How to take acetylsalicylic acid. Trade names of drugs with the active ingredient acetylsalicylic acid

Formula: C9H8O4, chemical name: 2-(Acetyloxy)benzoic acid.
Pharmacological group: non-narcotic analgesics/antiplatelet agents, non-steroidal anti-inflammatory drugs/derivatives salicylic acid.
Pharmachologic effect: anti-inflammatory, antipyretic, analgesic, antiaggregant.

Pharmacological properties

Acetylsalicylic acid inhibits the enzyme cyclooxygenase (COX-1, COX-2) and irreversibly inhibits metabolism arachidonic acid, blocks the formation of thromboxane and prostaglandins (PGD2, PGA2, PGF2alpha, PGE2, PGE1 and others). Reduces hyperemia, capillary permeability, exudation, hyaluronidase activity, reduces the energy supply of the inflammation process by blocking the formation of ATP. Acts on subcortical centers pain sensitivity and thermoregulation. Reduces the level of prostaglandins (mainly PGE1) in the thermoregulatory center, which leads to a decrease in body temperature due to dilation of skin vessels and increased sweating. The analgesic effect is determined by the effect on the center of pain sensitivity, the peripheral anti-inflammatory effect and the ability of salicylates to reduce the algogenic effect of bradykinin. A decrease in the level of thromboxane A2 in platelets leads to irreversible suppression of aggregation and slightly dilates blood vessels. The antiplatelet effect persists for a week after a single dose. During clinical trials It has been shown that at doses up to 30 mg, a significant reduction in platelet adhesiveness is achieved. Increases the fibrinolytic activity of plasma and reduces the level of coagulation factors (VII, II, IX, X), which depend on vitamin K. Enhances the excretion of uric acid, since its reabsorption into the bloodstream is impaired. renal tubules. Acetylsalicylic acid is almost completely absorbed after oral administration. If available on dosage form shell that is resistant to gastric juice, which prevents absorption of the drug in the stomach, is absorbed into small intestine (upper section). When absorbed, it undergoes presystemic elimination in the intestines and liver (deacetylation process). The absorbed part is hydrolyzed very quickly, so the half-life of acetylsalicylic acid is no more than 20 minutes. Circulates in the body and is distributed in tissues as an anion of salicylic acid. The maximum concentration develops after 2 hours. Does not bind to plasma proteins. After biotransformation processes in the liver, metabolites are formed that are found in urine and many tissues. Salicylates are eliminated by active secretion in the renal tubules in the form of metabolites and in unchanged form. Excretion depends on urine pH (with alkaline reaction urine increases the ionization of salicylates, which worsens their reabsorption and significantly increases excretion).

Indications

Ischemic disease; painless myocardial ischemia; myocardial infarction (to reduce the risks of death and recurrent infarction); unstable angina; development prevention coronary disease(in the presence of several predisposing factors); ischemic stroke in men; repeated transient ischemia brain; prosthetic heart valves (for the prevention and treatment of thromboembolism); balloon coronary angioplasty and with stenting (to reduce the possibility restenosis and therapy for secondary dissection coronary arteries); aortoarteritis (Takayasu's disease); non-atherosclerotic lesions of the coronary arteries (Kawasaki disease); vices mitral valve; atrial fibrillation; recurrent thromboembolism pulmonary artery; mitral valve prolapse (to prevent thromboembolism); Dressler's syndrome; acute thrombophlebitis; pulmonary infarction; fever in infectious and inflammatory diseases; weak and medium pain syndrome of various origins, including lumbago, thoracic radicular syndrome, headache, neuralgia, migraine, toothache, arthralgia, myalgia, algomenorrhea; in allergology and immunology it is used for “aspirin” desensitization and the formation of tolerance to non-steroidal anti-inflammatory drugs in patients with the “aspirin” triad and “aspirin” asthma. According to the indications, it is used for rheumatism, rheumatic chorea, rheumatoid arthritis, infectious-allergic myocarditis, pericarditis - but now it is very rare.

