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

Excipients: potato starch 0.0237 g; talc 0.0010 g; lactose monohydrate (sugar milk) 0.0240 g; povidone (low molecular weight polyvinylpyrrolidone) 0.0003 g; Stearic acid 0.0010 g.

Description:

Tablets are white, slightly marble, flat-cylindrical 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:

The drug has analgesic, antipyretic, anti-inflammatory effect, which is due to the inhibition of cyclooxygenase enzymes involved in the synthesis of prostaglandins. Acetylsalicylic acid inhibits platelet aggregation by blocking the synthesis of thromboxane A₂.

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 rapidly hydrolyzed, with special esterases, so the elimination half-life is no more than 15-20 min.

In the body it circulates (75-90% in association with albumin) and is distributed in tissues as an anion of salicylic acid.

The time to reach the maximum concentration is 2 hours. The serum salicylate level is very variable. Salicylates easily penetrate into many tissues and body fluids, including. in spinal, 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 salicylic acid is converted to a non-ionized acid that penetrates well into the tissue, including. in the brain. Rapidly passes through the placenta_; in small amounts 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 tubule in an 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 deteriorates and the excretion increases significantly). The rate of excretion depends on the dose: when taking small doses, the half-life period is 2-3 hours, with an increase in the dose it can increase to 15-30 hours.

Indications:

Symptomatic treatment of pain syndrome: headache (including abstinence syndrome), toothache, sore throat, back and muscle pain, joint pain, menstruation pain.

The raised temperature of a body at cold and other infectious-inflammatory diseases (at adults and children is more senior 15 years).

Contraindications:

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

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

- gastrointestinal bleeding;

- hemorrhagic diathesis;

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

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

- The bronchial asthma, induced by the intake of salicylates and NSAIDs;

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

- Children's age (up to 6 years, up to 15 years - when used as an antipyretic).

The drug is not prescribed for children under 15 with acute respiratory infections caused by viral infections, because of the risk of developing Reye's syndrome (encephalopathy and acute fatty liver disease 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; with renal and / or hepatic insufficiency, deficiency of glucose-6-phosphate dehydrogenase; hyperuricemia, bronchial asthma, chronic obstructive pulmonary disease, hay fever, nasal polyposis, drug allergy, concomitant use of methotrexate in a dose of less than 15 mg / week, pregnancy (II trimester).

Pregnancy and lactation:

Acetylsalicylic acid has a teratogenic effect; when applied in the first trimester leads to the development ofsplitting of the upper sky; in the III trimester causes inhibition of labor (inhibition of the synthesis of prostaglandins), 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.

Dosing and Administration:

Inside, adults and children over 12 years of age: a single dose of 0.25-0.5 g, the maximum single dose of 1.0 g (2 tablets of 0.5 g), the maximum daily value of 3.0 g (6 tablets to 0 , 5 g), a single dose, if necessary, can be taken 3 ^ 4 times a day with an interval of at least 4 hours.

For children from the age of 6, except for the use of acute respiratory infections caused by viral infections, because of the risk of developing Reye's syndrome (encephalopathy and acute fatty liver disease with acute development of liver failure), a single dose of 0.25 g (1/2 tablet 0.5 g) at the reception.

Mode of application: the drug should be taken after a meal, washed down with water, milk or alkaline mineral water.

Frequency and time of admission: a single dose, if necessary, can be taken 3-4 times a day with an interval of at least 4 hours. Regular adherence to the regimen allows you to avoid a sharp increase in temperature and reduce the intensity of the pain syndrome.

The duration of treatment (without consulting a doctor) should not exceed 7 days when prescribed as an anesthetic and more than 3 days - as an antipyretic.

Side effects:

From the gastrointestinal tract: loss of appetite, abdominal pain, heartburn, nausea, vomiting, obvious (vomiting with blood, tarry stools) or hidden signs of gastrointestinal bleeding that can lead to iron deficiency anemia, erosive-ulcerative lesions (including perforations) of the gastrointestinal hemorrhage, intestinal tract, single cases - violations of the liver (increased liver transaminases), diarrhea.

From the central nervous system: dizziness, tinnitus (usually a sign of an overdose); with prolonged use - headache, visual impairment, decreased acuity of hearing, aseptic meningitis.

From the cardiovascular system: with prolonged use - increased symptoms of chronic heart failure.

On the part of the hematopoiesis system: increased risk of bleeding, which is a consequence of the effect of acetylsalicylic acid on platelet aggregation, thrombocytopenia, anemia, and leukopenia.

