal bleeding. Overdose is especially dangerous in elderly patients.

With the combination of ASA with alcohol, the risk of damage to the mucous membrane of the gastrointestinal tract is increased and the bleeding time is prolonged.

During the treatment period, care must be taken when performing potentially hazardous activities requiring increased concentration of attention and speed of psychomotor reactions (driving, working with moving mechanisms, dispatcher and operator work, etc.), as vertigo is possible.

ASA is administered with caution to patients with gout, hyperuricemia; if there is an anamnesis of ulcerative lesions of the gastrointestinal tract or gastrointestinal bleeding; renal failure (QC more than 30 ml / min); Hepatic insufficiency (below class B according to Child-Pugh classification); bronchial asthma,chronic diseases of the respiratory system, hay fever, nasal polyposis, drug allergy, including the group of NSAIDs (analgesics, anti-inflammatory, antirheumatic drugs); in the second trimester of pregnancy; vitamin K deficiency; with severe forms of glucose-6-phosphate dehydrogenase deficiency; with the proposed surgical intervention (including minor, for example, tooth extraction); (with methotrexate in a dose of less than 15 mg per week, with anticoagulant, thrombolytic or antiplatelet agents, with NSAIDs ibuprofen, high-dose salicylic acid derivatives, with digoxin, with hypoglycemic agents for ingestion (sulfonylureas derivatives ) and insulin, with valproic acid, with alcohol, with selective serotonin reuptake inhibitors), with uricosuric drugs, ACE inhibitors, diuretics, glucocorticos theroids.

Effect on the ability to drive transp. cf. and fur:

During the treatment period, care must be taken when performing potentially Hazardous activities requiring increased concentration of attention and speed psychomotor reactions (driving vehicles, working with moving mechanisms, the work of the dispatcher and operator, etc.), since it is possible to develop dizziness.

Form release / dosage:Tablets are enteric, film-coated, 100 mg.

Packaging:

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

For 30, 50, 60 or 100 tablets in cans of polymeric.

Each jar or 1, 2, 3, 5, 6, 10 contour squares with instructions for use are placed in a pack of cardboard.

Storage conditions:

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

Keep out of the reach of children.

Shelf life:

4 years.

Do not use the product after the expiration date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:LS-002367

Date of registration:23.01.2012 / 10.08.2017

Expiration Date:Unlimited

The owner of the registration certificate:MEDISORB, CJSC MEDISORB, CJSC Russia

Manufacturer: & nbsp

MEDISORB, CJSC Russia

Information update date: & nbsp11.10.2017

Illustrated instructions

Instructions

ASA cardio® (ASK-cardio®)