Аспирин® cardio

General characteristics. Structure:

Active agent acetylsalicylic acid of 100 mg or 300 mg;
excipients: cellulose, powder of 10 mg or 30 mg, starch of corn 10 mg or 30 mg; cover: methacrylic acid and ethyl acrylate copolymer 1:1 (Eudragit of L30D) of 7,857 mg or 27,709 mg, polysorbate 80 0,186 of mg or 0,514 mg, sodium lauryl sulfate of 0,057 mg or 0,157 mg, talc of 8,100 mg or 22,380 mg, triethyl citrate of 0,800 mg or 2,240 mg.

Description: round biconvex tablets of white color; on cross section the homogeneous mass of white color surrounded with a cover of white color.

Pharmacological properties:

Pharmacodynamics. Irreversible inhibition of cyclooxygenase (TsOG-1) therefore synthesis of A2 thromboxane is blocked is the cornerstone of the mechanism of antiagregantny effect of acetylsalicylic acid (ASK) and aggregation of thrombocytes is suppressed. The Antiagregantny effect is most expressed in thrombocytes as they are not capable to synthesize cyclooxygenase repeatedly. It is considered that ASK has also other mechanisms of suppression of aggregation of thrombocytes that broadens area of its use at various vascular diseases.
ASK renders also antiinflammatory, analgeziruyushchy and febrifugal action.

Pharmacokinetics. After intake of ASK it is quickly and completely soaked up from the digestive tract (DT). ASK is partially metabolized during absorption. In time and after absorption of ASK turns into the main metabolite - salicylic acid which is metabolized, mainly, in a liver under the influence of enzymes with formation of such metabolites as salol, a glucuronide salicylate and salitsilurovy acid, found in many fabrics and in urine. At women process of metabolism takes place more slowly (smaller activity of enzymes in blood serum). The maximum concentration of ASK in a blood plasma is reached in 10-20 minutes after intake, salicylic acid - in 0,3-2 hours. Because tablets are covered with an acid resisting cover, ASK is released not in a stomach (the cover effectively blocks dissolution of drug in a stomach), and in the alkaline environment of a duodenum. Thus, absorption of ASK in the form of the tablets covered with a kishechnorastvorimy cover is slowed down for 3-6 hours in comparison with usual (without such cover) tablets.
ASK and salicylic acid strongly contact proteins of a blood plasma (from 66% to 98% depending on a dose) and are quickly distributed in an organism. Salicylic acid gets through a placenta and is emitted with breast milk.
Removal of salicylic acid is dozozavisimy as her metabolism is limited by opportunities of enzymatic system. The elimination half-life makes of 2-3 o'clock at use of ASK in low doses and till 15 o'clock at use of drug in high doses (usual doses of acetylsalicylic acid as analgeziruyushchy means). Unlike other salicylates, at multiple dose of drug not hydrolyzed ASK does not collect in blood serum. Salicylic acid and its metabolites are removed by kidneys. At patients with normal function of kidneys of 80-100% of a single dose of drug it is removed by kidneys within 24-72 hour.

Indications to use:

• Primary prevention of an acute myocardial infarction with risk factors (for example, a diabetes mellitus, a lipidemia, arterial hypertension, obesity, smoking, advanced age) and a repeated myocardial infarction;
• Unstable stenocardia (including suspicion on development of an acute myocardial infarction) and stable stenocardia;
• Prevention of a stroke (including at patients with passing disturbance of cerebral circulation);
• Prevention of passing disturbance 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 and stenting of coronary arteries, angioplasty of carotid arteries)
• Prevention of a deep vein thrombosis and thromboembolism of a pulmonary artery and its branches (including, at a long immobilization as a result of extensive surgical intervention).

