What does acetyl acid help with: instructions for use. Acetylsalicylic acid for fever in children and adults

ATX code: N02BA01

Trade name: Acetylsalicylic acid International generic name: Acetylsalicylic acid Release form: tablets 500 mg Description: tablets white, slightly marbled, with a characteristic smell, flat-cylindrical, with a notch, a chamfer. Composition: 1 tablet contains: active substance- acetyl salicylic acid- 500 mg; excipients: potato starch, edible citric acid, talc, stearic acid, anhydrous colloidal silicon dioxide. Pharmacotherapeutic group: Other analgesics and antipyretics. Salicylic acid and its derivatives.

Acute rheumatic fever, rheumatoid arthritis, pericarditis, Dressler's syndrome, rheumatic chorea;
- pain syndrome of weak and moderate intensity (including headache, migraine, toothache, pain due to osteoarthritis, arthritis, menalgia, algodismenorrhea);
- diseases of the spine accompanied by pain: lumbago, sciatica;
- neuralgia, myalgia;
- febrile syndrome in acute infectious, infectious-inflammatory diseases;
- prevention of the development of myocardial infarction in case of ischemic heart disease, the presence of several factors risk of ischemic heart disease, silent myocardial ischemia, unstable angina;
- prevention of recurrent myocardial infarction in persons with a history of heart attack;
- prevention of ischemic stroke in persons with a transient ischemic attack, a history of ischemic stroke (in men);
- reducing the risk of re-stenosis and secondary dissection of the coronary artery after balloon coronary angioplasty and stent installation;
- prevention of thromboembolism in vasculitis coronary arteries(Kawasaki disease, Takayasu aortoarteritis), valvular mitral heart defects, atrial fibrillation, prolapse mitral valve.

Glucose-6-phosphate dehydrogenase deficiency;
- increased sensitivity to acetylsalicylic and salicylic acid;
- erosive and ulcerative lesions Gastrointestinal tract in the acute phase;
- gastrointestinal bleeding;
- “aspirin” asthma and “aspirin” triad;
- hemorrhagic diathesis (von Willebrand disease, thrombocytopenic purpura, telangiectasia), hypoprothrombinemia, hemophilia;
- dissecting aortic aneurysm;
- portal hypertension;
- vitamin K deficiency;
- taking methotrexate at a dose of 15 mg/week or more;
- renal and liver failure;
- pregnancy I and III trimester, lactation;
- gout and gouty arthritis;
- childhood up to 15 years in combination with hyperthermia due to viral diseases.

Use internally, preferably between meals. The tablet is placed in 100 ml boiled water(1/2 cup) and, stirring, achieve its disintegration, after which they drink the resulting suspension.
Adults are prescribed 1 - 2 tablets 3 times a day. Maximum single dose- 2 tablets, maximum daily dose- 6 tablets.
Children (for the treatment of acute rheumatic fever, pericarditis, pain relief) are prescribed at a rate of 20-30 mg/kg. At the age of 2 - 3 years, 100 mg/day. At the age of 4-6 years at a dose of 200 mg/day. At the age of 7-9 years at a dose of 300 mg/day. Over the age of 12 years, a single dose of 250 mg (1/2 tablet) 2 times a day, maximum daily dose of 750 mg.
For myocardial infarction, as well as for secondary prevention in people who have had a heart attack, 40 - 325 mg 1 time per day, in the evening (usually 1/4-1/2 tablet).
As a means to reduce platelet aggregation and prevent thromboembolic complications, 250-325 mg/day (1/2-3/4 tablets) for a long period.
For transient ischemic attacks or cerebral thromboembolic complications in men, use 250-325 mg/day (1/2-3/4 tablets) with a gradual increase to a maximum of 1000 mg/day.
For the prevention of thrombosis or occlusion of the aortic shunt - 325 mg (3/4 tablets) every 7 hours through a nasogastric tube. Then orally at the same dose 3 times a day in combination with dipyridamole (after 1 week, dipyridamole is discontinued).
As an antipyretic, it is prescribed at a body temperature of more than 38.5 ° C (in patients with febrile seizures history - at a temperature of more than 37.5 ° C) at a dose of 500-1000 mg.

Gross formula

C9H8O4

Pharmacological group of the substance Acetylsalicylic acid

Nosological classification (ICD-10)

CAS code

50-78-2

Characteristics of the substance Acetylsalicylic acid

White fine needle-shaped crystals or light crystalline powder, odorless or faint odor, slightly sour taste. Slightly soluble in water at room temperature, soluble in hot water, easily soluble in ethanol, solutions of caustic and carbonic alkalis.

Pharmacology

Pharmacological action- anti-inflammatory, antipyretic, antiaggregation, analgesic.

Inhibits cyclooxygenase (COX-1 and COX-2) and irreversibly inhibits the cyclooxygenase pathway of arachidonic acid metabolism, blocks the synthesis of PG (PGA 2, PGD 2, PGF 2alpha, PGE 1, PGE 2, etc.) and thromboxane. Reduces hyperemia, exudation, capillary permeability, hyaluronidase activity, limits energy supply inflammatory process by inhibiting ATP production. Affects the subcortical centers of thermoregulation and pain sensitivity. A decrease in the content of PG (mainly PGE 1) in the thermoregulation center leads to a decrease in body temperature due to dilation of skin vessels and increased sweating. The analgesic effect is due to the effect on pain sensitivity centers, as well as the peripheral anti-inflammatory effect and the ability of salicylates to reduce the algogenic effect of bradykinin. A decrease in the content of thromboxane A 2 in platelets leads to irreversible suppression of aggregation and slightly dilates blood vessels. The antiplatelet effect lasts for 7 days after a single dose. During the series clinical trials It has been shown that 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 coagulation factors (II, VII, IX, X). Stimulates excretion uric acid, since its reabsorption in the kidney tubules is impaired.

