Which acetylsalicylic acid is best? What does acetylsalicylic acid help with? What is acetylsalicylic acid

(Acidum acetylsalicylicum)

Registration number:

Р№ 003889/01

Tradename: Acetylsalicylic acid

International (nonproprietary) name: Acetylsalicylic acid

Dosage form:

pills

Compound:

Active substance: acetylsalicylic acid - 0.25 g or 0.5 g.
Excipients: potato starch, talc, citric acid.

Description: pills white, slightly marbled, odorless or with a weak characteristic odor, flat-cylindrical with a score and a chamfer.

Pharmacotherapeutic group:

non-steroidal anti-inflammatory drug (NSAID).

ATX code: N02BA01

Pharmacological properties:

It has anti-inflammatory, analgesic and antipyretic effects associated with the suppression of cyclooxygenase 1 and 2, which regulate the synthesis of prostaglandins. Reduces platelet aggregation, adhesiveness and thrombus formation by suppressing the synthesis of thromboxane A2 in platelets. The antiaggregation effect persists for 7 days after a single dose (more pronounced in men than in women).

Indications for use:

Moderate or mild pain syndrome in adults of various origins (headache, toothache, migraine, neuralgia, arthralgia, muscle pain, menstrual pain).
Increased body temperature during colds and other infectious and inflammatory diseases (in adults and children over 15 years of age).

Contraindications:

- hypersensitivity to acetylsalicylic acid and other NSAIDs;
- erosive and ulcerative lesions (in the acute phase) of the gastrointestinal tract;
- severe dysfunction of the liver or kidneys;
- “aspirin asthma”;
- hemorrhagic diathesis (hemophilia, von Willebrand disease, telangiectasia, hypoprothrombinemia, thrombocytopenia, thrombocytopenic purpura);
- dissecting aortic aneurysm;
- portal hypertension, vitamin K deficiency;
- deficiency of glucose-6-phosphate dehydrogenase;
- pregnancy (I and III trimester), period breastfeeding.
- The drug is not prescribed as an antipyretic for children under 15 years of age with acute respiratory diseases caused by viral infections, due to the risk of developing Reye's syndrome (encephalopathy and acute fatty degeneration liver with acute development liver failure).

Carefully- hyperuricemia, urate nephrolithiasis, gout, peptic ulcer stomach and/or duodenum(history), decompensated heart failure.

Directions for use and doses
For pain syndrome of mild to moderate intensity and feverish conditions, the single dose is 0.5-1 g, the maximum single dose is 1 g, the maximum daily dose should not exceed 3 g. Intervals between doses of the drug should be at least 4 hours. For decreasing irritating effect on gastrointestinal tract the drug should be taken after meals with water, milk, alkaline mineral water.
The duration of treatment (without consulting a doctor) should not exceed 7 days when prescribed as an analgesic and more than 3 days when prescribed as an antipyretic.

Side effect
- allergic reactions - skin rash, bronchospasm, Quincke's edema;
- formation based on the hapten mechanism of the “aspirin” triad (combination bronchial asthma, recurrent polyposis of the nose and paranasal sinuses, and intolerance acetylsalicylic acid and drugs of the pyrazolone series);
- gastrointestinal disorders- nausea, vomiting, pain in epigastric region, diarrhea;
- thrombocytopenia, anemia, leukopenia;
- hemorrhagic syndrome (nose bleed, bleeding gums), increased blood clotting time;
- at long-term use in large doses, erosive and ulcerative lesions of the gastrointestinal tract, bleeding, black “tarry” stools may occur, general weakness, interstitial nephritis, prerenal azotemia with an increase in creatinine in the blood and hypercalcemia, bronchospasm, papillary necrosis, acute renal failure, nephrotic syndrome, increased activity of “liver” transaminases, aseptic meningitis, increased symptoms of chronic heart failure, edema.
When similar symptoms It is recommended to stop taking the drug and consult your doctor immediately.

Overdose (intoxication) of the drug
IN initial stage poisoning, symptoms of central excitation develop nervous system, dizziness, severe headache, decreased hearing acuity, blurred vision, nausea, vomiting, increased breathing. Later, depression of consciousness occurs, up to coma, respiratory failure, disturbances of water-electrolyte metabolism

Treatment: if there are signs of poisoning, induce vomiting or do a gastric lavage, prescribe activated charcoal and a laxative, and consult a doctor. Treatment should be carried out in a specialized department.

