Acetylsalicylic acid - instructions for use, dose, side effects, contraindications

Has anti-inflammatory, analgesic and antipyretic effects associated with the suppression of cyclooxygenase 1 and 2, regulating the synthesis of prostaglandins.

Reduces aggregation, adhesiveness, platelets and thrombus formation due to persistence for 7 days after a single dose (more pronounced in men, than in women).

Pharmacokinetics:

When taken orally, the absorption is complete.The absorbed part is quickly hydrolyzed by non-specific cholinesterases of plasma and albumin esterase, therefore the elimination half-life is no more than 15-20 minutes. In the body it circulates (75% due to albumin) and is distributed in tissues as an anion of salicylic acid.

The time to reach the maximum concentration is 2 hours. Serum Concentration salicylates is variable. Salicylates easily penetrate into many tissues and body fluids, including spinal, peritoneal and synovial fluids. Penetration into the joint cavity is accelerated when presence of hyperemia and edema and slows down in the proliferative phase of inflammation. In small amounts, salicylates are found in the nervous tissue, traces in bile, sweat, feces. When acidosis occurs, most of the salicylic acid is converted to a non-ionized acid that penetrates well into the tissue, including the brain. Penetrates through the placenta and into breast milk.

Metabolized mainly in the liver. It is excreted through the kidneys - in the form of salicylic acid (60%) and in the form of metabolites. Excretion depends on the pH of the urine (urine alkalinization significantly increases excretion).The rate of excretion depends on the dose: when taking small doses, the elimination half-life is 2-3 hours, with an increase in the dose it can increase to 15-30 hours.

Indications:

Pain syndrome is mild or mild, of different origins (headache pain, toothache, back and muscle pain, joint pain, menstruation pain) - in adults and children over 6 years old.

Elevated body temperature for colds and other infectious-inflammatory diseases in adults and children older than 15 years.

Contraindications:

- Hypersensitivity to acetylsalicylic acid and other NSAIDs or other components of the drug;

- erosive and ulcerative lesions of the gastrointestinal tract (in the phase of exacerbation);

- gastrointestinal bleeding;

- hemorrhagic diathesis;

- simultaneous reception of methotrexate in a dose of 15 mg per week or more;

- bronchial asthma induced by the intake of salicylates or other NSAIDs, a combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid;

- pregnancy (I and III trimester), the period of breastfeeding.

The drug is not prescribed as an antipyretic agent for children under 15 years of age with acute respiratory infections caused by viral infections, because of risk of development of Reye's syndrome (encephalopathy and acute fatty liver dystrophy with acute development of hepatic insufficiency) and as an analgesic funds for children under 6 years.

Carefully:

With concomitant therapy with anticoagulants, gout, peptic ulcer and / or duodenal ulcer (in the anamnesis), including chronic or recurrent ulcer disease, hyperuricemia, bronchial asthma, chronic obstructive pulmonary disease, hay fever, nasal polyposis, drug allergy, concurrent administration of methotrexate in a dose of less than 15 mg per week, second trimester of pregnancy, renal and / or liver failure, deficiency glucose-6-phosphate dehydrogenase.

Pregnancy and lactation:

Has a teratogenic effect; when applied in the first trimester leads to the development of splitting of the upper sky; in the III trimester causes inhibition of labor (inhibition of synthesis Pg), premature closure of the arterial duct in the fetus, hyperplasia of pulmonary vessels and hypertension in the "small" circle of blood circulation. Excreted in breast milk, which increases the risk of bleeding in the child due to impaired functionthrombocytes.

If you need to use the drug during lactation, breastfeeding should be discontinued.

Dosing and Administration:

With pain syndrome weak and medium intensity in adults and children over 12 years, a single dose is 0.5 g, the maximum single dose is 1 g, the maximum daily dose should not exceed 3 g. The intervals between doses of the drug should be at least 4 hours.

Children aged 6 to 12 years as an anesthetic, single dose is 250 mg per reception, taken up to 3 times a day.

As an antipyretic agent for colds and other infectious and inflammatory diseases in adults and children over 15 years, a single dose is 0.5 g, the maximum single dose is 1 g, the maximum daily dose should not exceed 3 g. The intervals between doses of the drug should be at least 4 hours.

To reduce the irritant effect on the gastrointestinal tract, the drug should be taken after meals, washed down with water, milk, alkaline mineral water.

The duration of treatment (without consulting a doctor) should not exceed 5 days with an appointment as an anesthetic and more than 3 days - as antipyretics.

Side effects:

Nausea, decreased appetite, gastralgia, diarrhea; allergic reactions (skin rash, angioedema, bronchospasm); impaired liver and / or kidney function; thrombocytopenia, anemia, leukopenia, Reye's syndrome (encephalopathy and acute fatty liver disease with rapid development of hepatic insufficiency).

