Instructions for use of acetylsalicylic acid. Acetylsalicylic acid - instructions for use, principle of action, temperature, acne (for face) Treatment with acetylsalicylic acid

Instructions

Salicylic acid - active ingredient plants rich in salicylate. Even in the time of Hippocrates, this medicine was obtained from the bark of the white willow, brewing it instead of tea. Then the therapeutic agent had side effects, causing nausea and severe pain in a stomach. The purified form was isolated in Germany only in the 19th century.

Salicylic acid is the active component of plants rich in salicylate.

Name

The discovery of the chemical structure of salicylic acid made it possible to build the first factory in Dresden for the production of drugs based on it. Laboratory-derived chemically pure samples were registered under the name Aspirin:

  1. The basis was taken from the Latin name of the plant from which salicylic acid was first isolated - Spiraea ulmaria.
  2. An “a” was added to the first four letters (spir), emphasizing the important role of acetylation (a chemical reaction that replaces hydrogen atoms with acetic acid).
  3. On the right (in accordance with the generally accepted tradition among pharmacists) the ending “in” was added.

The result was a name that was easy to pronounce and remember - Aspirin.

Latin name

Acidum acetylsalicylicum (lat.) is organic compound salicylic ester and acetic acid. The structure of the drug is based on chemical formula: COOH-C6H4-O-C(O)-CH3.

Tradename

This medicine was patented by the German company Bayer in 1988 under the brand name “Aspirin”. International generic name drug, which can be seen on the packaging of domestic manufacturers - Acetyl salicylic acid(Acetylsalicylic acid). The abbreviated name is ASK.

Composition and action

The medicinal composition is obtained from salicylic acid and acetic emulsion (anhydride). By chemical reactions a powder is released, which is white needle-shaped crystals. This easy drug:

  • has a slightly sour taste;
  • slightly soluble in cold water;
  • soluble in hot water;
  • easily dissolves in alcohol.

The tablets contain the active substance (ASA), as well as auxiliary components:

  • starch - binder;
  • talc is a source of magnesium and silicon;
  • lemon acid- stimulates the secretion of gastric juice;
  • stearic acid - preservative;
  • Silicon dioxide is an enterosorbent that removes toxic substances from the body.

Release form

More often, the drug is found in the form of 500 mg tablets, hermetically packaged in contour blisters. You can also purchase effervescent tablets containing the same active substance and auxiliary components:

  • sodium citrate anhydrous;
  • monosubstituted sodium carbonate;
  • citric acid.

Aspirin is also sold in pharmacies in the form of an effervescent powder packaged in sachets. One sachet contains 500 mg (0.5 g) ASA, as well as:

  • phenylephrine hydrotartrate;
  • chlorphenamine maleate;
  • sodium bicarbonate;
  • dyes and flavors.

Pharmacological group

Salicylic acid and its derivatives belong to the pharmacological group of nonsteroidal anti-inflammatory drugs (NSAIDs), which are all analgesics and antipyretics that have the same actions:

  • anti-inflammatory;
  • antipyretic;
  • analgesic.

pharmachologic effect

The mechanism of action consists of the process of inhibition (braking) of enzymes involved in the regulation of short-range actions. This pharmacological inhibition promotes:

  1. Reducing inflammation. Under the influence of the drug in the lesion, capillary permeability decreases, and the activity of hyaluronidase (an enzyme for tissue permeability), which is involved in the energy supply of the inflammatory phenomenon, decreases.
  2. Reduce fever. This is due to the effect of the drug on the hypothalamic thermoregulation centers located in the central nervous system.
  3. Pain relief. The process is due to the ability of salicin to influence the centers of pain sensitivity by thinning the blood and expanding blood vessels.

Pharmacodynamics

Pharmacodynamics depends on dosage:

  • from 75 mg to 250 mg per day ( small dose) - causes inhibition of platelet aggregation (gluing);
  • up to 2 g (average dose) - has an analgesic and antipyretic effect;
  • up to 6 g (large dose) - has an anti-inflammatory effect.

In a large dose (from 4 to 6 g, which is equal to 8-12 tablets of 500 mg), Aspirin promotes excretion uric acid from the body.

Pharmacokinetics

Aspirin, like all NSAIDs, is well absorbed by the gastrointestinal tract. Absorption will be enhanced if the tablet is crushed and washed down warm water. Under the action of esterases (enzymes that catalyze the breakdown of esters into alcohols and acids through hydrolysis), salicylate, which has the main pharmacological activity, is cleaved from ASA.

Metabolism occurs in the liver with the formation of metabolites:

  • salicylurate;
  • glucuronides;
  • gentisic and gentisuric acids.

Metabolites are excreted through the kidneys, the process is dose-dependent:

  • low doses (up to 100 mg) - after 2-3 hours;
  • average doses - after 5-8 hours;
  • high - after 12-15 hours.

What does acetylsalicylic acid help with?

In addition to its antipyretic and analgesic properties, ASA has also been shown to have other properties.

  • the drug was found to have glucosuric properties (blood purification), which made it possible to use it as a remedy for gout;
  • the risk of stroke and death from myocardial infarction is reduced;
  • plays an anti-inflammatory role in the treatment of rheumatoid arthritis;
  • effective for preventing breast cancer, prostate gland and colon (although the mechanism of the effect is not completely clear, and clinical researches continue).

The medicine is indicated for:

  • headache and toothache;
  • heat and chills;
  • high blood pressure;
  • inflammatory processes.

