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

Excipients: povidone low molecular weight (polyvinylpyrrolidone low molecular weight medical 12600 + 2700), corn starch, cellulose microcrystalline, magnesium stearate, talc, lactose monohydrate (sugar milk).

Auxiliary substances for coating: cellulose acetate (acetylphthalylcellulose), titanium dioxide, castor oil.

Description:Round biconvex tablets, covered with a film membrane white or almost white. On the cross-section, one layer of white or almost white color is visible.

Pharmacotherapeutic group:Antiaggregant agent

ATX: & nbsp

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

Pharmacodynamics:

The mechanism of antiplatelet action of acetylsalicylic acid (ASA) is based on irreversible inhibition of cyclooxygenase (COX-1),as a result of which synthesis of thromboxane A2 is blocked and aggregation of platelets is suppressed. Antiaggregant effect develops even after application of small doses of the drug and persists for 7 days after a single dose. It is believed that ASA has other mechanisms for suppressing platelet aggregation.

In high doses ASA (over 300 mg / day) also has anti-inflammatory, antipyretic and analgesic effects.

Pharmacokinetics:

After oral administration ASA is quickly and completely absorbed from the gastrointestinaltract(JCTT). ASA is partially metabolizedduring 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, salicylic acid glucuronide 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 by 3-6 hours compared to conventional tablets (without such a coating).

ASA and salicylic acid 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 into breast milk.

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

Indications:

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

Unstable angina;

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

Prevention of thromboembolism after surgery and invasive vascular interventions (eg, 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, erosive-ulcerative lesions of the gastrointestinal tract (in the phase of exacerbation), gastrointestinal bleeding, hemorrhagic diathesis, bronchial asthma induced by the intake of salicylates,complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to ASA, marked renal failure (creatinine clearance less than 30 ml / min), severe hepatic insufficiency (class B and C on the Child-Pugh scale), chronic cardiac failure (III-IV functional class by classification NYHA), simultaneous reception of methotrexate at a dose of 15 mg / week or more, pregnancy (I and III trimester), lactation period, children under 18 years of age, lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

If you have any of these diseases, consult a doctor before taking the drug.

Carefully:

With gout, hyperuricemia, because. ASA in low doses reduces the excretion of uric acid; it should be borne in mind that ASA in low doses can provoke the development of gout in predisposed patients (having decreased urinary acid excretion); gastric ulcer and duodenal ulcer or gastrointestinal bleeding (in the anamnesis); abnormal liver function (class A on the Child-Pugh scale); impaired renal function (QC more than 30 ml / min); bronchial asthma, chronic diseases of the respiratory system, hay fever,polyposis of the nose, drug allergy, simultaneous reception of methotrexate in a dose less than 15 mg / week; concomitant therapy with anticoagulants, pregnancy (II trimester); with the proposed surgical intervention (including minor, for example, tooth extraction), since ASA can cause a tendency to develop bleeding within a few days after taking the drug.

If you have any of these diseases, consult a doctor before taking the drug.

Pregnancy and lactation:

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). The appointment of salicylates in the first trimester of pregnancy is contraindicated. In the second trimester of pregnancy, salicylates can be given only with a strict risk assessment for the fetus and benefit to the mother, preferably at doses not exceeding 150 mg / day and for a short time.

In the last trimester of pregnancy, salicylates in high doses (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 hemorrhages, especially in premature infants. The appointment of salicylates in the last trimester of pregnancy is contraindicated.

Salicylates and their metabolites penetrate into breast milk in small amounts, so breastfeeding should be abolished during lactation.

Dosing and Administration:

Tablets of the drug Accekarol should be taken before meals, washed down with a large amount of liquid, once a day. Acetacarbol is intended for long-term use. The duration of therapy is determined by the doctor.

Preventive maintenance at suspicion of an acute myocardial infarction: 100 mg per day or 300 mg every other day (the first tablet must be chewed for faster absorption).

Prevention of the first acute acute myocardial infarction in the presence of risk factors: 100 mg daily or 300 mg every other day.

Prevention of recurrent myocardial infarction and unstable angina: 100 - 300 mg per day.

Prophylaxis of ischemic stroke and transient impairment of cerebral circulation: 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: 100 mg daily or 300 mg every other day.

Side effects:

From the digestive system: nausea, heartburn, vomiting, abdominal pain; 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: the appointment of ASA is accompanied by an increased risk of bleeding due to the inhibitory effect of ASA on platelet aggregation, anemia.

Allergic reactions: skin rash, skin itching, urticaria, Quincke's edema, rhinitis, nasal mucosal edema, cardiorespiratory distress syndrome, as well as severe reactions, including anaphylactic shock.

From the respiratory system: bronchospasm.

From the central nervous system: dizziness, hearing loss, headache, tinnitus.

If any of these side effects are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:

Overdose is unlikely because of the low content of ASA in the drug.

Excess dose of ASA is associated with a risk of gastrointestinal bleeding.

Overdose is especially dangerous in elderly patients.

Symptoms of an overdose from mild to moderate severity: dizziness, tinnitus, worseninghearing, increased sweating (including profuse), nausea, 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-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;

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

- violations of water-electrolyte balance: dehydration,the 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. When carrying out alkaline diuresis, it is necessary to achieve pH values between 7.5 and 8. Forced alkaline diuresis should be performed when the concentration of salicylates in the plasma is more than 500 mg / L (3.6 mmol / L) in adults and 300 mg / L (2, 2 mmol / l) in children.

Interaction:

ASA, when used simultaneously, enhances the effect of the following drugs:

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

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

- thrombolytic agents and antiplatelet agents;

- 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 by displacing it from the bond with plasma proteins.

The combination of acetylsalicylic acid with anticoagulants, thrombolytic agents and antiplatelet agents is accompanied by an increased risk of bleeding.

With the simultaneous administration of acetylsalicylic acid with alcohol, there is an increase in the toxic effect of alcohol on the central nervous system,the risk of damage to the mucous membrane of the gastrointestinal tract increases and the time of bleeding prolongs.

ASA weakens the effect of uricosuric drugs - benzbromarone (a decrease in uricosuric effect due to competitive suppression of renal tubular excretion of uric acid), angiotensin converting enzyme (ACE) inhibitors (a dose-dependent decrease in glomerular filtration rate due to inhibition of prostaglandins with vasodilating action, respectively, weakening of hypotensive action), diuretics (when combined with ASA in high doses, there is a decrease in glomerular filtration rate as a result of a decrease in the synthesis of prostaglandins in the kidneys).

ReinforcingElimination of salicylates, systemic glucocorticosteroids (GCS) weaken their effect.

Special instructions:

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).

The inhibitory effect of ASA on platelet aggregation persists for several days after ingestion, which may increase the risk of bleeding during surgery or in the postoperative period. If absolute elimination of bleeding is necessary in the course of surgical intervention, it is necessary to completely abandon the use of ASA in the preoperative period, if possible.

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

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

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

Effect on the ability to drive transp. cf. and fur:Caution should be exercised when administering the drug Accekarol while controlling vehicles, mechanisms and other potentially hazardous activities requiring increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets, coated with enteric coating, 50 mg, 100 mg and 300 mg.

Packaging:

10 tablets per contour cell pack.

1, 2, 3 or 5 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:4 years.

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

Terms of leave from pharmacies:Without recipe

Registration number:LS-000680

Date of registration:24.06.2010 / 04.06.2013

Expiration Date:Unlimited

The owner of the registration certificate:SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products Russia

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Information update date: & nbsp03.10.2017

Illustrated instructions

Instructions

Acecardol® (Acecardol®)