Method of application of acetylsalicylic acid and doses

Acetylsalicylic acid is taken orally, preferably after meals, drinking enough water, dosage depends on the disease. Usually for adults as an analgesic and antipyretic agent - 500–1000 mg/day (up to 3 g) divided into 3 doses. For the treatment of myocardial infarction, as well as for its prevention in patients who have previously had a heart attack, 40–325 mg (usually 160 mg) once a day. To reduce platelet aggregation for a long time, 300-325 mg / day. For cerebral thromboembolism, dynamic circulatory disorders in men, including for the prevention of relapses, 325 mg/day, gradually increasing to 1 g/day. To prevent occlusion or thrombosis of the aortic shunt - 325 mg every 7 hours after gastric tube, administered intranasally, then 325 mg orally 3 times a day for a long time.
If you miss your next dose of acetylsalicylic acid, you need to take it as you remember. next appointment produce through set time from the last appointment.
The use of acetylsalicylic acid together with glucocorticoids and other non-steroidal anti-inflammatory drugs is not recommended. A week before the proposed surgical intervention, you need to stop taking the drug (to reduce bleeding during the operation and in the period after it). The possibility of developing gastropathy is reduced when consumed after meals and when using tablets that are coated with special enteric coatings or contain buffer additives. The risk of bleeding is considered to be the lowest when used in doses

Contraindications and restrictions for use

Hypersensitivity (including “aspirin” asthma, “aspirin” triad), hemorrhagic diathesis (von Willebrand disease, hemophilia, telangiectasia), heart failure, aortic aneurysm (dissecting), erosive-ulcerative acute and recurrent diseases gastrointestinal tract, acute liver or kidney failure, gastrointestinal bleeding, hypoprothrombinemia (before treatment), thrombocytopenia, vitamin K deficiency, glucose-6-phosphate dehydrogenase deficiency, thrombotic thrombocytopenic purpura, breastfeeding, pregnancy (I and III trimester), age up to 15 years when used as an antipyretic. Limit the intake of acetylsalicylic acid for hyperuricemia, nephrolithiasis, gout, peptic ulcer, severe violations kidney and liver function, bronchial asthma, COPD, nasal polyposis, uncontrolled arterial hypertension.

Use during pregnancy and breastfeeding

The use of salicylates in the first trimester of pregnancy in large doses ax is associated with an increased frequency of fetal developmental defects (heart defects, cleft palate). Salicylates can be prescribed in the second trimester of pregnancy, but only taking into account an assessment of benefits and risks. In the third trimester of pregnancy, the use of salicylates is contraindicated. Salicylates and their metabolites pass into breast milk in small quantities. Accidental intake of salicylates during breastfeeding is usually not accompanied by adverse reactions in the child and does not require stopping breastfeeding. However, if you take salicylates for a long time or in large doses, then breastfeeding should be stopped.

Side effects of acetylsalicylic acid

Blood system: thrombocytopenia, leukopenia, anemia;
digestive system: gastropathy (pain in epigastric region, dyspepsia, nausea and vomiting, heartburn, heavy bleeding), loss of appetite; allergic reactions: hypersensitivity reactions (laryngeal edema, bronchospasm, urticaria), the formation of an "aspirin" triad (recurrent nasal polyposis, eosinophilic rhinitis, hyperplastic sinusitis) and “aspirin” bronchial asthma;
other: disorders of the kidneys and/or liver, Reye's syndrome in children, impaired potency in men (with long-term use).
Don't use aspirin healthy people to avoid bleeding in the brain and gastrointestinal tract.
At long-term use: headache, dizziness, tinnitus, blurred vision, decreased hearing acuity, prerenal azotemia with increased blood creatinine and hypercalcemia, interstitial nephritis, acute renal failure, papillary necrosis, nephrotic syndrome, blood diseases, increased symptoms of congestive heart failure, aseptic meningitis, edema, increased concentration of aminotransferases in the blood.