The powder solution is used as an antiseptic in cosmetology:

  • for skin disinfection;
  • for acne;
  • as part of a face mask;
  • when rinsing oily hair.

For nephritis

The use of Aspirin at home for inflammatory processes of unknown origin is prohibited. So in the case of jade ( inflammatory disease kidneys), the functioning of the renal tubules responsible for receiving urine and its reabsorption (reabsorption) is disrupted.

ASA can cause damage to the tubular epithelium.

How to use

ASA is taken orally after meals.

Dose 0.25 to 1 g 3-4 times a day (adults):

  • reduces temperature during colds;
  • relieves muscle and joint pain;
  • helps with headaches and neuralgia.

From 2 to 4 g per day (adults) is prescribed for:

  • rheumatism;
  • rheumatoid polyarthritis;
  • infectious-allergic myocarditis.

How long does it take for acetylsalicylic acid to work?

The accumulation of the maximum concentration of salicylate in the blood is observed 2 hours after taking the medicine. But the product begins to act after 20-30 minutes.

Aspirin in the form of a powder diluted in warm water has a therapeutic effect in an even shorter time - 10-15 minutes.

Contraindications when using the drug acetylsalicylic acid

ASA should not be taken by patients suffering from:

  • bronchial asthma;
  • allergies;
  • stomach diseases (gastritis, ulcers);
  • hemophilia;
  • Dengue fever (tropical fever).

Aspirin is not prescribed to children and adolescents 4 to 12 years of age with unconfirmed flu-like symptoms, as fever may be associated with Reye's syndrome. It's rare, but dangerous condition occurs in young patients during treatment of viral fever (measles, chickenpox) with drugs containing ASA.

This acid should not be given to children with Kawasaki disease (vasculosis) - inflammation of the walls of blood vessels, leading to their expansion. Vasculosis manifests itself in the form of flu and acute respiratory infections symptoms: fever, chills, and fever.

Side effects

Side effects from the gastrointestinal tract and hematopoietic system:

  • heartburn;
  • nausea;
  • abdominal pain;
  • stomach bleeding.

In some patients, taking Aspirin can trigger an allergy:

  • hives;
  • anaphylactic reaction;
  • bronchospasm;
  • Quincke's edema.

An allergic reaction is most often caused not by intolerance to salicylate, but by an inability to metabolize the drug, which leads to an overdose.

Overdose

Overdose may cause acute poisoning with the following consequences from the central nervous system:

  • dizziness;
  • noise in ears;
  • pressure on the temporal areas.

With a single large dose, there is a 2% risk of death. In case of chronic poisoning caused by long-term use large doses of Aspirin, death may occur in 25% of cases.

special instructions

The drug, by thinning the blood, increases bleeding. This must be taken into account during surgical interventions, including minor ones (for example, tooth extraction), as well as during menstruation.

Varieties effervescent tablets aspirin-based (Alka-Seltzer, Blowfish) reduce pain faster than the pure drug.

Caution should be exercised when consuming salicylates together with natural ingredients that suppress the properties of the COX-2 cyclooxygenase isoenzyme (formed in peripheral tissues during inflammation), such as:

  • garlic extract;
  • fish fat;
  • ginkgo;
  • curcumin, etc.

Can I take it during pregnancy and lactation?

ASA is contraindicated for use in the 1st and 3rd trimesters of pregnancy. This is due to the risk of fetal developmental abnormalities. The drug is not prescribed during lactation.

Can children take it?

Aspirin should not be prescribed to children without first consulting a doctor (due to the risk of developing Reye's syndrome or Kawasaki disease).

For children daily norm depends on age:

  • 1 year - Aspirin 0.05 g can be prescribed;
  • 2 years - 0.1 g;
  • 3 years - 0.15 g;
  • 4 years - 0.2 g.

From 5 years of age, tablets are prescribed at 0.25 g (250 mg or 1/2 tablet) per dose.

For impaired renal function

ASA should be taken with caution in case of nephrotic syndrome (impaired kidney function). If the drug is taken in excess, the excretion of uric acid by the kidneys is delayed. People with conditions such as gout (deposition of uric acid crystals in the organs) or hyperuricemia (increased levels of uric acid) should not take Aspirin to avoid making the condition worse.

For liver dysfunction

Aspirin is not prescribed if there is various diseases liver (cirrhosis, hepatitis). When liver function is impaired, increased activity of liver enzymes is observed. Acid causes an additional increase in their activity, which can aggravate the disease.

Benefits and harms

The benefits of the drug in the absence of contraindications to its use are obvious.

Aspirin is an effective anti-inflammatory, antipyretic and analgesic (for some types of pain).

But ASA thins the blood, frequent use can cause gastrointestinal bleeding, this is its main danger and harm.

Alcohol compatibility

The medicine does not take part in the process of ethanol breakdown, so it is useless for alcohol intoxication. Aspirin just makes it easier general state in case of a hangover, it promotes the speedy recovery of the body. By thinning the blood, the drug increases its circulation and provides cells with glucose and oxygen.

Drug interactions

Interaction of ASA with other drugs:

  • together with vitamin C, protects the stomach walls from damage (which often happens when using pure Aspirin);
  • combination with caffeine enhances the analgesic effect;
  • ammonium chloride and acetazolamide enhance the effect of salicylate;
  • Aspirin suppresses the effect of antidiabetic drugs (Tolbutamide and Chlorpropamide, Warfarin, Methotrexate, Phenytoin, Probenecid);
  • steroid hormones (corticosteroids) reduce the concentration of ASA in the blood;
  • combination with Ibuprofen reduces the effect of cardioprotection.

