KardiASK - instructions for use, dose, side effects, contraindications

Excipients: corn starch 3 mg; lactose (milk sugar) 80 mg; cellulose microcrystalline 54 mg; Povidone (plastidone K-90) 10 mg; calcium stearate 2 mg, polysorbate (Tween 80) 1 mg;

auxiliary substances for obtaining an enteric coating: colliquite MAE 100 P 27.4 mg; Copovidone (plasdone Es-630) 3.3 mg; talc 2.8 mg; propylene glycol 8.6 mg; castor oil 0,9 mg; titanium dioxide 2 mg.

Description:

The tablets covered with an enteric coating of white color, round, biconcave form. Light roughening and faint smell of acetic acid.

Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID)

ATX: & nbsp

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

Pharmacodynamics:

The mechanism of antiplatelet action of acetylsalicylic acid (ASA) is based on the irreversible inhibition of cyclooxygenase (COX-1), which blocks the synthesis of thromboxane A₂ and aggregation of platelets is suppressed. The antiaggregant effect is most pronounced in platelets, since they are not able to re-synthesize cyclooxygenase. Antiaggregant effect persists for 7 days after a single dose (more pronounced in men than in women).

Increases fibrinolytic activity of blood plasma and reduces the concentration of vitamin K-dependent coagulation factors (II, VII, IX, X).

ASA also has anti-inflammatory, analgesic and antipyretic 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 into a major metabolite, salicylic acid, which is metabolized 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 form of enteric coated tablets is slowed down by 3-6 hours compared to conventional tablets (without the shell).

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 excreted in breast milk.

Elimination of salicylic acid is dose-dependent, since its metabolism is limited by the possibilities of the enzymatic system. The half-life period (T1 / 2) is from 2-3 hours when using ASA in low doses and up to 15 hours when the drug is used in high doses (usual doses of ASA 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 kidney function, 80-100% of a single dose of the drug is excreted by the kidneys within 24-72 hours.

Indications:

- Primary prevention of acute myocardial infarction in the presence of risk factors (diabetes mellitus, hyperlipidemia, arterial hypertension, obesity, smoking, old 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);

- Prophylaxis of transient cerebral circulation disorder;

- Preventive maintenance of thromboembolism after surgery and invasive vascular interventions (coronary artery bypass grafting, carotid endarterectomy, arteriovenous shunting, angioplasty and stenting of the coronary arteries, carotid angioplasty);

- Prophylaxis of deep vein thrombosis and thromboembolism of the pulmonary artery and its branches (including, with prolonged immobilization as a result of extensive surgical intervention).

Contraindications:

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

- Deficiency of lactase, lactose intolerance, glucose-galactose malabsorption;

- Erosive-ulcerative lesions of the gastrointestinal tract (in the stage of exacerbation);

- Gastrointestinal bleeding;

- Hemorrhagic diathesis;

- Bronchial asthma induced by the intake of salicylates and other NSAIDs; a combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and ASA intolerance;

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

- Pregnancy (I and III trimester), lactation period;

- Age to 18 years;

- Severe renal insufficiency (creatinine clearance (CK) less than 30 ml / min);

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

- Chronic heart failure (III-IV functional class by classification NYHA - New York Association of Cardiology).

Carefully:

Gout; hyperuricemia, t. ASA in low doses reduces the excretion of uric acid, it can provoke the development of gout in predisposed patients (having a decreased urinary excretionacid); peptic ulcer disease of the stomach and duodenum or gastrointestinal bleeding in the anamnesis; impaired liver function (below grade B on the Child-Pugh scale); impaired renal function (QC more than 30 ml / min); bronchial asthma, chronic respiratory diseases, hay fever, nasal polyposis, drug allergy, including NSAIDs; II trimester of pregnancy; with the proposed surgical intervention (including minor), because ASA may cause a tendency to develop bleeding within a few days after taking the drug; simultaneous reception of the following drugs: methotrexate in a dose of less than 15 mg per week; anticoagulants, thrombolytic or antiplatelet drugs; NSAIDs and salicylic acid derivatives in high doses; digoxin; hypoglycemic drugs for oral administration (sulfonylureas derivatives) and insulin; valproic acid; alcohol; selective serotonin reuptake inhibitors; ibuprofen.

