Acetylsalicylic acid, tablets 500 mg 10 pcs

The drug has analgesic, antipyretic and anti-inflammatory effects.

The mechanism of action of acetylsalicylic acid is based on inhibition of activity of COX-1 and COX-2 cyclooxygenase enzymes, involved in the synthesis of prostaglandins, prostacyclins and thromboxane. As the result the synthesis of prostaglandins providing formation of edema and hyperalgesia is disturbed.

The decrease of prostaglandins (mainly E1) in the thermoregulation center leads to decrease of the body temperature due to expansion of the skin vessels and increased sweating processes.

The analgesic effect is due to both central (influence on the centers of pain sensitivity) and peripheral (reduction of bradykinin algogenic activity) action.

The anti-inflammatory activity of the preparation is caused by decrease of prostaglandins synthesis, capillaries permeability reduction, decrease of hyaluronidase activity and limitation of energy supply of inflammatory process by inhibition of adenosine triphosphoric acid formation.

Decreases aggregation and adhesion of platelets and inhibits the process of thrombosis by inhibiting the synthesis of thromboxane A2 in platelets.

Blockade of COX-1 in gastric mucosa leads to inhibition of synthesis of gastro-protective prostaglandins, which may contribute to gastric mucosa ulceration and subsequent bleeding.

Indications

Active ingredient

Composition

Active substance:

Acetylsalicylic acid – 500 mg.

Auxiliary substances:

potato starch – 72.1 mg,

citric acid – 0.2 mg,

stearic acid – 6.0 mg,

talc – 12.7 mg,

How to take, the dosage

Ingestion, adults and children over 12 years of age: a single dose is 0.5 g, maximum single dose is 1.0 g (2 0.5 g tablets), maximum daily dose is 3.0 g (6 0.5 g tablets).

How to use: The drug should be taken after a meal with water, milk or alkaline mineral water.

Frequency and timing of administration: A single dose may be taken 3-4 times a day with an interval of at least 4 hours, if necessary. Regular adherence to the regimen of taking the drug helps to avoid a spike in fever and reduce the intensity of pain syndrome.

The duration of treatment (without consulting a doctor) should not exceed 5 days when prescribed as an analgesic and more than 3 days as an antipyretic.

Interaction

Co-administration:

– with methotrexate at a dose of 15 mg per week or more: increased hemolytic cytotoxicity of methotrexate (decreased renal clearance of methotrexate and methotrexate is replaced by salicylates in binding to plasma proteins);

– with indirect anticoagulants and heparin: increased risk of bleeding due to inhibition of platelet function, gastrointestinal mucosal damage, displacement of anticoagulants (oral) from binding to plasma proteins;

– with other non-steroidal anti-inflammatory drugs: synergistic interaction increases the risk of gastric ulceration and bleeding;

– with uricosuric drugs, such as benzbromaron: decreases the uricosuric effect;

– with digoxin: digoxin concentrations are increased due to decreased renal excretion;

– – enhances the effects of oral hypoglycemic drugs;

– with drugs of the thrombolytic group: the risk of bleeding increases;

– with systemic glucocorticosteroids, excluding hydrocortisone used as replacement therapy for Addison’s disease: glucocorticosteroids decrease blood levels of salicylates by increasing the excretion of the latter;

– with angiotensin-converting enzyme inhibitors: decreases glomerular filtration due to inhibition of prostaglandins and, consequently, decreases the antihypertensive effect;

– with valproic acid: increased toxicity of valproic acid;

– with ethanol (alcoholic beverages): increases the risk of damaging effects on gastrointestinal mucosa and increases the risk of gastrointestinal bleeding;

– increases the effects of narcotic analgesics, thrombolytics and platelet aggregation inhibitors, sulfonamides (including co-trimoxazole);

– increases the plasma concentration of barbiturates, lithium salts;

– antacids containing magnesium and/or aluminum slow down and impair absorption of acetylsalicylic acid;

– myelotoxic drugs increase the manifestations of hematotoxicity of the drug;

– enhances the effects of triiodothyronine;

– reduces the effect of hypotensive drugs, diuretics (spironolactone, furosemide).

Glucocorticoids, ethanol and ethanol-containing drugs increase the damaging effect of acetylsalicylic acid on the gastrointestinal mucosa, increase the risk of gastrointestinal bleeding.

