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Acetylsalicylic acid: instructions for use, analogues, reviews. Acetylsalicylic acid - from what? Analgesic drugs

Acetyl salicylic acid– a drug that has a pronounced anti-inflammatory effect. The medicine eliminates high temperature and pain, reduces platelet aggregation. Find out how to use the drug, in what quantities to use and what acetylsalicylic acid helps with - detailed instructions for use contain all necessary information.

Pharmacological action

The drug prevents the synthesis of prostaglandins, which are involved in inflammatory processes and contribute to the appearance of pain and fever. As a result of a significant decrease in the amount of prostaglandins, blood vessels dilate, which promotes increased sweating. So the drug has an antipyretic effect.

When using the medication, the nerve endings become less sensitive to pain. The medicine is taken orally, the maximum level of the active substance in the blood is achieved in a short time - after 10-20 minutes. The level of salicylate resulting from metabolism increases within two hours. The components of the drug are excreted by the kidneys. Partial elimination occurs 20 minutes after taking the drug; salicylate is partially removed from the body after 2 hours.

Release form and composition

Acetylsalicylic acid is available in tablets. Composition presented different amounts active substance – 100, 250, 50 mg, supplemented with citric acid and potato starch.

Aspirin and Analgin

Many people are interested in whether aspirin is acetylsalicylic acid or not? Is acetylsalicylic acid aspirin or analgin? Aspirin is a derivative of salicylic acid. Acetylsalicylic acid, often called aspirin, was obtained by replacing one hydroxyl group. Therefore, analgin is a completely different drug.

What does Acetylsalicylic acid help with?

For many decades, aspirin has been the most popular drug in the world.

The medicine is prescribed when it is detected:

  • fever;
  • rheumatoid arthritis;
  • rheumatic fever, occurring in acute form;
  • Dressler's syndrome;
  • rheumatic chorea;
  • a heart attack in which the lungs are affected;
  • acute thrombophlebitis;
  • headaches, including migraines;
  • osteoarthritis;
  • neuralgia;
  • various pain sensations - during dental diseases, during menstruation, accompanied by discomfort; pain in muscles and joints;
  • diseases of the spine accompanied by syndromes, the list is presented by osteochondrosis, sciatica, lumbago;
  • myocardial infarction, ischemic heart disease, atrial fibrillation, thromboembolism (used for prevention).

Contraindications and side effects

Contraindications to the use of the medicine are presented in a list that includes:

  • portal hypertension;
  • bleeding in the digestive tract;
  • Reye's syndrome;
  • hemorrhagic diathesis;
  • aspirin triad;
  • insufficient amount of vitamin K in the body and glucose-6-phosphate dehydrogenase;
  • the presence of erosive and ulcerative lesions in the gastrointestinal tract in an acute form;
  • hemophilia;
  • insufficiency of liver and kidney functions;
  • the presence of a dissecting aortic aneurysm;
  • hypoprothrombinemia;
  • periods of pregnancy, lactation;
  • excessive sensitivity of the body to components this tool and other drugs that eliminate inflammatory reactions, which is manifested by the development of rhinitis and the appearance of urticaria.

Possible negative reactions

Some people may develop side effects:

  • diarrhea;
  • nausea;
  • skin rashes;
  • the appearance of tinnitus;
  • the occurrence of erosive and ulcerative lesions, bleeding in the digestive tract;
  • angioedema;
  • development of the aspirin triad;
  • the appearance of pain in the abdomen;
  • the occurrence of thrombocytopenia, anemia;
  • development of anorexia;
  • Reye's syndrome;
  • bronchospasm;
  • the appearance of headaches, dizziness;
  • visual impairment;
  • hemorrhagic syndrome;
  • deterioration of the condition in chronic heart failure;
  • disorders of the kidneys and liver.

If the doctor has prescribed acetylsalicylic acid, the instructions for use and contraindications should be carefully studied to avoid negative consequences.

