Active substanceAcetylsalicylic acidAcetylsalicylic acid
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  • Dosage form: & nbsppills
    Composition:

    Composition per one tablet:

    Active substance: acetylsalicylic acid 500 mg,

    Excipients: potato starch - 77.62 mg, citric acid monohydrate food - 0.18 mg, talc - 10.80 mg, stearic acid - 4.20 mg, silicon dioxide colloid - 7.20 mg.

    Description:Tablets of white color, slightly marble with a characteristic odor, flat-cylindrical, with a risk, a facet.
    Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID)
    ATX: & nbsp

    N.02.B.A   Salicylic acid and its derivatives

    Pharmacodynamics:

    NSAIDs; has anti-inflammatory, analgesic and antipyretic effect associated with indiscriminate inhibition of the activity of COX1 and COX2, regulating the synthesis Pg. As a result, no Pg, providing formation of edema and hyperalgesia. Reduction of content Pg (predominantly E1) at the center of thermoregulation leads to a decrease in body temperature due to the expansion of skin vessels and increased sweating.The analgesic effect is due to both central and peripheral action. Reduces aggregation, platelet adhesion and thrombus formation by suppressing the synthesis of thromboxane A2 in platelets. Antiaggregant effect persists for 7 days after a single dose (more pronounced in men than in women). Reduces the mortality and risk of myocardial infarction with unstable angina. Effective in the primary prevention of SSS, especially myocardial infarction in men over 40, and with secondary prevention of myocardial infarction.

    In a daily dose of 6 g or more suppresses the synthesis of prothrombin in the liver and increases prothrombin time.

    Increases fibrinolytic activity of plasma and reduces the concentration of vitamin K-dependent coagulation factors (II, VII, IX, X). It increases hemorrhagic complications during surgical interventions, increases the risk of bleeding on the background of therapy with anticoagulants.

    Stimulates the excretion of uric acid (violates its reabsorption in the renal tubules), but in high doses.

    The blockade of COX1 in the gastric mucosa leads to inhibition of gastroprotective Pg, which can cause ulceration of the mucosa and subsequent bleeding.

    Pharmacokinetics:

    At intake the absorption is complete. During absorption, it undergoes systemic elimination in the intestinal wall and in the liver (deacetylated). The resorbed part is quickly hydrolyzed by special esterases, therefore T1 / 2 - no more than 15-20 minutes.

    In the body it circulates (75-90% in association with albumin) and is distributed in tissues as an anion of salicylic acid. TSmah -2h (for medicinal forms with buffer properties, 35-40 min).

    The serum level of salicylates is very variable. In newborn infants, salicylates can displace bilirubin from binding to albumin and promote the development of bilirubin encephalopathy. Salicylates easily penetrate into many tissues and body fluids, including. in the CSF, peritoneal and synovial fluid. Penetration into the joint cavity is accelerated in the presence of hyperemia and edema and slows down in the proliferative phase of inflammation. In small amounts, salicylates are found in the brain tissue, traces - in bile, sweat, feces. When acidosis occurs, most of the salicylate is converted to non-ionized acid,well penetrating into tissues, incl. in the brain. Rapidly passes through the placenta, in small quantities is excreted in breast milk.

    Metabolized mainly in the liver with the formation of 4 metabolites, found in many tissues and urine.

    It is excreted mainly by active secretion in the renal tubules in unchanged form (60%) and in the form of metabolites. Removal of unchanged salicylate depends on the pH of the urine (with alkalinization of urine ionization of salicylates increases, their reabsorption worsens and the excretion increases significantly). The rate of excretion depends on the dose: when taking small doses of T1 / 2 2-3 hours, with an increase in the dose may increase to 15-30 hours. In newborns, the elimination of salicylates is much slower than in adults.

    Indications:Feverish syndrome with infectious and inflammatory diseases. Pain syndrome (of various origins): headache (including associated with alcohol withdrawal syndrome), migraine, toothache, neuralgia, lumbago, thoracic radicular syndrome, myalgia, arthralgia, algodismenorea.
    Contraindications:

    Hypersensitivity to ASA (including to others.NSAIDs), erosive and ulcerative lesions of the gastrointestinal tract (in the phase of exacerbation), gastrointestinal bleeding, hemorrhagic diathesis, bronchial asthma induced by the intake of salicylates and NSAIDs, a combination of bronchial asthma, recurrent nasal polypsis and paranasal sinuses and intolerance to ASA, simultaneous reception of methotrexate in a dose 15 mg / week and more, pregnancy (I and III trimester), lactation period, children's age (up to 15 years - when used as an antipyretic).