Interaction of acetylsalicylic acid with other substances

Acetylsalicylic acid increases the toxicity of methotrexate (by reducing its renal clearance), effects narcotic analgesics(propoxyphene, oxycodone, codeine), heparin, oral antidiabetic drugs, indirect anticoagulants, inhibitors of platelet aggregation and thrombolytics, reduces the effects of uricosuric drugs (sulfinpyrazone, benzbromarone), diuretics (furosemide, spironolactone), antihypertensive drugs. Paracetamol, antihistamines, caffeine increases the risk of side effects. Glucocorticoids, ethanol (and preparations containing it) enhance the negative effect on the gastrointestinal mucosa and increase clearance. Increases the concentration of barbiturates, lithium salts, digoxin in plasma. Antacids that contain aluminum or magnesium inhibit and impair the absorption of acetylsalicylic acid. Myelotoxic drugs enhance the hematotoxicity of acetylsalicylic acid.

Overdose

May occur with long-term therapy or after taking a large dose once (less than 150 mg/kg mild poisoning, 150–300 mg/kg - moderate, with more high doses– heavy). Symptoms of overdose: salicylicism (vomiting, tinnitus, nausea, blurred vision, severe headache, dizziness, general malaise, fever). In more severe poisonings - stupor, coma and convulsions, pulmonary edema, severe dehydration, renal failure, acid-base disorders (first respiratory alkalosis, then metabolic acidosis), shock. In chronic overdoses, plasma concentrations do not correlate well with the severity of poisoning. Chronic intoxication most often develops in elderly patients when consuming more than 100 mg/kg/day for several days. In such patients and children initial signs in the form of salicylicism do not always manifest themselves, therefore it is periodically necessary to determine the level of salicylates in the blood (more than 70 mg% indicates moderate or severe poisoning; more than 100 mg% - extremely severe, which is prognostically unfavorable). Moderate poisoning requires hospitalization for at least a day. Treatment: induce vomiting, take laxatives and activated charcoal, monitor electrolyte balance and acid-base status; administration of sodium bicarbonate, sodium lactate solution or citrate - if necessary. Alkalinization of urine is necessary when the level of salicylates is more than 40 mg%; sodium bicarbonate is administered intravenously - 88 mEq in 1 liter of 5% glucose solution, at a rate of 10–15 ml/kg/h. It should be remembered that intensive fluid administration to elderly patients can lead to pulmonary edema. Acetazolamide should not be used to alkalinize urine. Hemodialysis is recommended when the concentration of salicylates is more than 100-130 mg%, and in chronic poisoning - 40 mg% and below, if there are indications (refractory acidosis, severe CNS damage, progressive deterioration, renal failure, pulmonary edema). In case of pulmonary edema, mechanical ventilation with an oxygen-enriched mixture in positive end-expiratory pressure mode is necessary; osmotic diuresis and hyperventilation are used to treat cerebral edema.

Trade names of drugs with the active ingredient acetylsalicylic acid

Researchers at Vanderbilt University School of Medicine found that daily exposure to aspirin for five years or more markedly reduced the risk of stomach, colon, lung, breast, pancreatic, and prostate glands. The risk is reduced even when taking small doses of acetylsalicylic acid (for example, 81 milligrams per day). In addition, if a person between the ages of 50 and 65 started taking aspirin daily and continued taking it for at least 10 years, the risk of developing cancer and cardiovascular diseases decreased by 9% in men and by about 7% in women. But when aspirin is discontinued, this risk increases sharply.

In each home first aid kit There is acetylsalicylic acid - Aspirin. The medicine helps to reduce the temperature, get rid of a toothache or migraine, it is also useful for the face. But for some categories of people this drug is strictly contraindicated. What features of the product should be taken into account during treatment?

Acetylsalicylic acid - what is it?

Acetylsalicylic acid (ASA), the name in Latin - Acetylsalicylic acid, white crystalline powder, belongs to the group of analgesics and antipyretics. In medicine, it is used as a non-steroidal anti-inflammatory and analgesic agent, as adjuvant drug against the aggregation of blood cells. The substance has a slight odor, is highly soluble in water and ethanol, and is included in more than 100 drugs for various purposes.

Release form - tablets that contain 100, 250, 500 mg of acetylsalicylic acid. Additionally, the composition contains ingredients that do not affect therapeutic effect drug. You can buy acetylsalicylic acid tablets at any pharmacy without presenting a prescription, the price does not exceed 20 rubles.