Analogs

Aspirin has many analogues. Any prescription of medication must be agreed with a doctor.

Analogues include:

  • Ibuprofen;
  • Analgin;
  • Anopyrine;
  • Cardiopyrin;
  • Colfarit:
  • Mikristin;
  • Thrombo ACC;
  • Upsarin;
  • Fluspirin and many others. etc.

Aspirin and acetylsalicylic acid are the same thing

Aspirin is a patented name for a drug whose main active ingredient is ASA (this is the international nonproprietary name for the same drug).

Which is better: paracetamol or acetylsalicylic acid?

Aspirin and Paracetamol are similar in their effects, but each drug has additional benefits:

  1. Paracetamol only limits the synthesis of cyclooxygenase, suppressing pain signals. Aspirin in addition has an effect on thromboxanes.
  2. ASA has a harsh effect on the gastrointestinal tract, so patients with such problems should give preference to the second remedy.
  3. Aspirin reduces fever faster, but Paracetamol is considered the safest.
  4. Paracetamol can be used in pediatric therapy; the medicine is prescribed to pregnant and lactating women.

Terms and conditions of storage

The shelf life of the drug is 5 years from the release date indicated on the packaging.

Conditions for dispensing from pharmacies

Aspirin is available without a prescription.

Price

The cost of the medicine varies, it depends on the form, manufacturer, additional ingredients:

  • blister 10 pcs. 500 mg each - 5 rubles;
  • packing 20 pcs. 500 mg (Reneval) - 17 rubles;
  • Aspirin Cardio (20 pcs. 300 mg) - 75 rubles;
  • Aspirin C (enteric-coated effervescent tablets) - 250 rubles. for 10 pcs.;
  • Aspirin Complex (effervescent powder 10 sachets) - 430 rub.

The cost of the medicine varies, it depends on the form, for example Aspirin C - 250 rubles. for 10 pcs.

Acetylsalicylic acid is a non-selective non-steroidal anti-inflammatory drug (NSAID), which has anti-inflammatory, antipyretic, analgesic effects, and can also inhibit platelet activity.

The mechanism of action is due to the ability active substance interfere with the synthesis of prostaglandins, which play a major role in the development of inflammatory processes, fever and pain.

The antipyretic effect is based on the influence of acetylsalicylic acid on the thermoregulation center of the hypothalamus, and the analgesic properties are associated with an effective effect on the pain sensitivity center in the central nervous system.

Inhibits the activity of the enzyme cyclooxygenase, which regulates the synthesis of prostaglandin in the body, which is responsible for the formation of edema and hyperalgesia. Since prostaglandins are not produced, the severity of inflammatory process and pyrogenic influence on the thermoregulation center.

Acetylsalicylic acid helps reduce the risk of myocardial infarction, is effective in primary prevention cardiovascular diseases.

High doses of the drug stimulate the excretion of uric acid, but also increase the risk of bleeding during treatment with anticoagulants.

When taken orally, the maximum concentration of acetylsalicylic acid in the blood can be observed after 10-20 minutes, and the salicylate formed as a result of metabolism - after 0.3-2 hours. Excreted through the kidneys, the half-life is 20 minutes, the half-life for salicylate is 2 hours.

Composition of the tablet:

  • Acetylsalicylic acid – 250 or 500 mg;
  • Excipients: citric acid (in the form of monohydrate) and potato starch.

Is acetylsalicylic acid Aspirin or not?

Yes, it's Aspirin. However, many other drugs contain Acetylsalicylic acid as the main (or only) active ingredient - see the Analogs section below.

Is it worth paying extra for them? Some drugs are enteric-coated or presented in the form of effervescent tablets - such forms cause less trauma to the gastrointestinal tract and have fewer side effects - the choice is up to the doctor and you.

Indications for use

What does Acetylsalicylic acid help with? According to the instructions, the drug is prescribed in the following cases:

  • Acute rheumatic fever, rheumatic chorea, Dressler's syndrome, rheumatoid arthritis;
  • Diseases of the spine that are accompanied by pain syndromes (lumbago, sciatica, osteochondrosis);
  • Migraine, headaches, joint, muscle, menstrual and toothaches, neuralgia, osteoarthritis;
  • Fever syndrome;
  • Coronary heart disease, thromboembolism, atrial fibrillation and myocardial infarction (as a prophylactic agent);
  • Prevention of thromboembolism (blockage of a vessel with a blood clot), valvular mitral heart defects, prolapse (dysfunction) of the mitral valve, atrial fibrillation (loss of the ability of the muscle fibers of the atria to work synchronously);
  • Acute thrombophlebitis (inflammation of the vein wall and the formation of a blood clot that closes the lumen in it), pulmonary infarction (blockage of a vessel supplying the lung by a blood clot), recurrent pulmonary embolism.

IN " folk medicine» Acetylsalicylic acid is used to relieve symptoms of hangover and headaches.

Instructions for use Acetylsalicylic acid, dosage

The tablets are intended for oral use - it is recommended to take after meals with milk, regular or alkaline mineral water.

Standard dosages of Acetylsalicylic acid according to the instructions for use for adults are from 500 mg to 1 g (1-2 tablets) up to 4 times a day.