Special Instructions

Acetylsalicylic acid may cause bronchospasm, an attack of bronchial asthma or other hypersensitivity reactions. Risk factors include the presence of bronchial asthma, nasal polyps, fever, chronic bronchopulmonary disease, history of allergies (allergic rhinitis, skin rashes).

Acetylsalicylic acid may increase the tendency to bleeding, which is associated with its inhibitory effect on platelet aggregation. This should be considered when surgical interventions are necessary, including minor interventions such as tooth extraction. Before surgical intervention, in order to reduce bleeding during surgery and in the postoperative period, the drug administration should be stopped 5-7 days in advance and the physician should be informed.

In children with acute viral infections, drugs containing acetylsalicylic acid should not be prescribed because the risk of Reye’s syndrome increases if there is a viral infection. Symptoms of Reye syndrome include prolonged vomiting, acute encephalopathy, and enlarged liver.

Breastfeeding should be discontinued if the drug has to be used during lactation.

Acetylsalicylic acid reduces excretion of uric acid from the body, which may cause an acute attack of gout in predisposed patients. No effect of taking the drug on driving motor transport and other mechanisms has been found.

At the time of treatment it is necessary to refrain from taking ethanol.

Impact on driving and operating machinery

At the time of treatment, caution should be exercised while driving vehicles and engaging in potentially hazardous activities requiring increased concentration and psychomotor reactions, as the use of the drug acetylsalicylic acid may cause dizziness in rare cases.

Contraindications

– hypersensitivity to acetylsalicylic acid and other nonsteroidal anti-inflammatory drugs or other components of the drug;

– gastrointestinal erosive-ulcerative lesions (acute phase), gastrointestinal bleeding;

– bronchial asthma induced by taking salicylates and nonsteroidal anti-inflammatory drugs;

Hemorrhagic diathesis;

Combined use of methotrexate at a dose of 15 mg or more per week;

Pregnancy, breastfeeding;

– combination of bronchial asthma, recurrent polyposis of the nose and sinuses, and intolerance to acetylsalicylic acid;

– children under 12 years of age (for this dosage form).

The drug is not indicated in children under 15 years of age with acute respiratory diseases caused by viral infections due to the risk of Reye’s syndrome (encephalopathy and acute fatty liver dystrophy with acute development of liver failure).

With caution – with concomitant therapy with anticoagulants, gout, gastric and/or duodenal ulcer (history), including chronic or recurrent ulcer disease, or episodes of gastrointestinal bleeding; renal and/or hepatic insufficiency, glucose-6-phosphate dehydrogenase deficiency; hyperuricemia, bronchial asthma, chronic obstructive pulmonary disease, hay fever, nasal polyposis, drug allergy, concomitant administration of methotrexate at a dose less than 15 mg/week, pregnancy.

Side effects

Gastrointestinal tract: decreased appetite, diarrhea, abdominal pain, heartburn,nausea, vomiting, overt (vomiting with blood, tarry stools) or latent signs of gastrointestinal bleeding, which may lead to iron deficiency anemia, gastrointestinal erosive ulcerative lesions (including with perforation), single cases – liver function disorders (increased liver transaminases).

Central nervous system disorders: dizziness, tinnitus (usually a sign of overdose).

Hematopoietic system disorders: increased risk of bleeding, which is a consequence of the effect of acetylsalicylic acid on platelet aggregation, thrombocytopenia, anemia, leukopenia.

Allergic reactions: skin rash, anaphylactic reactions, bronchospasm, Quincke’s edema.

Urinary system disorders: impaired renal function.

Others: when taken as an antipyretic agent – Reye syndrome (encephalopathy and acute fatty liver dystrophy with rapid development of liver failure).

Overdose

Symptoms

Moderate overdose: nausea, vomiting, tinnitus, hearing loss, headache, dizziness and confusion.

Severe overdose: fever, hyperventilation, ketoacidosis, respiratory alkalosis, metabolic acidosis, coma, cardiogenic shock, respiratory failure, severe hypoglycemia.

Treatment: Hospitalization, gastric lavage, administration of activated charcoal, monitoring of acid-base balance, alkaline diuresis to obtain urine pH between 7.5-8 (forced urine alkalinization is considered achieved if plasma salicylate concentration is more than 500 mg/L (3.6 mmol/L) in adults or 300 mg/L (2.2 mmol/L) in children), hemodialysis, fluid loss compensation, symptomatic therapy.

Similarities