Polokard

General characteristics. Structure:

Active agent: acetylsalicylic acid of 75 mg

Other ingredients: starch corn, cellulose powdery, sodium is krakhmalglikolit, a gipromelloza.

Active agent: acetylsalicylic acid of 150 mg

Other ingredients: starch corn, cellulose powdery, sodium is krakhmalglikolit, a gipromelloza.

Pharmacological properties:

Polokard contains acetyl derivative salicylic acid with antiagregantny, febrifugal, analgeziruyushchy and antiinflammatory action.
The mechanism of oppression of aggregation of thrombocytes acetylsalicylic acid consists in an irreversible inactivation in thrombocytes of blood of TsOG-1 enzyme which transforms arachidonic acid to cyclic peroxides (PGG2 and PGH2), being predecessors of platelet prostaglandins and thromboxane (A2).
Oppression of aggregation comes after use of medicine in low doses and remains within several days after reception of a single dose.
These properties of acetylsalicylic acid were used for prevention and treatment of the complications connected with blood clots and also for prevention of a myocardial infarction and an ischemic heart disease.
Polokard the tablets covered with an enterosoluble cover — a dosage form which does not break up in a stomach because of what the risk of direct contact of acetylsalicylic acid with a mucous membrane of a stomach decreases. Disintegration of a tablet and release of active ingredient happen only in more alkaline environment of a duodenum.
Absorption of acetylsalicylic acid comes from the tablets covered with an enterosoluble cover more slowly in comparison with standard forms. It begins in 3–6 h after medicine reception that demonstrates that the cover effectively blocks disintegration of a medicinal product in a stomach.
Cmax in a blood plasma is reached approximately in 6 h and averages 12,7 mkg/ml for tablets of 150 mg and 6,72 mkg/ml for tablets of 75 mg.
Meal slows down absorption of medicine in a GIT, but does not reduce bioavailability of acetylsalicylic acid.
Acetylsalicylic acid is soaked up in a GIT for 80–100%.
Acetylsalicylic acid is quickly and substantially distributed in the majority of fabrics and biological liquids of an organism.
The relative volume of distribution makes about 0,15-0,2 l/kg of body weight and increases according to increase in concentration of medicine in a blood plasma.
About 33% of medicine contact proteins of a blood plasma when concentration makes 120 mkg/ml.
Linkng of medicine with proteins depends on concentration of albumine; at healthy volunteers it decreases according to decrease in this concentration.
At a renal failure, at pregnancy and at newborns linkng of acetylsalicylic acid with proteins of a blood plasma decreases not only because of a hypoalbuminemia, but also owing to cumulation of internal causes which force out drug from connections with proteins.
Acetylsalicylic acid is partially metabolized during absorption. This process happens under the influence of esterase, generally in a liver, and also in a blood plasma, erythrocytes and in synovial fluid.
Salicylates generally connect to glycine with formation of salitsilurovy acid and with glucuronic acid with education salicyl - phenolic and salicyl-atsilovogo of a glyukuronat, only their small part is exposed to a hydroxylation to gentisic acid, 2,3-dihydroxybenzoic and 2,3,5-trigidroksibenzoyny acids.
At women process of a hydroxylation takes place more slowly (smaller activity of esterase in a blood plasma).
Т½ in a phase of elimination of acetylsalicylic acid makes about 2-3 h of a blood plasma.
Unlike other salicylates, not hydrolyzed acetylsalicylic acid does not kumulirut in a blood plasma after repeated introduction.
About 1% of a dose of the acetylsalicylic acid accepted inside is removed with urine in not hydrolyzed form, other part is removed in the form of salicylates and their metabolites.
At patients with the kept function of kidneys of 80-100% of a single dose it is removed with urine during 24–72 h.