After oral administration, it is absorbed quite completely. In the presence of an enteric coating (resistant to the action gastric juice and does not allow absorption acetylsalicylic acid in the stomach) is absorbed into upper section small intestine. During absorption, it undergoes presystemic elimination in the intestinal wall and in the liver (deacetylated). The absorbed part is very quickly hydrolyzed by special esterases, so T1/2 of acetylsalicylic acid is no more than 15-20 minutes. It circulates in the body (75-90% in connection with albumin) and is distributed in tissues in the form of salicylic acid anion. Cmax is reached after approximately 2 hours. Acetylsalicylic acid practically does not bind to blood plasma proteins. During biotransformation in the liver, metabolites are formed that are found in many tissues and urine. Excretion of salicylates occurs primarily through active secretion in the renal tubules in unchanged form and in the form of metabolites. The excretion of unchanged substance and metabolites depends on the pH of the urine (with alkalinization of urine, the ionization of salicylates increases, their reabsorption worsens and excretion increases significantly).

Application of the substance Acetylsalicylic acid

IHD, the presence of several risk factors for IHD, silent myocardial ischemia, unstable angina, myocardial infarction (to reduce the risk of recurrent myocardial infarction and death after myocardial infarction), recurrent transient cerebral ischemia and ischemic stroke in men, heart valve replacement (prevention and treatment of thromboembolism), balloon coronary angioplasty and stent placement (reducing the risk of recurrent stenosis and treatment secondary coronary artery dissection), as well as non-atherosclerotic lesions of the coronary arteries (Kawasaki disease), aortoarteritis (Takayasu disease), valvular mitral heart defects and atrial fibrillation, mitral valve prolapse (prevention of thromboembolism), recurrent thromboembolism pulmonary artery, Dressler's syndrome, pulmonary infarction, acute thrombophlebitis. Fever in infectious and inflammatory diseases. Pain syndrome low to medium intensity of various origins, incl. chest radicular syndrome, lumbago, migraine, headache, neuralgia, toothache, myalgia, arthralgia, algodismenorrhea. In clinical immunology and allergology, it is used in gradually increasing doses for long-term “aspirin” desensitization and the formation of stable tolerance to NSAIDs in patients with “aspirin” asthma and the “aspirin” triad.

According to indications: rheumatism, rheumatic chorea, rheumatoid arthritis, infectious-allergic myocarditis, pericarditis - currently used very rarely.

Contraindications

Hypersensitivity, incl. “aspirin” triad, “aspirin” asthma; hemorrhagic diathesis(hemophilia, von Willebrand disease, telangiectasia), dissecting aortic aneurysm, heart failure, acute and recurrent erosive and ulcerative diseases of the gastrointestinal tract, gastrointestinal bleeding, acute renal or liver failure, initial hypoprothrombinemia, vitamin K deficiency, thrombocytopenia, thrombotic thrombocytopenic purpura, deficiency glucose-6-phosphate dehydrogenase, pregnancy (I and III trimester), breastfeeding, children and adolescence up to 15 years when used as an antipyretic (risk of developing Reye's syndrome in children with fever due to viral diseases).

Restrictions on use

Hyperuricemia, nephrolithiasis, gout, peptic ulcer stomach and duodenum(in history), severe violations liver and kidney function, bronchial asthma, COPD, nasal polyposis, uncontrolled arterial hypertension.

Use during pregnancy and breastfeeding

Application large doses salicylates in the first trimester of pregnancy is associated with an increased incidence of fetal development defects (cleft palate, heart defects). In the second trimester of pregnancy, salicylates can be prescribed only after assessing the risks and benefits. The administration of salicylates in the third trimester of pregnancy is contraindicated.

Salicylates and their metabolites in small quantities penetrate into breast milk. Accidental intake of salicylates during lactation is not accompanied by the development adverse reactions in a child and does not require termination breastfeeding. However, when long-term use or appointment in high doses ah breastfeeding should be stopped.

Side effects of the substance Acetylsalicylic acid

From the outside cardiovascular system and blood (hematopoiesis, hemostasis): thrombocytopenia, anemia, leukopenia.

From the gastrointestinal tract: NSAID gastropathy (dyspepsia, pain in the epigastric region, heartburn, nausea and vomiting, severe bleeding in the gastrointestinal tract), loss of appetite.

Allergic reactions: hypersensitivity reactions (bronchospasm, laryngeal edema and urticaria), the formation of “aspirin” based on the hapten mechanism bronchial asthma and the “aspirin” triad (eosinophilic rhinitis, recurrent nasal polyposis, hyperplastic sinusitis).

Others: liver and/or kidney dysfunction, Reye's syndrome in children (encephalopathy and acute fatty degeneration liver with rapid development liver failure).

With prolonged use - dizziness, headache, tinnitus, decreased hearing acuity, blurred vision, interstitial nephritis, prerenal azotemia with increased blood creatinine levels and hypercalcemia, papillary necrosis, spicy renal failure, nephrotic syndrome, blood diseases, aseptic meningitis, increased symptoms of congestive heart failure, edema, increased levels of aminotransferases in the blood.

Interaction

Increases the toxicity of methotrexate, reducing its renal clearance, effects narcotic analgesics(codeine), oral antidiabetic drugs, heparin, indirect anticoagulants, thrombolytics and platelet aggregation inhibitors, reduces the effect of uricosuric drugs (benzbromarone, sulfinpyrazone), antihypertensive drugs, diuretics (spironolactone, furosemide). Paracetamol and caffeine increase the risk of developing side effects. Glucocorticoids, ethanol and ethanol-containing drugs enhance negative impact on the gastrointestinal mucosa and increase clearance. Increases the concentration of digoxin, barbiturates, lithium salts in plasma. Antacids containing magnesium and/or aluminum slow down and impair the absorption of acetylsalicylic acid. Myelotoxic drugs enhance the manifestations of hematotoxicity of acetylsalicylic acid.