Route of administration and doses:

It is desirable to take a pill of the drug ASPIRIN® KARDIO before food, washing down with a large amount of liquid. The pill KARDIO ASPIRIN is taken 1 time a day. ASPIRIN® KARDIO is intended for prolonged use. Learn on this website, than this medicine differs from usual aspirin and as it is long recommended to accept it.
Primary prevention of an acute myocardial infarction with risk factors:
100 mg/day or 300 mg every other day.

Prevention of a repeated heart attack, stable and unstable stenocardia:
100-300 mg/day.

Unstable stenocardia (at suspicion on development of an acute myocardial infarction):
the initial dose of 100-300 mg (the first tablet needs to be chewed for more bystry absorption) has to be accepted by the patient as soon as possible after there was a suspicion on development of an acute myocardial infarction. In the next 30 days after development of a myocardial infarction the dose of 200-300 mg/day has to be supported. In 30 days it is necessary to appoint the corresponding therapy for prevention of a repeated myocardial infarction.

Prevention of a stroke and passing disturbance of cerebral circulation:
100-300 mg/day.
Prevention of a thromboembolism after operations and invasive interventions on vessels:
100-300 mg/day.

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

Actions at the admission of reception of one or several doses of medicine:

Take the passed pill at once as soon as remember it and further continue reception in the usual mode. In order to avoid doubling of a dose do not take the passed pill if time of reception of the following tablet comes.
Features of effect of medicine at the first reception and at its cancellation:
Features of effect of drug at the first reception and its cancellation were not observed.

Features of use:

• Drug should be used on doctor's orders.
• ASK can provoke a bronchospasm, and also cause attacks of bronchial asthma and other hypersensitivity reactions. Risk factors are existence of bronchial asthma in the anamnesis, hay fever, the polypose of a nose, chronic diseases of respiratory system, and also allergic reactions to other drugs (for example, skin reactions, an itch, urticaria).
• The inhibiting effect of ASK on aggregation of thrombocytes remains within several days after reception in this connection, increase in risk of bleedings is possible during an operative measure or in the postoperative period. In need of an absolute exception of bleeding during an operative measure it is necessary to refuse whenever possible completely use of ASK in the preoperative period.
• Exceeding of a dose of ASK is accompanied by risk of gastrointestinal bleeding.
• The overdose is especially dangerous at patients of advanced age.
• At severe forms of deficit of a glyukozo-6-phosphate-dehydrogenase of ASK can cause hemolysis and hemolitic anemia. Factors which can increase risk of development of hemolysis are fever, acute infections and high doses of drug.

Influence on ability to manage the car / moving mechanisms
Administration of drug of Aspirin®kardio does not influence ability to manage the car / moving mechanisms.

Side effects:

From the alimentary system: nausea, heartburn, vomiting, abdominal pains are most often noted; seldom - ulcers of a mucous membrane of a stomach and a duodenum; very seldom - ruptured ulcers of a mucous membrane of a stomach and duodenum, gastrointestinal bleedings (with the corresponding clinical symptoms and laboratory changes), passing abnormal liver functions with increase in activity of "hepatic" transaminases.
From system of a hemopoiesis: purpose of ASK is followed by the increased risk of bleedings owing to an inhibiting effect of ASK on aggregation of thrombocytes. Increase in frequency perioperatsionny (intra-and post-operating rooms) bleedings, hematomas (bruises), nasal bleedings, bleeding of gums, bleedings from urinogenital ways is registered. There are messages on serious cases of bleedings to which gastrointestinal bleedings and hematencephalons (especially at the patients with arterial hypertension who did not reach target figures of the arterial pressure (AP) and/or receiving the accompanying therapy by anticoagulating means) which in some cases can have life-threatening character belong (see the section "Special Instructions").
Bleedings can lead to development of an acute or chronic posthemorrhagic/iron deficiency anemia (for example, owing to the concealed hemorrhage) with the corresponding clinical laboratory signs and symptoms (an adynamy, pallor, hypoperfusion).
Patients have messages on cases of hemolysis and hemolitic anemia with severe forms of deficit dehydrogenase glyukozo-6-phosphate.
Allergic reactions: hypersensitivity reactions with the corresponding laboratory and clinical manifestations, such as asthmatic syndrome (bronchospasm), reactions easy and moderately severe from integuments, airways, digestive tract and cardiovascular system, including such symptoms as skin rash, a skin itch, a small tortoiseshell, a Quincke's edema, rhinitis, a rhinedema, a cardiorespiratory distress syndrome, and also heavy reactions, including an acute anaphylaxis.
From the central nervous system (CNS): there are messages on cases of emergence of dizziness, decrease in hearing, a headache, a sonitus that can be a drug overdose sign (see the section "Overdose").
From an urinary system: there are messages on cases of development of a renal failure and an acute renal failure.