Indications to use:

For decrease in risk:

• death at patients with suspicion of an acute myocardial infarction;
• death at the patients who had a myocardial infarction;
• the tranzitorny ischemic attacks (TIA) and a stroke at patients with TIA;
• incidences and death at stable and unstable stenocardia.
For prevention:

• thromboses and an embolism after operations on vessels (transdermal translyuminarny catheter angioplasty (RTSA), endarterectomy of a carotid artery, aortocoronary shunting (CABG), arteriovenous shunting);
• a deep vein thrombosis and an embolism of lungs after a long immobilization (after surgeries);
• a myocardial infarction at patients with high risk of development of cardiovascular complications (a diabetes mellitus, controlled AG) and to persons with multifactorial risk of cardiovascular diseases (a lipidemia, obesity, smoking, advanced age, etc.).

Route of administration and doses:

The adult usually appoint on 1–2 tablets 75 mg or 1 tablet of 150 mg a day in time or after food. It is necessary to swallow of tablets whole, washing down with a small amount of water.
At recently postponed myocardial infarction or for patients with suspicion of a myocardial infarction: the initial sating dose of 225-300 mg of acetylsalicylic acid of 1 times a day for the purpose of achievement of bystry oppression of aggregation of thrombocytes. The dose of 300 mg/days can quickly be applied according to therapeutic indications.
Tablets can be chewed for more bystry absorption.

Features of use:

Polokard apply with care at:

• hypersensitivity to analgetic, anti-inflammatory, antirheumatic drugs, and also in the presence of an allergy to other substances;
• GIT ulcers, including chronic and recurrent or gastrointestinal bleedings in the anamnesis;
• simultaneous use of anticoagulants;
• disturbances of functions of kidneys and/or liver.
At prolonged use of drug before reception of an ibuprofen the patient has to consult with the doctor.
At patients with allergic complications, including with OH, allergic rhinitis, a small tortoiseshell, a skin itch, hypostasis of a mucous membrane and polipozy a nose, and also in combination with persistent infections of respiratory tracts and at patients with hypersensitivity to NPVP against the background of treatment by Polokard development of a bronchospasm or attack OH is possible.
At surgeries (including dental) use of the drugs containing acetylsalicylic acid can increase probability of emergence/strengthening of bleeding.
At use of acetylsalicylic acid in low doses removal of uric acid can decrease. It can lead to developing of gout at patients with reduced removal of uric acid.
Period of pregnancy and feeding by a breast. Polokard it is possible to apply during pregnancy only in that case when other medicines are inefficient.
Use of salicylates in the I trimester of pregnancy in some retrospective epidemiological researches was associated with the increased risk of development of inborn defects (палатосхиз ("a wolf mouth"), heart diseases). However at prolonged use of drug in the therapeutic doses exceeding 150 mg/days, this risk was low: as a result of the research conducted at 32 000 couples "mother — the child", communication between use of acetylsalicylic acid and increase in amount of inborn defects is not revealed.
Salicylates can be applied in I and II trimesters of pregnancy only after ratio assessment risk/advantage. According to preliminary estimates at prolonged use of Polokard it is desirable not to accept acetylsalicylic acid in the dose exceeding 150 mg/days.
In the III trimester of pregnancy reception of salicylates in high doses (more than 300 mg/days) can lead to a perenashivaniye of pregnancy and weakening of pains at the time of delivery, and also to cardiopulmonary toxicity (premature closings of ductus arteriosus) at children.
Use of acetylsalicylic acid in high doses shortly before childbirth can lead to intracranial bleedings, especially at premature children. Thus, except extremely special cases caused by cardiological or obstetric medical indications on the basis of special monitoring, use of acetylsalicylic acid in the last trimester of pregnancy is contraindicated.
Salicylates and their metabolites get into breast milk in a small amount.
As side reactions at newborns after accidental use Polokard are noted, it is not required to interrupt feeding with a breast, as a rule. At prolonged use of drug or use of acetylsalicylic acid in high doses it is necessary to resolve an issue of the breastfeeding termination.
Children. It is not necessary to use the drugs containing acetylsalicylic acid at children with a SARS which is followed or is not followed by fervescence. At some viral diseases, especially flu A, B and chicken pox, there is a risk of development of a syndrome of Ray which is very rare, but life-threatening disease demanding urgent medical intervention. The risk can be increased if acetylsalicylic acid is applied as the accompanying drug, however relationship of cause and effect in this case is not proved. If such states are followed by long vomiting, it can be a sign of a syndrome of Ray.
Considering the above-stated reasons, aged up to 16 years use of drug without existence of special indications (a disease of Kawasaki) is contraindicated to children.
Influence on ability to manage vehicles and to work with other mechanisms. Does not influence.