Pregnancy and lactation:

The use of ASA in the first trimester of pregnancy at a dose of more than 300 mg per day can lead to the development of defects in the fetus (heart defects, cleavage of the upper sky). The use of ASA in the first trimester is contraindicated.

In the second trimester of ASA used only with the strong risk assessment and benefits to the mother and the fetus at doses less than 150 mg per day, and short-lived Application ASA in the third trimester of pregnancy at a dose of 300 mg daily can cause weakening of labor, premature closure of the blood flow in the fetus, increased bleeding in the mother and the fetus, and the application before birth can cause intracranial hemorrhage in the newborn. The use of ASA in the third trimester is contraindicated.

A one-time or occasional intake of salicylates during breastfeeding is not accompanied by the development of adverse reactions in the fetus and does not require stopping breastfeeding. However, with prolonged use of the drug or its administration in high doses, breast-feeding should be stopped immediately.

Dosing and Administration:

Cardi ASK® tablets are taken once a day inside, before eating, with a sufficient amount of liquid. The drug is intended for long-term use. The duration of therapy is determined by the doctor.

- With primary prevention of acute myocardial infarction in the presence of risk factors; 100 mg per day or 300 mg every other day;

- In the prevention of repeated myocardial infarction: 100-300 mg per day;

- With unstable angina: 100-300 mg per day;

- In case of unstable angina in case of suspected development of 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 the development of acute myocardial infarction was raised. In the next 30 days after the development of myocardial infarction, a dose of 200-300 mg per day should be maintained. After 30 days, appropriate therapy should be used to prevent recurrent myocardial infarction.

- Stable angina: 100-300 mg per day;

- Prevention of stroke (including in patients with transient impairment of cerebral circulation): 100-300 mg per day;

- Prophylaxis of a transient cerebral circulation disorder: 100-300 mg per day;

- 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 (including, with prolonged immobilization as a result of extensive surgical intervention): 100-200 mg per day or 300 mg every other day.

If you need to use ASA in a dose of 100 - 200 mg, you can take the drug Cardiask ® tablets,coated with a film enteric coating of 50 mg and 100 mg.

Side effects:

From the digestive system

Nausea, heartburn, vomiting, abdominal pain, ulcerous lesions of the mucous membrane of the stomach and duodenum, perforated ulcers of the mucous membrane of the stomach and duodenum, gastrointestinal bleeding, transient liver dysfunction with increased activity of "liver" transaminases.

On the part of the hematopoiesis system

The use of ASA is accompanied by an increased risk of bleeding due to the inhibitory effect of ASA on platelet aggregation. An increase in the frequency of perioperative (intra- and post-operative) bleeding, hematomas, nasal bleeding, gingival hemorrhage, and bleeding from the urogenital tract has been reported. 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 blood pressure (BP) and / or are receiving concomitant therapy with anticoagulant drugs), which in some cases may have a life-threatening character (see para.section "Special instructions").

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

Hypersensitivity reactions with appropriate clinical and laboratory manifestations, such as asthmatic syndrome (bronchospasm), mild to moderate-to-severe reactions from the skin, respiratory tract, gastrointestinal tract and cardiovascular system, including symptoms such as skin rash, dermal itching, urticaria, Quincke's edema, rhinitis, swelling of the nasal mucosa, rhinitis, cardio-respiratory distress syndrome, severe reactions, including anaphylactic shock.

From the central nervous system

Dizziness, hearing loss, headache, tinnitus, which may be a sign of drug overdose (see "Overdose").

Co the side of the urinary system

There are reports of cases of development of renal dysfunction and acute renal failure.

Overdose:

Salicylate intoxication (developing with the use of ASA in a dose of more than 100 mg / kg / day for more than 2 days) may result from prolonged use of toxic doses of the drug (chronic intoxication) or a single dose of a toxic dose of the drug (acute intoxication).

Treatment of intoxication depends on the severity of intoxication and should be aimed at accelerating the elimination of the drug and restoring the water-electrolyte balance and the acid-base state.