Using large doses of the drug

When using the drug in large quantities, not corresponding to the recommended doses, are possible negative reactions body. Overdose leads to the following problems:

  • violations acid-base balance and electrolyte;
  • confusion;
  • nausea accompanied by vomiting, pain in the abdomen;
  • dehydration of the body;
  • hearing and vision problems;
  • tremor;
  • drowsy state.

IN in rare cases abuse of the drug leads to metabolic acidosis and coma.

How to take

According to the instructions for use of acetylsalicylic acid, tablets are taken after meals. You can drink the drug not only with plain water, but also with alkaline mineral water, as well as with milk.

The dosage is determined by the doctor. If it is not possible to see a doctor and the problem is not significant, you can take aspirin in the amount of 1-2 tablets, which corresponds to 500-1000 mg. The dose is indicated for an adult. 3-4 doses of medication are allowed per day.

Is it possible to use 2 tablets of acetylsalicylic acid 4 times a day? It is prohibited to use the medicine in such quantities. Maximum daily dose corresponds to 6 tablets. You can be treated with the drug for no longer than two weeks.

Effect on blood clotting

Acetylsalicylic acid thins the blood. To find out how to take tablets to improve the rheological properties of blood, you should consult a doctor. The specialist will select an individual dosage. To prevent platelet aggregation, the drug is used in the amount of 0.5 tablets/day. The course duration is usually 2-3 months.

Myocardial infarction

To prevent myocardial infarction, use 250 mg of the drug per day. For thromboembolism and disorders cerebral circulation also use 0.5 tablets/day. Gradually the amount of the drug is increased to 1000 mg (2 tablets/day).

Instructions for the use of Acetylsalicylic acid for fever in children and adults

Aspirin is usually prescribed for colds.

Tablets for fever should not be used on an empty stomach. If you need to bring down the temperature of an adult, the recommended dosage is 250-1000 mg of the drug. You can take the medicine 3 or 4 times a day.

For fever, children are given from 100 to 300 mg of the drug. It is advisable that the dose of the medication be selected by a doctor. The dosage size for children is determined according to age.

  1. To the child over two years old give 100 mg of medicine.
  2. From three years old 150 mg is allowed.
  3. When treating a child over four years old it is necessary to use 200 mg of the drug, and when treating a child of age over five years old– 250 mg.
  4. Acetylsalicylic acid in the recommended amount can be given to a child 3 or 4 times a day.

For headaches

Acetylsalicylic acid is an effective remedy for headaches. You can also take Paracetamol. The drug is potent, so it can either benefit the body or harm it. When determining the appropriate dose of the drug, you should be as careful as possible. If rest is not planned in the near future, take two tablets. If after taking the drug it is possible to sleep or relax, the dose of the drug should be reduced to 0.5-1 tablet. To obtain the desired effect, the medication must be taken immediately after the onset of discomfort.

The indicated doses of the medicine are intended for use by adults. This treatment option is not suitable for children.

Hangover

Regardless of the reasons for the development of headaches, it is possible to effectively solve the problem. For example, in everyday life people often take the drug for a hangover. But we should not forget that the medication only eliminates the pain, but not the hangover itself. To get rid of the problem, use other medications when you have a hangover.

How does aspirin affect blood pressure?

Does aspirin increase or decrease blood pressure? The medication does not affect the indicators in any way blood pressure. The ability of the drug to eliminate migraine pain and reduce intracranial pressure is explained by its ability to thin the blood. Using the drug for hypertension is harmful due to the risk of bleeding.

Treatment for menstruation and toothache

Can the product be used during menstruation? In such cases, you can use the drug, but with caution and obtaining prior consultation with a doctor. The recommended dose is 1 tablet 2 times a day, but it is still better to use other painkillers for these purposes - analgin, spasmalgon, no-shpu.

Aspirin also helps against toothache, as it can have a pronounced analgesic effect. But you cannot use more than 4000 mg of the product per day. Otherwise, severe damage to the brain and internal organs may occur. Children under 12 years of age should choose other medications, as should pregnant women. When a toothache occurs, Paracetamol will also help.