Overdose

May occur after a single large dose or when long-term use. If a single dose is less than 150 mg/kg, acute poisoning considered mild, 150-300 mg/kg - moderate, when using higher doses - severe.

Symptoms: salicylic syndrome (nausea, vomiting, tinnitus, blurred vision, dizziness, severe headache, general malaise, fever - a poor prognostic sign in adults). More severe poisoning includes stupor, convulsions and coma, non-cardiogenic pulmonary edema, severe dehydration, acid-base balance disorders (first respiratory alkalosis, then metabolic acidosis), renal failure and shock.

At chronic overdose the concentration determined in plasma does not correlate well with the severity of intoxication. Greatest risk of development chronic intoxication observed in elderly people when taking more than 100 mg/kg/day for several days. In children and elderly patients initial signs Salicylism is not always noticeable, so it is advisable to periodically determine the concentration of salicylates in the blood. Levels above 70 mg% indicate moderate or severe poisoning; above 100 mg% - extremely severe, prognostically unfavorable. In case of poisoning moderate severity hospitalization for at least 24 hours is required.

Treatment: provocation of vomiting, purpose activated carbon and laxatives, monitoring of acid-base balance and electrolyte balance; depending on the metabolic state - administration of sodium bicarbonate, sodium citrate solution or sodium lactate. Increasing reserve alkalinity enhances the excretion of acetylsalicylic acid due to alkalinization of urine. Alkalinization of urine is indicated when the level of salicylates is above 40 mg%, provided by intravenous infusion of sodium bicarbonate - 88 mEq in 1 liter of 5% glucose solution, at a rate of 10-15 ml/kg/h. Restoration of bcc and induction of diuresis (achieved by administering bicarbonate in the same dose and dilution, repeat 2-3 times); It should be borne in mind that intensive fluid infusion in elderly patients can lead to pulmonary edema. The use of acetazolamide for alkalinization of urine is not recommended (may cause acidemia and increase toxic effect salicylates). Hemodialysis is indicated when the level of salicylates is more than 100-130 mg%, and in patients with chronic poisoning- 40 mg% and lower if indicated (refractory acidosis, progressive deterioration, heavy defeat CNS, pulmonary edema and renal failure). For pulmonary edema - mechanical ventilation with an oxygen-enriched mixture in positive end-expiratory pressure mode; Hyperventilation and osmotic diuresis are used to treat cerebral edema.

Routes of administration

Inside.

Precautions for the substance Acetylsalicylic acid

Undesirable joint use with other NSAIDs and glucocorticoids. 5-7 days before surgical intervention it is necessary to stop taking it (to reduce bleeding during surgery and in the postoperative period).

The likelihood of developing NSAID gastropathy is reduced when prescribed after meals, using tablets with buffer additives or coated with a special enteric coating. The risk of hemorrhagic complications is considered to be lowest when used in doses<100 мг/сут.

It should be borne in mind that in predisposed patients, acetylsalicylic acid (even in small doses) reduces the excretion of uric acid from the body and can cause the development of an acute attack of gout.

During long-term therapy, it is recommended to regularly perform blood tests and examine stool for occult blood. Due to observed cases of hepatogenic encephalopathy, it is not recommended for the relief of febrile syndrome in children.

Interactions with other active ingredients

Related news

Trade names

Name The value of the Vyshkowski Index ®
0.1073
0.0852
0.0676
0.0305
0.0134
0.0085
0.0079

Acetylsalicylic acid contains:

Acetylsalicylic acid 500 mg.

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

Pharmacological action

NSAIDs. It has anti-inflammatory, analgesic and antipyretic effects, and also inhibits platelet aggregation. The mechanism of action is associated with inhibition of the activity of COX, the main enzyme in the metabolism of arachidonic acid, which is a precursor of prostaglandins, which play a major role in the pathogenesis of inflammation, pain and fever. A decrease in the content of prostaglandins (mainly E1) in the thermoregulation center leads to a decrease in body temperature due to dilation of skin vessels and increased sweating. The analgesic effect is due to both central and peripheral effects. Reduces platelet aggregation, adhesion and thrombus formation by suppressing the synthesis of thromboxane A2 in platelets.

Reduces mortality and the risk of myocardial infarction in unstable angina. Effective in the primary prevention of diseases of the cardiovascular system and in the secondary prevention of myocardial infarction. In a daily dose of 6 g or more, it suppresses prothrombin synthesis in the liver and increases prothrombin time. Increases fibrinolytic activity of plasma and reduces the concentration of vitamin K-dependent coagulation factors (II, VII, IX, X). Increases the incidence of hemorrhagic complications during surgical interventions and increases the risk of bleeding during anticoagulant therapy. Stimulates the excretion of uric acid (impairs its reabsorption in the renal tubules), but in high doses. Blockade of COX-1 in the gastric mucosa leads to inhibition of gastroprotective prostaglandins, which can cause ulceration of the mucous membrane and subsequent bleeding.

What does Acetylsalicylic acid help with: indications

  • Rheumatism.
  • Rheumatoid arthritis.
  • Infectious-allergic myocarditis.
  • Fever in infectious and inflammatory diseases.
  • Pain syndrome of weak and moderate intensity of various origins, including: neuralgia, myalgia, headache.
  • Prevention of thrombosis and embolism.
  • Primary and secondary prevention of myocardial infarction.
  • Prevention of ischemic cerebrovascular accidents.
  • In clinical immunology and allergology: in gradually increasing doses for long-term “aspirin” desensitization and the formation of stable tolerance to NSAIDs in patients with “aspirin” asthma and the “aspirin triad”.