Interaction with other drugs
Acetylsalicylic acid increases the toxicity of methotrexate, the effects of narcotic analgesics, other NSAIDs, oral hypoglycemic drugs, heparin, indirect anticoagulants, thrombolytics and platelet aggregation inhibitors, sulfonamides (including cotrimoxazole), triiodothyronine; reduces - uricosuric drugs (benzbromarone, sulfinpyrazone), antihypertensive drugs and diuretics (spironolactone, furosemide).
Glucocorticosteroids, alcohol and alcohol-containing drugs increase the damaging effect on the gastrointestinal mucosa and increase the risk of developing gastrointestinal bleeding.
Acetylsalicylic acid increases the concentration of digoxin, barbiturates and lithium drugs in the blood plasma.
Antacids containing magnesium and/or aluminum hydroxide slow down and impair the absorption of acetylsalicylic acid.

special instructions
Acetylsalicylic acid reduces excretion uric acid from the body, which can cause acute attack gout in predisposed patients.
With long-term use of the drug, you should periodically general analysis blood and stool test occult blood.
In the second trimester of pregnancy it is possible one-time appointment the drug in recommended doses only for strict indications.
If it is necessary to use the drug during lactation, breastfeeding should be discontinued.

Release form
10 tablets in blister or cell-free packaging.

Storage conditions
In a dry place, out of reach of children.

Best before date
4 years. Do not use after the expiration date stated on the package.

Conditions for dispensing from pharmacies
Over the counter.

Manufacturing company
CJSC "Altaivitamins", 659325, Altai region, Biysk, Zavodskaya st., 69.

Tablets with a flat surface, white, with a chamfer and a score. Marbling is allowed on the surface of the tablets.

Pharmacotherapeutic group

Other analgesics-antipyretics. Salicylic acid and its derivatives.

Acetylsalicylic acid.

ATX code N 02B A01

Pharmacological properties"type="checkbox">

Pharmacological properties

Pharmacokinetics

P After ingestion, acetylsalicylic acid is converted into the main metabolite - salicylic acid. Absorption of acetylsalicylic and salicylic acids in the digestive tract occurs quickly and

fully. The maximum level of concentration in blood plasma is achieved after 10-20 minutes (acetylsalicylic acid) or 45-120 minutes ( general level salicylates). The degree of binding of acids to plasma proteins depends on the concentration, which is 49-70% for acetylsalicylic acid and 66-98% for salicylic acid. 50% of the administered dose of the drug is metabolized during the initial passage through the liver. Metabolites of acetylsalicylic and salicylic acids are the glycine conjugant of salicylic acid, gentisic acid and its glycine conjugant. The drug is excreted from the body in the form of metabolites, mainly by the kidneys. The half-life of acetylsalicylic acid is 20 minutes. The half-life of salicylic acid increases proportionally dose taken of the drug and is 2, 4 and 20 hours for doses of 0.5 g, 1 g and 5 g respectively. The drug penetrates the blood-brain barrier and is also detected in breast milk and synovial fluid.

Pharmacodynamics

The drug has antipyretic, analgesic and anti-inflammatory effects, and also reduces platelet aggregation. The main mechanism of action of acetylsalicylic acid is the inactivation of the enzyme cyclooxygenase, as a result of which the synthesis of prostaglandins, prostacyclins and thromboxane is disrupted. Due to a decrease in the production of prostaglandins, their pyrogenic effect on thermoregulation centers is weakened. In addition, the sensitizing effect of prostaglandins on sensitive nerve endings, which reduces their sensitivity to pain mediators. Irreversible disturbances in the synthesis of thromboxane A2 in platelets cause the antiplatelet effect of the drug. Acetylsalicylic acid also blocks cyclooxygenases of endothelial cells, in which prostacyclin, which has antiplatelet activity, is synthesized. Cyclooxygenases of endothelial cells are less sensitive to the action of acetylsalicylic acid and, unlike a similar platelet enzyme, are blocked reversibly.