Popular preparations of acetylsalicylic acid:

Citramon;
Paracetamol;
Aspirin Cardio;
Antigrippin;
Upsarin Upsa.

Note! Aspirin is compressed acetylsalicylic acid plus cellulose and cornstarch. There is no difference in the therapeutic effect between the drugs, the cost and manufacturers may differ, so you can safely buy cheaper analogues.

Therapeutic effect

After taking acetylsalicylic acid in the body, hyperemia decreases, capillary permeability at the site of inflammation decreases - all this leads to a noticeable analgesic and anti-inflammatory effect. The drug quickly penetrates into all tissues and fluids, absorption occurs in the intestines and liver.

Action of acetylsalicylic acid:

provides a persistent anti-inflammatory effect 24-48 hours after the start of the medication;
eliminates weak pain and medium degree intensity;
reduces elevated body temperature, while not affecting normal performance;
acetylsalicylic acid thins the blood, disrupts platelet aggregation - the load on the heart muscle decreases, the risk of occurrence decreases.

The drug can be taken to prevent thrombosis, reduce the risk of developing circulatory disorders in the brain.

Note! The antiaggregatory effect of ASA is observed within 7 days after a single dose of the drug. Therefore, the remedy should not be drunk before surgical interventions, shortly before menstruation.

Regularly taken acetylsalicylic acid inhibits (slows down) the formation of blood clots (clots) that can block the lumen of the artery. This reduces the risk of heart attack by almost half

Indications

Due to a wide spectrum of action, acetylsalicylic acid is used for the treatment and prevention of diseases. of various etiologies in adults, children over 15 years of age.

What does acetylsalicylic acid help with:

febrile conditions that accompany pathologies of an infectious and inflammatory nature;
rheumatism, pericarditis;
migraine, dental, muscle, joint, menstrual pain, ;
prevention of heart attack, stroke due to problems with blood circulation, increased blood viscosity;
prevention of blood clots with a genetic predisposition to thrombophlebitis;
unstable

ASA is included in complex therapy in the treatment of pleurisy, lumbago, heart defects, mitral valve prolapse. This drug is recommended for use when the first signs of flu or cold appear - it helps increased sweating, that leads to rapid improvement condition.

Advice! Aspirin is one of the the best means to eliminate the effects of a hangover, the drug thins the blood, eliminates headaches and swelling, and reduces intracranial stress.

Acetylsalicylic acid is popularly called aspirin or a universal head pill. It is an anti-inflammatory and antipyretic agent

Contraindications and adverse reactions

The instructions for acetylsalicylic acid detail all contraindications, possible negative consequences when taking the drug. Before using the product, you should carefully study the annotation to avoid serious complications.

Contraindications:

and diathesis of a hemorrhagic nature;
aspirin;
exacerbation of peptic ulcer, gastric and intestinal bleeding;
vitamin K deficiency, poor clotting blood, hemophilia;
increased blood pressure in the portal vein system;
renal and liver failure;
dissecting aneurysm.

You should not drink acetylsalicylic acid when individual intolerance salicylates, while taking Methotrexate, it is forbidden to take it simultaneously with alcoholic beverages, ethanol-based drugs.

Most of negative consequences while taking ASA, it is associated with the digestive system - most often, patients complain of pain in the epigastric region, nausea, vomiting,. During treatment, pain in the head may increase, tinnitus may appear, and the functioning of organs may deteriorate. urinary system. If you are prone to allergies, a rash, bronchospasm, and swelling may occur. IN rare cases erosions and ulcers develop in organs digestive tract, renal or liver failure. But if patients drink the medicine, clearly following the annotation, then adverse reactions rarely occur.

Do not take acetylsalicylic acid together with other non-steroidal drugs anti-inflammatory action, anticoagulants, Aspirin reduces the therapeutic effect of diuretics.

Note! With long-term use of ASA, temporary deterioration in hearing and vision often occurs. The consequences are reversible, disappear on their own after discontinuation of the drug.

Can pregnant and lactating women and children take Aspirin?

