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

Excipients: cellulose microcrystalline - 122.0 mg; lactose monohydrate - 60.0 mg; croscarmellose sodium - 12.0 mg; silicon dioxide colloidal - 3.0 mg; stearic acid - 3.0 mg;

enteric membrane: methacrylic acid and ethyl acrylate copolymer (1: 1) (partially neutralized methacrylic acid and ethyl acrylate copolymer) - 10.3 mg; talc - 1,7 mg; propylene glycol 1.4 mg; titanium dioxide - 1.2 mg; Macrogol 4000 (polyethylene glycol 4000) - 0.4 mg.

Description:Round biconvex tablets of white or almost white color, covered with enteric coating. On the cross-section, the core of white or almost white colors.

Pharmacotherapeutic group:Antiaggregant agent

ATX: & nbsp

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

Pharmacodynamics:

The drug Aspicor ® due to the active ingredient - acetylsalicylic acid - with prolonged use in low doses has antiaggregant effect. The main mechanism of action of acetylsalicylic acid - non-selective inactivation of the enzyme cyclooxygenase (COX), thereby breaks the synthesis of prostaglandins and prostacyclin by endothelial cells (at doses of 300 mg) and thromboxane A2 in platelets, that causes the antiplatelet effect of the drug. Acetylsalicylic acid and may have other effects on the process of blood coagulation, enhancing fibrinolytic activity and reducing blood concentration of vitamin K-dependent coagulation factors (II, VII, IX, X). Acetylsalicylic acid in high doses can have anti-inflammatory, analgesic and antipyretic effects.

Blockage of COX-1 in the gastric mucosa leads to inhibition of gastroprotective prostaglandins, which can cause ulceration of the mucosa and subsequent bleeding. The presence of enteric coating provides less

irritating effect on the mucous membrane of the gastrointestinal tract (GIT).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.

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

Pharmacokinetics:

Suction

After ingestion, due to the acid-resistant enteric-insoluble coat, the active substance is released not in the stomach, but in the alkaline medium of the small intestine. Acetylsalicylic acid absorbed in the proximal small intestine.

Distribution

The maximum concentration in blood plasma is observed on average 3 hours after taking the drug inside. In the body it circulates (75-90% in association with albumin) and is distributed in tissues as an anion of salicylic acid. Salicylates easily penetrate into many tissues and body fluids, including spinal, peritoneal and synovial fluids.In small amounts, salicylates are found in the nervous tissue, traces in bile, sweat, feces. When acidosis occurs, most of the salicylate is converted to deionized acid, which penetrates well into tissues, including the brain. Rapidly passes through the placenta, in small quantities is excreted in breast milk.

Metabolism

Acetylsalicylic acid undergoes partial metabolism in the liver with the formation of less active metabolites.

Excretion

It is excreted by the kidneys, both in the unchanged form and in the form of metabolites; the half-life for acetylsalicylic acid is about 15 minutes, for metabolites - about 3 hours. Removal of unchanged salicylate depends on the pH of the urine (with alkalization of urine ionization of salicylates increases, their reabsorption worsens and the excretion increases significantly). The rate of excretion depends on the dose: when taking small doses, the elimination half-life is 2-3 hours, with increasing dosage it can increase to 15-30 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 (including suspected development of acute myocardial infarction) and stable angina pectoris;

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

- prophylaxis of transient impairment of cerebral circulation;

- prevention of thromboembolic complications after surgery and invasive vascular interventions (eg, coronary artery bypass grafting, carotid endarterectomy, arteriovenous shunting, carotid angioplasty);

- prophylaxis of deep vein thrombosis and pulmonary artery thromboembolism and ce branches, for example, with prolonged immobilization as a result of extensive surgical intervention).

Contraindications:

- Hypersensitivity to the drug components and non-steroidal anti-inflammatory drugs (NSAIDs);

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

- gastrointestinal hemorrhage;

- hemorrhagic diathesis;

- bronchial asthma induced by the intake of salicylates and other NSAIDs, the Fernan-Vidal triad (complete or incomplete combination of bronchial asthma,recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid);

- 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 up 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;

- Lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

Carefully:

- 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 urinary acid excretion);

- history of gastrointestinal ulceration or gastrointestinal bleeding;

- impaired liver function (below class B according to Child-Pugh classification);

- impaired renal function (QC more than 30 ml / min);

- bronchial asthma, chronic respiratory diseases, hay fever, nasal polyposis, allergic reactions to other drugs;

- I trimester of pregnancy;

- before 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;

- deficiency of vitamin K and glucose-6-phosphate dehydrogenase;

- 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 antiaggregant drugs;

- with NSAIDs and salicylic acid derivatives in large doses;

- with digoxin;

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

- with valproic acid;

- with ethanol;

- with selective serotonin reuptake inhibitors;

with ibuprofen.