Indications for use

Pain syndrome low to medium intensity of various etiologies(including inflammatory) genesis

Increased temperature (fever) due to influenza, colds (ARVI) and other infectious and inflammatory diseases

Directions for use and doses

Acetylsalicylic acid is taken orally, after meals, with a drink big amount water.

For pain and fever during infectious and inflammatory diseases, a single dose for adults and children over 15 years of age is 0.5 - 1 g. The maximum daily dose is 3 g. For older people, the maximum daily dose is 1 g.

The duration of treatment should not exceed 5 days as an analgesic and 3 days as an antipyretic.

In patients with associated disorders liver and kidney function, it is necessary to reduce the dose or increase the interval between taking the drug.

Side effects"type="checkbox">

Side effects

Tinnitus, dizziness, hearing loss, visual impairment

Nausea, abdominal pain, heartburn, vomiting

Anorexia

Reye/Reye syndrome (encephalopathy combined with acute fatty liver)

Hypersensitivity reaction (bronchospasm, skin rash, angioedema, urticaria, aspirin-induced asthma)

Interstitial nephritis, prerenal azotemia with increased creatinine in the blood and hypercalcemia, acute renal failure, nephrotic syndrome

Papillary necrosis

Breathing problems

Drowsiness

Convulsions

Erosive and ulcerative lesions digestive tract, sometimes complicated by latent or clinically significant (melena) bleeding, liver failure

Increased symptoms of congestive heart failure

Thrombocytopenia, leukopenia, anemia

Aseptic meningitis

Increased aminotransferase levels

Contraindications

Hypersensitivity to acetylsalicylic and salicylic acid

Peptic ulcer of the stomach and duodenum

Increased tendency to bleed

Kidney disease, renal and/or liver dysfunction

Simultaneous treatment with anticoagulants (with the exception of heparin therapy in low doses with frequent and careful monitoring of blood clotting)

Glucose-6-phosphate dehydrogenase deficiency

Bronchial asthma

Chronic or recurrent dyspeptic symptoms

History of erosive and ulcerative lesions of the upper gastrointestinal tract

Gastrointestinal bleeding

- “aspirin” bronchial asthma and “aspirin” triad

Vitamin K deficiency, hypoprothrombinemia

Dissecting aortic aneurysm

Pregnancy period and lactation period

Portal hypertension

Taking methotrexate at a dose of 15 mg/week or more

Childhood and adolescence up to 15 years

Drug interactions"type="checkbox">

Drug interactions

With the simultaneous use of acetylsalicylic acid and anticoagulants, the risk of bleeding increases. With the simultaneous use of acetylsalicylic acid and non-steroidal anti-inflammatory drugs, the therapeutic and side effects the latter. During treatment with acetylsalicylic acid, the side effects of methotrexate are aggravated. With the simultaneous use of acetylsalicylic acid and oral antidiabetic drugs from the group of sulfonylurea derivatives, the hypoglycemic effect of the latter is enhanced. When used simultaneously with corticosteroids, the risk of gastrointestinal bleeding increases. Acetylsalicylic acid weakens the effect of spironolactone, furosemide, antihypertensive drugs and agents that promote the removal of uric acid.

Purpose antacids during treatment with acetylsalicylic acid (especially in doses exceeding 3 g of acetylsalicylic acid for adults and 1.5 g for children) can reduce high stable levels of salicylates in the blood.

special instructions

Special Warnings and Cautions

The drug is not prescribed to children and adolescents under 15 years of age with acute respiratory diseases caused by viral infections, with diseases accompanied by hyperthermia due to the risk of developing Reye/Rea syndrome.

In patients with allergic diseases, including bronchial asthma, allergic rhinitis, hives, skin itching, swelling of the mucous membrane and nasal polyposis, as well as when they are combined with chronic infections respiratory tract and in patients with hypersensitivity to non-steroidal anti-inflammatory drugs during treatment with acetylsalicylic acid, attacks of bronchial asthma may develop.

Use during surgical interventions. Before any surgical procedure, inform your doctor, surgeon, anesthesiologist or dentist that you are taking acetylsalicylic acid. 5-7 days before the planned surgical intervention it is necessary to stop taking acetylsalicylic acid to reduce the risk of bleeding during surgery and postoperative period.