Contraindications

  • Erosive and ulcerative lesions of the gastrointestinal tract in the acute phase.
  • Gastrointestinal bleeding.
  • "Aspirin triad".
  • A history of indications of urticaria, rhinitis caused by taking acetylsalicylic acid and other NSAIDs.
  • Hemophilia.
  • Hemorrhagic diathesis.
  • Hypoprothrombinemia.
  • Dissecting aortic aneurysm.
  • Portal hypertension.
  • Vitamin K deficiency.
  • Renal and/or liver failure.
  • Glucose-6-phosphate dehydrogenase deficiency.
  • Reye's syndrome.
  • Children's age (up to 15 years - the risk of developing Reye's syndrome in children with hyperthermia due to viral diseases).
  • I and III trimesters of pregnancy.
  • Lactation period.
  • Hypersensitivity to acetylsalicylic acid and other salicylates.

With caution: liver and kidney diseases, bronchial asthma, history of erosive and ulcerative lesions and bleeding from the gastrointestinal tract, increased bleeding or simultaneous anticoagulation therapy, decompensated chronic heart failure.

Acetylsalicylic acid during pregnancy and breastfeeding

Contraindicated for use in the first and third trimesters of pregnancy. In the second trimester of pregnancy, a one-time dose is possible according to strict indications.

It has a teratogenic effect: when used in the first trimester it leads to the development of cleft palate, in the third trimester it causes inhibition of labor (inhibition of prostaglandin synthesis), premature closure of the ductus arteriosus in the fetus, hyperplasia of the pulmonary vessels and hypertension in the pulmonary circulation.

Acetylsalicylic acid is excreted in breast milk, which increases the risk of bleeding in the baby due to impaired platelet function, so acetylsalicylic acid should not be used by the mother during lactation.

Acetylsalicylic acid: instructions for use

Individually.

For adults, a single dose varies from 40 mg to 1 g, daily - from 150 mg to 8 g, frequency of use - 2-6 times / day.

Side effects

From the digestive system: nausea, vomiting, anorexia, epigastric pain, diarrhea rarely - the occurrence of erosive and ulcerative lesions, bleeding from the gastrointestinal tract, impaired liver function.

From the side of the central nervous system: with prolonged use, dizziness, headache, reversible visual impairment, tinnitus, and aseptic meningitis are possible.

From the hematopoietic system: rarely - thrombocytopenia, anemia.

From the blood coagulation system: rarely - hemorrhagic syndrome, prolongation of bleeding time.

From the urinary system: rarely - impaired renal function with long-term use - acute renal failure, nephrotic syndrome.

Allergic reactions: rarely - skin rash, Quincke's edema, bronchospasm, "aspirin triad" (a combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid and pyrazolone-type drugs).

Other: in some cases - Reye's syndrome with long-term use - increased symptoms of chronic heart failure.

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 using acetylsalicylic acid in high doses, medical supervision and regular monitoring of hemoglobin levels are required.

The use of acetylsalicylic acid 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 in the postoperative period, you should stop taking salicylates for 5-7 days.

During long-term therapy, it is necessary to conduct a complete blood count 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 under the influence of acetylsalicylic acid, the risk of developing Reye's syndrome increases. Symptoms of Reye's syndrome are prolonged vomiting, acute encephalopathy, and liver enlargement.

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

During the treatment period, the patient must abstain from drinking alcohol.

Compatibility with other drugs

When used simultaneously, antacids containing magnesium and/or aluminum hydroxide slow down and reduce the absorption of acetylsalicylic acid.

With the simultaneous use of calcium channel blockers, drugs that limit the intake of calcium or increase the excretion of calcium from the body, the risk of bleeding increases.

When used simultaneously with acetylsalicylic acid, the effect of heparin and indirect anticoagulants, hypoglycemic agents, sulfonylurea derivatives, insulins, methotrexate, phenytoin, and valproic acid is enhanced.

When used simultaneously with GCS, the risk of ulcerogenic effects and gastrointestinal bleeding increases.

With simultaneous use, the effectiveness of diuretics (spironolactone, furosemide) decreases.

With the simultaneous use of other NSAIDs, the risk of side effects increases. Acetylsalicylic acid may reduce plasma concentrations of indomethacin and piroxicam.

When used simultaneously with gold preparations, acetylsalicylic acid can induce liver damage.

With simultaneous use, the effectiveness of uricosuric drugs (including probenecid, sulfinpyrazone, benzbromarone) is reduced.

With the simultaneous use of acetylsalicylic acid and sodium alendronate, severe esophagitis may develop.

With simultaneous use of griseofulvin, the absorption of acetylsalicylic acid may be impaired.

A case of spontaneous hemorrhage into the iris was described when taking Ginkgo biloba extract against the background of long-term use of acetylsalicylic acid at a dose of 325 mg/day. It is believed that this may be due to an additive inhibitory effect on platelet aggregation.

With simultaneous use of dipyridamole, an increase in Cmax of salicylate in blood plasma and AUC is possible.

When used simultaneously with acetylsalicylic acid, the concentrations of digoxin, barbiturates and lithium salts in the blood plasma increase.

With the simultaneous use of salicylates in high doses with carbonic anhydrase inhibitors, salicylate intoxication is possible.

Acetylsalicylic acid in doses less than 300 mg/day has a minor effect on the effectiveness of captopril and enalapril. When using acetylsalicylic acid in high doses, the effectiveness of captopril and enalapril may be reduced.

With simultaneous use, caffeine increases the rate of absorption, plasma concentration and bioavailability of acetylsalicylic acid.

With simultaneous use, metoprolol may increase the Cmax of salicylate in the blood plasma.

When using pentazocine against the background of long-term use of acetylsalicylic acid in high doses, there is a risk of developing severe adverse reactions from the kidneys.

With simultaneous use, phenylbutazone reduces uricosuria caused by acetylsalicylic acid.

With simultaneous use, ethanol may enhance the effect of acetylsalicylic acid on the gastrointestinal tract.