How to get rid of acne

The drug helps get rid of acne. It acts quickly and is one of the most effective remedies. Acetylsalicylic acid, when used on the face, destroys bacteria, which helps stop inflammatory process, and dry the skin. For treatment, the tablet must be dissolved in water and the liquid used for wiping. The solution is applied pointwise, directly to pimples.

Masks

  1. A face mask with honey promotes healthy skin. For 3-4 tablets, honey and water in the amount of 1 tsp are required. and 5 drops respectively. A paste is prepared from these components and applied for a quarter of an hour. The remaining product is washed off with warm water.
  2. A mask with acetylsalicylic acid for acne may also contain other ingredients, for example, black clay. The component is prepared in the amount of several tablespoons, diluted with water to obtain a homogeneous mass. Then the last and main ingredient is added - Acetylsalicylic acid in powder form (1 tablet per 1 tablespoon of clay). Cover the face with the prepared gruel for 20 minutes, then wash off with cool water.

If you decide to use acetylsalicylic acid to fight acne, do not forget that the courses should be short, otherwise you can dry out the skin. If you have dry skin, be careful when choosing this acne treatment method.

Acetylsalicylic acid is suitable for the face in cases where the skin is oily

Before using masks, make sure that the body's reaction to the effects of the components is normal. Otherwise there is a risk of irritation. When searching for a product with acetylsalicylic acid for acne, reviews will help you make the most correct choice.

Acetylsalicylic acid for hair

Aspirin has a beneficial effect on hair follicles. Preparation:

  • restores shine;
  • eliminates the consequences of unsuccessful staining;
  • Lightens undyed hair naturally;
  • increases volume;
  • accelerates the growth process;
  • neutralizes negative influence chlorine when visiting the pool;
  • eliminates electrification and alopecia.

However, not everyone can use aspirin for hair restoration and not always. You can’t make compresses and masks often. When used externally, the main component of the product penetrates well through tissue. Aspirin for hair can be used from the age of 12, since with earlier use there is high risk occurrence of Reye's syndrome. For those who have eczema, psoriasis or dry seborrhea, as well as those with sensitive skin care based on the use of acetylsalicylic acid is not suitable.

Easy to use: dissolve 2-3 tablets in warm water and add to any hair mask.

Carrying a child, lactation

During pregnancy, it is strictly forbidden to use Acetylsalicylic acid. A nursing mother should also not use the medicine. The medication is not prescribed to pregnant women due to the harmful substances it contains.

Aspirin and alcohol

It is important to know how to take medicine so as not to harm your body.

Are acetylsalicylic acid and alcohol compatible?

When used simultaneously, the mucous membranes are irritated. digestive tract, you can provoke the development of allergies, the appearance of ulcers and intragastric bleeding, the occurrence of a stroke, heart attack. Possible death.

You should take the medicine before drinking alcohol. Using it a day in advance will reduce the severity of your hangover.

Combination with caffeine

Caffeine can be used with the drug. However, there are contraindications, so you should consult your doctor.

Best before date

The shelf life of the medicine is 2 years. The product should be stored at room temperature in a place where light and moisture do not penetrate, children and animals do not have access.

What acetylsalicylic acid is, what it helps with and how to take it is indicated in the instructions for use. It is especially important to consult a doctor when treating children. For young patients, the drug can be very dangerous.