During the period of use of the drug you should refrain from drinking alcohol.

Use during pregnancy

Inhibition of prostaglandin synthesis may have negative effects on pregnancy and embryonic or fetal development. Data from epidemiological studies indicate increased risk development of defects and malformations when using synthesis inhibitors

prostaglandins on early periods pregnancy. It is believed that the risk increases with increasing dose and duration of treatment.

Animal studies have shown reproductive toxicity; therefore, the use of drugs containing acetylsalicylic acid during pregnancy is not indicated.

Acetylsalicylic acid, tablets: instructions for use

Compound

Each tablet contains: active substance: acetylsalicylic acid - 500 mg.

pharmachologic effect

Acetylsalicylic acid belongs to the group of acid-forming NSAIDs with analgesic, antipyretic and anti-inflammatory properties. Their mechanism of action is based on irreversible inhibition of cyclooxygenase enzymes involved in the synthesis of prostaglandins. In doses from 0.3 g to 1.0 g it is used for mild treatment and moderate pain and fever, such as a cold or flu, to reduce fever and treat joint and muscle pain. Acetylsalicylic acid also inhibits platelet aggregation by blocking the synthesis of thromboxane A2 in platelets. For this reason, it is used for some cardiovascular diseases, in doses of 75-300 mg per day.

Pharmacokinetics

After oral administration, acetylsalicylic acid is quickly and completely absorbed from the gastrointestinal tract. During and after resorption, acetylsalicylic acid is converted into active metabolites of salicylic acid. The maximum concentration in blood plasma of acetylsalicylic and salicylic acids is achieved after 10-20 minutes. About 80% of salicylic acid is bound to plasma proteins. Salicylates easily penetrate into tissues and body fluids, incl. into synovial, cerebrospinal, and peritoneal fluids. IN small quantities salicylates are found in brain tissue, penetrate the placental barrier, and are excreted in small quantities in breast milk. Acetylsalicylic acid is metabolized in the liver by hydrolysis to form salicylic acid, followed by conjugation with glycine or glucuronide. The metabolism of salicylic acid depends on the dose and the activity of liver enzymes. The half-life varies from 2 to 3 hours when using low doses and up to 15 hours when taking high doses. Salicylic acid and its metabolites are excreted mainly through the kidneys.

Indications for use

Fever in infectious and inflammatory diseases;

Pain syndrome of weak and medium intensity of various origins.

Contraindications

Hypersensitivity; erosive and ulcerative lesions of the gastrointestinal tract (in the acute phase), gastrointestinal bleeding; “aspirin” triad; hemorrhagic diathesis (hemophilia, von Willibrand's disease, telangiectasia, hypoprothrombinemia, thrombocytopenia, thrombocytopenic purpura); bronchial asthma induced by taking salicylates and other NSAIDs, a combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid, dissecting aortic aneurysm, portal hypertension; vitamin K deficiency; liver/renal failure; glucose-6-phosphate dehydrogenase deficiency, 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 and lactation.

Directions for use and doses

To reduce irritation to the gastrointestinal tract medicine should be taken after meals with water, milk or alkaline mineral water. For pain of mild to moderate intensity and febrile conditions, for children over 15 years of age the maximum single dose is 500 mg, for adults - 1000 mg. If necessary, the drug can be taken 3 times a day with an interval of at least 4 hours. The maximum daily dose for children over 15 years of age is 1500 mg; for adults - 3000 mg. You should not take the drug for more than 5 days as an analgesic and for more than 3 days as an antipyretic without a doctor’s prescription.

Side effect

When estimating frequency adverse reactions The following gradation is used:

Very common: ≥1/10;

Very rarely:

Not known: frequency cannot be estimated due to lack of data.

From the outside digestive system: often - 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: uncommon - skin rash; rarely - 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).

Others: very rarely - Reye's syndrome; with long-term use - increased symptoms of chronic heart failure.

Overdose

Overdose is possible with a single administration of excessively high doses of the drug or with long-term use.

Symptoms: salicylic syndrome (nausea, vomiting, tinnitus, general malaise, fever). More severe poisoning - stupor, convulsions and coma, non-cardiogenic pulmonary edema, severe dehydration, impairment of CBS (first - respiratory alkalosis, then metabolic acidosis), kidney failure and shock.