    The drug is not prescribed for children under 15 years with acute respiratory infections caused by viral infections (the risk of development of Ray's syndrome).

    Carefully:Gout, hyperuricaemia, peptic ulcer and duodenal ulcer or gastrointestinal hemorrhage (history), renal / hepatic insufficiency, bronchial asthma, COPD, hay fever, nasal polyposis, drug allergy, concomitant use of methotrexate in a dose of less than 15 mg / Ned, concomitant therapy with anticoagulants, pregnancy (II trimester).
    Pregnancy and lactation:

    Has a teratogenic effect; when applied in the first trimester leads to the development of cleavage of the upper palate; in the II trimester of pregnancy, one-time administration of the drug at recommended doses is possible according to strict indications,in the III trimester causes inhibition of labor (inhibition of synthesis Pg), premature closure of the arterial duct in the fetus, hyperplasia of the pulmonary vessels and hypertension in the "small" circulation. Isolated with breast milk, which increases the risk of bleeding in the child due to impaired platelet function.

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

    Dosing and Administration:

    The duration of treatment (without consulting a doctor) should not exceed 7 days with an appointment as an analgesic drug and more than 3 days as an antipyretic. Currently, the use of ASA as an anti-inflammatory drug in a daily dose of 5-8 g is limited due to the high likelihood of side effects from the gastrointestinal tract (NSAIDs). By indications rheumatism, rheumatoid arthritis, infectious-allergic myocarditis, pericarditis, rheumatic chorea is not currently applied.

    Before surgical intervention, to reduce bleeding during surgery and in the postoperative period, it is necessary to cancel the reception of salicylates for 5-7 days and inform the doctor.During prolonged therapy, a general blood test and examination of feces for latent blood should be performed.

    Children (in the treatment of acute rheumatic fever, pericarditis, elimination of pain) are prescribed at the rate of 20-30 mg / kg. At the age of 3 years, 100 mg / day. At the age of 4-6 years in a dose of 200 mg / day. At the age of 7-9 years in a dose of 300 mg / day. At the age of 12 years in a single dose of 250 mg (1/2 tablets) 2 times a day, the maximum daily dose of 750 mg.
    Side effects:

    When used as an antipyretic: 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 dystrophy with rapid development of hepatic insufficiency). With prolonged use - dizziness, headache, vomiting, erosive and ulcerative lesions of the gastrointestinal tract, hypocoagulation, bleeding (including in the gastrointestinal tract); visual impairment, decreased hearing acuity, tinnitus, bronchospasm, interstitial nephritis, prerenal azotemia with increased creatinine in the blood and hypercalcemia, papillary necrosis,acute renal failure, nephrotic syndrome, aseptic meningitis, increased symptoms of CHF, edema, increased activity of "liver" transaminases.

    When used as an antiaggregant: allergic reactions (urticaria, Quincke's edema), anaphylaxis; nausea, heartburn, vomiting, abdominal pain, ulcers of the gastric mucosa and duodenum, incl. with perforation, gastrointestinal bleeding; increased activity of "hepatic" enzymes; bronchospasm; increased bleeding, anemia (rarely); dizziness, noise in the ears.
    Overdose:

    It occurs when taking single-dose high doses of acetylsalicylic acid (more than 100 mg / kg) or prolonged use of acetylsalicylic acid in elevated doses (salicilism).

    When taking acetylsalicylic acid in a dose of 150-200 mg / kg (or at a level of salicylates in the plasma 50-80 mg / dL), light-type poisoning develops. Characteristic is the appearance of ringing in the ears, hyperventilation due to stimulation of the respiratory center, respiratory alkalosis due to loss FROMO2.

    When taking acetylsalicylic acid in a dose of 200-300 mg / kg (or at a level of salicylates in the plasma 80-110 mg / dL), moderate severity is developed.

