Аспикор®

General characteristics. Structure:

Active ingredient: 0,1 g of acetylsalicylic acid.

Excipients: cellulose microcrystallic, lactoses monohydrate, croscarmellose sodium, silicon dioxide colloid (aerosil), stearic acid.

Kishechnorastvorimy cover: methacrylic acid and ethyl acrylate copolymer (methacrylic acid copolymer), propylene glycol, macrogoal 4000 (polyethyleneglycol 4000, poly(ethylene oxide) 4000), titanium dioxide, talc.

Pharmacological properties:

Pharmacodynamics. Аспикор® at the expense of active active ingredient - acetylsalicylic acid - at prolonged use in low doses has antiagregantny effect. The main mechanism of effect of acetylsalicylic acid - a non-selective inactivation of enzyme of cyclooxygenase (TsOG) therefore synthesis of prostaglandins is broken, prostacyclins endothelial cells (in doses more than 300 mg) and A2 thromboxane in thrombocytes that causes antiagregantny effect of drug. Acetylsalicylic acid can make also other impacts on blood coagulation process, increasing fibrinolitic activity and reducing concentration in blood of blood-coagulation factors, dependent on vitamin K (II, VII, IX, X). As well as other drugs of acetylsalicylic acid, in higher doses of Aspikor® has antiinflammatory, febrifugal, analgeziruyushchy effect.

The Antiagregantny effect remains during 7 days after a single dose (it is more expressed at men, than at women). Reduces a lethality and risk of development of a myocardial infarction at unstable stenocardia. It is effective at primary prevention of diseases of cardiovascular system, especially at men 40 years are more senior than a myocardial infarction, and at secondary prevention of a myocardial infarction.

Pharmacokinetics. At intake absorption full. During absorption is exposed to system elimination in a wall of intestines and in a liver it (is deacetylated). The absorbed part quickly is hydrolyzed by cholinesterases of plasma and albuminesterase therefore the poluvy-maintaining period no more than 15-20 min. Acetylsalicylic acid is soaked up in proximal department of a small bowel. The maximum concentration in a blood plasma is noted on average in 3 hours after administration of drug inside. In an organism circulates (for 75-90% in connection with albumine) and it is distributed in fabrics in the form of anion of salicylic acid.

Serumal concentration of salicylates is very variable. At newborn children salicylates can force out bilirubin from communication with albumine and promote development of bilirubinovy encephalopathy. Salicylates easily get into many fabrics and liquids of an organism, including into spinal, peritoneal and synovial liquids. Penetration into a cavity of a joint accelerates in the presence of a hyperemia and hypostasis and is slowed down in a proliferative phase of an inflammation.

In small amounts salicylates are found in nervous tissue, traces - in bile, sweat, excrements. When developing acidosis the most part of salicylate turns into not ionized acid which is well getting into fabrics including, into a brain. Quickly passes through a placenta, in small amounts it is removed with breast milk.

Salicylic acid is metabolized preferential in a liver with formation of 4 metabolites found in many fabrics and urine.

It is removed preferential by active secretion in tubules of kidneys in the form of actually salicylic acid (60%) and its metabolites. Removal of not changed salicylate depends on urine pH (at alkalinization of urine the ionizirovaniye of salicylates increases, their reabsorption worsens and considerably removal increases). Speed of removal depends on a dose: at reception of small doses the elimination half-life of 2-3 h, with increase in a dose can increase up to 15-30 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, arterial hypertension, obesity, smoking, advanced age), a repeated myocardial infarction and at suspicion of an acute myocardial infarction.
- Unstable 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 of carotid arteries).
- Prevention of a deep vein thrombosis and thromboembolism of a pulmonary artery and its branches (for example, at a long immobilization as a result of big surgical intervention).

Route of administration and doses:

Аспикор® it is necessary to accept inside, before food, without chewing, washing down with big amount of liquid. Drug is intended for prolonged use. Duration of therapy is defined by the attending physician.

Prevention at suspicion of an acute myocardial infarction
100-200 mg/days (the first tablet needs to be chewed for more bystry absorption).

Prevention of primary acute myocardial infarction with risk factors - 100 mg/days.