  • The maximum single dosage is 1 gram (2 tablets).
  • Maximum daily dosage – 3 grams (6 tablets)

In order to improve the rheological properties of blood, as well as as an inhibitor of platelet aggregation, half a tablet of acetylsalicylic acid is prescribed per day for several months.

For myocardial infarction and for the prevention of secondary myocardial infarction, it is recommended to take 250 mg per day.

Dynamic disturbances cerebral circulation and cerebral thromboembolism suggest taking half a tablet with a gradual increase in the dose to 2 tablets of Acetylsalicylic acid per day.

Side effects

The instructions warn about the possibility of developing the following side effects when prescribing Acetylsalicylic acid:

  • epigastric pain, nausea, vomiting;
  • diarrhea;
  • dizziness and weakness;
  • loss of appetite;
  • impaired visual acuity;
  • bleeding – intestinal, nasal, gingival, stomach;
  • change clinical picture blood – decrease in the amount of hemoglobin and platelets;
  • disorders of the liver and kidneys;
  • development of acute renal failure;
  • bronchospasm, in severe cases development angioedema and anaphylactic shock.

Contraindications

Acetylsalicylic acid is contraindicated in the following cases:

  • gastrointestinal bleeding;
  • aspirin triad;
  • exacerbation of erosive and ulcerative lesions of the digestive tract;
  • reactions to the use of acetylsalicylic acid and other anti-inflammatory drugs in the form of urticaria and rhinitis;
  • hemorrhagic diathesis;
  • hemophilia;
  • hypoprothrombinemia;
  • portal hypertension;
  • arterial hypertension, risk of hemorrhagic stroke;
  • dissecting aortic aneurysm;
  • deficiency of glucose-6-phosphate dehydrogenase;
  • vitamin K deficiency;
  • renal and liver failure;
  • Reye's syndrome.

Also, the drug is contraindicated in pregnant women, during lactation and during hypersensitivity to the components.

Acetylsalicylic acid is not used to treat children and adolescents who are sick or recovering from chickenpox and influenza, as acute hepatic encephalopathy may develop.

Overdose

An overdose of acetisalicylic acid is accompanied by disturbances in the acid-base and electrolyte balance. There is nausea, vomiting, painful sensations in the epigastric region, decreased hearing and visual acuity.

Incoherence of thinking, confusion, tremors, drowsiness, dehydration, alkaline reaction, coma, metabolic acidosis, impaired carbohydrate metabolism.

Treatment is based on accelerating the elimination of the drug, as well as normalizing acid-base balance.

Analogues of Acetylsalicylic acid, price in pharmacies

If necessary, you can replace Acetylsalicylic acid with an analogue according to active substance- these are drugs:

  1. Colfarit,
  2. Mikristin,
  3. Polocard,
  4. Taspir,
  5. Thrombogard 100,
  6. Thrombopol,
  7. Upsarin UPSA.

By ATX code:

  • Aspinat,
  • Aspirin,
  • Acenterine,
  • Bufferin,
  • Taspir.

When choosing analogues, it is important to understand that the instructions for use of Acetylsalicylic acid, price and reviews of the drugs similar action do not apply. It is important to consult a doctor and not change the drug yourself.

Price in Russian pharmacies: Acetylsalicylic acid tablets 500 mg 10 pcs. – from 4 to 9 rubles, 20 tablets – from 15 to 21 rubles, according to 592 pharmacies.

Store out of the reach of children at a temperature not exceeding +25°C. Shelf life – 4 years. Sale in pharmacies without a prescription.

special instructions

Use with caution in patients with liver and kidney diseases, bronchial asthma, erosive and ulcerative lesions and bleeding from the gastrointestinal tract in history, with increased bleeding or while carrying out anticoagulant therapy, decompensated chronic heart failure.

Acetylsalicylic acid, even in small doses, reduces the excretion of uric acid from the body, which can cause an acute attack of gout in predisposed patients. When carrying out long-term therapy and/or use in high doses, medical supervision and regular monitoring of hemoglobin levels are required.

Use as an anti-inflammatory agent in a daily dose of 5–8 g is limited due to the high likelihood of developing side effects from the gastrointestinal tract.

Before surgery, to reduce bleeding during surgery and during postoperative period You should stop taking salicylates 5 to 7 days in advance.

During long-term therapy it is necessary to carry out general analysis blood and stool examination for occult blood.

The use of acetylsalicylic acid in pediatrics is contraindicated, since in the case of a viral infection in children the risk of developing Reye's syndrome increases. Symptoms of Reye's syndrome are prolonged vomiting, acute encephalopathy, and liver enlargement.

Interaction with other drugs and alcohol

In combination with anticoagulants, the risk of bleeding increases.

In combination with non-steroidal anti-inflammatory drugs, they increase side effects the latter.

In combination with methotrexate, it increases side effect the last one.

An increase in the hypoglycemic effect is observed when acetylsalicylic acid is combined with antidiabetic drugs.

In combination with glucocorticoids and when drinking alcohol, the risk of gastrointestinal bleeding increases.

In combination with interferon, a decrease in the activity of the latter is possible.

In combination with antihypertensive drugs, furosemide and anti-gout drugs weaken the effect of the latter.

Antacid medications combined with the use of acetylsalicylic acid help reduce the level of salicylate in the blood.

