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

Excipients: cellulose microcrystalline - 42.0 mg, povidoy-K25 - 24.0 mg, croscarmellose sodium - 24.0 mg, citric acid monohydrate - 6.0 mg, magnesium stearate - 4.0 mg.

Description:Round flat cylindrical tablets of white or almost white color with a risk on one side and chamfers on both sides, with a weak characteristic smell. Allowed a slight marbling.

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

ATX: & nbsp

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

Pharmacodynamics:

Acetylsalicylic acid is an ester of salicylic acid, belongs to the group of non-steroidal anti-inflammatory drugs. The mechanism of action is based on the irreversible inactivation of the enzyme cyclooxygenase (COX-1), which blocks the synthesis of prostaglandins, prostacyclin and thromboxane.Has anti-inflammatory, analgesic and antipyretic effect.

Pharmacokinetics:

Suction:

At intake the absorption is complete. During absorption, subject to systemic elimination in the intestinal wall and in the liver (deacetylated). The resorbed part is quickly hydrolyzed by esterases, so the half-life of the drug 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.

The time to reach the maximum plasma concentration is 2 hours. The serum salicylate level is very variable.

Distribution:

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.

Metabolism and excretion:

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. Excretion of unchanged salicylate depends on the pH of the urine (urine alkalinization increases the ionization of salicylates, their reabsorption deteriorates and the excretion increases significantly). The rate of excretion depends on the dose: when taking small doses, the half-life of the drug is 2-3 hours, with an increase in the dose it can increase to 15-30 hours.

Indications:

Symptomatic treatment in adults with moderate or mild pain syndrome of different origin: headache (including those associated with alcoholic abstinence syndrome), toothache, migraine, neuralgia, radicular syndrome, muscle and joint pain, algodismenorea (pain in menstruation), febrile syndrome for colds and other diseases in adults and children over 15 years of age.

Contraindications:

- DUp to 15 years of age;

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

- deficiency of glucose-6-phosphate dehydrogenase;

- complete or incomplete combination of bronchial asthma, recurrent polyposis of the nasal mucosa and paranasal sinuses and intolerance of LSK and other NSAIDs (including in the anamnesis);

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

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

- hemorrhagic diathesis (hemophilia, von Willebrand's disease, telangiectasia, hypoprothrombinemia, thrombocytopenia, thrombocytopenic purpura);

- severe hepatic impairment or active liver disease;

- exacerbation of inflammatory bowel diseases (ulcerative colitis, Crohn's disease);

- cerebrovascular bleeding or other bleeding;

- deficiency of vitamin K;

- simultaneous reception with methotrexate in a dose of 15 mg / day or more;

- simultaneous reception of oral anticoagulants and acetylsalicylic acid in a dose exceeding 3 g per day;

- Severe renal insufficiency (creatinine clearance less than 30 ml / min).

Carefully:Hyperuricemia, urate nephrolithiasis, gout, peptic ulcer and / or duodenal ulcer or gastrointestinal hemorrhage (history), renal insufficiency (creatinine clearance 30-60 ml / min), liver failure, bronchial asthma, chronic obstructive pulmonary disease, polyposis nose, hay fever, drug allergy, pregnancy (II trimester), simultaneous reception of anticoagulants and acetylsalicylic acid in a dose of less than 3 g per day, simultaneous reception of methotrexate in a dose of less than 15 mg / day, metrorrhagia klicheskie uterine bleeding), hypermenorrhoea (heavy and prolonged menstruation).

Pregnancy and lactation:

A drug Acetylsalicylic acid contraindicated in the first and third trimester of pregnancy. Use in the second trimester of pregnancy - with caution, only if the potential use of the application exceeds the potential risk to the fetus. It is necessary to consult a doctor.

During breastfeeding, taking the drug is contraindicated.

Dosing and Administration:

Inside, after eating, washed down with water or alkaline mineral water.

Adults and children over 15 years of age: a single dose of 500 mg, a maximum single dose of 1000 mg (2 tablets of 500 mg), a maximum daily dose of 3000 g (6 tablets of 500 mg).

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 5 days with an appointment as an anesthetic and more than 3 days - as an antipyretic.