Systematic (IUPAC) name: 2-acetoxybenzoic acid
Legal status: Dispensed by pharmacist only (S2) (Australia); allowed for free sale (Great Britain); available without a prescription (USA).
In Australia the drug is Schedule 2, except for intravenous use (in which case the drug is Schedule 4), and is used in veterinary medicine (Schedule 5/6).
Application: most often orally, also rectally; Lysine acetylsalicylate can be used intravenously or intramuscularly
Bioavailability: 80–100%
Protein binding: 80–90%
Metabolism: hepatic, (CYP2C19 and possibly CYP3A), some hydrolyzed to salicylate in the esophageal wall.
Half-life: dose dependent; 2–3 hours when taking small doses, and up to 15–30 hours when taking large doses.
Excretion: urine (80–100%), sweat, saliva, feces
Synonyms: 2-acetoxybenzoic acid; acetylsalicylate;
acetylsalicylic acid; O-acetylsalicylic acid
Formula: C9H8O4
Mol. mass: 180.157 g/mol
Density: 1.40 g/cm³
Melting point: 136 °C (277 °F)
Boiling point: 140 °C (284 °F) (decomposes)
Solubility in water: 3 mg/ml (20 °C)
Aspirin (acetylsalicylic acid) is a salicylate drug used as an analgesic to relieve mild pain, and also as an antipyretic and anti-inflammatory agent. Aspirin is also an antiplatelet agent and inhibits the production of thromboxane, which normal conditions binds platelet molecules and creates a patch over damaged blood vessel walls. Because this patch can also grow and block blood flow, aspirin is also used to prevent heart attacks, stroke, and blood clots. Low-dose aspirin is used immediately after a heart attack to reduce the risk of another attack or death of heart tissue. Aspirin maybe effective means for prevention certain types cancer, especially colorectal cancer. The main side effects of aspirin are: stomach ulcers, stomach bleeding and tinnitus (especially when taken in large doses). Aspirin is not recommended for children and adolescents with flu-like symptoms or viral diseases due to the risk of developing Reye's syndrome. Aspirin is part of a group of drugs called nonsteroidal anti-inflammatory drugs (NSAIDs), but has a different mechanism of action than most other NSAIDs. Although aspirin and drugs with a similar structure act similarly to other NSAIDs (exhibiting antipyretic, anti-inflammatory, analgesic effects) and inhibit the same enzyme cyclooxygenase (COX), aspirin differs from them in that it acts irreversibly and, unlike other drugs, affects more COX-1 than COX-2.

The active component of aspirin was first discovered in willow bark in 1763 by Edward Stone of Wadham College, Oxford. The doctor discovered salicylic acid, the active metabolite of aspirin. Aspirin was first synthesized by Felix Hoffmann, a chemist at the German company Bayer, in 1897. Aspirin is one of the most widely used medicines in the world. Approximately 40,000 tons of aspirin are consumed worldwide each year. In those countries where aspirin is a registered trademark from Bayer, a generic version of acetylsalicylic acid is sold. The drug is on the list of essential medicines of the World Health Organization.

Use of aspirin in medicine

Aspirin is used to treat a range of symptoms, including fever, pain, rheumatic fever and inflammatory diseases such as rheumatoid arthritis, pericarditis and Kawasaki disease. In low doses, aspirin is used to reduce the risk of death from a heart attack or stroke. There is evidence that aspirin can be used to treat colorectal cancer, but the mechanism of its action in this case has not been proven.

Aspirin analgesic

Aspirin is an effective analgesic for treating acute pain, inferior, however, to ibuprofen, since the latter is associated with a lower risk of stomach bleeding. Aspirin is not effective for pain caused by muscle spasms, flatulence, bloating, or severely broken skin. As with other NSAIDs, the effectiveness of aspirin is increased when taken in combination with. Effervescent aspirin tablets, such as Alko-Seltzer or Blowfish, provide pain relief faster than regular tablets and are effective for treating migraines. Aspirin ointment is used to treat some types of neuropathic pain.

Aspirin and headache

Aspirin, alone or in combination formulas, is effective in treating some types of headaches. Aspirin may not be effective for treating secondary headaches (caused by other illnesses or injuries). The international classification of diseases associated with headaches distinguishes tension headaches among primary headaches. headache(the most common type of headache), migraine and cluster headaches. Tension headaches are treated with aspirin or other over-the-counter analgesics. Aspirin, especially as a component of the acetaminophen/aspirin/ formula (Excedrin Migraine), is considered an effective first-line treatment for migraine, and is comparable in effectiveness to low-dose sumatriptan. The drug is most effective in stopping migraines at their onset.