Overdose

Symptoms (single dose less than 150 mg/kg - acute poisoning is considered mild, 150-300 mg/kg - moderate, more than 300 mg/kg - severe): salicylic syndrome (nausea, vomiting, tinnitus, blurred vision, dizziness, severe headache, general malaise, fever - a poor prognostic sign in adults). Severe poisoning - hyperventilation of the lungs of central origin, respiratory alkalosis, metabolic acidosis, confusion, drowsiness, collapse, convulsions, anuria, bleeding. Initially, central hyperventilation of the lungs leads to respiratory alkalosis - shortness of breath, suffocation, cyanosis, cold sticky sweat with increasing intoxication, respiratory paralysis and uncoupling of oxidative phosphorylation, causing respiratory acidosis.

In 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 elderly people when taking more than 100 mg/kg/day for several days. In children and elderly patients, the initial signs of salicylicism 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% indicates extremely severe, prognostically unfavorable. Moderate poisoning requires hospitalization for 24 hours.

Treatment: provocation of vomiting, administration of activated carbon and laxatives, constant monitoring of CBS and electrolyte balance depending on the metabolic state - administration of sodium bicarbonate, sodium citrate solution or sodium lactate. Increasing reserve alkalinity enhances the excretion of ASA due to alkalinization of urine. Alkalinization of urine is indicated when the level of salicylates is above 40 mg% and is provided by intravenous infusion of sodium bicarbonate (88 mEq in 1 liter of 5% dextrose solution, at a rate of 10-15 ml/h/kg); restoration of bcc and induction of diuresis is achieved by introducing sodium bicarbonate into the same doses and dilution, which is repeated 2-3 times. Caution should be exercised in elderly patients in whom intensive fluid infusion may lead to pulmonary edema. The use of acetazolamide for alkalinization of urine is not recommended (it can cause acidemia and enhance the toxic effect of salicylates). Hemodialysis is indicated when the salicylate level is more than 100-130 mg%, in patients with chronic poisoning - 40 mg% or lower if indicated (refractory acidosis, progressive deterioration, severe central nervous system damage, pulmonary edema and renal failure). For pulmonary edema - mechanical ventilation with an oxygen-enriched mixture.

Storage conditions and shelf life

  • In a dry place, at a temperature not exceeding 25 °C.
  • Keep out of the reach of children.

Analogues and prices

Among foreign and Russian analogues of Acetylsalicylic acid there are:

Aspirin. Manufacturer: Bayer 254 rub.
Aspirin complex. Manufacturer: Bayer (Germany). Price in pharmacies from 401 rub.
Aspirin-c. Manufacturer: Bayer (Germany). Price in pharmacies from 227 rubles.
Thrombo ass. Manufacturer: G.L.Pharma GmbH (Austria). Price in pharmacies from 41 rubles.
Thrombopol. Manufacturer: Polpharma (Poland). Price in pharmacies from 48 rubles.

In this article you can read the instructions for use of the drug Acetylsalicylic acid. Reviews of site visitors - consumers of this medicine, as well as the opinions of specialist doctors on the use of Acetylsalicylic acid in their practice are presented. We kindly ask you to actively add your reviews about the drug: whether the medicine helped or did not help get rid of the disease, what complications and side effects were observed, perhaps not stated by the manufacturer in the annotation. Analogues of Acetylsalicylic acid in the presence of existing structural analogues. Use for the treatment of inflammatory diseases, fever, headaches, dental and other pain in adults, children, as well as during pregnancy and lactation.

Acetylsalicylic acid- non-steroidal anti-inflammatory drug. It has anti-inflammatory, analgesic and antipyretic effects, and also inhibits platelet aggregation. The mechanism of action is associated with inhibition of the activity of COX, the main enzyme in the metabolism of arachidonic acid, which is a precursor of prostaglandins, which play a major role in the pathogenesis of inflammation, pain and fever. A decrease in the content of prostaglandins (mainly E1) in the thermoregulation center leads to a decrease in body temperature due to dilation of skin vessels and increased sweating. The analgesic effect is due to both central and peripheral effects. Reduces platelet aggregation, adhesion and thrombus formation by suppressing the synthesis of thromboxane A2 in platelets.

Reduces mortality and the risk of myocardial infarction in unstable angina. Effective in the primary prevention of diseases of the cardiovascular system and in the secondary prevention of myocardial infarction. In a daily dose of 6 grams or more, it suppresses prothrombin synthesis in the liver and increases prothrombin time. Increases fibrinolytic activity of plasma and reduces the concentration of vitamin K-dependent coagulation factors (2, 7, 9, 10). Increases the incidence of hemorrhagic complications during surgical interventions and increases the risk of bleeding during anticoagulant therapy. Stimulates the excretion of uric acid (impairs its reabsorption in the renal tubules), but in high doses. Blockade of COX-1 in the gastric mucosa leads to inhibition of gastroprotective prostaglandins, which can cause ulceration of the mucous membrane and subsequent bleeding.

Pharmacokinetics

When taken orally, it is rapidly absorbed mainly from the proximal small intestine and to a lesser extent from the stomach. The presence of food in the stomach significantly changes the absorption of acetylsalicylic acid. Metabolized in the liver by hydrolysis to form salicylic acid, followed by conjugation with glycine or glucuronide. The concentration of salicylates in blood plasma is variable.

About 80% of salicylic acid binds to blood plasma proteins. Salicylates easily penetrate many tissues and body fluids, incl. into the cerebrospinal, peritoneal and synovial fluids. Salicylates are found in small quantities in brain tissue, traces in bile, sweat, and feces. Quickly penetrates the placental barrier and is excreted in small quantities in breast milk.

In newborns, salicylates can displace bilirubin from its binding to albumin and contribute to the development of bilirubin encephalopathy.

Penetration into the joint cavity accelerates in the presence of hyperemia and edema and slows down in the proliferative phase of inflammation.