With prolonged use - dizziness, headache, vomiting, erosive ulcerative lesions of the gastrointestinal tract (GIT), hypocoagulation, bleeding (including in the gastrointestinal tract), visual impairment, decreased hearing aches, tinnitus, bronchospasm, interstitial nephritis, prerenal azotemia with hypercreatinemia and hypercalcemia, papillary necrosis, acute renal failure, nephrotic syndrome, aseptic meningitis, increased symptoms of chronic cardiac insufficiency (CHF), edema, increased activity of "liver" transaminases.

Overdose:

Symptoms

Overdose of moderate severity: nausea, vomiting, tinnitus, hearing impairment, headache, dizziness and confusion. These symptoms occur with a decrease in the dose of the drug.

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

With chronic overdose the concentration determined in plasma does not correlate well with the severity of intoxication. The greatest risk of developing chronic intoxication is observed in the elderly with the intake of a few days more than 100 mg / kg / day. In children and the elderly, patients with initial signs salicylism is not always noticeable, so it is advisable to periodically determine the concentration of salicylates in the blood: a concentration above 70 mg% indicates moderate or severe poisoning; above 100 mg% - about extremely severe, prognostically unfavorable. When poisoning the moderate and severe degree of severity, hospitalization is necessary.

Treatment: hospitalization, gastric lavage, reception of activated charcoal, monitoring of acid-base balance, alkaline diuresis in order to obtain a urine pH between 7.5-8 (forced alkaline diuresis is considered achieved if the concentration of salicylate in the blood plasma 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.Caution should be exercised in elderly patients in whom intensive fluid infusion can lead to pulmonary edema. It is not recommended to use acetazolamide for alkalinization of urine (can cause acidosis and enhance the toxic effect of salicylates). Hemodialysis is indicated at a salicylate concentration of more than 100-130 mg%, in patients with chronic poisoning - 40 mg% and lower in the presence of indications (refractory acidosis, progressive deterioration, severe central nervous system damage, pulmonary edema and kidney failure). When swelling of the lungs - artificial ventilation of the lungs with a mixture enriched with oxygen.

Interaction:

Acetylsalicylic acid increases the toxicity of methotrexate, reducing its renal clearance, valproic acid; enhances the effects of narcotic analgesics, other NSAIDs, oral hypoglycemic drugs, heparin, indirect anticoagulants, thrombolytics and antiaggregants, sulfonamides (including co-trimoxazole), triiodothyronine; reduces the effect of uricosuric drugs (benzbromarone, sulfinpyrazone), antihypertensive drugs and diuretics (spironolactone, furosemide). Glucocorticosteroids, ethanol and ethanol containing drugs increase the damaging effect on the gastrointestinal mucosa, increase the risk of developing gastrointestinal bleeding.

Acetylsalicylic acid increases the concentration of digoxin, barbiturates and lithium salts in blood plasma.

Antacids containing Mg²⁺, and / or Al³⁺, slow down and worsen the absorption of acetylsalicylic acid. Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

Special instructions:

Acetylsalicylic acid can cause bronchospasm, an attack of bronchial asthma or other hypersensitivity reactions. Risk factors are the presence of bronchial asthma, polyps of the nose, fever, chronic bronchopulmonary diseases, cases of allergy in the anamnesis (allergic rhinitis, skin rashes). Acetylsalicylic acid can increase the tendency to bleeding, which is due to its inhibitory effect on platelet aggregation. This should be taken into account when necessary surgical interventions, including such minor interventions as tooth extraction. Before surgical intervention to reduce bleeding during surgery and in the post-operation period, you should cancel taking the drug for 5-7 days and inform the doctor.

Children should not prescribe drugs containing acetylsalicylic acid, because in the case of a viral infection, the risk of developing Ray's syndrome increases. Symptoms of Ray's syndrome are prolonged vomiting, acute encephalopathy, enlargement of the liver.

During the treatment it is necessary to refrain from taking ethanol.

Acetylsalicylic acid reduces the excretion of uric acid from the body, which can cause an acute attack of gout in predisposed patients.

Effect on the ability to drive transp. cf. and fur:There was no evidence of the effect of drug administration on vehicle management and other mechanisms.

Form release / dosage:Tablets 250 mg, 500 mg.

Packaging:

10 tablets per contour cell pack.

For 10, 30, 50 or 100 tablets in a jar of polymer materials.

Each jar or 1, or 2, or 3, or 5, or 10 contour cell packs of 10 tablets together with instructions for use in the pack.

For 10 tablets in a contour non-cellular package of paper with a polymer coating. Contour non-cellular packages with instructions for use are placed directly in the group package.

Storage conditions:

In a dry place. Keep out of the reach of children.

Shelf life:4 years. Do not use after the time specified on the package.

Terms of leave from pharmacies:Without recipe

Registration number:LS-001338

Date of registration:25.07.2011 / 29.12.2014

Expiration Date:Unlimited

The owner of the registration certificate:PHARMACY 36.6, CJSC PHARMACY 36.6, CJSC Russia

Manufacturer: & nbsp

MEGA PHARM, CJSC Russia

VEROPHARM SA Russia

Information update date: & nbsp02.10.2017

Illustrated instructions

Instructions

Acetylsalicylic acid (Acetylsalicylic acid)