Aspirin and fever

Aspirin affects not only pain, but also fever through the prostaglandin system by irreversible inhibition COX. Although aspirin is widely approved for use in adults, multiple medical societies and regulatory agencies (including the American Academy of Family Physicians, the American Academy of Pediatricians, and the FDA) do not recommend the use of aspirin as a fever reducer in children. Aspirin may be associated with a risk of Reye's syndrome, a rare but often fatal condition associated with the use of aspirin or other salicylates in children due to a viral or bacterial infection. In 1986, the FDA required manufacturers to place a warning on all aspirin labels about the risks of using aspirin in children and adolescents.

Aspirin and heart attacks

The first research into the effects of aspirin on the heart and heart attacks was carried out in the early 1970s by Professor Peter Slate, emeritus professor of heart medicine at Oxford University, who formed the Aspirin Research Society. In some cases, aspirin may be used to prevent heart attacks. At lower doses, aspirin is effective in preventing the development of existing cardiovascular diseases, as well as in reducing the risk of developing these diseases in people with a history of such diseases. Aspirin is less effective for people at low risk of a heart attack, such as people who have never had a heart attack. similar diseases in the past. Some studies recommend taking aspirin on a chronic basis, while others discourage such use due to side effects such as stomach bleeding, which usually outweigh any potential benefit of the drug. When using aspirin for preventive purposes, the phenomenon of aspirin resistance may occur, manifested in a decrease in the effectiveness of the drug, which may lead to an increased risk of heart attack. Some authors suggest testing for resistance to aspirin or other antithrombotic drugs before starting treatment. Aspirin has also been proposed as a drug component for the treatment of cardiovascular diseases.

Post-surgical treatment

The US Agency for Healthcare Research and Quality Guidelines recommends long-term use of aspirin after a percutaneous coronary intervention procedure, such as coronary artery stent placement. Often, aspirin is combined with adenosine diphosphate receptor inhibitors, such as clopidogrel, prasugrel, or ticagrelol, to prevent blood clotting (dual antiplatelet therapy). Recommendations for the use of aspirin in the United States and Europe differ somewhat regarding how long and for what indications this combination therapy should be administered after surgery. In the United States, dual antiplatelet therapy is recommended for a minimum of 12 months, and in Europe for 6–12 months after drug-eluting stent use. However, recommendations in both countries are consistent regarding the indefinite use of aspirin after completion of antiplatelet therapy.

Aspirin and cancer prevention

The effects of aspirin on cancer, especially colon cancer, have been widely studied. Numerous meta-analyses and reviews indicate that chronic use of aspirin reduces the long-term risk of colon cancer and mortality. However, no relationship was found between aspirin dose, duration of use, and various risk measures, including mortality, disease progression, and disease risk. Although most of the data regarding aspirin and colorectal cancer risk comes from observational studies rather than randomized controlled trials, available randomized trial data suggest that long-term use of low-dose aspirin may be effective in preventing some types of colorectal cancer. In 2007, the US Preventive Services Agency issued a policy statement on the issue, giving the use of aspirin for the prevention of colon cancer a "D" rating. The service also does not recommend that doctors use aspirin for these purposes.

Other uses of aspirin

Aspirin is used as first-line therapy for symptoms of fever and joint pain in acute rheumatic fever. Treatment often lasts for one to two weeks, and the drug is rarely prescribed for long periods of time. After getting rid of fever and pain, there is no need to take aspirin, but the drug does not reduce the risk of cardiac complications and residual rheumatic disease hearts. Naproxen has equal efficacy to aspirin and is less toxic, however, due to limited clinical data, naproxen is recommended only as second-line treatment. In children, aspirin is recommended only for Kawasaki disease and rheumatic fever, due to a lack of high-quality data on its effectiveness. At low doses, aspirin shows moderate effectiveness in preventing preeclampsia.