Acetylsalicylic acid is contraindicated in children under 14 years of age, since the drug can displace bilirubin, which can cause the development of severe kidney and liver pathologies in infants and preschoolers and adolescents. Children's dosage is 250 mg twice a day, the maximum permissible daily dose is 750 mg.

Acetylsalicylic acid is strictly prohibited during pregnancy in the first trimester - the drug has a teratogenic effect and can provoke development in the child birth defects heart, cleft palate.

Note! ASA often becomes the cause in the early stages.

You cannot take acetylsalicylic acid or paracetamol even in the third trimester - the drug causes pulmonary hypertension in the fetus, which causes the development of pathologies in respiratory tract, blood flow disorders. Using ASA at this time can cause severe uterine bleeding.

ASA should not be taken during breastfeeding, since the acid penetrates into the milk, which can lead to a deterioration in the baby’s health and the development of severe allergic reactions.

During the second trimester, admission is possible, but only in the presence of acute indications and with the permission of the doctor; in the last period of gestation, admission is completely prohibited

Instructions for use of acetylsalicylic acid

ASA should be taken only after meals so as not to cause deterioration in performance digestive system, you can drink water without gas or milk. The standard dosage is 1-2 tablets 2-4 times a day, but not more than 1000 mg at a time. You can drink no more than 6 tablets per day.

How to take ASA for certain pathologies:

To thin the blood, like prophylactic against a heart attack - 250 mg daily for 2-3 months. IN in case of emergency dose increase up to 750 mg is allowed.
Acetylsalicylic acid for headaches - it is enough to take 250-500 mg of ASA; if necessary, you can repeat the dose after 4-5 hours.
For flu, colds, fever, toothache - 500-1000 mg of the drug every 4 hours, but no more than 6 tablets per day.
To eliminate pain during menstruation, drink 250–500 mg of ASA, if necessary, repeat the dose after 8–10 hours.

Advice! Take Aspirin when slight increase arterial parameters, if there are no antihypertensive drugs at hand.

Acetylsalicylic acid in home cosmetology

Acetylsalicylic acid can be used in homemade recipes for face masks, hair restoration, and dandruff removal.

Acetylsalicylic acid effectively helps against - grind 3 ASA tablets into powder, add 5 ml of liquid and fresh juice aloe. Mixture thin layer apply to the steamed skin, leave until completely dry. Before removing the composition, you need to massage the dermis with light movements and wash warm water. Carry out the procedure twice a week.

Recipe for an anti-wrinkle mask with acetylsalicylic acid - dissolve 6 ASA tablets in 5 ml of lemon juice, add 5 g of fine salt, blue clay and honey. The skin should first be steamed, apply the mixture for a quarter of an hour. Sessions are held every 2-3 days.

To reduce oily hair and eliminate dandruff, one Aspirin tablet should be added to a portion of shampoo. Use remedy maybe once a week.

Acetylsalicylic acid - available and effective remedy to relieve pain and inflammatory process. The drug has not only wide range actions, but also many contraindications, so you should first consult with your doctor and carefully study the instructions for use.

Acetylsalicylic acid contains:

Acetylsalicylic acid 500 mg.

Excipients: potato starch, stearic acid, lemon acid, talc

pharmachologic effect

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 developing myocardial infarction with unstable angina. Effective when primary prevention diseases of the cardiovascular system and in the secondary prevention of myocardial infarction. IN daily dose 6 g or more 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 helps Acetylsalicylic acid: indications

Rheumatism.
Rheumatoid arthritis.
Infectious-allergic myocarditis.
Fever in infectious and inflammatory diseases.
Pain syndrome of mild to moderate intensity various genesis, including: neuralgia, myalgia, headache.
Prevention of thrombosis and embolism.
Primary and secondary prevention myocardial infarction.
Prevention of violations cerebral circulation according to the ischemic type.
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.

Has a teratogenic effect: when used in the first trimester, it leads to the development of cleavage upper sky, in the third trimester - causes inhibition labor activity(inhibition of prostaglandin synthesis), premature closure ductus arteriosus in the fetus, pulmonary vascular hyperplasia and hypertension in the pulmonary circulation.