    There are severe shortness of breath, hyperthermia due to dissociation of oxidation and phosphorylation (poor prognostic sign in adults), metabolic acidosis due to increased anaerobic glycolysis.

    When taking acetylsalicylic acid in a dose of 300-500 mg / kg (or at a level of salicylates in plasma 110-160 mg / dL) severe poisoning develops. There is a collapse, coma, convulsions, hypoprothrombinemia.

    At reception of acetylsalicylic acid in a dose> 500 mg / kg (or at a level of salicylates in a plasma> 160 mg / dl) extremely serious poisoning with renal and respiratory insufficiency develops.

    Measures of assistance include drug cancellation, vomiting provocation or gastric lavage with activated charcoal and the appointment of salt laxatives to prevent absorption of the drug in the stomach and intestines. The introduction of alkalizing agents to maintain the pH of the urine at a level of 7.5-8.0. At the level of salicylates in plasma more than 300 mg / l (2.2 mmol / l) in children and 500 mg / l (3.6 mmol / L) in adults, an intensive alkaline diuresis (provided by intravenous infusion of sodium bicarbonate 88 meq / l and 5% glucose at a rate of 10-15 ml / kg / h with furosemide 40-60 mg).The recovery of the bcc and the correction of the KHS are carried out. At the level of salicylates more than 1000 mg / l, as well as with refractory acidosis, hemodialysis is indicated. When the brain is swollen, the IVL is shown to be a mixture enriched with oxygen in the positive pressure mode at the end of the exhalation. With edema of the brain, hyperventilation is performed in combination with the administration of osmotic diuretics. There is no specific antidote.

    Use for urine alkalinization acetazolamide when treating intoxication is not recommended in connection with the possibility of developing acidemia and enhancing the toxic effect of salicylate on the patient's body.

    Interaction:

    Increases the toxicity of methotrexate, reducing its renal clearance, valproic acid; intensifies the effects of other NSAIDs, narcotic analgesics, oral hypoglycemic drugs, heparin, indirect anticoagulants, thrombolytic agents and platelet aggregation inhibitors, sulfonamides (including co-trimoxazole), T3; reduces the effect of uricosuric drugs (benzbromarone, sulfinpyrazone), hypotensive drugs, diuretics (spironolactone, furosemide). GCS, ethanol and ethanol containing drugs increase the damaging effect on the gastrointestinal mucosa,increase the risk of developing gastrointestinal bleeding. Increases the concentration of digoxin, barbiturates, salts Li+ in the plasma.

    Antacids containing Mg2+ and / or A13 +, slow down and worsen the absorption of ASA. Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

    Special instructions:

    Caution should be used acetylsalicylic acid for gout, liver disease. Acetylsalicylic acid reduces the excretion of uric acid from the body, which can cause an acute attack of gout in predisposed patients.

    The appointment of tablets after meals, their careful grinding, the use of tablets with buffer additives, as well as the simultaneous use of drugs that neutralize the acidity of gastric juice, reduce the irritating effect on the digestive tract. During treatment should refrain from taking ethanol.

    With prolonged use of the drug should periodically make a general blood test and analysis of feces for latent blood.

    Form release / dosage:Tablets of 500 mg.
    Packaging:

    In contour mesh, non-jawed packaging of 10 pcs.

    1, 2, 3 or 5 contour squares with instructions for use in a pack of cardboard.

    1 contour non-cellular package together with instructions for use (without bundle).

    390 contour non-cellular packages together with instructions for use, in an amount equal to the number of packages in a cardboard box.

    For hospitals: 390 contour non-jammed packages or 300 contour mesh packages together with 20 instructions for use in a cardboard box.

    Storage conditions:

    In a dry place, at a temperature of no higher than 30 ° C.

    Keep out of the reach of children.

    Shelf life:4 years. The drug should be used before the date indicated on the package.
    Terms of leave from pharmacies:Without recipe
    Registration number:П N016154 / 01
    Date of registration:18.03.2010
    Expiration Date:Unlimited
    The owner of the registration certificate:BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC Republic of Belarus
    Manufacturer: & nbsp
    Representation: & nbspBORISOVSKIY FACTORY OF MEDPREPARATES, OJSCBORISOVSKIY FACTORY OF MEDPREPARATES, OJSC
    Information update date: & nbsp02.10.2017
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