Treatment: immediate hospitalization, gastric lavage, use activated carbon, CBS check. Depending on the state of the WWTP and electrolyte balance carry out infusion administration solutions of sodium bicarbonate, sodium citrate and sodium lactate; when urine pH is from 7.5 to 8.0 and the content of salicylates in the blood plasma is more than 500 mg/l (for adults) or 300 mg/l (for children from 15 to 18 years old) intensive care alkaline diuretics; in case of serious poisoning, hemodialysis is indicated; replenishment of fluid loss; symptomatic treatment.

Interaction with other drugs

When used simultaneously with acetylsalicylic acid:

Antacids containing magnesium and/or aluminum hydroxide slow down and reduce the absorption of acetylsalicylic acid;

Calcium channel blockers, drugs that limit the intake of calcium or increase the excretion of calcium from the body - the risk of bleeding increases;

The effect of heparin and indirect anticoagulants, methotrexate, phenytoin, valproic acid is enhanced;

Antidiabetic agents - lowering blood sugar levels;

GCS - increases the risk of ulcerogenic effects and gastrointestinal bleeding;

The effectiveness of diuretics (spirolactone, furosemide) decreases;

Other NSAIDs - increases the risk of side effects;

Acetylsalicylic acid may reduce plasma concentrations of indomethacin, iroxicam;

The effectiveness of uricosuric drugs decreases;

Griseofulvin - possible disruption of absorption of acetylsalicylic acid;

The concentrations of digosin, barbiturates and lithium salts in the blood plasma increase;

Reduced effectiveness of captopril and enalapril (when using acetylsalicylic acid in high doses);

Caffeine - increases the rate of absorption, plasma concentration and bioavailability of acetylsalicylic acid, the risk of adverse reactions;

Platelet aggregation inhibitors - increased risk bleeding;

Alcohol - increased risk of developing gastrointestinal ulcers and bleeding;

Serotonin reuptake inhibitors - increases the risk of gastrointestinal bleeding.

Precautionary measures

5-7 days before surgery, it is necessary to stop taking the drug (to reduce bleeding during surgery and in the postoperative period). The irritant effect on the gastrointestinal tract is reduced when administered after meals. During long-term therapy, it is recommended to regularly perform blood tests and examine stool for occult blood. Not recommended for relief of febrile syndrome in children.

ASA, even in small doses, reduces the excretion of uric acid from the body, which can cause the development of an acute attack of gout in predisposed patients. During the treatment period, you should refrain from taking ethanol.

Use during pregnancy and lactation. Contraindicated for use in I and III trimester pregnancy, during lactation.

Has a teratogenic effect; when used in the first trimester leads to the development of clefting upper sky; in the third trimester causes inhibition labor activity(inhibition of Pg synthesis), premature closure ductus arteriosus in the fetus, pulmonary vascular hyperplasia and hypertension in the “lesser” circulation. It is excreted in breast milk, which increases the risk of bleeding in the baby due to impaired platelet function. Breastfeeding should be stopped during treatment.

Impact on the ability to drive a car and other potentially dangerous mechanisms. Due to the possibility of developing adverse reactions from the nervous system, it should be taken with caution.

Release form

10 tablets in a blister pack.

10 tablets in contour-free packaging.

One, two or three contour cell or cell-free packages together with instructions for use are placed in a pack of cardboard boxes.

Self-medication can be harmful to your health.
You should consult your doctor and read the instructions before use.

Every family always has a medicine such as acetylsalicylic acid in their medicine cabinet. But every second person is interested in the following question: “Is acetylsalicylic acid “Aspirin” or not?” That's what it's about we'll talk in our article, and we will also tell you about the properties and application this drug.

A little history

Acetylsalicylic acid was first discovered at the end of the 19th century by the young chemist Felix Hoffman, who at that time worked at Bayer. He really wanted to develop a remedy that would help his father relieve joint pain. The idea of ​​where to look for the required composition was suggested to him by his father’s attending physician. He prescribed sodium salicylate to his patient, but the patient could not take it, as it severely irritated the gastric mucosa.