Acetylsalicylic acid is released from breast milk, which increases the risk of bleeding in the child 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 long-term use possible dizziness, headache, reversible visual impairment, tinnitus, aseptic meningitis.

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 medicines pyrazolone series).

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 with simultaneous anticoagulant therapy, decompensated chronic heart failure.

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

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

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

During prolonged 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 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 analgesic and more than 3 days as an antipyretic.

During the treatment period, the patient should refrain from drinking alcohol.

Compatibility with other drugs

At simultaneous use antacids containing magnesium and/or aluminum hydroxide slow down and reduce the absorption of acetylsalicylic acid.

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

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/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 long-term use acetylsalicylic acid in high doses there is a risk of developing severe adverse reactions from the side of 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 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 leads to respiratory alkalosis- shortness of breath, suffocation, cyanosis, cold sticky sweat with increased intoxication, respiratory paralysis and uncoupling of oxidative phosphorylation increases, causing respiratory acidosis.

At chronic overdose the concentration determined in plasma does not correlate well with the severity of intoxication. Greatest risk The development of 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% - 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 (may cause acidemia and increase toxic effect 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 Acetylsalicylic acid is isolated:

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.

Name:

Acetylsalicylic acid (Acidum acetylsalicylicum)

Pharmacological
action:

Acetylsalicylic acid has anti-inflammatory, antipyretic, and analgesic effects. It is widely used for feverish conditions ( elevated temperature body), headaches, neuralgia (pain spreading along the nerve), etc. and as an antirheumatic agent.
Anti-inflammatory effect acetylsalicylic acid is explained by its influence on the processes occurring in the source of inflammation.
Antipyretic effect is also associated with an 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 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 - 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 decreases. In addition, the effect of prostaglandins on sensitive nerve endings, leading to a decrease in their sensitivity to pain mediators. It also has an antiaggregation effect.

Indications for
application:

Acetylsalicylic acid has wide application as an anti-inflammatory, antipyretic and analgesic agent.
Important feature acetylsalicylic acid is the ability of the drug to have an antiaggregation effect, inhibit spontaneous and induced platelet aggregation.

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.

Mode of application:

In tablet form 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) is prescribed long-term for adults at 2-3 g (less often 4 g) per day, for 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.
Also used soluble form of aspirin- Acylpyrine is soluble. For fever ( sharp increase body temperature) and/or pain syndrome is prescribed in a single dose of 1-2 tablets of 0.5 g. If necessary, the drug is taken again in the same dose. The maximum daily dose is 6 tablets. At acute rheumatism prescribed in a daily dose of 100 mg/kg body weight 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.

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 - renal dysfunction; 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).

Contraindications:

Chronic or recurrent dyspeptic symptoms, peptic ulcer stomach and duodenum(including history), increased tendency to hemorrhages, kidney disease, simultaneous treatment anticoagulants, glucose-6-phosphate dehydrogenase deficiency, asthma, renal or liver dysfunction, pregnancy, increased sensitivity to acetylsalicylic acid and other salicylates.

Interaction
other medicinal
by other means:

When used simultaneously with anticoagulants the risk of bleeding increases.
When used simultaneously with other NSAIDs are intensifying side effects the latter, including an increased risk of developing gastropathy. During treatment with acetylsalicylic acid, the nephrotoxic effect of methotrexate is aggravated, and when used simultaneously with oral hypoglycemic drugs - sulfonylurea derivatives - an increase in the hypoglycemic effect is noted.
When used simultaneously with GCS the risk of developing gastropathy and gastrointestinal bleeding increases. Acetylsalicylic acid weakens the effect of spironolactone, furosemide, antihypertensive drugs and drugs used for gout.

Pregnancy:

It should be borne in mind that taking salicylates (in high doses) in the first 3 months. pregnancy has been linked in many epidemiological studies x s high risk development of deformities(cleft palate, heart defects). However, with normal therapeutic doses this risk appears to be small, as a study of approximately 3,200 mother-child pairs found no association with an increased rate 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 the mother takes acetylsalicylic acid 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 doctor supervision The drug should be taken only in normal doses and only for a few days.

