Acetylsalicylic acid tab.0,5 No. 10

General characteristics. Structure:

Active ingredient: acetylsalicylic acid; 1 tablet contains acetylsalicylic acid 500 mg; excipients: cellulose powdery, starch corn.

Pharmacological properties:

Drug has febrifugal, analgeziruyushchy and antiinflammatory effect, and also reduces aggregation of thrombocytes. The inactivation of enzyme of cyclooxygenase (TsOG) therefore synthesis of prostaglandins, prostacyclins and thromboxane is broken is the main mechanism of effect of acetylsalicylic acid. Owing to reduction of products of prostaglandins their pyrogenic influence on the centers of thermal control weakens. Besides, the sensibilizing effect of prostaglandins decreases by the sensitive nerve terminations causing decrease in their sensitivity to pain mediators. Irreversible disturbances of synthesis in thrombocytes of A2 thromboxane cause antiagregantny effect of drug. Acetylsalicylic acid also blocks TsOG of endothelial cells in which the prostacyclin having antiagregantny activity is synthesized. TsOG of endothelial cells is less sensitive to effect of acetylsalicylic acid and, unlike similar enzyme of thrombocytes, is blocked reversibly.
After use acetylsalicylic acid turns into the main metabolite – salicylic acid. Absorption of acetilsalicylic and salicylic acids in a digestive tract happens quickly and completely. The maximum level of concentration in a blood plasma is reached in 10-20 minutes (acetylsalicylic acid) or 45-120 minutes (the general level of salicylates). Extent of binding of acids proteins of plasma depends on concentration, it makes 49-70% for acetylsalicylic acid and 66-98% – for salicylic. 50% of the entered dose of drug are metabolized at primary passing through a liver. Gentisic acid and it глицинконъюгат is metabolites of acetilsalicylic and salicylic acids глицинконъюгат salicylic acid. Drug is removed from an organism in the form of metabolites, preferential by kidneys. The elimination half-life of acetylsalicylic acid makes 20 minutes. The elimination half-life of salicylic acid increases in proportion to the accepted dose of drug and makes 2, 4 and 20 hours for doses of 0,5 g, 1 g and 5 g according to. Drug gets through a blood-brain barrier, and also is defined in breast milk and synovial fluid.

Indications to use:

Symptomatic treatment of a pain syndrome of weak and average intensity of various genesis (including inflammatory); feverish states; rheumatic diseases.

Route of administration and doses:

Acetylsalicylic acid is accepted orally, after food. Tablets can be crushed before reception or to swallow whole, washing down with a large amount of liquid.
Drug is appointed to adults and children 15 years – 500-1000 mg as a single dose are more senior. Repeated reception is possible in 4-8 hours. The maximum daily dose should not exceed 4 g.

Features of use:

Drug is not appointed to children with acute respiratory diseases, caused by viral infections, because of risk of development of a syndrome of Ray (encephalopathy and acute fatty dystrophy of a liver with acute development of a liver failure).
Acetylsalicylic acid is applied with care: at simultaneous treatment by anticoagulants; chronic ulcers of digestive tract, including chronic or recurrent peptic ulcers or chronic gastrointestinal bleedings; disturbances of functions of kidneys and/or liver; hypersensitivity to NPVS; the acute respiratory viral infection (ARVI) which can serve as the reason of development of a syndrome of Ray.
In the patients having allergic diseases, including bronchial asthma, allergic rhinitis, a small tortoiseshell, a skin itch, hypostasis of a mucous membrane and polyposes of a nose and also at their combination to persistent infections of respiratory tracts and in patients with hypersensitivity to NPVS against the background of treatment with acetylsalicylic acid development of attacks of bronchial asthma is possible.
At surgeries (including dental) use of the drugs containing acetylsalicylic acid can increase probability of strengthening of bleeding.
At use of small doses acetylsalicylic acid can reduce removal of uric acid. It can lead to developing of gout in the patients having lowered removal of uric acid.

Use during pregnancy or feeding by a breast.
Acetylsalicylic acid in this dosage do not apply in І and ІІІ trimesters pregnancy because of threat of a perenashivaniye of pregnancy and weakening of pains at the time of delivery, and also the increased risk of cardiopulmonary toxicity (premature closing of ductus arteriosus), inborn defects and intracranial bleedings (especially at premature children).
Use of drug in ІІ a trimester of pregnancy is admissible taking into account a ratio advantage for mother/risk for a fruit.
During treatment it is necessary to stop feeding by a breast.