Prevention of a repeated myocardial infarction. Unstable stenocardia. Prevention of a stroke and passing disturbance of cerebral circulation. Prevention of tromboembolic episodes after surgeries or invasive researches - 100-300 mg/days.

Prevention of a deep vein thrombosis and thromboembolism of a pulmonary artery and its branches - 100-200 mg/days.

Features of use:

Acetylsalicylic acid can provoke a bronchospasm, and also cause attacks of bronchial asthma and other reactions of hypersensitivity. 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).

Acetylsalicylic acid can cause bleedings of various degree of expressiveness in time and after surgical interventions.

Acetylsalicylic acid in low doses can provoke development of gout in the predisposed persons (having reduced excretion of uric acid).

High doses of acetylsalicylic acid render hypoglycemic effect that patients need to mean at appointment it with the diabetes mellitus receiving hypoglycemic drugs.

At the combined use of GKS and salicylates it is necessary to remember that during treatment concentration of salicylates in blood is reduced, and after cancellation of GKS it is possible передозиров salicylates.

The combination of acetylsalicylic acid to an ibuprofen as the last worsens beneficial effect of Аспикора on life expectancy is not recommended.

Exceeding of a dose of acetylsalicylic acid is accompanied by risk of gastrointestinal bleeding.

Influence on control of vehicles and mechanisms. During administration of drug it is necessary to manage with care transport means and to be engaged in other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Use at pregnancy and in the period of a lactation. Use of high doses of salicylates in the first 3 months of pregnancy is associated with the increased frequency of defects of fetation (the split sky, heart diseases). In the II trimester of pregnancy it is possible to appoint salicylates only taking into account strict assessment of risk for a fruit and advantage for mother.

In the last trimester of pregnancy salicylates in a high dose (more than 300 mg/days) 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 last trimester of pregnancy is contraindicated.

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

Side effects:

Allergic reactions (small tortoiseshell, Quincke's edema), anaphylaxis; nausea, heartburn, vomiting, abdominal pain, ulcers of a mucous membrane of a stomach and a 12-perstny gut, including with perforation, gastrointestinal bleeding; increase in activity of "hepatic" enzymes; bronchospasm; the raised bleeding, anemia; dizziness, sonitus.

Interaction with other medicines:

Аспикор® at simultaneous use strengthens effect of the following medicines:
- a methotrexate due to decrease in renal clearance and its replacement from communication with proteins of plasma;
- heparin and indirect anticoagulants due to dysfunction of thrombocytes and replacement of indirect anticoagulants from communication with proteins of plasma;
- thrombolytic and antiagregantny drugs (tiklopidin);
- digoxin owing to decrease in its renal excretion;
- hypoglycemic means (insulin and derivatives of sulphonylurea) due to hypoglycemic properties of the most acetylsalicylic acid in high doses and replacement of derivatives of sulphonylurea from communication with proteins of plasma;
- valproic acid due to its replacement from communication with proteins of plasma;
- other non-steroidal anti-inflammatory drugs;
- hypotensive medicines, diuretics (Spironolactonum, furosemide).

The combination of acetylsalicylic acid to anticoagulants, trombolitika and antiagre-gantny drugs is followed by the increased risk of development of bleeding.

The combination of acetylsalicylic acid to a methotrexate is followed by the increased frequency of development of side effects from bodies of a hemopoiesis.

Ethanol and etanolsoderzhashchy лекарственнык means increase the damaging action by a mucous membrane of digestive tract, increase risk of development of gastrointestinal bleedings. Acetylsalicylic acid weakens effect of uricosuric drugs (a benzbromaron, a sudfinpirazon) owing to competitive tubular elimination of uric acid.

Strengthening elimination of salicylates, system glucocorticosteroids (GKS) weaken their action. Increases concentration of digoxin, barbiturates, lithium salts in plasma.

The antacids containing magnesium and/or aluminum slow down and worsen absorption of acetylsalicylic acid. Miyelotoksichny medicines strengthen manifestations of a gematotoksichnost of drug.