After two years, a drug such as “Aspirin” was patented in Berlin, so acetylsalicylic acid is “Aspirin”. This is a shortened name: the prefix "a" is an acetyl group that is attached to salicylic acid, the root "spire" indicates spiraic acid (this type of acid is present in the form of an ester in plants, one of them is spirea), and the ending "in" in those distant times, they were often used in the names of medicines.

"Aspirin": chemical composition

It turns out that acetylsalicylic acid is “Aspirin”, and its molecule contains two active acids: salicylic and acetic. If you store the drug at room temperature, then at high humidity it quickly decomposes into two acidic compounds.

That is why Aspirin always contains acetic and salicylic acids; after a short period of time, the main component becomes much smaller. The shelf life of the drug depends on this.

Taking a pill

After Aspirin enters the stomach, and then into the duodenum, the juice from the stomach does not affect it, since the acid dissolves best in alkaline environment. After the duodenum, it is absorbed into the blood, and only there does its transformation occur and salicylic acid is released. While the substance reaches the liver, the amount of acids decreases, but their water-soluble derivatives become much larger.

And already passing through the vessels of the body, they reach the kidneys, from where they are excreted along with urine. At the exit from Aspirin, a tiny dose remains - 0.5%, and the remaining amount is metabolites. They are exactly what medicinal composition. I would also like to say that the drug has 4 therapeutic effects:

  • Preventing blood clots.
  • Anti-inflammatory properties.
  • Antipyretic effect.
  • Relieves pain syndrome.

Acetylsalicylic acid has a wide range of applications; the instructions contain detailed recommendations by use. You should definitely read it or consult a doctor.

"Aspirin": application

We found out how acetylsalicylic acid works. What it helps with, we’ll figure out further.

  1. Used for pain.
  2. At high temperature.
  3. At various kinds inflammatory processes.
  4. In the treatment and prevention of rheumatism.
  5. For the prevention of thrombosis.
  6. Prevention of stroke and heart attack.

An excellent drug is acetylsalicylic acid, the price of it will also please everyone, because it is low and ranges from 4-100 rubles, depending on the manufacturer and dosage.

"Aspirin": the fight against blood clots

Blood clots form in those places blood vessel, where there is any damage to the walls. In these places, fibers are exposed, which hold the cells together. Blood platelets are retained on them, releasing a substance that helps enhance adhesion, and in such places the vessel narrows.

Most often in healthy body thromboxane is opposed by another substance - prostacyclin, it does not allow platelets to stick together and, on the contrary, dilates blood vessels. When the vessel is damaged, the balance between these two substances shifts, and prostacyclin simply stops being produced. Thromboxane is produced in excess, and the platelet clump grows. Thus, blood flows through the vessel more and more slowly every day. This can later lead to a stroke or heart attack. If acetylsalicylic acid is constantly taken (the price of the drug, as already noted, is more than affordable), then everything changes dramatically.

The acids contained in Aspirin prevent fast growth thromboxane, help remove it from the body. Thus, the drug protects blood vessels from blood clots, but it is worth taking the medicine for at least 10 days, since only after this time do platelets restore their ability to stick together.

Acetylsalicylic acid as an antipyretic agent

Due to the fact that this drug has the ability to dilate blood vessels, the secretion human body heat is removed much better - the temperature drops. Acetylsalicylic acid from temperature is considered the best drug. In addition, this drug also acts on the thermoregulatory centers of the brain, giving it a signal to reduce the temperature.

It is not advisable to give this medicine to children as an antipyretic because of its strong irritant effect on the stomach.

Aspirin as an anti-inflammatory and pain reliever

This drug also interferes with the inflammatory processes of the body, it prevents the release of blood to the sites of inflammation, as well as those substances that cause pain. It has the ability to enhance the production of the hormone histamine, which dilates blood vessels and increases blood flow to the site inflammatory process. It also helps strengthen the walls of thin blood vessels. All this creates an anti-inflammatory and analgesic effect.

As we found out, acetylsalicylic acid is effective against temperature. However, this is not its only advantage. It is effective for all types of inflammation and pain occurring in the human body. That is why this drug is most often found in home medicine cabinets.

"Aspirin" for children

Acetylsalicylic acid is prescribed to children for fever, infectious and inflammatory diseases and severe pain. It should be taken with caution by children under 14 years of age. But for those who have reached the age of 14, you can take half a tablet (250 mg) in the morning and evening.