It is excreted mainly by active secretion in the renal tubules unchanged (60%) and in the form of metabolites.

Indications

  • rheumatism;
  • rheumatoid arthritis;
  • infectious-allergic myocarditis;
  • fever in infectious and inflammatory diseases;
  • pain syndrome of weak and moderate intensity of various origins (including neuralgia, myalgia, headache);
  • prevention of thrombosis and embolism;
  • primary and secondary prevention of myocardial infarction;
  • prevention of ischemic cerebrovascular accidents;
  • in gradually increasing doses for long-term “aspirin” desensitization and the formation of stable tolerance to NSAIDs in patients with “aspirin” asthma and the “aspirin triad”.

Release forms

Tablets 250 mg and 500 mg.

Instructions for use and dosage

Individual. For adults, a single dose varies from 40 mg to 1 g, daily - from 150 mg to 8 g; frequency of use - 2-6 times a day. It is preferable to drink milk or alkaline mineral waters.

Side effect

  • nausea, vomiting;
  • anorexia;
  • epigastric pain;
  • diarrhea;
  • the occurrence of erosive and ulcerative lesions;
  • bleeding from the gastrointestinal tract;
  • dizziness;
  • headache;
  • reversible visual impairment;
  • tinnitus;
  • thrombocytopenia, anemia;
  • hemorrhagic syndrome;
  • prolongation of bleeding time;
  • renal dysfunction;
  • acute renal failure;
  • skin rash;
  • Quincke's edema;
  • bronchospasm;
  • “aspirin triad” (a combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid and pyrazolone drugs);
  • Reye's syndrome (Raynaud's);
  • increased symptoms of chronic heart failure.

Contraindications

  • erosive and ulcerative lesions of the gastrointestinal tract in the acute phase;
  • gastrointestinal bleeding;
  • "aspirin triad";
  • a history of indications of urticaria, rhinitis caused by taking acetylsalicylic acid and other NSAIDs;
  • hemophilia;
  • hemorrhagic diathesis;
  • hypoprothrombinemia;
  • dissecting aortic aneurysm;
  • portal hypertension;
  • vitamin K deficiency;
  • liver and/or kidney failure;
  • deficiency of glucose-6-phosphate dehydrogenase;
  • Reye's syndrome;
  • childhood (up to 15 years - the risk of developing Reye's syndrome in children with hyperthermia due to viral diseases);
  • 1st and 3rd trimesters of pregnancy;
  • lactation period;
  • hypersensitivity to acetylsalicylic acid and other salicylates.

Use during pregnancy and breastfeeding

Contraindicated for use in the 1st and 3rd trimesters of pregnancy. In the 2nd trimester of pregnancy, a one-time dose is possible according to strict indications.

It has a teratogenic effect: when used in the 1st trimester it leads to the development of cleft palate, in the 3rd trimester it causes inhibition of labor (inhibition of prostaglandin synthesis), premature closure of the ductus arteriosus in the fetus, hyperplasia of the pulmonary vessels and hypertension in the pulmonary circulation.

Acetylsalicylic acid is excreted in breast milk, which increases the risk of bleeding in the baby due to impaired platelet function, so acetylsalicylic acid should not be used by the mother during lactation.

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 using acetylsalicylic acid in high doses, medical supervision and regular monitoring of hemoglobin levels are required.

The use of acetylsalicylic acid as an anti-inflammatory agent in a daily dose of 5-8 grams is limited due to the high likelihood of developing side effects from the gastrointestinal tract.

Before surgery, to reduce bleeding during surgery and in the postoperative period, you should stop taking salicylates for 5-7 days.

During long-term therapy, it is necessary to conduct a complete blood count 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 under the influence of acetylsalicylic acid, the risk of developing Reye's syndrome increases. Symptoms of Reye's syndrome are prolonged vomiting, acute encephalopathy, and liver enlargement.

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

During the treatment period, the patient must abstain from drinking alcohol.

Drug interactions

When used simultaneously, antacids containing magnesium and/or aluminum hydroxide slow down and reduce the absorption of acetylsalicylic acid.

With the simultaneous use of calcium channel blockers, drugs that limit the intake of calcium or increase the excretion of calcium from the body, the risk of bleeding increases.

When used simultaneously with acetylsalicylic acid, the effect of heparin and indirect anticoagulants, hypoglycemic agents, sulfonylurea derivatives, insulins, methotrexate, phenytoin, and valproic acid is enhanced.

When used simultaneously with GCS, the risk of ulcerogenic effects and gastrointestinal bleeding increases.

With simultaneous use, the effectiveness of diuretics (spironolactone, furosemide) decreases.

With the simultaneous use of other NSAIDs, the risk of side effects increases. Acetylsalicylic acid may reduce plasma concentrations of indomethacin and piroxicam.

When used simultaneously with gold preparations, acetylsalicylic acid can induce liver damage.

With simultaneous use, the effectiveness of uricosuric drugs (including probenecid, sulfinpyrazone, benzbromarone) is reduced.

With the simultaneous use of acetylsalicylic acid and sodium alendronate, severe esophagitis may develop.

With simultaneous use of griseofulvin, the absorption of acetylsalicylic acid may be impaired.

A case of spontaneous hemorrhage into the iris was described when taking Ginkgo biloba extract during long-term use of acetylsalicylic acid at a dose of 325 mg per day. It is believed that this may be due to an additive inhibitory effect on platelet aggregation.

When used simultaneously with acetylsalicylic acid, the concentrations of digoxin, barbiturates and lithium salts in the blood plasma increase.

With the simultaneous use of salicylates in high doses with carbonic anhydrase inhibitors, salicylate intoxication is possible.

Acetylsalicylic acid in doses less than 300 mg per day has a minor effect on the effectiveness of captopril and enalapril. When using acetylsalicylic acid in high doses, the effectiveness of captopril and enalapril may be reduced.