Interaction with other medicines:

At simultaneous use of ASK strengthens effect of the listed below medicines; in need of co-administration of ASK with the transferred funds it is necessary to consider a question of need of reduction of a dose of the specified drugs:
• a methotrexate due to decrease in renal clearance and its replacement from communication with proteins; ASK combination to a methotrexate is followed by the increased frequency of development of side effects from bodies of a hemopoiesis; drug Aspirin® use of Kardio together with a methotrexate is contraindicated if the dose of the last exceeds 15 mg a week (see the section "Contraindications") and it is possible with care - at a methotrexate dose less than 15 mg a week;
• heparin and indirect anticoagulants due to dysfunction of thrombocytes and replacement of indirect anticoagulants from communication with proteins;
• at simultaneous use with anticoagulants, thrombolytic and antiagregantny means (тиклопидин) increase in risk of bleedings as a result of a synergism of the main therapeutic effects of the used drugs is noted;
• at simultaneous use with the drugs possessing anticoagulating, thrombolytic or antiagregantny action strengthening of the damaging action on a mucous membrane of digestive tract is noted;
• selective serotonin reuptake inhibitors that can lead to increase in risk of bleeding from upper parts of digestive tract (a synergism with ASK)
• digoxin owing to decrease in its renal excretion that can lead to its overdose
• hypoglycemic means for intake (sulphonylurea derivatives) and insulin due to hypoglycemic properties of the ASK in high doses and replacement of derivatives of sulphonylurea from communication with proteins of a blood plasma; patients need to mean it at purpose of ASK with the diabetes mellitus receiving the listed medicines
• at simultaneous use with valproic acid its toxicity due to replacement from communication with proteins of a blood plasma increases;
• NPVP and derivatives of salicylic acid in high doses (increase in risk of ulcerogenic effect and bleeding from digestive tract as a result of an action synergism);
• Ethanol (alcoholic beverages) (the increased risk of injury of a mucous membrane of digestive tract and lengthening of a bleeding time as a result of mutual strengthening of effects of ASK and ethanol).
Co-administration of ASK in high doses can weaken effect of the listed below medicines. In need of co-administration of ASK with the listed drugs it is necessary to consider a question of need of dose adjustment of the listed below means:
• any diuretics (at combined use with ASK in high doses reduction in the rate of glomerular filtering as a result of decrease in synthesis of prostaglandins in kidneys is noted);
• inhibitors of an angiotensin-converting enzyme (APF) (dozozavisimy reduction in the rate of glomerular filtering (SKF) as a result of inhibition of prostaglandins possessing vasodilating action, respectively weakening of hypotensive action is noted. Clinical value of decrease in SKF is noted at a daily dose of ASK more than 160 mg. Besides, decrease in positive cardioprotective effect of the APF inhibitors appointed to patients for treatment of chronic heart failure is noted. This effect is also shown at use together with ASK in high doses);
• drugs with uricosuric action - бензбромарон, пробенецид (decrease in uricosuric effect owing to competitive suppression of renal canalicular excretion of uric acid).