To reduce the risk of developing adverse events from the gastrointestinal tract (GIT), a minimum effective dose should be used with the minimum possible short course.

Side effects:

The undesirable phenomena presented below are listed depending on the anatomical and physiological classification and frequency of occurrence. The frequency of occurrence is determined by WHO and has the following gradation: often - more than 1%; infrequently, 0.1-1%; rarely - 0,01-0,1%; very rarely - less than 0.01%, including individual cases.

From the gastrointestinal tract: often - nausea, vomiting, pain in the epigastric region, decreased appetite, rarely - diarrhea (diarrhea), gastrointestinal bleeding (vomiting like "coffee grounds", black "tarry" stool); very rarely - increased activity of "liver" transaminases.in some cases - ulcer and perforation of the stomach.

From the nervous system: infrequently - headache, dizziness, in some cases - reduced severity of hearing, ringing in the ears.

From the side of the blood and lymphatic system: infrequently - hemorrhagic syndrome (epistaxis, bleeding gums, hemorrhagic rash), increase in clotting time. These effects persist for 4-8 days after discontinuation of the drug and should be taken into account in planning subsequent operations for patients.

From the immune system: often - skin rash, very rarely - bronchospasm, angioedema. Formation on the basis of the hapten mechanism of the "aspirin" triad (combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses, and intolerance to acetylsalicylic acid and pyrazolone preparations);

From the liver and bile ducts: very rarely - Reye's syndrome (encephalopathy and acute fatty liver dystrophy with acute development of liver failure).

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; higher than 100 mg% - oextremely severe, prognostically unfavorable. When moderate and severe poisoning is required hospitalization.

Treatment: provocation of vomiting, the appointment of activated carbon and laxatives, constant monitoring of the acid-base state (CBS) 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 ACAS by alkalinizing urine. The alkalinization of urine is shown at a salicylate concentration 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 (BCC) 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 the use of 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 - IVL with a mixture enriched with oxygen.

Interaction:

Acetylsalicylic acid increases the toxicity of methotrexate (reduces its renal clearance), valproic acid, the effects of narcotic analgesics, other nonsteroidal anti-inflammatory drugs, oral hypoglycemic drugs, heparin, indirect anticoagulants, thrombolytic agents and platelet aggregation inhibitors, sulfonamides (including co-trimoxazole) , triiodothyronine; reduces the effectiveness of uricosuric drugs (benzbromarone, sulfinpyrazone), antihypertensive drugs and diuretics (spironolactone, furosemide).

Glucocorticosteroids, alcohol and alcohol-containing drugs increase the damaging effect on the mucous membrane of the gastrointestinal tract, increase the risk of developing gastrointestinal bleeding.

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

Antatsida, containing magnesium and / or aluminum hydroxide, slow down and worsen the absorption of acetylsalicylic acid.

Special instructions:

When using drugs containing acetylsalicylic acid in acute respiratory infections in children under 15 due to viral infections, there is a risk of developing Reye's syndrome (encephalopathy and acute fatty liver disease with acute liver failure). Symptoms of Reye's syndrome include prolonged vomiting, acute encephalopathy, and enlargement of the liver. Acetylsalicylic acid reduces the excretion of uric acid from the body, which can cause an acute attack of gout in predisposed patients.

With prolonged use of the drug should periodically conduct a general blood test and analysis of feces for latent blood, monitor the functional state of the liver.

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.

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

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Tablets 500 mg.

Packaging:

For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 10, 20, 30, 40, 50, 60, 70, 80, 90 or 100 tablets in cans of polyethylene terephthalate or cans of polymeric for medicines.

One bank or 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 20, 30, 40, 50, 60, 70, 80, 90, 100 of the contour mesh packages together with the instruction for use are placed in cardboard packaging (bundle).

Storage conditions:

In the dark place at a temperature of no higher than 25 ^aboutFROM.

Keep out of the reach of children.

Shelf life:

3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002950

Date of registration:08.04.2015

Expiration Date:08.04.2020

The owner of the registration certificate:ATOLL, LLC ATOLL, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Information update date: & nbsp02.10.2017

Illustrated instructions

Instructions

Acetylsalicylic acid (Acetylsalicylic acid)