With simultaneous use, caffeine increases the rate of absorption, plasma concentration and bioavailability of acetylsalicylic acid.

When using pentazocine against the background of long-term use of acetylsalicylic acid in high doses, there is a risk of developing severe adverse reactions from the kidneys.

With simultaneous use, phenylbutazone reduces uricosuria caused by acetylsalicylic acid.

With simultaneous use, ethanol may enhance the effect of acetylsalicylic acid on the gastrointestinal tract.

Analogs of the drug Acetylsalicylic acid

Structural analogues of the active substance:

  • Anopyrine;
  • ASK-cardio;
  • Aspicor;
  • Aspinat;
  • Aspinath Cardio;
  • Aspirin "York";
  • Aspirin;
  • Aspirin 1000;
  • Aspirin Cardio;
  • Acecardole;
  • Acenterine;
  • Acetylsalicylic acid Cardio;
  • Acetylsalicylic acid MS;
  • Acetylsalicylic acid-LecT;
  • Acetylsalicylic acid-Rusfar;
  • Acetylsalicylic acid-UBF;
  • Acylpyrine;
  • Acsbirin;
  • Bufferin;
  • Zorex Morning;
  • CardiASK;
  • Colfaritis;
  • Mikristin;
  • Plidol 100;
  • Plidol 300;
  • Taspir;
  • Thrombo ACC;
  • Thrombopol;
  • Walsh-asalgin;
  • Upsarin UPSA;
  • H-el-pain.

If there are no analogues of the drug for the active substance, you can follow the links below to the diseases for which the corresponding drug helps, and look at the available analogues for the therapeutic effect.

Name:

Acetylsalicylic acid (Acidum acetylsalicylicum)

Pharmacological action:

Acetylsalicylic acid has anti-inflammatory, antipyretic, and analgesic effects. It is widely used for feverish conditions (high body temperature), headaches, neuralgia (pain spreading along the nerve), etc., and as an antirheumatic agent. The anti-inflammatory effect of acetylsalicylic acid is explained by its influence on the processes occurring at the site of inflammation. The antipyretic effect is also associated with the effect on the hypothalamic (located in the brain) thermoregulation centers. The analgesic (pain-relieving) effect is due to the influence on pain sensitivity centers located in the central nervous system.

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. (Prostaglandins are biologically active substances produced in the body. Their role in the body is extremely multifaceted; in particular, they are responsible for the appearance of pain and swelling at the site of inflammation).

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 are reduced. In addition, the influence of prostaglandins on sensory nerve endings is reduced, leading to a decrease in their sensitivity to pain mediators. It also has an antiaggregation effect.

Indications for use:

Acetylsalicylic acid has wide application as an anti-inflammatory, antipyretic and analgesic agent.

An important feature of acetylsalicylic acid is the ability of the drug to have an antiaggregation effect and inhibit spontaneous and induced platelet aggregation.

Method of application:

In tablet form, it is prescribed orally after meals. Usual doses for adults as an analgesic and antipyretic (for febrile illnesses, headaches, migraines, neuralgia, etc.) 0.25-0.5-1 g 3-4 times a day, for children depending on age - from 0 ,1 to 0.3 g per dose.

For rheumatism, infectious-allergic myocarditis (heart disease), rheumatoid polyarthritis (an infectious-allergic disease from the group of collagenoses, characterized by chronic progressive inflammation of the joints), long-term prescribed for adults 2-3 g (less often 4 g) per day, children 0.2 g per year of life per day. A single dose for children aged 1 year is 0.05 g, 2 years - 0.1 g, 3 years - 0.15 g, 4 years - 0.2 g. Starting from the age of 5, it can be prescribed in tablets of 0 .25 g per dose.

A soluble form of aspirin is also used - Acylpirin soluble. In case of fever (sharp increase in body temperature) and/or pain, 1-2 tablets of 0.5 g are prescribed in a single dose. If necessary, the drug is taken again in the same dose. The maximum daily dose is 6 tablets. For acute rheumatism, a daily dose of 100 mg/kg body weight is prescribed in 5-6 divided doses. Single doses for children depend on age and are: children up to 6 months. - 50-100 mg, from 6 months. up to 1 year - 100-150 mg, from 1 year to 6 years - 150-250 mg, from 6 to 15 years - 250-500 mg, prescribed 3 times a day. The drug is used at the end of a meal or immediately after a meal. Immediately before use, the tablet must be dissolved in 1/2 cup of water.

Adverse events:

When using the drug, profuse (profuse) sweating may develop, tinnitus and hearing loss, angioedema (allergic) edema, skin and other allergic reactions may appear.

It is important to consider that with long-term (without medical supervision) use of acetylsalicylic acid, phenomena such as dyspeptic disorders (digestive disorders) and gastric bleeding may occur; the mucous membrane of not only the stomach, but also the duodenum may be affected.

The so-called ulcerogenic (ulcer-causing) effect is characteristic to varying degrees of various anti-inflammatory drugs: corticosteroids, butadione, indomethacin, etc. The appearance of stomach ulcers and gastric bleeding when using acetylsalicylic acid is explained not only by the resorptive effect (the effect of a substance that manifests itself after its absorption into blood) (inhibition of blood clotting factors, etc.), but also its direct irritating effect on the gastric mucosa, especially if the drug is taken in the form of uncrushed tablets. This also applies to sodium salicylate.

To reduce the ulcerogenic effect and prevent the development of gastric bleeding, you should take acetylsalicylic acid only after meals; it is recommended to crush the tablets thoroughly and wash them down with plenty of liquid (preferably milk). There are, however, indications that gastric bleeding may also occur when taking acetylsalicylic acid after meals. To reduce the irritating effect on the stomach, they resort to taking alkaline mineral waters or sodium bicarbonate solution after acetylsalicylic acid.