At simultaneous use with an ibuprofen antagonism concerning the irreversible oppression of thrombocytes caused by action of ASK that leads to decrease in cardioprotective effects of ASK is noted. Therefore ASK combination to an ibuprofen at patients with the increased risk of cardiovascular diseases is not recommended.
At simultaneous use with system glucocorticosteroids (GKS) (except for a hydrocortisone or other GKS used for replacement therapy of a disease of Addison) strengthening of elimination of salicylates and respectively weakening of their action is noted. At the combined use of GKS and salicylates it is necessary to remember that during treatment the level of salicylates in blood is reduced, and after cancellation of GKS the overdose of salicylates is possible.

Contraindications:

• Hypersensitivity to acetylsalicylic acid, excipients as a part of drug and other NPVP
• The bronchial asthma induced by reception of salicylates and other NPVP; a combination of bronchial asthma, the nose recuring a polypose and okolonosovy bosoms and intolerance of ASK

• Digestive tract erosive cankers (in an aggravation stage)
• Gastrointestinal bleeding
• Hemorrhagic diathesis
• The combined use with a methotrexate in a dose of 15 mg a week and more
• Pregnancy (I and III trimester) and lactation period
• Children's and teenage age (up to 18 years)
• The expressed renal failure (the clearance of creatinine (CC) less than 30 ml/min.)
• The expressed liver failure (a class B above on a scale of Chayld-Pyyu)
• Chronic heart failure of the III-IV functional class on NYHA classification

With care:
• At gout, a hyperuricemia since ASK in low doses reduces excretion of uric acid; it must be kept in mind that ASK in low doses can provoke development of gout in the predisposed patients (having reduced excretion of uric acid)
• In the presence in the anamnesis of cankers of digestive tract or gastrointestinal bleedings
• At an abnormal liver function (below a class B on a scale of Chayld-Pyyu)
• At a renal failure (KK more than 30 ml/min.), and also at the disturbances of blood circulation arising owing to atherosclerosis of renal arteries, congestive heart failure, a hypovolemia, extensive surgical intervention, sepsis, cases of massive bleeding as in all listed cases of ASK can increase risk of development of an acute renal failure and a renal failure.
• At bronchial asthma, chronic diseases of a respiratory organs, hay fever, a polypose of a nose, a medicinal allergy, including the NPVP group (analgetics, anti-inflammatory, antirheumatic drugs)
• In the II trimester of pregnancy
• At estimated surgical intervention (including insignificant, for example, extraction of tooth) as ASK can cause tendency to development of bleedings within several days after administration of drug
• At the combined use with the following medicines (see the section "Interaction with Other Medicines"):

- with a methotrexate in a dose less than 15 mg a week;
- with anticoagulating, thrombolytic or other antiagregantny means
- with NPVP and derivatives of salicylic acid in high doses;
- with digoxin;
- with hypoglycemic means for intake (sulphonylurea derivatives) and insulin;
- with valproic acid;
- with alcohol (alcoholic beverages in particular);
- with selective serotonin reuptake inhibitors;
- with an ibuprofen.

PREGNANCY AND PERIOD OF THE LACTATION
The inhibition of synthesis of prostaglandins can make negative impact on pregnancy and development of an embryo or fruit.
Use of high doses of salicylates (more than 300 mg/days; it is about usual doses of ASK from 500 mg as anesthetic) in the I trimester of pregnancy is associated with the increased frequency of defects of fetation (splitting of the upper sky, heart diseases). Purpose of salicylates in the I trimester of pregnancy is contraindicated.
In the III trimester of pregnancy salicylates in a high dose (more than 300 mg/days; it is about usual doses of ASK from 500 mg as anesthetic) can cause braking of patrimonial activity, premature closing of an arterial channel in a fruit, the raised bleeding in mother and a fruit, and appointment just before childbirth can cause intracraneal hemorrhages, especially in premature children. Purpose of salicylates in the III trimester of pregnancy is contraindicated.
In the II trimester of pregnancy it is possible to appoint salicylates only taking into account strict assessment of risk and advantage for mother and a fruit, not higher than 150 mg/days are preferable in doses and it is short.
Use in the period of a lactation
Salicylates and their metabolites in small amounts get into breast milk. Accidental reception of salicylates in the period of a lactation is not followed by development of side reactions in the child and does not demand the breastfeeding termination. However at prolonged use of drug or appointment it in a high dose feeding by a breast should be stopped immediately.

