Atsekor Kardio of the tab. of 100 mg No. 100

Pharmacological properties

Pharmacodynamics. acetylsalicylic acid oppresses aggregation of thrombocytes by thromboxane synthesis blocking a2. the mechanism of action consists in an irreversible inactivation of enzyme tsog 1. the specified inhibiting effect is especially significant for thrombocytes as they are not capable to resynthesis of the specified enzyme. acetylsalicylic acid renders also other inhibiting effects on thrombocytes. thanks to these effects it can be applied in many vascular diseases.

Acetylsalicylic acid belongs to the NPVP group with analgeziruyushchy, febrifugal and anti-inflammatory properties. Orally in higher doses acetylsalicylic acid can be applied to reduction of severity of pain and at easy febrile states, such as cold and flu, to decrease in body temperature and reduction of severity of a joint pain and muscles, in acute and chronic inflammatory diseases, such as pseudorheumatism, osteoarthritis and ankylosing spondylitis.

Pharmacokinetics. After intake, acetylsalicylic acid is quickly and completely soaked up in a GIT. In time and after absorption it turns into the main active metabolite — salicylic acid. The C _max acetylsalicylic acid in blood plasma is reached in 10–20 min., salicylic acid — in 20–120 min. according to. Thanks to an enterosoluble cover of the tablets Atsekor Kardio on 100 mg the release of active agent is carried out not in a stomach, and in the alkaline environment of intestines. Therefore absorption of acetylsalicylic acid slows down up to 3–6 h after reception of the tablet covered with an enterosoluble cover in comparison with a usual tablet of acetylsalicylic acid. Acetilsalicylic and salicylic acids completely contact proteins of blood plasma and are quickly distributed in an organism. Salicylic acid gets through a placenta and also into breast milk.

Salicylic acid is exposed to metabolism mainly in a liver. Metabolites of salicylic acid are salitsilmochevy acid, salitsilfenolglyukuronid, salitsilatsilglyukuronid, gentisic acid and gentizinmochevy acid.

Kinetics of removal of salicylic acid depends on a dose as metabolism is limited to activity of enzymes of a liver. T _½ depends on a dose and increases of 2–3 h at use in low doses to 15 h — at use in high doses. Salicylic acid and its metabolites are emitted from an organism mainly with kidneys.

Indication

For risk reduction:

• a lethal outcome at patients with suspicion of an acute myocardial infarction;
• incidence and a lethal outcome at the patients who had a myocardial infarction;
• tranzitorny ischemic attacks (TIA) and a stroke at patients with TIA;
• incidence and a lethal outcome in stable and unstable stenocardia;
• a myocardial infarction at patients with high risk of development of cardiovascular complications (diabetes, controlled AG) and at persons with multiple-factor risk of developing cardiovascular diseases (lipidemia, obesity, tobacco smoking, advanced age).

For prevention:

• thrombosis and an embolism after operations on vessels (transdermal transluminal catheter angioplasty (PTCA), endarterectomy of a carotid, aortocoronary shunting (CABG), arteriovenous shunting);
• a deep vein thrombosis and an embolism of a pulmonary artery after a long immobilization (after surgeries).

For secondary prevention of a stroke.

Use

Drug is taken inside in 30–60 min. prior to food, without chewing, washing down with enough liquid.

For reduction of risk of a lethal outcome at patients with suspicion of an acute myocardial infarction to use medicament in a dose of 100-300 mg/days. Within 30 days after a heart attack to continue reception of a maintenance dose of 100-300 mg/days. In 30 days it is necessary to consider a question of further prevention of a recurrence of a myocardial infarction.

to reach fast absorption at use for this indication, the first tablet it is necessary to chew.

To reduction of risk of incidence and a lethal outcome at the patients who had a myocardial infarction to apply 100–300 mg/days

To secondary prevention of a stroke to use medicament in a dose of 100-300 mg/days

To reduction of risk of TIA and a stroke at patients with TIA to apply 100–300 mg/days

To reduction of risk of development of a disease and a lethal outcome at patients with stable and unstable stenocardia — 100–300 mg/days

For prevention of a thrombembolia after operations on vessels (transdermal transluminal catheter angioplasty (PTCA), endarterectomy of a carotid, aortocoronary shunting (CABG), arteriovenous shunting) to use medicament in a dose of 100-200 mg/days daily or 300 mg/days every other day.

For prevention of a deep vein thrombosis and an embolism of a pulmonary artery after a long condition of an immobilization (after surgeries) — 100–200 mg/days or 300 mg/days every other day.