Due to the effect on platelet aggregation (sticking together), as well as some anticoagulating (anti-clotting) activity, blood tests should be carried out periodically during treatment with acetylsalicylic acid. With bleeding disorders, especially with hemophilia (a hereditary disease manifested by increased bleeding), bleeding may develop. For early detection of ulcerogenic effects, it is necessary to periodically examine the stool for the presence of blood.

It should be taken into account that under the influence of acetylsalicylic acid, the effect of anticoagulants (drugs that inhibit blood clotting 8), sugar-lowering drugs (sulfonylurea derivatives) is enhanced, and the risk of developing gastric bleeding increases while taking corticosteroids (hydrocortisone, cortisone, dexamethasone, etc. 8, 586, 583 ) and non-steroidal anti-inflammatory drugs (sodium salicylate, acelysin, salicylamide, methyl salicylate 7, 273, 288). During treatment with acetylsalicylic acid, the side effects of methotrexate increase. The effect of diuretics (furosemide, veroshpiron, etc., 302) is somewhat weakened.

In case of overdose with mild intoxication (poisoning), nausea, vomiting, pain in the epigastrium (the area of ​​the abdomen located directly below the convergence of the costal arches and sternum), as well as (especially in children and elderly patients) tinnitus, dizziness, headaches are possible. , decreased vision and hearing. With a significant overdose, incoherent thinking, confusion, drowsiness, collapse (a sharp drop in blood pressure), tremor (trembling limbs), shortness of breath, suffocation, dehydration, hyperthermia (increased body temperature), coma (unconsciousness), alkaline urine reaction, metabolic acidosis (acidification due to metabolic disorders), respiratory (gas) alkalosis (alkalization), carbohydrate metabolism disorders.

The lethal (capable of leading to death) dose of acetylsalicylic acid for adults is more than 10 g, for children - more than 3 g.

In case of overdose, depending on the state of acid-base balance and electrolyte (ionic) balance, solutions of sodium bicarbonate, sodium citrate or sodium lactate are infused.

Contraindications:

Peptic ulcer of the stomach and duodenum and gastrointestinal bleeding are contraindications to the use of acetylsalicylic acid and sodium salicylate. The use of acetylsalicylic acid is also contraindicated in case of a history of peptic ulcer disease, portal hypertension (increased pressure in the portal vein system of the liver), venous stasis (due to decreased resistance of the gastric mucosa), and blood clotting disorders.

With long-term use of salicylates, the possibility of developing anemia (decreased hemoglobin in the blood) should be taken into account and blood tests should be systematically performed and the presence of blood in the stool should be checked.

Due to the possibility of allergic reactions, caution should be exercised when prescribing acetylsalicylic acid (and other salicylates) to persons with hypersensitivity to penicillins and other “allergenic” (allergy-causing) drugs.

With increased sensitivity to acetylsalicylic acid, “aspirin” asthma (acute attacks of asthma caused by taking acetylsalicylic acid) may develop, for the prevention and treatment of which methods of desensitizing (preventing or inhibiting allergic reactions) therapy have been developed.

For children and adolescents (up to 14 years of age) with diseases accompanied by hyperthermia (increased body temperature), it is advisable to prescribe acetylsalicylic acid only if other drugs are ineffective. In patients suffering from allergic diseases, including bronchial asthma, allergic and hay rhinitis (runny nose), urticaria, itching, swelling of the mucous membrane and nasal polyps, as well as in combination with chronic respiratory tract infections, in patients with increased sensitivity to painkillers and antirheumatic drugs of any type, the development of “aspirin” asthma is possible.

It should be borne in mind that taking salicylates (in high doses) in the first 3 months. pregnancy is associated in many epidemiological studies with a high risk of developing deformities (cleft palate, heart defects). However, at usual therapeutic doses, this risk appears to be small, as a study of approximately 3,200 mother-child pairs found no association with increased rates of deformities. In the last 3 months. pregnancy, taking salicylates can lead to a prolongation of the pregnancy period and a weakening of labor pains. The mother and child had an increased tendency to bleed. When acetylsalicylic acid is taken by the mother shortly before birth, intracranial bleeding is possible in newborns (especially premature ones).

During breastfeeding, when taking the drug in usual doses, interruption of breastfeeding is usually not required. If you regularly take large doses of the drug, you should consider stopping breastfeeding.

Without medical supervision, the drug should be taken only in normal doses and only for a few days.

Release form of the drug:

Acetylsalicylic acid is available for oral administration in the form of tablets of 0.25 and 0.5 g (for adults) and 0.1 g (scored) for children. “Effervescent” tablets of 0.5 g in a package of 15 pieces.

Storage conditions:

In a well-closed container, protected from light.

Synonyms:

Aspisol, Aspirin, Aspro-500, Colfarit, Mikristin, Acetol, Acetylene, Aspozal, Astrin, Ataspin, Bedaspin, Bispirin, Caprin, Cetazal, Cytopyrin, Claripirin, Darozal, Endosalil, Isopyrine, Novosprin, Prodol, Rodopyrin, Ruspirin, Salacetin, Temperal, Vikapirin, Aspro, Acesal, Acetyl, Acetofen, Acetosal, Acetylsal, Acetisal, Acylpirin, Bayaspirin, Bebaspin, Benaspir, Clariprin, Durosal, Easprin, Endospirin, Eutosal, Genasprin, Helicon, Istopirin, Monasalil, Panspiril, Polopirina, Saletin, Zorprin, Acetylsalicil bene, Novandol, Plidol, Aspirin UPSA, Aspilight, ApoAsa, Asalgin, Acylspirin, Aspro 500, Salorin, Janprin.

Additionally:

Acetylsalicylic acid is also included in the preparations Mexavit, Presotsil.

Drugs with similar effects:

Diclo-F Remisid Rapten gel Rapten Dolgit

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