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

    1 tablet contains

    Active substance: acetylsalicylic acid - 500 mg,

    Excipients: citric acid, potato starch, talc.

    Description:

    Tablets of white color, slightly marble, odorless or with a weak characteristic odor, flat-cylindrical shape with a facet and a risk.

    Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID)
    ATX: & nbsp

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

    Pharmacodynamics:

    Acetylsalicylic acid, blocking the enzyme cyclooxygenase, disrupts the synthesis of prostaglandins, has analgesic, antipyretic and weak anti-inflammatory effect. Reduces the aggregation capacity of platelets. The analgesic effect is due to both central and peripheral action.

    Pharmacokinetics:

    At intake the absorption is complete.During absorption, it undergoes systemic elimination in the intestinal wall and in the liver (deacetylated). The absorbed part is rapidly hydrolyzed by plasma cholinesterases and albumin esterase, therefore the elimination half-life (T1 / 2) is 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.

    Time to reach the maximum concentration (TCmah) -2 hours.

    Serum concentration 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 cerebrospinal fluid, 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 nervous tissue, traces in bile, sweat, feces. When acidosis occurs, most of the salicylate is converted to a non-ionized acid that penetrates well into the tissue, including the brain.Rapidly passes through the placenta, in small quantities is excreted in breast milk.

    Salicylic acid is metabolized predominantly in the liver with the formation of 4 metabolites found in many tissues and urine.

    It is excreted mainly by active secretion in renal tubules in the form of actually salicylic acid (60%) and its metabolites. Removal of unchanged salicylate depends on the pH of the urine (with alkalization 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, the period half-life (T1/2) - 2-3 hours, with increasing dose can increase to 15-30 hours.

    Indications:

    Acetylsalicylic acid-UBF is only used in adults with moderately or weakly expressed pain syndrome of various origin (headache, toothache, migraine pain, neuralgia, muscle pain, pain during menstruation). The raised temperature of a body at "catarrhal" and other infectious-inflammatory diseases.

    Contraindications:

    - Hypersensitivity to acetylsalicylic acid and other non-steroidal anti-inflammatory drugs or other components of the drug;

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

    - hemorrhagic diathesis;

    - combined use of methotrexate in a dose of 15 mg per week or more;

    - complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses, and intolerance to acetylsalicylic acid;

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

    - children's age till 6 years.

    The drug is not prescribed for children under 15 with acute respiratory infections caused by viral infections, because of the risk of developing the syndrome Flight (encephalopathy and acute fatty liver with acute development of liver failure).

    Carefully:

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

    Pregnancy and lactation:

    In the second trimester of pregnancy, one-time administration of the drug at recommended doses is possible only on strict indications. If you need to use the drug during lactation, breastfeeding should be discontinued.

    Dosing and Administration:

    Inside, adults and children over 12 years of age: a single dose of 250-500 mg, the maximum single dose of 1.0 g (2 tablets of 500 mg), the maximum daily - 3.0 g (6 tablets of 500 mg).

    Frequency and time of reception: a single dose, if necessary, can be taken 3-4 times a day with an interval of at least 4 hours. Compliance with the regimen of taking the drug avoids a sharp rise in temperature and reduces the intensity of the pain syndrome.

    For children from 6 years of age, a single dose of 250 mg (1/2 tablet) to 3 times a day, except for acute respiratory infections caused by viral infections, due to the risk of developing Reye syndrome (encephalopathy and acute fatty liver with acute development of hepatic insufficiency).

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

    Side effects:

    - Allergic reactions - skin rash, bronchospasm, angioedema;

    - gastrointestinal disorders - nausea, vomiting, epigastric pain, diarrhea;

    - with prolonged use, there may be erosive and ulcerative lesions of the gastrointestinal tract up to the bleeding, black "tarry" stool, general weakness, hearing impairment, liver and kidney function. From the central nervous system may be dizziness, visual impairment, tinnitus.

    - hemorrhagic syndrome (epistaxis, bleeding gums), increase in clotting time.

    When such symptoms appear, it is recommended to stop taking the drug and immediately consult a doctor.

    If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, inform the doctor about it.

    Overdose:

    Symptoms: (single dose less than 150 mg / kg - acute poisoning is considered light, 150-300 mg / kg - moderate,more than 300 mg / kg - severe): salicylism syndrome (nausea, vomiting, tinnitus, visual impairment, dizziness, severe headache, general malaise, fever - poor prognostic sign in adults).

    Severe poisoning - hyperventilation of the lungs of the central genesis, respiratory alkalosis, metabolic acidosis, confused consciousness, drowsiness, collapse, convulsions, anuria, bleeding. Initially, central hyperventilation of the lungs leads to respiratory alkalosis - dyspnea, choking, cyanosis, cold sticky sweat; with increasing intoxication, paralysis of respiration and dissociation of oxidative phosphorylation, causing respiratory acidosis, increase.