Aspirin is taken only after meals, and children should definitely crush the tablet well and wash it down with plenty of water.

Contraindications

Acetylsalicylic acid (this is “Aspirin”, as most people call it) can not only benefit the body, but also harm it. It is considered a very aggressive agent.

The first thing you should not do is to use an expired drug, since Aspirin can irritate the gastric mucosa, which will ultimately lead to an ulcer. In addition, those who have gastrointestinal diseases should take the drug only as prescribed by a doctor and it is best to take the medicine with milk. People with kidney and liver diseases should also take it with extreme caution.

Women during pregnancy are not recommended to take the drug, as there is evidence that it can adversely affect the development of the fetus. And you should not use it before childbirth, as this will weaken contractions or may cause prolonged bleeding.

If you think that acetylsalicylic acid is completely harmless, the instructions say something completely different. It has a lot of contraindications and side effects. Before use, you need to weigh all the pros and cons.

Conclusion

So, let's summarize. What does acetylsalicylic acid help with? This drug helps with elevated temperature, from the formation of blood clots, it is an excellent anti-inflammatory and analgesic.

Even though the drug has serious contraindications for use, it is promised a bright future. Currently, most scientists are looking for additives that could reduce harmful influence funds for individual organs. It is also believed that others medications will not be able to displace Aspirin, but, on the contrary, it will have new areas of application.

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

Pharmacology

pharmachologic effect- 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 the energy supply of the 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 adhesion blood platelets achieved at doses up to 30 mg. Increases fibrinolytic activity of plasma and reduces the concentration of vitamin K-dependent coagulation factors (II, VII, IX, X). Stimulates the excretion of uric acid, since its reabsorption in the kidney tubules is disrupted.

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 the absorption of 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 factors risk of ischemic heart disease, silent myocardial ischemia, unstable angina, myocardial infarction (to reduce the risk of recurrent myocardial infarction and death after myocardial infarction), repeated 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 re-stenosis and treating secondary coronary artery dissection), as well as for non-atherosclerotic lesions coronary arteries(Kawasaki disease), aortoarteritis (Takayasu disease), valvular mitral valves hearts and atrial fibrillation, prolapse mitral valve(prevention of thromboembolism), recurrent thromboembolism pulmonary artery, Dressler's syndrome, pulmonary infarction, acute thrombophlebitis. Fever in infectious and inflammatory diseases. Pain syndrome of weak and medium intensity of various origins, incl. thoracic 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 Gastrointestinal bleeding, gastrointestinal bleeding, acute renal or liver failure, initial hypoprothrombinemia, vitamin K deficiency, thrombocytopenia, thrombotic thrombocytopenic purpura, glucose-6-phosphate dehydrogenase deficiency, pregnancy (I and III trimester), breastfeeding, childhood and adolescence under 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 of the stomach and duodenum (history), severe violations liver and kidney function, bronchial asthma, COPD, nasal polyposis, uncontrolled arterial hypertension.

Use during pregnancy and breastfeeding

The use of large doses of salicylates in the first trimester of pregnancy is associated with an increased incidence of fetal 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 of adverse reactions in the child and does not require cessation of breastfeeding. However, with long-term use or high doses, breastfeeding should be discontinued.

Side effects of the substance Acetylsalicylic acid

From the outside of cardio-vascular 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” bronchial asthma and the “aspirin” triad (eosinophilic rhinitis, recurrent nasal polyposis, hyperplastic sinusitis) based on the hapten mechanism.

Others: impaired liver and/or kidney function, Reye's syndrome in children (encephalopathy and acute fatty liver with rapid development of 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, acute 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 it renal clearance, the effects of 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 dose large dose or with 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. A level above 70 mg% indicates moderate or severe poisoning; above 100 mg% - extremely severe, prognostically unfavorable. In case of poisoning moderate severity hospitalization required at least for 24 hours

Treatment: provocation of vomiting, administration of 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 (it can cause acidemia and enhance the toxic effect of 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, severe central nervous system damage, 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 surgery, it is necessary to stop taking the drug (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. Risk hemorrhagic complications considered the smallest 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

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