Contraindications:

- Hypersensitivity to components of drug and other non-steroidal anti-inflammatory drugs (NPVP).
- Digestive tract erosive cankers; gastrointestinal bleeding.
- Hemorrhagic diathesis.
- The bronchial asthma induced by reception of salicylates and NPVP, Fernán-Vidal's triad (a full or incomplete combination of bronchial asthma, the nose recuring a polypose and okolonosovy bosoms and intolerance of acetylsalicylic acid).
- The combined use with a methotrexate in a dose of 15 mg a week and more.
- Deficit of lactase, lactose intolerance, glyukozo-galaktozny malabsorption.
- Pregnancy (I and III trimester) and lactation period.
- Age up to 18 years.

With care. At gout, a hyperuricemia, in the presence in the anamnesis: cankers of digestive tract or gastrointestinal bleedings, renal and hepatic insufficiency, bronchial asthma, chronic diseases of a respiratory organs, hay fever, polypose of a nose, medicinal allergy; in the II trimester of pregnancy; in a combination to a methotrexate in a dose less than 15 mg a week; deficit of vitamin K and glyukozo-6-fosfatdegidrogenazy.

Overdose:

Symptoms (the single dose less than 150 mg/kg - acute poisoning is considered a lung, 150-300 mg/kg - moderate, more than 300 mg/kg - heavy): a salitsilizm syndrome (nausea, vomiting, a sonitus, a vision disorder, dizziness, a severe headache, the general indisposition, fever - a bad predictive sign at adults). A serious poisoning - a hyperventilation of lungs of the central genesis, a respiratory alkalosis, a metabolic acidosis, the confused consciousness, drowsiness, a collapse, spasms, an anury, bleedings. Originally central hyperventilation of lungs leads to a respiratory alkalosis - short wind, suffocation, cyanosis, a cold clammy sweat; with strengthening of intoxication the paralysis of breath and dissociation of oxidizing phosphorylation causing respiratory acidosis accrues.

At chronic overdose the concentration defined in plasma badly correlates with severity of intoxication. The greatest risk of development of chronic intoxication is noted at elderly people at reception within several days more than 100 mg/kg/days. At patients of advanced age initial signs of a salitsilizm are not always noticeable therefore it is reasonable to determine periodically the content of salicylates in blood: concentration higher than 70 mg of % testifies to moderate or heavy poisoning; higher than 100 mg % extremely heavy, predictively adverse. At poisoning of average and heavy degree hospitalization is necessary.

Treatment: provocation of vomiting, purpose of absorbent carbon and laxatives, constant control behind an acid-base state and electrolytic balance; in dependence on a condition of a metabolism - introduction of Natrii hydrocarbonas, solution of sodium of citrate or sodium of a lactate. Increase in reserve alkalinity strengthens removal of acetylsalicylic acid due to urine alkalinization. Alkalinization of urine is shown at concentration of salicylates higher than 40 mg of % and is provided in/in infusion of sodium of a gidrokar-bonat (88 мЭкв in 1 l of 5% of solution of a dextrose, with a speed of 10-15 ml/h/kg); recovery of volume of the circulating blood and induction of a diuresis are reached by introduction of Natrii hydrocarbonas in the same doses and cultivation which is repeated by 2-3 times.

It is necessary to be careful at elderly patients at whom intensive infusion of liquid can lead to a fluid lungs. Use of acetazoleamide for urine alkalinization is not recommended (can cause acidosis and strengthen toxic effect of salicylates). The hemodialysis is shown at concentration of salicylates more than 100-130 mg of %, patients with chronic poisoning have 40 mg of % and below in the presence of indications (refractory acidosis, the progressing aggravation of symptoms, severe damage of the central nervous system, a fluid lungs and a renal failure). At a fluid lungs — artificial ventilation of the lungs  by the mix enriched with oxygen.

Storage conditions:

In the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity 2 years. Not to use after a period of validity.

Issue conditions:

Without recipe

Packaging:

The tablets covered with a kishechnorastvorimy cover, 100 mg. On 10 or 20 tablets in a blister strip packaging from a film of polyvinyl chloride and aluminum foil. 1, 2, 3 or 6 blister strip packagings on 10 tablets or 3 blister strip packagings on 20 tablets together with the application instruction in a pack from a cardboard.