Aspikard

General characteristics. Structure:

Active ingredient: 75 mg or 150 mg of acetylsalicylic acid in 1 tablet.

Excipients: starch 1500, cellulose microcrystallic, stearic acid, опадрай (contains: a gipromelloza, triacetin, talc), акрилиз (contains: methacrylic acid and ethyl acrylate copolymer (1: 1), talc, triethyl citrate, silicon dioxide colloid anhydrous, sodium carbonate, sodium lauryl sulfate, titanium dioxide (Е 171), ferrous oxide yellow (E 172), ferrous oxide red (E 172)).

Pharmacological properties:

Pharmacodynamics. Acetylsalicylic acid is non-steroidal anti-inflammatory drug of group of salicylates, inhibits aggregation of thrombocytes. In doses to 300 mg has antiagregantny effect, in doses over 500 mg/days are shown febrifugal and antiinflammatory action.

The main mechanism of effect of acetylsalicylic acid is the irreversible inactivation of enzyme of cyclooxygenase therefore synthesis of prostaglandins, prostacyclins and thromboxane is broken. Irreversible disturbance of synthesis in thrombocytes of A2 thromboxane causes antiagregantny effect of acetylsalicylic acid which is shown even after its use in doses of 50 mg/days. After reception of a single dose the effect remains for 2-3 days. Antiagregantny effect of acetylsalicylic acid (ASK) is applied to primary and secondary prevention of trombotichesky oslozheniye, a myocardial infarction and an ischemic heart disease.

The tablets covered with a kishechnorastvorimy cover are a dosage form which does not break up in a stomach, and thus the risk of direct irritant action of acetylsalicylic acid on a mucous membrane of a stomach and its damage decreases. Destruction of a tablet and release of active ingredient happens only in the alkaline environment of a small intestine.

Pharmacokinetics. At intake it is absorbed preferential from proximal department of a small bowel. The maximum concentration (Cmax) in blood serum is reached approximately in 3 h and averages 12,7 mkg/ml for tablets on 150 mg and 6,72 mkg/ml for tablets on 75 mg. Existence of food in a digestive tract slows down drug absorption. AUC makes 56,42 мкг×ч/мл for tablets 75 mg and 108,08 мкг×ч/мл for tablets on 150 mg. During absorption is exposed to presistemny elimination in a wall of intestines and in a liver it (is deacetylated). The Rezorbirovanny part is very quickly hydrolyzed by special esterases therefore T½ makes no more than 15-20 min.

Acetylsalicylic acid circulates in an organism (for 75 - 90% in connection with albumine) in the form of anion which is quickly distributed in the majority of fabrics and liquids of an organism. The relative volume of distribution makes about 0,15 - 0,2 l/kg of body weight and increases with increase in concentration in blood serum. Extent of linkng of drug with proteins depends on concentration of albumine; at healthy faces it decreases with decrease in concentration of the last. Quickly gets through a placenta, in small amounts it is removed with breast milk.

At a renal failure, during pregnancy and at children linkng of acetylsalicylic acid with serum proteins decreases owing to a hypoalbuminemia and replacement of drug from communication with protein by internal causes.

It is metabolized preferential in a liver with formation of 4 metabolites (salicylic acid, глицинконъюгат salicylic acid, gentisic acid and it глицинконъюгат) found in many fabrics and urine. Excretion is carried out preferential by active secretion in tubules of kidneys in not changed form (60%) and in the form of metabolites. Removal of not changed salicylate depends on urine pH (when alkalifying urine the ionizirovaniye of salicylates increases, their reabsorption worsens and considerably excretion increases). Speed of excretion depends on a dose – at reception of doses in 150-300 mg of T½ salicylate ion makes 2 - 3 h. At newborns elimination of salicylates is carried out much more slowly, than at adults.

Indications to use:

Prevention of an acute myocardial infarction with risk factors (for example a diabetes mellitus, a lipidemia, an arterial hypertension, obesity, smoking, advanced age) and a repeated myocardial infarction; unstable stenocardia; prevention of a stroke (including at patients with the taking place disturbances of cerebral circulation).

Prevention of a thromboembolism after operations and invasive interventions on vessels (for example aortocoronary shunting, endarterectomy of carotid arteries, arteriovenous shunting, angioplasty of carotid arteries).

Prevention of a deep vein thrombosis and thromboembolism of a pulmonary artery and its branches (at a long immobilization as a result of big surgical intervention).

Route of administration and doses:

Accept inside, before food, swallowing a tablet entirely and washing down small (½ glasses) with an amount of water.

For primary prevention of a myocardial infarction with risk factors, and also prevention of a deep vein thrombosis and a thromboembolism of a pulmonary artery and its branches at patients with risk factors apply 75.150 mg daily or 300 mg every other day.