Aspirin resistance

In some people, aspirin is not as effective on platelets as in others. This effect is called “aspirin resistance,” or insensitivity. One study found that women are more likely to become resistant than men. An aggregation study involving 2930 patients showed that 28% of patients developed aspirin resistance. A study of 100 Italian patients showed that, on the other hand, of the 31% of patients resistant to aspirin, only 5% had actual resistance, and the rest were non-compliant (non-compliance with drug intake). Another study of 400 healthy volunteers found that none of the patients had true resistance, but some had "pseudo-resistance reflecting delayed or reduced absorption of the drug."

Aspirin dosage

Adult aspirin tablets come in standard strengths that vary slightly from country to country, for example 300 mg in the UK and 325 mg in the US. Reduced dosages are also related to existing standards, for example, 75 mg and 81 mg. Tablets of 81 mg are conventionally called the “child dose,” although they are not recommended for use in children. The difference between 75 and 81 mg tablets is not significant medical value. Interestingly, in the US, 325 mg tablets are equivalent to 5 grains of aspirin used before metric system used today. In general, to treat fever or arthritis, adults are recommended to take aspirin 4 times a day. To treat rheumatic fever, doses close to the maximum have historically been used. For the prevention of rheumatoid arthritis in persons with existing or suspected coronary artery disease, lower doses once daily are recommended. The US Preventive Services recommends the use of aspirin for primary prevention coronary diseases hearts in men aged 45–79 years and women aged 55–79 years, only if potential positive effects(reducing the risk of myocardial infarction in men or stroke in women) exceed the potential risk of gastric damage. The Women's Health Initiative study demonstrated that regular use of low-dose aspirin (75 or 81 mg) in women reduced the risk of death from cardiovascular disease by 25% and the risk of death from other causes by 14%. Use of low-dose aspirin is also associated with a reduced risk of cardiovascular disease, and doses of 75 or 81 mg/day may optimize efficacy and safety in patients taking aspirin for long-term prevention. In children with Kawasaki disease, the dose of aspirin is based on body weight. The drug is started with four times a day for a maximum of four weeks, and then, over the next 6-8 weeks, the drug is taken at a lower dose once a day.

Side effects of aspirin

Contraindications

Aspirin is not recommended for individuals with an allergy to ibuprofen or naproxen or for individuals with salicylate intolerance or more general intolerance to NSAIDs. Caution should be exercised by persons suffering from asthma or bronchospasms caused by taking NSAIDs. Because aspirin affects the stomach lining, manufacturers recommend that patients with stomach ulcers, diabetes, or gastritis consult a doctor before using aspirin. Even in the absence of the above conditions, the risk of stomach bleeding increases when taking aspirin and alcohol together. Patients with hemophilia or other bleeding disorders are not recommended to take aspirin or other salicylates. Aspirin may cause hemolytic anemia in persons with genetic disease deficiency of glucose-6-phosphate dehydrogenase, especially in high doses and depending on the severity of the disease. The use of aspirin for dengue fever is not recommended due to the increased risk of bleeding. Aspirin is also not recommended for those with kidney disease, hyperuricemia, or gout because aspirin inhibits the kidneys' ability to excrete uric acid and thus may aggravate these conditions. Aspirin is not recommended for children and adolescents to treat flu and cold symptoms because such use may be associated with the development of Reye's syndrome.

Gastrointestinal tract

Aspirin has been shown to increase the risk of stomach bleeding. Even though enteric-coated aspirin tablets are available and marketed as “gentle on the stomach,” one study found that even this did not help reduce the harmful effects of aspirin on the stomach. When aspirin is combined with other NSAIDs, the risk also increases. When using aspirin in combination with clopidogrel or clopidogrel, the risk of stomach bleeding also increases. Aspirin blockade of COX-1 causes defensive reaction in the form of an increase in COX-2. The use of COX-2 inhibitors and aspirin leads to increased erosion of the gastric mucosa. Therefore, caution should be exercised when combining aspirin with any natural supplements that inhibit COX-2, such as garlic extracts, curcumin, blueberry, pine bark, ginkgo, fish oil, genistein, quercetin, resorcinol and others. To reduce the harmful effects of aspirin on the stomach, in addition to the use of enteric coatings, manufacturing companies use a “buffer” method. "Buffering" agents serve to prevent aspirin from accumulating on the stomach wall, but the effectiveness of such drugs is disputed. Almost any agent used in antacids is used as “buffers”. Bufferin, for example, uses MgO. Other preparations use CaCO3. Recently, vitamin C was added to protect the stomach when taking aspirin. When taken together, there is a decrease in the amount of damage compared to using aspirin alone.