INN: Acetylsalicylic acid

Manufacturer: Marbiopharm OJSC

Anatomical-therapeutic-chemical classification: Acetylsalicylic acid

Registration number in the Republic of Kazakhstan: No. RK-LS-5No. 020068

Registration period: 07.08.2013 - 07.08.2018

Instructions

Tradename

Acetylsalicylic acid

International nonproprietary name

Acetylsalicylic acid

Dosage form

Tablets, 500 mg

Compound

One tablet contains

active substance: acetylsalicylic acid - 500 mg

Excipients: potato starch, acid stearic acid, citric acid monohydrate, talc

Description

Flat-cylindrical tablets, white, chamfered and scored, slightly marbled

Pharmacotherapeutic group

Analgesics. Other analgesics and antipyretics. Salicylic acid and its derivatives. Acetylsalicylic acid

ATX code N02BA01

Pharmacological properties

Pharmacokinetics

After ingestion, acetylsalicylic acid is converted into the main metabolite - salicylic acid. Absorption of acetylsalicylic and salicylic acids in digestive tract happens quickly and completely. The maximum level of concentration in blood plasma is achieved after 10-20 minutes (acetylsalicylic acid) or 45-120 minutes ( general level salicylates). The degree of binding of acids to plasma proteins depends on the concentration, which is 49-70% for acetylsalicylic acid and 66-98% for salicylic acid. 50% of the administered dose of the drug is metabolized during the initial passage through the liver.

The drug penetrates the blood-brain barrier and is also detected in breast milk and synovial fluid.

Metabolites of acetylsalicylic and salicylic acids are the glycine conjugant of salicylic acid, gentisic acid and its glycine conjugant. The biotransformation of salicylates occurs primarily in the liver with the formation of 4 main metabolites found in many tissues and urine. Excretion of salicylates is carried out mainly by active secretion in the renal tubules in unchanged form (60%) and in the form of metabolites. The rate of excretion depends on the dose - when taking small doses, the half-life is 2-3 hours, and with increasing doses it can increase to 15-30 hours. In newborns, the elimination of salicylates is much slower than in adults. The anti-inflammatory effect of the drug occurs after 1-2 days of administration (after creating a constant therapeutic level of salicylates in the tissues, which is approximately 150-300 mcg/ml), reaches a maximum at a concentration of 20-30 mg% and persists throughout the entire period of use.

Pharmacodynamics

Acetylsalicylic acid has anti-inflammatory, antipyretic, and analgesic effects.

The anti-inflammatory effect of acetylsalicylic acid is explained by its influence on the processes occurring at the site of inflammation: a decrease in capillary permeability, a decrease in hyaluronidase activity, limiting the energy supply of the inflammatory process by inhibiting the formation of ATP, etc.

The antipyretic effect is associated with the effect on the hypothalamic thermoregulation centers.

The analgesic effect is due to the effect on pain sensitivity centers and the ability of salicylates to reduce the algogenic effect of bradykinin.

One of the main mechanisms of action of acetylsalicylic acid is the inactivation (suppression of activity) of the enzyme cyclooxygenase (an enzyme involved in the synthesis of prostaglandins), as a result of which the synthesis of prostaglandins is disrupted. Impaired prostaglandin synthesis leads to loss of sensitivity of peripheral nerve endings to kinins and other inflammatory and pain mediators (transmitters). Due to the disruption of prostaglandin synthesis, the severity of inflammation and their pyrogenic (increasing body temperature) effect on the thermoregulation center decreases. In addition, the effect of prostaglandins on sensory nerve endings is reduced, leading to a decrease in their sensitivity to pain mediators. It also has an antiaggregation effect.

The antiaggregation effect of the drug is to reduce the ability of platelets and other blood cells to aggregate and reduce the likelihood of thrombus formation. The mechanism of this action is associated with blocking the cyclooxygenase pathway of arachidonic acid metabolism, inhibition of the enzymes thromboxane synthetase, phosphodiesterase, an increase in the concentration of cAMP in platelets, a decrease in the level of intracellular calcium, inhibition of the synthesis of prostaglandins and the endogenous (synthesized in the body) compound of the prostaglandin group (eicosanoids) - thromboxane A2, which is a very active proaggregation (promoting platelet aggregation) factor, increasing the concentration of adenosine in the blood, blockade of glycoprotein GP IIb/IIIa receptors. As a result, platelet aggregation is inhibited, their resistance to deformation increases, the rheological properties of blood are improved, thrombus formation is suppressed, and microcirculation is normalized. Significant inhibition of platelet adhesiveness is achieved at doses of up to 30 mg. Increases fibrinolytic activity of plasma and reduces the concentration of vitamin K-dependent blood clotting factors. Stimulates the excretion of uric acid in high doses, since its reabsorption in the kidney tubules is disrupted.

Indications for use

    acute rheumatic fever, rheumatoid arthritis, pericarditis, Dressler's syndrome, rheumatic chorea

    pain syndrome weak and medium intensity (including headache, migraine, toothache, pain due to osteoarthritis, arthritis, menalgia, algodismenorrhea)

    diseases of the spine accompanied by pain (lumbago, sciatica)

    neuralgia, myalgia

    elevated temperature body at colds and other infectious and inflammatory diseases (in adults and children over 15 years old)

Directions for use and doses

Acetylsalicylic acid is taken orally, after meals, with plenty of liquid - water, milk or mineral water.

For fever and pain syndrome It is recommended to take 0.25 - 0.5 g / day (1/2-1 tablet) 3 - 6 times a day. The interval between doses should be at least 4 hours. Maximum single dose 1 g. Maximum daily dose is 3.0 g.

If pain or fever persists after taking acetylsalicylic acid for 5 days, you should stop treatment and consult a doctor.