After surgeries or invasive researches apply 150-300 mg to prevention of a repeated myocardial infarction, unstable stenocardia, prevention of a stroke and passing disturbance of cerebral circulation, tromboembolic episodes daily.

Features of use:

After administration of drug there can be bleeding from a GIT and become aggravated a peptic ulcer of a stomach or duodenum.

Acetylsalicylic acid can cause a suffocation attack in patients with bronchial asthma.

Because acetylsalicylic acid and its metabolites are removed with urine, the risk of undesirable effects at patients with renal failures increases.

Long reception of acetylsalicylic acid in doses more than 1000 mg/days can cause development of an iron deficiency anemia and nephrotoxic action; in these cases it is necessary to control periodically function of kidneys and indicators of a hematocrit.

At patients with the accompanying damages of a liver toxicity of salicylates increases; at such patients it is necessary to control function of a liver.

It is necessary to apply with care to patients with disturbances of a hemostasis in the anamnesis, thrombocytopenia, a dysmenorrhea, chronic heart failure and arterial hypertension, deficit glyukozo-6-fosfatdegidrogenazy, at simultaneous use of other antitrombotichesky means, and also to the women applying intrauterine contraceptives.

In connection with decrease in a svetyvayemost of blood and high risk of development of bleeding, reception of acetylsalicylic acid should be stopped for 5. 7 days to planned surgical intervention.

It is recommended to stop reception of salicylates for 24 - 48 h before carrying out pulse therapy a methotrexate.

During treatment by acetylsalicylic acid it is not necessary to take alcoholic beverages as at the same time the risk of undesirable effects from a GIT increases.

To patients 65 years acetylsalicylic acid are more senior it is necessary to apply in lower doses and with big intervals. They to a thicket have an irritation of a mucous membrane of a stomach and bleeding from a GIT, and also the pharmacokinetics of acetylsalicylic acid can change.

Use of acetylsalicylic acid by children is younger than 15 years against the background of a hyperthermia in cases of chicken pox or flu can cause development of a syndrome to Reja.

Pregnancy and feeding by a breast. At children whose mothers applied acetylsalicylic acid before childbirth, noted such phenomena as subconjunctival hemorrhage, a hamaturia, exudates, a subperiosteal hematoma of a skull.

According to results of other tests intracranial bleedings arose more often at premature babies whose mothers accepted acetylsalicylic acid one week prior to childbirth.

Use by mother of acetylsalicylic acid can lead to premature closing of an arterial channel that can become AG reason at some newborns.

Use of acetylsalicylic acid by pregnant women can detain childbirth and serve as the bleeding reason.

If mother accepted acetylsalicylic acid for the last 1 – 2 weeks before childbirth, the child should be observed on a case of developing of bleeding.

It is possible to apply acetylsalicylic acid in I and II trimesters of pregnancy only if the advantage for mother exceeds potential danger to the child.

Acetylsalicylic acid gets into breast milk. It is not recommended to nurse during prolonged treatment by acetylsalicylic acid in high doses though its short-term use does not pose a threat for the child.

Side effects:

At use of acetylsalicylic acid side effects are possible:

- from a GIT: dyspepsia, heartburn, heavy feeling in epigastric area, nausea, vomiting, diarrhea, lack of appetite, a stomach ache, bleeding, injury of a mucous membrane of a stomach, an aggravation of a peptic ulcer of a stomach and duodenum. 15% of patients who applied acetylsalicylic acid throughout a long time had a stomach ulcer;

- from a liver: acute, temporary injury of a liver, a focal necrosis of cells of a liver, morbidity and increases in a liver, especially at patients with a juvenile pseudorheumatism, a system lupus erythematosus, a rheumatic disease or with injury of a liver to the anamnesis; increase in activity of aminotransferases in blood serum, an alkaline phosphatase, concentration of bilirubin, decrease in concentration of thromboxane.

- from hearing: sonitus, temporary hearing loss. Noise and a ring in ears are the first symptoms of poisoning with salicylates.

- from kidneys: an albuminuria, a leukocyte - and an erythrocyturia, a nephropathy with papillonekrozy;

In case of overdose: considerable decrease in clearance of creatinine or an acute necrosis of renal tubules with a renal failure.

- from integuments: different types of an enanthesis, in rare instances - bubbles or a purpura, bleeding from a mucous membrane and even a toxic kollikvatsionny epidermal necrosis.

- from blood: a leukopenia, thrombocytopenia, aplastic anemia, an agranulocytosis, an eosinopenia, a purpura, the disseminated intravascular blood coagulation.

- from the blood circulatory system: a fluid lungs of noncardiac genesis which generally arises at chronic or acute poisoning.