Central effects of aspirin

In experiments on rats, large doses of salicylate, a metabolite of aspirin, have been shown to cause temporary tinnitus. This occurs as a result of effects on arachidonic acid and the NMDA receptor cascade.

Aspirin and Reye's syndrome

Reye's syndrome, rare but very dangerous disease, characterized by acute encephalopathy and fatty liver, and occurs when children and adolescents take aspirin to reduce fever or treat other symptoms. From 1981 to 1997, there were 1,207 cases of Reye's syndrome in patients under 18 years of age in the United States. In 93% of cases, patients felt unwell three weeks before developing Reye's syndrome, and most often complained of respiratory infections, chicken pox or diarrhea. Salicylates were found in the body of 81.9% of children. After the link between Reye's syndrome and aspirin use was proven and safety measures were implemented (including a statement from the Surgeon General and packaging changes), aspirin use among children in the United States fell sharply, resulting in a decrease in the incidence of Reye's syndrome; a similar situation was observed in Great Britain. The US FDA does not recommend that children under 12 years of age take aspirin or aspirin-containing products if they have fever symptoms. UK regulatory agency medical supplies And medicines does not recommend taking aspirin to children under 16 years of age without a doctor's prescription.

Allergic reactions to aspirin

In some people, aspirin may cause allergy-like symptoms, including red and swollen skin and headache. This reaction is caused by salicylate intolerance and is not an allergy in the strict sense of the word, but rather an inability to metabolize even small amounts of aspirin, which can quickly lead to an overdose.

Other side effects of aspirin

In some people, aspirin can cause angioedema (swelling of skin tissue). One study showed that some patients develop angioedema 1 to 6 hours after taking aspirin. However, angioedema developed only when taking aspirin in combination with other NSAIDs. Aspirin causes an increased risk of cerebral microbleeds, which are shown on MRI as dark spots diameter 5-10 mm or less. This bleeding may be the first sign ischemic stroke or hemorrhagic stroke, Binswanger's disease and Alzheimer's disease. Study of a group of patients taking average dose aspirin 270 mg per day showed a mean absolute increase in the risk of hemorrhagic stroke of 12 cases per 10,000 people. In comparison, the absolute risk reduction for myocardial infarction was 137 per 10,000 people, and the absolute risk reduction for ischemic stroke was 39 per 10,000 people. In cases of pre-existing hemorrhagic stroke, aspirin use increases the risk of mortality, with doses of approximately 250 mg per day associated with a reduced risk of mortality within three months after hemorrhagic stroke. Aspirin and other NSAIDs may cause hyperkalemia by inhibiting prostaglandin synthesis; however, these drugs do not tend to cause hyperkalemia provided that hepatic function is normal. Aspirin can increase postoperative bleeding for up to 10 days. One study found that 30 of 6499 elective surgery patients required reoperation due to bleeding. 20 patients had diffuse bleeding, and 10 had local bleeding. In 19 of 20 patients, diffuse bleeding was associated with preoperative use of aspirin alone or in combination with other NSAIDs.

Aspirin overdose

Aspirin overdose can be acute or chronic. Acute overdose is associated with a single dose of aspirin. Chronic overdose is associated with prolonged use of doses above the recommended norm. Acute overdose is associated with a 2% risk of mortality. Chronic overdose is more dangerous and more likely to have death(in 25% of cases); Chronic overdose is especially dangerous in children. In case of poisoning apply various means, including activated carbon, sodium dicarbonate, intravenous dextrose and salt, and dialysis. To make a diagnosis of poisoning, measurements of salicylate, the active metabolite of aspirin, in plasma are used using automated spectrophotometric methods. Salicylate plasma levels are 30–100 mg/L at the usual dose, 50–300 mg/L at high doses, and 700–1400 mg/L at acute overdose. Salicylate is also produced by the use of bismuth subsalicylate, methyl salicylate and sodium salicylate.