Side effects:

Disturbances from a GIT: dyspepsia, pain in epigastric area and an abdominal pain, in some cases — a GIT inflammation, clinical manifestations of an erosive canker of a GIT which can cause in rare instances gastrointestinal hemorrhages and perforation with the corresponding laboratory indicators.
Owing to antiagregantny action on thrombocytes acetylsalicylic acid can increase risk of development of bleedings. Noted such bleedings as intraoperative hemorrhages, hematomas, bleedings from bodies of urinogenital system, nasal bleedings, odontorrhagias, it is rare or very rare — serious bleedings, such as GIT hemorrhages, brain hemorrhages (especially at patients from uncontrollable AG and/or at simultaneous use of anti-hemostatics), in some cases could threaten life potentially.
Hemorrhages can lead to acute and chronic posthemorrhagic anemia / an iron deficiency anemia (owing to the so-called latent microbleeding) with the corresponding laboratory manifestations and clinical symptoms, such as an adynamy, pallor of integuments, hypoperfusion.
At patients with individual hypersensitivity to salicylates development of allergic reactions of skin, including such symptoms as rash, urticaria, hypostasis, an itch is possible. At patients increase in frequency of emergence of a bronchospasm is OH possible; allergic reactions from easy to moderate degree which potentially affect skin, respiratory system, a GIT and cardiovascular system. Very seldom noted heavy reactions, including an acute anaphylaxis.
Seldom — a tranzitorny liver failure with increase in level of transaminases in a liver.
Revealed dizziness and a ring in ears that can demonstrate overdose.

Interaction with other medicines:

Contraindications for interaction
Use of a methotrexate in doses of 15 mg/week and increases hematologic toxicity of a methotrexate above (decrease in renal clearance of a methotrexate by antiinflammatory agents and replacement by methotrexate salicylates from communication with proteins of a blood plasma).
Combinations which should be applied with care
At use of a methotrexate in doses lower than 15 mg/week increase hematologic toxicity of a methotrexate (decrease in renal clearance of a methotrexate by antiinflammatory agents and replacement by methotrexate salicylates from communication with proteins of a blood plasma).
Simultaneous use of an ibuprofen interferes with irreversible oppression of thrombocytes acetylsalicylic acid. Treatment by an ibuprofen of patients with risk of cardiovascular diseases can limit kardioprootektorny effect of acetylsalicylic acid.
At simultaneous use of Polokard and anticoagulants the risk of development of bleeding increases.
At simultaneous use of salicylates in high doses with NPVP (thanks to synergy effect) the risk of developing of ulcers and gastrointestinal bleedings increases.
Simultaneous use with uricosuric means, such as бензобромарон, пробенецид, reduces effect of removal of uric acid (thanks to the competition of removal of uric acid renal tubules).
At simultaneous use with digoxin concentration of the last in a blood plasma increases owing to decrease in renal excretion.
At simultaneous use of acetylsalicylic acid in high doses and peroral antidiabetic drugs from group of derivatives of sulphonylurea or insulin the hypoglycemic effect of the last due to hypoglycemic effect of acetylsalicylic acid and replacement of the sulphonylurea connected with proteins of a blood plasma amplifies.
Diuretics in a combination with high doses of acetylsalicylic acid reduce glomerular filtering thanks to decrease in synthesis of prostaglandins in kidneys.
System GKS (except for a hydrocortisone) which are applied to replacement therapy at Addison's disease, during treatment of GKS reduce the level of salicylates in blood and increase risk of overdose after the end of treatment.
At use with GKS the risk of development of gastrointestinal bleeding increases.
Selective serotonin reuptake inhibitors: the risk of bleeding from upper parts of a GIT because of a possibility of synergy effect increases.
APF in a combination with high doses of acetylsalicylic acid cause decrease in filtering in balls owing to inhibition of vazodilatatorny prostaglandins and decrease in anti-hypertensive effect.
At simultaneous use with valproic acid acetylsalicylic acid forces out it from communication with proteins of a blood plasma, increasing toxicity of the last.
Alcohol promotes injury of a mucous membrane of a GIT and prolongs a bleeding time owing to a synergism of acetylsalicylic acid and alcohol.