Side effects

    dizziness, tinnitus, hearing loss

    NSAID gastropathy: pain in the epigastric region, heartburn, nausea, vomiting, severe bleeding in the gastrointestinal tract

    thrombocytopenia, anemia, leukopenia

    Reye/Reye syndrome (progressive encephalopathy: nausea and uncontrollable vomiting, respiratory failure, drowsiness, convulsions; fatty infiltration liver, hyperammonemia, increased levels of AST, ALT)

    allergic reactions: laryngeal edema, bronchospasm, urticaria, aspirin bronchial asthma and the “aspirin” triad (eosinophilic rhinitis, recurrent nasal polyposis, hyperplastic sinusitis)

With long-term use:

    interstitial nephritis, prerenal azotemia with increased blood creatinine and hypercalcemia, acute renal failure, nephrotic syndrome

    papillary necrosis

    blood diseases (anemia, agranulocytosis, thrombocytopenic purpura)

    aseptic meningitis

    increased symptoms of congestive heart failure, edema

    increased levels of aminotransferases in the blood.

Contraindications

    hypersensitivity to any component of the drug, including “aspirin” asthma, “aspirin” triad

    hemorrhagic diathesis(hemophilia, von Willebrand disease, telangioethasia, thrombocytopenic purpura)

    dissecting aortic anervism

    decompensated chronic heart failure

    acute and recurrent erosive and ulcerative diseases of the gastrointestinal tract (including gastrointestinal bleeding)

    renal and liver failure

    initial hypoprothrombinemia, vitamin K deficiency, thrombocytopenia

  • pregnancy and lactation

    childhood up to 15 years.

Drug interactions

When using acetylsalicylic acid together with drugs valproic acid, cephalosporins or anticoagulants increases the risk of bleeding. With simultaneous use of the drug and NSAIDs, the main and side effects the latter.

During treatment with the drug, it worsens side effect methotrexate (when taking the latter more than 15 mg/week, acetylsalicylic acid is contraindicated).

When used simultaneously with oral hypoglycemic drugs - sulfonylurea derivatives - the hypoglycemic effect is enhanced.

When used simultaneously with glucocorticosteroids and alcohol consumption, the risk of gastrointestinal bleeding increases.

The drug weakens the effect of spironolactone, furosemide, antihypertensive and anti-gout drugs that promote the excretion of uric acid.

Prescribing antacids during treatment with the drug (especially in doses of more than 3.0 g for adults) may cause a decrease in high steady-state levels of salicylate in the blood.

special instructions

Acetylsalicylic acid increases the risk of bleeding even when taking small doses and for several days after taking it. Before any surgical procedure, inform your doctor, surgeon, anesthesiologist or dentist that you are taking acetylsalicylic acid. 5-7 days before surgical intervention it is necessary to stop taking it (to reduce bleeding during surgery and in the postoperative period). During long-term therapy, it is recommended to regularly perform blood tests and examine stool for occult blood.

With simultaneous anticoagulant therapy with acetylsalicylic acid in small doses, the excretion of uric acid is reduced, which may be the cause of gout.

Use in pediatrics The drug acetylsalicylic acid is not prescribed to children under 15 years of age with acute respiratory diseases caused by viral infections, with diseases accompanied by hyperthermia due to the risk of developing Reye/Reye syndrome).

Features of influence medicine on the ability to manage vehicle or potentially dangerous mechanisms

There is no evidence of adverse effects on active attention, motor activity and reflexes.

Overdose

Csymptoms: dizziness, visual and hearing impairment, nausea, vomiting, increased breathing. Later, depression of consciousness occurs, up to coma, respiratory failure, acid-base imbalance (respiratory alkalosis, then metabolic acidosis), acute renal failure (ARF), shock. Deadly intoxication is possible when taking a dose of 200 to 500 mg/kg.

INN: Acetylsalicylic acid

Manufacturer: Marbiopharm OJSC

Anatomical-therapeutic-chemical classification: Acetylsalicylic acid

Registration number in the Republic of Kazakhstan: No. RK-LS-5No. 020068

Registration period: 07.08.2013 - 07.08.2018

Instructions

Tradename

Acetylsalicylic acid

International nonproprietary name

Acetylsalicylic acid

Dosage form

Tablets, 500 mg

Compound

One tablet contains

active substance: acetylsalicylic acid - 500 mg

Excipients: potato starch, acid stearic acid, citric acid monohydrate, talc

Description

Flat-cylindrical tablets, white, beveled and scored, slightly marbled

Pharmacotherapeutic group

Analgesics. Other analgesics and antipyretics. Salicylic acid and its derivatives. Acetylsalicylic acid

ATX code N02BA01

Pharmacological properties

Pharmacokinetics

After ingestion, acetylsalicylic acid is converted into the main metabolite - salicylic acid. Absorption of acetylsalicylic and salicylic acids in the digestive tract occurs quickly and completely. The maximum level of concentration in the blood plasma is reached after 10-20 minutes (acetylsalicylic acid) or 45-120 minutes (total level of salicylates). The degree of binding of acids to plasma proteins depends on the concentration, which is 49-70% for acetylsalicylic acid and 66-98% for salicylic acid. 50% of the administered dose of the drug is metabolized during the initial passage through the liver.

The drug penetrates the blood-brain barrier and is also detected in breast milk and synovial fluid.