Acetylsalicylic acid may not evoke any emotional response in the average person who is not privy to the mysteries of pharmaceutical terminology. But this is nothing more than the well-known aspirin. Or rather, on the contrary: aspirin is trade name acetylsalicylic acid, which, however, is available on pharmacy shelves not only under a “pseudonym”, but also under its original chemical name.

Acetylsalicylic acid is used as an analgesic, antipyretic, antithrombic and anti-inflammatory agent. At the biochemical level, the mechanism of action of this drug is based on inhibition of the synthesis of pain mediators and inflammatory reactions prostaglandins (this occurs due to inhibition of the enzyme cyclooxygenase) and thromboxane aggregates. Acetylsalicylic acid reduces blood flow to the site of inflammation, reduces permeability blood vessels, and, consequently, exudation, limits the amount of ATP used to maintain the energy consumption of the inflammatory process. The drug reduces the concentration of prostaglandins in the brain centers of pain and thermoregulation, which leads, accordingly, to a decrease in pain sensitivity and a decrease in body temperature.

The antiplatelet effect is associated with a decrease in the amount of thromboxane.

A drug called “acetylsalicylic acid” in Russia is available only in tablets. The drug should be taken after meals with a sufficient amount of liquid (water, milk, mineral water). Depending on the patient’s age, the recommended single and maximum daily doses of acetylsalicylic acid are respectively: 0.25-0.5 g and 3.0 g for adults and adolescents over 15 years of age; 0.25 g and 0.5 g for children from 6 to 15 years old. It is necessary to maintain an interval between doses of the drug of at least 4 hours when taking 3-4 times a day. In terms of using acetylsalicylic acid, the patient is given a certain amount of independence: 3 days as an antipyretic and 5 days as an analgesic, after which, if there is no improvement in the condition, it is necessary to consult a doctor. In case of accidental overdose of the drug, vomiting should be artificially induced and taken Activated carbon along with any strong laxative. Minor overdoses occur without significant consequences for the body.

Pharmacology

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 E 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 both central and peripheral effects. Reduces platelet aggregation, adhesion and thrombus formation by suppressing the synthesis of thromboxane A 2 in platelets.

Reduces mortality and the risk of developing 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.

Pharmacokinetics

When taken orally, it is rapidly absorbed mainly from the proximal region. 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. It 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 proliferative phase inflammation.

When acidosis occurs, most of the salicylate is converted into non-ionized acid, which penetrates well into tissues, incl. into the brain.

It is excreted primarily by active secretion in the renal tubules unchanged (60%) and in the form of metabolites. The excretion of unchanged salicylate depends on the pH of the urine (with alkalinization of the urine, the ionization of salicylates increases, their reabsorption worsens and excretion increases significantly). T 1/2 of acetylsalicylic acid is approximately 15 minutes. T1/2 of salicylate when taken in low doses is 2-3 hours, with increasing doses it can increase to 15-30 hours. In newborns, the elimination of salicylate is much slower than in adults.

Release form

10 pieces. - contour cellular packaging (1) - cardboard packs.
20 pcs. - contour cellular packaging (1) - cardboard packs.
30 pcs. - contour cellular packaging (1) - cardboard packs.
40 pcs. - polymer jars (1) - cardboard packs.

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/day.

Interaction

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 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.

With simultaneous use of dipyridamole, an increase in salicylate C max 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.

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.

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.

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

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, liver and/or kidney failure, glucose-6-phosphate dehydrogenase deficiency, Reye's syndrome, childhood(under 15 years of age - the risk of developing Reye's syndrome in children with hyperthermia due to viral diseases), I and III trimesters of pregnancy, lactation, hypersensitivity to acetylsalicylic acid and other salicylates.

Application features

Use 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.

Use for liver dysfunction

Contraindication: liver failure.

Use with caution in patients with liver disease.

Use for renal impairment

Contraindication: renal failure.

Use with caution in patients with kidney disease.

Use in children

Contraindication: childhood (under 15 years of age - the risk of developing Reye's syndrome in children with hyperthermia due to viral diseases).

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 should refrain from drinking alcohol.