- from immune system: small tortoiseshell, Quincke's disease, bronchospasm, rhinitis, dacryagogue, shock. At 0,3% of the population and 20% of patients with bronchial asthma or a chronic small tortoiseshell hypersensitivity to acetylsalicylic acid develops. In hypersensitivity cases the undesirable phenomena can develop within 3 h after reception of a tablet.

Other disturbances: vision disorder.

Interaction with other medicines:

Acetylsalicylic acid replaces or can be forced out from communication with proteins by other medicines (for example, indirect anticoagulants, sulphonylurea derivatives, benzylpenicillin, sulfonamides), and also itself changes extent of communication with protein of other medicines (increases phenylbutazone binding).

Acetylsalicylic acid can strengthen action:

– heparin and indirect anticoagulants (increases risk of development of bleeding);

– trombolitik, such as Streptokinasa, alteplaza;

– peroral anti-diabetic drugs from group of derivatives of sulphonylurea. At a concomitant use of these drugs at patients with diabetes it is necessary to define concentration of glucose in blood serum and to adjust their mode of dosing;

– a methotrexate (concentration of a methotrexate in blood serum increases in connection with oppression of its removal by kidneys; the pancytopenia can develop);

– side effect of valproic acid, salicylates and other medicines from the NPVP group, corticosteroids, digoxin, barbiturates and salts of lithium.

Acetylsalicylic acid can reduce effect:

– Spironolactonum (the natriuretic effect of Spironolactonum and absorption of its active metabolite - a kanrenon decreases);

– phenylbutazone and uricosuric means for treatment of gout (a probenetsid, Sulfinpyrazonum). In turn Sulfinpyrazonum reduces removal of acetylsalicylic acid kidneys.

Simultaneous use of acetylsalicylic acid and inhibitors of a karboangidraza (acetazoleamide) can increase concentration of these drugs by decrease in their excretion kidneys and strengthenings of undesirable action. Inhibitors of a karboangidraza can increase toxicity of salicylates also.

Antiacid substances in high doses reduce concentration of salicylates in blood serum.

Alcohol increases the frequency and intensity of bleeding from the GIT caused by acetylsalicylic acid. It is not necessary to accept alcohol and acetylsalicylic acid at the same time.

Contraindications:

Hypersensitivity to acetylsalicylic acid (including to other non-steroidal anti-inflammatory drugs (NPVP), digestive tract erosive cankers (in an aggravation phase), gastrointestinal bleeding, hemorrhagic diathesis, the bronchial asthma induced by reception of salicylates and non-steroidal anti-inflammatory drugs, a combination of bronchial asthma, the nose recuring a polypose and okolonosovy bosoms and intolerance of acetylsalicylic acid (ASK), the combined use with a methotrexate in a dose of 15 mg/week and more (risk gemato-and nephrotoxic action), pregnancy (I and III trimester), the lactation period, children's age (up to 15 years – at use as febrifugal).

With care appoint at gout, a hyperuricemia, at cankers of the digestive tract (DT) or bleedings from a GIT in the anamnesis, at a renal and liver failure, bronchial asthma, a chronic obstructive pulmonary disease, at hay fever, a nose polypose, at allergic reactions to medicines in the anamnesis, at simultaneous use with a methotrexate in the dose less than 15 mg/week accompanying therapy by anticoagulants, the II trimester of pregnancy.

Overdose:

Symptoms: the overdose of easy degree proceeds malosimptomno and is shown by the increased tendency to capillary bleedings, a hyperpnea, an asthma; at overdose of moderate severity (reception in doses of 150.300 mg/kg) there are nausea, vomiting, a sonitus, deterioration in hearing, dizziness, confusion of consciousness; at heavy extent of overdose (reception in a dose more than 300 mg/kg) – fever, a hyperventilation, ketoacidosis, a respiratory alkalosis, a coma, cardiovascular and respiratory insufficiency, the expressed hyperglycemia. The overdose is most probable at patients of advanced age and children.

Treatment: at overdose of moderate severity – a drug dose decline, at heavy - immediate hospitalization for performing the emergency therapy – absorbent carbon, a gastric lavage, definition of indicators of acid-base balance, the alkaline and forced alkaline diuresis, a hemodialysis, infusional therapy, a symptomatic treatment. When carrying out an alkaline diuresis it is necessary to achieve values рН between 7,5 - 8. The forced alkaline diuresis should be carried out at concentration of salicylates in plasma more than 500 mg/l (3,6 mmol/l) at adults and 300 mg/l) at children.

Storage conditions:

In the place protected from light and moisture, at a temperature not over 25 ºС. To store in the place, unavailable to children. A period of validity - 2 years. Not to use after the termination of a period of validity.

Issue conditions:

Without recipe

Packaging:

On 10 tablets in a blister strip packaging, in packaging No. 10х2; No. 10х5.