Symptoms of an overdose from mild to moderate severity;

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

Treatment: gastric lavage, repeated intake of activated charcoal, 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;

- heart rhythm disorder, arterial hypotension, oppression of cardiac activity;

- disturbances of water-electrolyte balance: dehydration, disturbance of kidney function from oliguria up to 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;

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

- neurological disorders: toxic encephalopathy, oppression of function central nervous system (drowsiness, confusion, coma, convulsions).

Treatment: immediate admission to specialized departments for emergency therapy - gastric lavage, repeated intake of activated charcoal, forced alkaline diuresis,hemodialysis, restoration of water-electrolyte balance and acid-base state, symptomatic therapy.

Interaction:

Cardiascac®, when used concomitantly, enhances the effect of the following drugs:

- methotrexate, by reducing renal clearance, and displacing it from the bond with plasma proteins; combined use increases the incidence of side effects from the hematopoiesis; use of the drug with methotrexate is contraindicated if the dose last exceeds 15 mg per week; and possibly with caution at a dose of methotrexate of less than 15 mg per week;

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

- when used simultaneously with anticoagulants, thrombolytic and antiplatelet agents, the risk of bleeding increases; In addition, the damaging effect on the mucosa of the gastrointestinal tract is enhanced;

- selective serotonin reuptake inhibitors, which can lead to an increased risk of bleeding from the gastrointestinal tract;

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

- hypoglycemic drugs for ingestion and insulin by displacing sulfonylurea derivatives and binding to plasma proteins;

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

- NSAIDs and salicylic acid derivatives in high doses increases the risk of ulcerogenic effect and bleeding from the gastrointestinal tract;

- ethanol (alcoholic beverages), the risk of damage to the mucosa of the gastrointestinal tract increases and the time of bleeding lengthens as a result of the synergism of the action.

If simultaneous use of ASA with the listed drugs is necessary, the need to reduce the dose of these drugs should be considered.

ASA reduces the effect of the following drugs:

- any diuretics (the rate of glomerular filtration decreases);

- inhibitors of angiotensin-converting enzyme (ACE) (a dose-dependent decrease in the glomerular filtration rate is observed, and, consequently, weakening of the hypotensive effect), a clinically significant decrease in the glomerular filtration rate is observed with a daily dose of ACA greater than 160 mg; In addition, the positive cardioprotective effect of ACE inhibitors decreases in the treatment of chronic heart failure.

- drugs with uricosuric action (benzbromarone, sulfinpyrazone, probenecid). If it is necessary to simultaneously use ASA with these drugs, correction of their dose is necessary.

With simultaneous use 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. It is not recommended to combine ASA with ibuprofen in patients with an increased risk of cardiovascular disease.

With simultaneous use with systemic glucocorticosteroids (SCS), except for SCS, used for the replacement therapy of Addison's disease, there is an increased elimination of salicylates and, accordingly, a weakening of their action.

Special instructions:

The drug is used as directed by a doctor.

ASA can provoke bronchospasm, as well as cause attacks of bronchial asthma and other reactions of hypersensitivity (see section "Side effect"). The inhibitory effect of ASA on platelet aggregation persists for several days after admission, which may increase the risk of bleeding during surgery or in the postoperative period.It is necessary to completely abandon the use of ASA in the preoperative period, if possible. Exceeding the dose of ASA increases the risk of gastrointestinal bleeding. Overdose is especially dangerous in elderly patients.

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

Admission of the drug does not affect the ability to drive vehicles and perform work that requires a high rate of psychomotor reactions.

Form release / dosage:

Intestine-soluble film coated tablets, 300 mg.

Packaging:

For 10 or 15 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 1, 3, 10 contiguous cell packs of 10 tablets or 2 contourcell packs of 15 tablets together with the instructions for use are placed in a pack of cardboard.

Storage conditions:

In a dry, protected from light 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 expiration date.

Terms of leave from pharmacies:Without recipe

Registration number:LS-002676

Date of registration:06.03.2012

Expiration Date:Unlimited

The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia

Manufacturer: & nbsp

CANONFARMA PRODUCTION, CJSC Russia

Information update date: & nbsp10.12.2017

Illustrated instructions

Instructions

Cardiasca® (CardiASK®)