Pregnancy and lactation:Pregnancy

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 per day) uproot the inhibition of labor, premature closure of the arterial duct in the fetus, increased bleeding in the mother and fetus, and application immediately before childbirth can cause intracranial hemorrhages, especially in premature infants. The appointment of salicylates in the last trimester of pregnancy is contraindicated.

Breastfeeding period

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 ns requires 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:Inside, before eating, without chewing, squeezed a lot of liquid.

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

Prevention of acute myocardial infarction in the presence of risk factors - 100 mg per day.

Suspicion of the development of acute myocardial infarction - 100-200 mg per day (the first tablet must be chewed for a faster suction).

Prevention of repeated myocardial infarction; stable and unstable angina; prevention of stroke and transient cerebral circulation disorders - 100 mg per day.

Preventing thromboembolic complications after surgery or invasive research - 100-200 mg per day.

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

Side effects:From the digestive system:

- nausea, decreased appetite, heartburn, vomiting, abdominal pain, diarrhea, gastric ulcer and duodenal ulcer (including perforating), gastrointestinal bleeding, transient liver dysfunction with increased activity of "liver" transaminases.

Co, the sides 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 (see section "Special instructions"). Bleeding can lead to the development of acute or chronic posthemorrhagic / iron deficiency anemia (eg, due to latent bleeding) with the corresponding 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:

- a false rash, skin itching, 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 indicate a drug overdose (see "Overdose").

From the urinary system:

- impaired renal function and acute renal failure.

Overdose:Overdose is especially dangerous in elderly patients.

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 body weight, acute poisoning is considered easy, 150-300 mg / kg - moderate, more than 300 mg / kg - heavy. The highest risk of chronic intoxication is observed in elderly patients with a dose of more than 100 mg / kg / day for several days. In 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.

Symptoms

Symptoms of chronic intoxication

Symptoms are nonspecific and often difficult to diagnose.

Intoxication of mild severity usually develops only after repeated use of large doses of the drug and is manifested by dizziness, noise in the ears, hearing loss, increased sweating, nausea and vomiting, headache and confusion. This symptomatology disappears after a decrease in the dose of the drug.Noise in the ears can appear with a concentration of acetylsalicylic acid in the blood plasma from 150 to 300 μg / ml. Severe symptoms appear at concentrations above 300 μg / ml.

Symptoms of acute intoxication

The main manifestation of acute intoxication is a severe violation of the acid-base equilibrium, the manifestations of which can vary depending on the age of the patient and the severity of intoxication. In children, the development of metabolic acidosis is most typical. Treatment of intoxication is carried out in accordance with accepted standards and depends on the severity of intoxication and clinical picture and should be directed mainly to accelerate the elimination of the drug and restore the water-electrolyte balance and acid-base state.

Symptoms of an overdose of mild to moderate severity

Dizziness, tinnitus, hearing impairment, increased sweating, nausea, vomiting, headache, confusion, profuse sweating, tachypnea, hyperventilation, respiratory alkalosis.

Symptoms of an overdose of moderate to severe severity:

- 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, arterial hypotension, oppression of cardiac activity, collapse;

- 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 and depression of the central nervous system (drowsiness, confusion, coma, convulsions).

Treatment

Treatment of an overdose of mild to moderate severity

Provocation of vomiting, repeated intake of adsorbents (activated carbon), forced alkaline diuresis (sodium bicarbonate, sodium citrate or sodium lactate), restoration of water-electrolyte balance and acid-base state.

Treatment of an overdose from moderate to severe severity

Immediate hospitalization in specialized departments for emergency therapy - gastric lavage, repeated intake of adsorbents (activated charcoal) and laxatives, alkalinization of urine (shown at a salicylate level in the blood plasma above 500 mg / l, is provided by intravenous infusion of sodium bicarbonate - 88 meq per liter 5% glucose solution, at a rate of 10-15 ml / kg / h), recovery of circulating blood volume and induction of diuresis (achieved by sodium bicarbonate administration at the same dose and dilution, repeated 2-3 times); it should be borne in mind that intensive fluid infusion to elderly patients can lead to pulmonary edema. It is not recommended to use acetosolamide for urine alkalinization (can cause acidemia and enhance the toxic effect of salicylates). When carrying out alkaline diuresis, it is necessary to achieve pH values of 7.5-8.