For prevention of a myocardial infarction at patients with high risk of development of cardiovascular complications (diabetes, controlled AG) and to persons with multiple-factor risk of developing cardiovascular diseases (a lipidemia, obesity, tobacco smoking, advanced age, etc.) — 100 mg/days or 300 mg/days every other day.

Contraindication

Hypersensitivity to acetylsalicylic acid, other salicylates or any of medicament components; oh, caused by use of salicylates or substances with similar action, especially npvp, in the anamnesis; acute round ulcer; hemorrhagic diathesis; renal failure of heavy degree; liver failure of heavy degree; heart failure of heavy degree; a combination with a methotrexate in a dose of ≥15 mg/week (see interactions).

Side effects

from a GIT: dyspepsia, pain in epigastric area and abdominal pain; inflammation of a GIT, GIT erosive cankers which in rare instances can cause gastrointestinal hemorrhages and perforation with the corresponding laboratory indicators and clinical manifestations.

from the system of blood and a hemopoiesis: intraoperative hemorrhages, hematomas, bleedings from bodies of an urinogenital system, nasal bleedings, odontorrhagias, GIT hemorrhages, brain hemorrhages (especially at patients from uncontrollable AG and/or at simultaneous use of anti-hemostatics). Hemorrhages can lead to acute and chronic posthemorrhagic anemia / an iron deficiency anemia (owing to the latent microbleeding) with the corresponding laboratory manifestations and clinical symptoms, such as asthenia, pallor of integuments, hypoperfusion.

At patients with severe forms of insufficiency glyukozo-6-fosfatdegidrogenazy noted hemolysis or hemolytic anemia.

from a cardiovascular system: pallor of integuments, hypoperfusion.

from the immune system: allergic reactions, including rash, urticaria, hypostasis, itching, acute anaphylaxis.

from a respiratory system: bronchospasm, cardiorespiratory insufficiency, rhinitis, congestion of a nose.

from an organ of hearing: a ring in ears.

Others: an asthenia, dizziness, a tranzitorny liver failure with increase in level of transaminases in a liver.

to

It was reported about a renal failure and development of OPN.

Hypersensitivity reaction with the corresponding laboratory and clinical manifestations are included by an asthmatic state, skin reactions of easy or average degree and also from a respiratory path, a GIT and a cardiovascular system.

Special instructions

Atsekor kardio apply

with care at:

• hypersensitivity to analgetic, anti-inflammatory, antirheumatic medicaments and also in the presence of an allergy to other substances;
• GIT ulcers, including a chronic and recurrent peptic ulcer or gastrointestinal bleedings in the anamnesis;
• simultaneous use of other anticoagulants;
• renal failures and/or liver;
• disturbances of cardiovascular blood circulation (for example pathology of vessels of a kidney, stagnant heart failure, a hypovolemia, extensive operations, sepsis or the profound bleedings) as acetylsalicylic acid can increase risk of a renal failure and OPN also;
• heavy insufficiency glyukozo-6-fosfatdegidrogenazy as acetylsalicylic acid can cause hemolysis or hemolytic anemia. Especially in the presence of factors which can increase risk of hemolysis, for example high doses of drug, fever or acute infectious process.

Ibuprofen can reduce expressiveness of the inhibiting effect of acetylsalicylic acid concerning aggregation of thrombocytes. In case of prolonged use of Atsekor Kardio before reception of an ibuprofen the patient needs to consult with the doctor.

At patients with allergic complications, including OH, allergic rhinitis, a small tortoiseshell, a skin itching, hypostasis of a mucous membrane and polipozy a nose and also at their combination to persistent infections of airways and at patients with hypersensitivity to NPVP against the background of treatment by Atsekor Kardio the development of a bronchospasm or attack OH is possible

.

Because of the inhibiting effect of acetylsalicylic acid concerning aggregation of thrombocytes which remains for several days after reception the use of the medicaments containing acetylsalicylic acid can increase the probability of emergence/strengthening of bleeding at surgeries (including insignificant surgical interventions, for example, odontectomy).

At use of acetylsalicylic acid in low doses the decrease in removal of uric acid is possible

. It can lead to developing of gout at patients with reduced removal of uric acid.

should not use the medicaments containing acetylsalicylic acid at children with a SARS which is followed or is not followed by fervescence, without consultation with the doctor. In some viral diseases, especially in flu A, flu B and chicken pox, there is a risk of development of a syndrome of Ray which is very rare, but life-threatening state demanding urgent medical intervention. The risk can increase if to apply acetylsalicylic acid as the accompanying medicine, however relationship of cause and effect in this case is not proved. If the specified states are followed by long vomiting, it can be sign of a syndrome of Ray.