    In chronic overdose, the concentration in the plasma is poorly correlated with the severity of intoxication. The greatest risk of developing chronic intoxication is observed in the elderly with more than 100 mg / kg / day for several days. In children and elderly patients, the initial signs of salicylism are not always noticeable, so it is advisable to periodically determine the salicylate content in the blood: a concentration above 70 mg% indicates moderate or severe poisoning; above 100 mg% - about extremely severe, prognostically unfavorable.With moderate and severe poisoning, hospitalization is necessary.

    Treatment: provocation of vomiting, the appointment of activated carbon and laxatives, constant monitoring of the acid-base state and electrolyte balance; depending on the state of metabolism - the introduction of sodium bicarbonate, sodium citrate solution or sodium lactate. The increase in reserve alkalinity increases the excretion of acetylsalicylic acid due to alkalinization of urine. Urinary alkalization shown at concentrations of salicylates higher than 40% and is provided mg intravenous infusion of sodium hydrogencarbonate (88 mEq in 1 L of 5% dextrose solution at a rate of 10- 15 ml / h / kg); restoration of circulating blood volume and diuresis induction is achieved by introducing sodium hydrogen carbonate at the same doses and dilution, which is repeated 2-3 times. Caution should be exercised in elderly patients in whom intensive fluid infusion can lead to pulmonary edema. It is not recommended the use of acetazolamide for alkalinization of urine (can cause acidosis and enhance the toxic effect of salicylates). Hemodialysis is indicated in salicylate concentration of 100-130 mg% in patients with chronic poisoning - 40 mg% or below in the presence of indications (refractory acidosis, progressive, deterioration, severe central nervous system damage, pulmonary edema and renal failure). When swelling of the lungs - artificial ventilation of the lungs with a mixture enriched with oxygen.

    Interaction:

    It is not recommended simultaneous use of other non-steroidal anti-inflammatory drugs or uricosuric agents, anticoagulants of indirect action, ticlopidine, heparin sodium, interferon alfa, methotrexate. Reduces, when combined, the effectiveness of diuretics, antihypertensive drugs, anti-gout agents that promote the excretion of uric acid. Strengthens the effect of oral hypoglycemic agents. Simultaneous reception with glucocorticosteroids increases the risk of erosive and ulcerative lesions of the gastrointestinal tract. Acetylsalicylic acid increases the concentration of digoxin, barbiturates and lithium salts in blood plasma, while simultaneous use with antacid agents containing magnesium and / or aluminum hydroxide, slows down and deteriorates the absorption of acetylsalicylic acid.

    Special instructions:

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

    Currently, the use of acetylsalicylic acid as an anti-inflammatory drug in a daily dose of 5-8 g is limited due to a high probability of side effects from the gastrointestinal tract (gastropathy, induced by non-steroidal anti-inflammatory drugs).

    According to 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 should not be prescribed medications containing acetylsalicylic acid, since in the case of a viral infection they can increase the risk the emergence of Reye's syndrome.Symptoms of Reye's syndrome include prolonged vomiting, acute encephalopathy, and enlargement of the liver.

    Purpose tablets after a meal, grinding them thoroughly, the use of buffer additives to tablets or coated with special enteric-coated as well as the simultaneous use of drugs, neutralizing gastric acidity, lower irritating effect on the gastrointestinal tract.

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

    During treatment should refrain from taking ethanol.

    Effect on the ability to drive transp. cf. and fur:

    During the treatment period, it is necessary to refrain from driving transport and practicing other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

    Form release / dosage:Tablets of 0.5 g.
    Packaging:

    For 10 tablets in a contour non-cellular package of paper with a polymer coating.

    By 10tablets into a contoured cell packaging made of a polyvinylchloride film and aluminum foil or paper with a polymeric coating.

    By 10, 20, 25, 30, 40, 50, 60 tablets in cans of polymeric.

    Each bank, or 1, 2, 3, 4, 5 contour non-jammed packages, or contour mesh packages together with the instruction for use, is placed in a bundle.

    Banks polymeric, or contour non-cellular packages, or contour mesh packages with an equal number of instructions for use are placed in a bag of polyethylene film or a cardboard box.

    Storage conditions:

    In a dry place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    4 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:Without recipe
    Registration number:P N002248 / 01
    Date of registration:15.01.2009 / 24.12.2013
    Expiration Date:Unlimited
    The owner of the registration certificate:URALBIOFARM, OJSC URALBIOFARM, OJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp02.10.2017
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