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

Excipients: potato starch - 35.546 mg or 71.093 mg, citric acid 0.111 mg or 0.234 mg, talc 6.213 mg or 12.427 mg, stearic acid 2.990 mg or 5.979 mg, magnesium stearate 0.586 mg or 1.172 mg, silicon dioxide colloid (aerosil) - 1.466 mg or 2.931 mg, sodium carboxymethyl starch - 3.082 mg or 6.164 mg.

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

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 inhibition of the first and second type cyclooxygenases 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). 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 a maximum concentration of 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 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, the elimination half-life is -2-3 hours, with an increase in the dose may increase to 15-30 hours.

Indications:

Symptomatic treatment of mild 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 and ulcerative lesions of the gastrointestinal tract (GIT) (in the phase 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, simultaneous taking of methotrexate in a dose 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 of cleavage of the upper palate; at 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.

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

Dosing and Administration:

Inside, after eating, washed down with water, milk or alkaline mineral water. Adults and children over 12 years of age: a single dose of 250 to 500 mg, a maximum single dose of -1.0 g (2 tablets of 500 mg), a maximum daily dose of 3 g (6 tablets of 500 mg), a single dose, if necessary, you can take 3-4 times a day with an interval of at least 4 hours.

For children from the age of 6, a single dose of 250 mg (1/2 tablet of 500 mg or 1 tablet of 250 mg) per reception. Do not use against the background of acute respiratory infections caused by viral infections.

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.

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 of violations of the liver (increased liver transaminases), diarrhea.

From the central nervous system: dizziness, tinnitus (usually signs of overdose); with prolonged use of 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 urinary 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.

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

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 by alkalinizing urine. Urine alkalization is indicated at a salicylate level above 40 mg% and is provided by intravenous infusion of sodium bicarbonate (88 mEq / in 1 L of 5% dextrose solution, at a rate of 10-15 ml / h / kg); the restoration of the volume of circulating blood and the induction of diuresis are achieved by the introduction of sodium bicarbonate in the same doses and dilutions, which are 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 to use acetazolamide for alkalinization of urine (it can cause acidemia and enhance the toxic effect of salicylates). Hemodialysis is indicated at a salicylate level 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:

Joint application:

- with methotrexate at a dose of 15 mg per week or more: the hemolytic cytotoxicity of methotrexate is increased (the 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), their association with blood plasma proteins;

- with other non-steroidal anti-inflammatory drugs: the risk of damage to the mucous membrane of the gastrointestinal tract increases, the risk of developing gastrointestinal bleeding increases;

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

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

- with hypoglycemic drugs: increased risk of hypoglycemia;

- with preparations of thrombolytics group: increased risk of bleeding;

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

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

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

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

- acetylsalicylic acid enhances the effects of narcotic analgesics, indirect anticoagulants and inhibitors of platelet aggregation, sulfonamides (including co-trimoxazole), triiodothyroxine;

- Acetylsalicylic acid reduces the effect of antihypertensive drugs, diuretics (spironolactone, furosemide);

- Acetylsalicylic acid 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 platelet aggregation. This should be taken into account when necessary surgical interventions, including such minor interventions as tooth extraction. Before surgery, 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.

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 250 mg or 500 mg.

Packaging:

For 10 tablets in a contour cell or cellulose package.

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

Contoured packages, together with an equal number of instructions for use, are placed in a group package.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

5 years. Do not use after the time specified on the package.

Terms of leave from pharmacies:Without recipe

Registration number:P N003094 / 01

Date of registration:15.12.2008 / 06.05.2010

Expiration Date:Unlimited

The owner of the registration certificate:PHARMSTANDART-TOMSKHIMFARM, OJSC PHARMSTANDART-TOMSKHIMFARM, OJSC Russia

Manufacturer: & nbsp

PHARMSTANDART-TOMSKHIMFARM, OJSC Russia

Information update date: & nbsp02.10.2017

Illustrated instructions

Instructions

Acetylsalicylic acid (Acetylsalicylic acid)