Contraindications:

• hypersensitivity to acetylsalicylic acid, other salicylates or any component of drug;
• chronic OH, caused by use of salicylates or NPVP in the anamnesis;
• acute round ulcer;
• hemorrhagic diathesis;
• the expressed renal failure;
• the expressed liver failure;
• the expressed heart failure;
• a combination with a methotrexate in a dose of 15 mg/week or above (see INTERACTIONS).

Overdose:

Salicylates it is possible owing to the chronic intoxication which arose against the background of long therapy (use can result more than 2 days more than 100 mg/kg/days in toxic effects), and also owing to acute intoxication which threatens life (overdose) and which reasons can be, for example, an accidental use by children or unexpected overdose.
Chronic poisoning with salicylates can have the hidden character as signs and symptoms its nonspecific. The moderate chronic intoxication caused by salicylates or a salitsilizm is noted, as a rule, only after repeated receptions in high doses.
The first symptoms of intoxication acetylsalicylic acid are dizziness, nausea, vomiting, a sonitus and increase of breath, balance disturbance.
Also noted other symptoms, such as a hearing loss, a vision disorder, a headache, the strengthened sweating, motor arousing, drowsiness and a coma, spasms, a hyperthermia, confusion of consciousness. At heavy intoxication there come the menacing disturbances of acid-base equilibrium and water and electrolytic exchange (a metabolic acidosis and dehydration).
Moderate or medium-weight toxic symptoms reveal after use of acetylsalicylic acid in a dose 150–300 mg/kg of body weight. Heavy symptoms of poisoning come after reception of a dose of 300-500 mg/kg of body weight. Potentially lethal dose of acetylsalicylic acid makes more than 500 mg/kg of body weight.
Death from intoxication acetylsalicylic acid was noted after reception by the adult of a single dose which makes 10–30 g. The case when the patient survived after reception of 130 g of acetylsalicylic acid is also described.
Actions at overdose
It is necessary to bring the patient to medical institution. There is no specific antidote.
Overdose treatment:

• to provoke vomiting or to carry out a gastric lavage (for the purpose of decrease in absorption of medicine). Such tactics is effective during 3–4 h after medicine reception, and in case of intoxication very high drug dose — even to 10 h;
• to accept absorbent carbon in the form of water suspension (in a dose of 50-100 g for adults and 30–60 g for children) to reduce absorption of acetylsalicylic acid;
• in case of a hyperthermia it is necessary to reduce body temperature by maintenance of low ambient temperature and use of cold compresses;
• it is necessary to carry out careful monitoring of water and electrolytic exchange and quickly to korrigirovat it;
• for the purpose of acceleration of release of acetylsalicylic acid kidneys, and also for treatment of acidosis it is necessary in/in to enter hydrosodium carbonate. It is necessary to support urine pH at the level of 7,0-7,5;
• at very serious poisoning when it is not possible to korrigirovat disturbances of acid-base equilibrium conservative treatment, and also in cases of the accompanying insufficiency of kidneys it is necessary to carry out a hemodialysis or peritoneal dialysis. Dialysis effectively brings acetylsalicylic acid out of an organism, and also facilitates normalization of disturbances of acid-base equilibrium and water and electrolytic exchange;
• in case of increase in a prothrombin time enter vitamin K;
• it is not necessary to accept medicines, the oppressing TsNS, for example barbiturates, considering a possibility of approach of respiratory acidosis and a coma;
• patients with disturbances of breath should provide inflow of fresh air, oxygen supply. If it is necessary, to carry out an intubation of a trachea and to provide IVL;
• in case of approach of shock to carry out standard antishock therapy.

Storage conditions:

In the dry place protected from light at a temperature up to 25 °C.

Issue conditions:

According to the recipe

Packaging:

Tab. enteroраств. 75 mg blister, No. 25.
Tab. enteroраств. 75 mg blister, No. 50.