Hemodialysis is indicated with a salicylate level in the blood plasma of more than 1000 mg / L, and in patients with chronic poisoning - 500 mg / L and lower if there are indications (refractory acidosis, progressive deterioration, severe central nervous system damage, pulmonary edema and kidney failure) .

It is shown in pulmonary edema artificial ventilation with a mixture enriched in oxygen at a positive pressure mode at the end of the exhalation; To treat edema of the brain, hyperventilation and osmotic diuresis are used.

Interaction:The drug Aspicor®, when used at the same time, enhances the effect of the following medicines:

- methotrexate by reducing renal clearance and displacing it from the connection 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, NSAIDs;

- hypoglycemic agents for oral administration;

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

- antiaggregant drugs;

- selective serotonin reuptake inhibitors, which may lead to an increased risk of bleeding from the upper gastrointestinal tract (synergism in 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 antiaggregant drugs is accompanied by an increased risk of bleeding.

Simultaneous reception of acetylsalicylic acid with barbiturates and lithium salts increases the concentration in the blood plasma of these drugs.

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.

With the simultaneous administration of acetylsalicylic acid with ethanol, an additive effect and an extended bleeding time are observed.

Acetylsalicylic acid weakens the effect of uricosuric drugs - benzbromarone, probenecid (due to competitive tubular elimination of uric acid), angiotensin converting enzyme inhibitors (a dose-dependent decrease in glomerular filtration rate due to inhibition of prostaglandins with vasodilating effect and, accordingly, attenuation of antihypertensive effect), diuretics joint application with acetylsalicylic acid in high doses, STI glomerular filtration by reducing the synthesis of prostaglandins in the kidneys). By enhancing the elimination of salicylates, systemic GCSs weaken their action. Myelotoxic drugs increase the manifestation of hematotoxicity of acetylsalicylic acid.

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

Special instructions:Acetylsalicylic acid can provoke bronchospasm, as well as cause seizures of bronchial asthma and other hypersensitivity reactions. Risk factors are the availability of a history of asthma, hay fever, nasal polyposis, chronic diseases of the respiratory system as well as of allergic reactions to other drugs (e.g., skin reactions, pruritus, urticaria).

Acetylsalicylic acid can cause bleeding of varying severity during and after surgical interventions.

Acetylsalicylic acid in low doses can provoke the development of gout in predisposed patients (having decreased uric acid excretion). High doses of acetylsalicylic acid have a hypoglycemic effect, which must be borne in mind when prescribing it to patients with diabetes mellitus, who prescribe hypoglycemic drugs.

The inhibitory effect of acetylsalicylic acid on platelet aggregation persists for several days after taking Aspicor®,in connection with which it is possible to increase the risk of bleeding during surgery or in the postoperative period. Before surgical intervention to reduce bleeding during surgery and in the postoperative period, you should cancel taking the drug for 5-7 days and inform the doctor.

The combination of acetylsalicylic acid with antiaggregant 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.

When combined appointment of 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.

It is not recommended to combine acetylsalicylic acid with ibuprofen, as the latter worsens the beneficial effect of Aspicor® on life expectancy.

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

In severe forms of deficiency of glucose-6-phosphate dehydrogenase acetylsalicylic acid can cause hemolysis and hemolytic anemia.Factors that may increase the risk of hemolysis are fever, acute infections and high doses of the drug.

When combined with acetylsalicylic acid and alcohol, the risk of damage to the mucosa of the gastrointestinal tract and prolonging the time of bleeding is increased.

During treatment should refrain from drinking alcohol.

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

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

During the administration of Aspicor®, care should be taken to drive vehicles and engage in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Intestine-soluble film coated tablets, 100 mg.

Packaging:

10, 15 or 20 tablets in a planar cell packaging made of polyvinylchloride film and foil aluminum.

1, 2, 3 or 6 contour mesh packs of 10 tablets, 2, 4 or 6 contour packs of 15 tablets or 3 out-of-round packs of 20 tablets together with instructions for use in a pack of cardboard.

Storage conditions:Store in a 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 expiry date.

Terms of leave from pharmacies:Without recipe

Registration number:LS-000440

Date of registration:31.08.2010 / 04.10.2016

The owner of the registration certificate:VERTEKS, AO VERTEKS, AO Russia

Manufacturer: & nbsp

VERTEKS, AO Russia

Information update date: & nbsp17.10.2017

Illustrated instructions

Instructions

Aspicor® (Aspicor®)