Use during pregnancy and feeding by a breast. Oppression of synthesis of prostaglandins can have negative effect on pregnancy and/or embryonic/pre-natal development. The available data of epidemiological researches indicate risk of an abortion and malformations of a fruit after use of inhibitors of synthesis of prostaglandins at the beginning of pregnancy. The risk increases depending on increase in a dose and increase in duration of therapy. According to the available data the communication between intake of acetylsalicylic acid and the increased risk of an abortion is not confirmed.

Available epidemiological data on developing of malformations are not consecutive, however the increased risk of a gastroshizis cannot be excluded at use of acetylsalicylic acid. Results of a prospective research of influence in early pregnancy (1-4th month) with participation the female child do not indicate about 14,800 couples any communication with the increased risk of development of malformation.

Research on animals demonstrate reproductive toxicity.

B I and the II trimester of pregnancy should not appoint the medicaments containing acetylsalicylic acid without accurate clinical need. For women who can probably be pregnant women or to women in I and II trimester of pregnancy the dose of the medicaments containing acetylsalicylic acid has to be as low as possible, and treatment duration — as it is possible well.

In the III trimester of pregnancy all inhibitors of synthesis of prostaglandins can influence a fruit as follows:

• cardiopulmonary toxicity (with premature closing of an arterial channel and pulmonary hypertensia);
• a renal failure with possible subsequent development of a renal failure with oligogidramniony.

at the end of pregnancy inhibitors of synthesis of prostaglandins can influence the woman and the child as follows:

• risk of lengthening of a bleeding time, antiagregantny effect which can arise even after reception of very low doses;
• slowing down of reductions of a uterus that can lead to a delay or increase in a duration of delivery.

Considering it, acetylsalicylic acid is contraindicated in the III trimester of pregnancy.

Salicylates and their metabolites get into breast milk in small amounts.

As did not reveal an adverse effect of medicament on the child after administration of medicament during feeding by a breast, it is not required to interrupt breastfeeding, as a rule. However in cases of regular use or at use of high doses the feeding by a breast needs to be stopped at early stages.

Children. According to indications (see INDICATIONS) the medicament Atsekor Kardio should not be applied at children.

Use of acetylsalicylic acid for children aged up to 16 years can cause heavy side effects (including Ray's syndrome, one of signs of which is constant vomiting). It is necessary to study information stated in the section SPECIAL INSTRUCTIONS.

Ability to influence speed of response at control of vehicles or work with other mechanisms. Did not note influence on ability to run vehicles and other mechanisms.

Interaction

Contraindication for simultaneous use. use of acetylsalicylic acid and a methotrexate in a dose of ≥15 mg/week increases hematologic toxicity of a methotrexate (decrease in renal clearance of a methotrexate by anti-inflammatory agents and replacement by methotrexate salicylates from communication with blood plasma proteins).

Combination which need to be applied with care. At use of acetylsalicylic acid and a methotrexate in a dose of 15 mg/week the hematologic toxicity of a methotrexate increases (decrease in renal clearance of a methotrexate by anti-inflammatory agents and replacement by methotrexate salicylates from communication with blood plasma proteins).

Simultaneous use of acetylsalicylic acid with an ibuprofen interferes with irreversible inhibition of thrombocytes acetylsalicylic acid. Treatment by an ibuprofen of patients with risk of developing of cardiovascular diseases can limit cardiotyre-tread effect of acetylsalicylic acid.

At simultaneous use of Atsekor Kardio and anticoagulants, trombolitikov / other inhibitors of aggregation of thrombocytes and a hemostasis risk of developing bleeding increases.

At simultaneous use in high doses of salicylates with NPVP (thanks to effect of mutual strengthening) the risk of developing of ulcers of a GIT and gastrointestinal bleedings increases.

At use with selective serotonin reuptake inhibitors the risk of developing gastrointestinal bleeding owing to possible effect of synergism increases.

At simultaneous use with digoxin the concentration of the last in blood plasma increases owing to decrease in renal excretion.

At simultaneous use in high doses of acetylsalicylic acid and antidiabetic medicaments of group of derivatives of sulphonylurea the hypoglycemic effect of the last due to replacement of the sulphonylurea connected with blood plasma proteins, acetylsalicylic acid amplifies.