Metabolites of acetylsalicylic and salicylic acids are the glycine conjugant of salicylic acid, gentisic acid and its glycine conjugant. The biotransformation of salicylates occurs primarily in the liver with the formation of 4 main metabolites found in many tissues and urine. Excretion of salicylates is carried out mainly by active secretion in the renal tubules in unchanged form (60%) and in the form of metabolites. The rate of excretion depends on the dose - when taking small doses, the half-life is 2-3 hours, and with increasing doses it can increase to 15-30 hours. In newborns, the elimination of salicylates is much slower than in adults. The anti-inflammatory effect of the drug occurs after 1-2 days of administration (after creating a constant therapeutic level of salicylates in the tissues, which is approximately 150-300 mcg/ml), reaches a maximum at a concentration of 20-30 mg% and persists throughout the entire period of use.

Pharmacodynamics

Acetylsalicylic acid has anti-inflammatory, antipyretic, and analgesic effects.

The anti-inflammatory effect of acetylsalicylic acid is explained by its influence on the processes occurring at the site of inflammation: a decrease in capillary permeability, a decrease in hyaluronidase activity, limiting the energy supply of the inflammatory process by inhibiting the formation of ATP, etc.

The antipyretic effect is associated with the effect on the hypothalamic thermoregulation centers.

The analgesic effect is due to the effect on pain sensitivity centers and the ability of salicylates to reduce the algogenic effect of bradykinin.

One of the main mechanisms of action of acetylsalicylic acid is the inactivation (suppression of activity) of the enzyme cyclooxygenase (an enzyme involved in the synthesis of prostaglandins), as a result of which the synthesis of prostaglandins is disrupted. Impaired prostaglandin synthesis leads to loss of sensitivity of peripheral nerve endings to kinins and other inflammatory and pain mediators (transmitters). Due to the disruption of prostaglandin synthesis, the severity of inflammation and their pyrogenic (increasing body temperature) effect on the thermoregulation center decreases. In addition, the effect of prostaglandins on sensory nerve endings is reduced, leading to a decrease in their sensitivity to pain mediators. It also has an antiaggregation effect.

The antiaggregation effect of the drug is to reduce the ability of platelets and other blood cells to aggregate and reduce the likelihood of thrombus formation. The mechanism of this action is associated with blocking the cyclooxygenase pathway of arachidonic acid metabolism, inhibition of the enzymes thromboxane synthetase, phosphodiesterase, an increase in the concentration of cAMP in platelets, a decrease in the level of intracellular calcium, inhibition of the synthesis of prostaglandins and the endogenous (synthesized in the body) compound of the prostaglandin group (eicosanoids) - thromboxane A2, which is a very active proaggregation (promoting platelet aggregation) factor, increasing the concentration of adenosine in the blood, blockade of glycoprotein GP IIb/IIIa receptors. As a result, platelet aggregation is inhibited, their resistance to deformation increases, the rheological properties of blood are improved, thrombus formation is suppressed, and microcirculation is normalized. Significant inhibition of platelet adhesiveness is achieved at doses of up to 30 mg. Increases fibrinolytic activity of plasma and reduces the concentration of vitamin K-dependent blood clotting factors. Stimulates the excretion of uric acid in high doses, since its reabsorption in the kidney tubules is disrupted.

Indications for use

    acute rheumatic fever, rheumatoid arthritis, pericarditis, Dressler's syndrome, rheumatic chorea

    pain syndrome of mild to moderate intensity (including headache, migraine, toothache, pain due to osteoarthritis, arthritis, menalgia, algomenorrhea)

    diseases of the spine accompanied by pain (lumbago, sciatica)

    neuralgia, myalgia

    elevated body temperature during colds and other infectious and inflammatory diseases (in adults and children over 15 years of age)

Directions for use and doses

Acetylsalicylic acid is taken orally, after meals, with plenty of liquid - water, milk or mineral water.

For fever and pain syndrome It is recommended to take 0.25 - 0.5 g / day (1/2-1 tablet) 3 - 6 times a day. The interval between doses should be at least 4 hours. The maximum single dose is 1 g. The maximum daily dose is 3.0 g.

If pain or fever persists after taking acetylsalicylic acid for 5 days, you should stop treatment and consult a doctor.

Side effects

    dizziness, tinnitus, hearing loss

    NSAID gastropathy: pain in the epigastric region, heartburn, nausea, vomiting, severe bleeding in the gastrointestinal tract

    thrombocytopenia, anemia, leukopenia

    Reye/Reye syndrome (progressive encephalopathy: nausea and uncontrollable vomiting, respiratory distress, drowsiness, convulsions; fatty liver, hyperammonemia, increased levels of AST, ALT)

    allergic reactions: laryngeal edema, bronchospasm, urticaria, “aspirin” bronchial asthma and “aspirin” triad (eosinophilic rhinitis, recurrent nasal polyposis, hyperplastic sinusitis)

With long-term use:

    interstitial nephritis, prerenal azotemia with increased blood creatinine and hypercalcemia, acute renal failure, nephrotic syndrome

    papillary necrosis

    blood diseases (anemia, agranulocytosis, thrombocytopenic purpura)

    aseptic meningitis

    increased symptoms of congestive heart failure, edema

    increased levels of aminotransferases in the blood.

Contraindications

    hypersensitivity to any component of the drug, including “aspirin” asthma, “aspirin” triad

    hemorrhagic diathesis (hemophilia, von Willebrand disease, telangioethasia, thrombocytopenic purpura)

    dissecting aortic anervism

    decompensated chronic heart failure

    acute and recurrent erosive and ulcerative diseases of the gastrointestinal tract (including gastrointestinal bleeding)

    renal and liver failure

    initial hypoprothrombinemia, vitamin K deficiency, thrombocytopenia

  • pregnancy and lactation

    children under 15 years of age.