Ability to influence speed of response at control of motor transport or work with other mechanisms. Influence is improbable, however it is necessary to consider a possibility of dizziness.

Children. Drug in this dosage is used to children aged from 15 years.
Acetylsalicylic acid is not appointed to children with acute respiratory diseases, caused by viral infections, because of risk of development of a syndrome of Ray (encephalopathy and acute fatty dystrophy of a liver with acute development of a liver failure).

Side effects:

Digestive tract: nausea, anorexia, pain in epigastric area. In some cases, especially at frequent and long use of drug, emergence of the erosive cankers of a digestive tract sometimes complicated by the latent or clinically expressed (melena) bleeding is possible.
Central nervous system: dizziness and sonitus.
Hemopoietic system: development of thrombocytopenia, anemia (as a result of the concealed hemorrhage from a digestive tract).
Allergic reactions: rash, a bronchospasm (especially in patients with bronchial asthma).

Interaction with other medicines:

At simultaneous use of acetylsalicylic acid and anticoagulants the risk of development of bleeding increases. At simultaneous use of acetylsalicylic acid and non-steroidal anti-inflammatory drugs therapeutic and side effects of the last amplify.
Use together with acetylsalicylic acid of a methotrexate in a dose of 15 mg a week and more increases hematologic toxicity of a methotrexate (decrease in renal clearance to a methotrexate by antiinflammatory agents and replacement by methotrexate salicylates from communication with blood plasma proteins).
Against the background of treatment by acetylsalicylic acid side effect of a methotrexate increases.
At simultaneous use of acetylsalicylic acid and peroral anti-diabetic drugs from group of derivatives of sulphonylurea the hypoglycemic effect of the last amplifies. At simultaneous use with corticosteroids the risk of development of gastrointestinal bleeding increases. Acetylsalicylic acid reduces action of Spironolactonum, the furosemide, anti-hypertensive drugs and means promoting removal of uric acid. Use of antiacid drugs against the background of treatment by acetylsalicylic acid (especially in the doses exceeding 3 g of acetylsalicylic acid) can cause decrease in high constant level of salicylates in blood.
Alcohol promotes injury of a mucous membrane of digestive tract and prolongs a bleeding time owing to a synergism of acetylsalicylic acid and alcohol.

Contraindications:

Hypersensitivity to acetylsalicylic acid or to any other component of drug, hypersensitivity to other salicylates;
asthma caused by use of salicylates or other non-steroidal anti-inflammatory drugs (NPVS) the anamnesis;
active round ulcer of a stomach and duodenum;
hemorrhagic diathesis, the increased tendency to bleedings;
the expressed renal failure;
the expressed liver failure;
the expressed heart failure;
the combined use with a methotrexate in a dosage of 15 mg a week or is more (see the section "Interaction with Other Medicines or Other Types of Interactions");
І and III trimester of pregnancy, feeding period breast;
children's age up to 15 years (for this dosage).

Overdose:

Symptoms: at intoxication of easy degree nausea, vomiting, pain in epigastric area, and also (especially in patients of advanced age) feeling of a sonitus, dizziness, decrease in visual acuity and hearing are possible.
At considerable overdose disturbances of thinking, confusion of consciousness, drowsiness, a collapse, a tremor, an otdyshka, dehydration, a hyperthermia, a coma, alkali reaction of urine, a metabolic acidosis, a respiratory alkalosis, disturbance of carbon exchange are noted. The lethal dose of acetylsalicylic acid for adults exceeds 10 g.
The overdose is especially dangerous to patients of advanced age as it can lead to a lethal outcome.
Treatment: immediate hospitalization; gastric lavage, use of absorbent carbon, check of acid-base balance; depending on a condition of acid-base equilibrium and electrolytic balance carry out infusional administration of solutions of Natrii hydrocarbonas, sodium of citrate and sodium of a lactate; at рН urine from 7,5 to 8,0 and contents of salicylates in plasma more than 500 mg/l apply an intensive care alkaline diuretics; at serious poisonings the hemodialysis is shown; liquid loss replenishment; symptomatic treatment.

Storage conditions:

To store at a temperature not over 30 to °s.khranit in the place, unavailable to children.

Period of validity - 3 years.

Issue conditions:

Without recipe

Packaging:

On 10 tablets in blisters. 1 blister in a pack from a cardboard.