Diuretic means in a combination with high doses of acetylsalicylic acid reduce glomerular filtration thanks to decrease in synthesis of prostaglandins in kidneys.

System GKS (including the hydrocortisone applied as replacement therapy in Addison's disease) reduce the level of salicylates in blood and increase risk of overdose after the end of therapy.

APF Inhibitors in a combination with high doses of acetylsalicylic acid cause decrease in filtration in balls owing to inhibition of vazodilatatorny effect of prostaglandins and decrease in antihypertensive effect.

At simultaneous use with valproic acid acetylsalicylic acid forces out it from communication with blood plasma proteins, increasing toxicity of the last.

Alcohol causes injury of a mucous membrane of a GIT and prolongs a bleeding time owing to synergism of acetylsalicylic acid and alcohol.

Simultaneous use with uricosuric means, such as benzobromaron, probenetsid, reduces effect of removal of uric acid (owing to the competition of removal of uric acid renal tubules).

Overdose

Toxic effect of salicylates is possible

owing to the chronic intoxication which arose against the background of long therapy (use of 100 mg/kg/days can cause more than 2 days toxic effects) and also owing to acute intoxication which threatens life (overdose) and which causes can be, for example, an accidental use for children or inadvertent overdose.

Chronic poisoning with salicylates can latentno as signs and symptoms its nonspecific pass

. Moderate chronic intoxication salicylates, or a salitsilizm, is noted, as a rule, only after repeated receptions in high doses.

Symptoms. Dizziness, vertigo, a ring in ears, deafness, the increased sweating, nausea and vomiting, a headache, confusion of consciousness. The specified symptoms can be controlled a dose decline. The ring in ears is possible at concentration of salicylates in blood plasma of 150-300 mkg/ml. More serious side reactions note at concentration of salicylates in blood plasma 300 mkg/ml.

significant change of acid-base balance which can differ depending on age and weight of intoxication testifies To acute intoxication. The most general manifestation for children is the metabolic acidosis. Weight of a state cannot be estimated only on the basis of concentration of salicylates in blood plasma. Absorption of acetylsalicylic acid can slow down in connection with a gastric emptying delay, forming of concrements in a stomach or in case of administration of medicament in the form of the tablets covered with an enterosoluble cover.

Treatment. Treatment of the acute intoxication caused by overdose of acetylsalicylic acid is defined by severity, clinical symptoms and is provided with the standard methods applied in poisoning. All held events have to be directed to acceleration of removal of medicament and recovery of electrolytic and acid-base balance. In view of complex pathophysiological effects of poisoning with salicylates of manifestation and symptoms/results of analyses can include:

Alkalemiya's

Manifestation and symptoms	Results of analyses	Therapeutic actions
Intoxication of easy or average degree		Gastric lavage, repeated administration of activated carbon, the forced alkaline diuresis
Tachypnea, a hyperventilation, a respiratory alkalosis	, an alkaluria	Recovery of electrolytic and acid-base balance
Diaforez (the strengthened sweating)		Diaforez
Nausea, vomiting
Intoxication of average and heavy degree		Gastric lavage, repeated administration of activated carbon, the forced alkaline diuresis, in hard cases — a hemodialysis
Respiratory alkalosis with a compensatory metabolic acidosis	Acidemia, an aciduria	Recovery of electrolytic and acid-base balance
Giperpireksiya		Recovery of electrolytic and acid-base balance
Respiratory: hyperventilation, not cardiogenic fluid lungs, respiratory insufficiency, asphyxia
Cardiovascular: arrhythmias, arterial hypotension, cardiovascular insufficiency	For example, changes of the ABP, ECG
Loss of liquid and electrolytes: dehydration, an oliguria, a renal failure	For example a hypopotassemia, a hypernatremia, a hyponatremia, changes of function of kidneys	Recovery of electrolytic and acid-base balance
glucose metabolism Disturbance, ketoacidosis	Hyperglycemia, a hypoglycemia (especially at children)
Ring in ears, deafness
Gastrointestinal: bleeding in a GIT
Hematologic: inhibition of thrombocytes, coagulopathy	For example prolongation of a prothrombin time, prothrombinopenia
Neurologic: toxic encephalopathy and oppression of central nervous system with such manifestations as a lethargy, confusion of consciousness, a lump and a spasm

Storage conditions

In original packing at a temperature not above 30 °C.