Overdose:

Salitsilatny intoxication (develops at reception of ASK in a dose more than 100 mg/kg/days on an extent of more than 2 days) can be result of the long use of toxic doses of drug within the wrong therapeutic use of drug (chronic intoxication) or single accidental or intended dose of a toxic dose of drug by the adult or child (acute intoxication).
Symptoms of chronic intoxication derivatives of salicylic acid are not specific and are often diagnosed hardly. Intoxication of easy severity usually develops only after numerous use of high doses of drug and is shown by the dizziness, a sonitus, decrease in hearing increased by sweating, nausea and vomiting, a headache and confusion of consciousness. The specified symptomatology disappears after reduction of a dose of drug. The sonitus can appear at concentration of ASK in a blood plasma from 150 to 300 mkg/ml. Heavier symptoms are shown at concentration of ASK in a blood plasma higher than 300 mkg/ml.
The main display of acute intoxication is heavy disturbance of an acid-base state which manifestations can vary depending on age of the patient and severity of intoxication. At children the most typical is development of a metabolic acidosis. Treatment of intoxication is carried out according to the accepted standards and depends on severity of intoxication and a clinical picture and has to be directed mainly to acceleration of removal of drug and recovery of water and electrolytic balance and an acid-base state.

• Overdose symptoms from easy to moderate severity:
Dizziness, sonitus, deterioration in hearing, the increased sweating, nausea, vomiting, headache, confusion of consciousness, profuse sweating, tachypnea, hyperventilation, respiratory alkalosis.
Treatment: gastric lavage, multiple dose of absorbent carbon, the forced alkaline diuresis, recovery of water and electrolytic balance and an acid-base state.

• Overdose symptoms from average to heavy degree:
- a respiratory alkalosis with a compensatory metabolic acidosis;
- hyper pyrexia (extremely high temperature of a body);
- breath disturbances: hyperventilation, not cardiogenic fluid lungs, respiratory depression, asphyxia;
- disturbances from cardiovascular system: disturbances of a heart rhythm, arterial hypotension, oppression of cordial activity;
- disturbances of water and electrolytic balance: dehydration, the renal failure from an oliguria up to development of a renal failure which is characterized by a hypopotassemia, a hypernatremia, a hyponatremia;
- glucose metabolism disturbance: a hyperglycemia, a hypoglycemia (especially at children), ketoacidosis;
- sonitus, deafness;
- gastrointestinal bleedings;
- hematologic disturbances: from inhibition of aggregation of thrombocytes to a coagulopathy, lengthening of a prothrombin time, a prothrombinopenia;
- neurologic disturbances: toxic encephalopathy and oppression of the TsNS function (drowsiness, confusion of consciousness, lump, spasm).
Treatment: immediate hospitalization in specialized departments for performing the emergency therapy - gastric lavage, multiple dose of absorbent carbon, the forced alkaline diuresis, a hemodialysis, recovery of water and electrolytic balance and an acid-base state, symptomatic therapy.

Storage conditions:

At a temperature not above 25 °C. To store in the place, unavailable to children! Precautionary measures at destruction unused medicinal to the preparatovena it is applicable. Period of validity of 5 years. Not to use after a period of validity.

Issue conditions:

According to the recipe

Packaging:

The tablets covered with a kishechnorastvorimy cover of 100 mg and 300 mg:
on 10 tablets in software the blister Is scarlet/; on 2 blisters (20 tablets) together with the application instruction in a cardboard pack;
on 14 tablets in It is scarlet / 1111 the blister; on 2 (28 tablets) or 4 (56 tablets) the blister together with the application instruction in a cardboard pack.