Drug interactions

When using acetylsalicylic acid together with valproic acid, cephalosporins or anticoagulants, the risk of bleeding increases. With simultaneous use of the drug and NSAIDs, the main and side effects of the latter increase.

During treatment with the drug, the side effects of methotrexate are aggravated (when taking the latter more than 15 mg/week, acetylsalicylic acid is contraindicated).

When used simultaneously with oral hypoglycemic drugs - sulfonylurea derivatives - the hypoglycemic effect is enhanced.

When used simultaneously with glucocorticosteroids and alcohol consumption, the risk of gastrointestinal bleeding increases.

The drug weakens the effect of spironolactone, furosemide, antihypertensive and anti-gout drugs that promote the excretion of uric acid.

Prescribing antacids during treatment with the drug (especially in doses of more than 3.0 g for adults) may cause a decrease in high steady-state levels of salicylate in the blood.

special instructions

Acetylsalicylic acid increases the risk of bleeding even when taking small doses and for several days after taking it. Before any surgical procedure, inform your doctor, surgeon, anesthesiologist or dentist that you are taking acetylsalicylic acid. 5-7 days before surgery, it is necessary to stop taking the drug (to reduce bleeding during surgery and in the postoperative period). During long-term therapy, it is recommended to regularly perform blood tests and examine stool for occult blood.

With simultaneous anticoagulant therapy with acetylsalicylic acid in small doses, the excretion of uric acid is reduced, which may be the cause of gout.

Use in pediatrics The drug acetylsalicylic acid is not prescribed to children under 15 years of age with acute respiratory diseases caused by viral infections, with diseases accompanied by hyperthermia due to the risk of developing Reye/Reye syndrome).

Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms

There is no evidence of adverse effects on active attention, motor activity and reflexes.

Overdose

Csymptoms: dizziness, visual and hearing impairment, nausea, vomiting, increased breathing. Later, depression of consciousness occurs up to coma, respiratory failure, acid-base imbalance (respiratory alkalosis, then metabolic acidosis), acute renal failure (ARF), shock. Deadly intoxication is possible when taking a dose of 200 to 500 mg/kg.

The tablet contains 0.1, 0.25 or 0.5 grams of the active substance, as well as citric acid (in the form of monohydrate) and potato starch.

Release form

  • tablets 0.1, 0.25 and 0.5 grams;
  • tablets are packaged in contour cell-free or contour cell packaging No. 10x1, No. 10x2, No. 10x3.

pharmachologic effect

The drug relieves pain, fever and inflammation , prevents aggregation.

Pharmacological group: NSAIDs.

Pharmacodynamics and pharmacokinetics

Acetylsalicylic acid - what is it?

Acetylsalicylic acid is a salicylic ester of acetic (ethanoic) acid.

The formula of acetylsalicylic acid is (ASA) - C₉H₈O₄.

OKPD code 24.42.13.142 ( acetylsalicylic acid mixed with other drugs).

Receiving ASA

In the production of ASA, the method of esterification with ethanoic acid is used.

Pharmacodynamics

The analgesic effect is due to both central and peripheral effects. In feverish conditions, it reduces the temperature by affecting the thermoregulation center.

Aggregation And platelet adhesiveness , and thrombus formation decrease due to the ability of ASA to suppress the synthesis of thromboxane A2 (TXA 2) in platelets. Inhibits synthesis prothrombin (coagulation factor II) in the liver and - at a dose exceeding 6 g/day. - increases PTV.

Pharmacokinetics

Absorption of the substance after taking the drug orally is almost complete. The half-life of unchanged ASA is no more than 20 minutes. TCmax of ASA - 10-20 minutes, total salicylate formed as a result - from 0.3 to 2.0 hours.

For children

In children, ASA cannot be used for hyperthermia related to viral infection , since such a combination can cause the development life-threatening child's condition - Reye's syndrome .

In newborn infants, salicylic acid can displace its connection with albumin bilirubin and promote development encephalopathy .

ASA easily penetrates into all fluids and tissues of the body, including cerebrospinal, synovial and peritoneal fluid.

In the presence of edema and inflammation, the penetration of salicylate into the joint cavity is accelerated. In the stage of inflammation, on the contrary, it slows down.

Acetylsalicylic acid and alcohol

Alcohol during the period of ASA is contraindicated. This combination can cause gastric and intestinal bleeding, as well as severe hypersensitivity reactions.

What is Acetylsalicylic acid used for hangovers?

ASC is very effective means from a hangover, which is due to the antiplatelet effect of the drug.

However, you should remember that it is better to take the tablet not while drinking alcohol, but about 2 hours before the feast. This reduces the risk of formation microthrombi in small vessels of the brain and - partly - tissue edema.

Use during pregnancy and breastfeeding

Acetylsalicylic acid is contraindicated during pregnancy. Especially in the first and last three months of gestation. On early stages taking the drug may increase the risk of developing birth defects, in the later stages - post-term pregnancy and weakening of labor.

ASA and its metabolites pass into milk in small quantities. After accidentally taking the drug, no side effects were observed in infants, and therefore interrupt breast-feeding(GV), as a rule, is not necessary.

If a woman is shown long-term treatment high doses of ASA, it is necessary to stop breastfeeding.