From the excretory system: impaired renal function; with prolonged use - interstitial nephritis, prerenal azotemia with increased creatinine in the blood and hypercalcemia, papillary necrosis, acute renal failure, nephrotic syndrome, edema.

Allergic reactions: skin rash, anaphylactic reactions, bronchospasm, angioedema.

Reye's syndrome (encephalopathy and acute fatty liver dystrophy with rapid development of liver failure).

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

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, ketoacidosis, 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 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 concentration of salicylates in the blood: a level above 70 mg% indicates a moderate or. severe poisoning; above 100 mg% - about extremely severe, prognostically unfavorable. With moderate poisoning, hospitalization is necessary for 24 hours.

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 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 (it can cause acidemia and enhance the toxic effect of salicylates). Hemodialysis is indicated with a salicylate level of more than 10-1-130 mg%, in patients with chronic poisoning - 40 mg% and lower in the presence of indications (refractory acidosis, progressive deterioration of the condition, severe damage to the central implicit system, pulmonary edema and renal failureaccuracy). When swelling of the lungs - artificial ventilation of the lungs with a mixture enriched with oxygen.

Interaction:

Joint application:

- with methotrexate at a dose of 15 mg per week or more: increases the hemolytic cytotoxicity of methotrexate (decreased renal clearance of methotrexate and methotrexate is replaced by salicylates in association with blood plasma proteins);

- with anticoagulants, for example, heparin: increased risk of bleeding due to inhibition of platelet function, damage to the mucosa of the gastrointestinal tract, displacement of anticoagulants (oral) from the connection with blood plasma proteins;

- with other non-steroidal anti-inflammatory drugs: as a result of synergistic interaction, the risk of ulcers and bleeding of the stomach increases;

- with uricosuric Medicines, for example, benzbromarone: reduces the uricosuric effect;

- with digoxin: Digoxin concentration is increased due to decreased renal excretion;

- with hypoglycemic drugs: hypoglycemic effect of hypoglycemic drugs increases due to hypoglycemic effect of acetylsalicylic acid;

- with preparations of thrombolytics group: the risk of bleeding increases;

- with systemic glucocorticosteroids, excluding hydrocortisone, used as a substitute therapy for Addison's disease: with the use of glucocorticoids, the level of salicylates in the blood decreases due to an increase in the excretion of the latter;

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

- with valproic acid: the toxicity of valproic acid increases;

- with glucocorticosteroids, ethanol (alcoholic beverages) and ethanol-containing drugs: the risk of damage to the mucous membrane of the gastrointestinal tract increases, the risk of developing gastrointestinal bleeding increases;

- enhances the effects of narcotic analgesics, indirect anticoagulants and inhibitors of platelet aggregation, sulfonamides (including co-trimoxazole), triiodothyroxine; reduces the effect of antihypertensive drugs, diuretics (spironolactone, furosemide);

- increases the concentration of barbiturates, lithium salts in plasma;

- antacids containing magnesium and / or aluminum 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, rashes on the skin).

Acetylsalicylic acid can increase the tendency to bleeding, which is due to its inhibitory effect on aggregation thrombocytes. This should be taken into account when necessary surgical interventions, including such minor interventions as tooth extraction. Before surgical intervention, to reduce bleeding during one-and in the post-operation period, it is necessary to cancel the drug intake for 5-7 days and inform the doctor.

Children should not be prescribed drugs containing acetylsalicylic acid, because in the case of a viral infection, the risk of developing Reye syndrome increases. Symptoms of Reye's syndrome include prolonged vomiting, acute encephalopathy, and enlargement of the liver.

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

In the treatment of vascular diseases, the daily dose of acetylsalicylic acid is 75 to 300 mg.

Acetylsalicylic acid reduces the excretion of uric acid from the body, which can cause 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:

There was no evidence of the effect of drug administration on vehicle management and other mechanisms.

Form release / dosage:

Tablets of 0.5 g.

Packaging:

For 10 tablets in contour non-jammed packaging.

For 10 tablets in a planar cell package.

1, 2, 5, 10 contour packs together with instructions for use are placed in a pack of cardboard.

It is allowed to place contour packs together with an equal number of instructions for use in group packaging.

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 the product after the expiry date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:P N002019 / 01

Date of registration:11.12.2008 / 08.04.2016

Expiration Date:Unlimited

The owner of the registration certificate:MEDISORB, CJSC MEDISORB, CJSC Russia

Manufacturer: & nbsp

MEDISORB, CJSC Russia

Information update date: & nbsp02.10.2017

Illustrated instructions

Instructions

Acetylsalicylic acid MS (Acetylsalicylic acid MS)