Interactions of aspirin with other drugs

Aspirin may interact with other drugs. For example, azetazolamide and ammonium chloride increase the harmful effects of salicylates, while alcohol increases gastric bleeding when taking aspirin. Aspirin may displace some drugs from protein binding sites, including the antidiabetic drugs tolbutamil and chlorpropamide, methotrexate, phenytoin, probenecid, valproic acid (by interfering with beta oxidation, important part valproate metabolism), and other NSAIDs. Corticosteroids may also decrease aspirin concentrations. Ibuprofen may reduce the antiplatelet effects of aspirin, which is used to protect the heart and prevent stroke. Aspirin may reduce pharmacological activity spironolactone. Aspirin competes with pinicillin G for renal tubular secretion. Aspirin may also inhibit the absorption of vitamin C.

Chemical characteristics of aspirin

Aspirin breaks down quickly in solutions of ammonium acetate or alkali metal acetates, carbonates, citrates or hydroxides. It is stable in dry form, but undergoes significant hydrolysis upon contact with acetyl or salicylic acid. In reaction with an alkali, hydrolysis occurs rapidly, and the resulting pure solutions may consist entirely of acetate or salicylate.

Physical characteristics of aspirin

Aspirin, an acetyl derivative of salicylic acid, is a white, crystalline, slightly acidic compound with a melting point of 136 °C (277 °F), and a boiling point of 140 °C (284 °F). The substance's acid dissociation constant (pKa) is 25 °C (77 °F).

Aspirin synthesis

Aspirin synthesis is classified as an esterification reaction. Salicylic acid is treated with acetyl anhydride, an acid derivative, causing a chemical reaction that converts the hydroxy group of salicylic acid into an ester group (R-OH → R-OCOCH3). As a result, aspirin and acetyl acid are formed, which is considered by-product this reaction. Small amounts of sulfuric acid (and sometimes phosphoric acid) are usually used as catalysts.

Mechanism of action of aspirin

Discovery of the mechanism of action of aspirin

In 1971, British pharmacologist John Robert Vane, who was subsequently accepted to the Royal College of Surgeons in London, demonstrated that aspirin inhibits the production of prostaglandins and thromboxanes. For this discovery, the scientist was awarded the 1982 Nobel Prize in Medicine, jointly with Sune Bergström and Bengt Samuelsson. In 1984 he was awarded the title of Knight Bachelor.

Suppression of prostaglandins and thromboxanes

Aspirin's ability to inhibit the production of prostaglandins and thromboxanes is due to its irreversible inactivation of the enzyme cyclooxygenase (COX; formal name prostaglandin endoperoxide synthase), associated with the synthesis of prostaglandin and thromboxane. Aspirin acts as an acetylating agent by covalently attaching an acetyl group to the active site residue of the COX enzyme. This is the main difference between aspirin and other NSAIDs (such as diclofenac and ibuprofen), which are reversible inhibitors. Low-dose aspirin irreversibly blocks the formation of thromboxane A2 in platelets, exerting an inhibitory effect on platelet aggregation during their life cycle(8–9 days). Due to this antithrombotic effect, aspirin is used to reduce the risk of heart attack. Aspirin 40 mg daily can inhibit a large percentage of maximal thromboxane A2 release, with little effect on prostaglandin I2 synthesis; however, high doses of aspirin may enhance inhibition. Prostaglandins, local hormones produced in the body, exhibit various effects, including influencing the transmission of pain signals to the brain, modulation of the hypothalamic thermostat and inflammation. Thromboxanes are responsible for the aggregation of platelets, which form blood clots. The main cause of heart attack is blood clotting, and low-dose aspirin is recognized as an effective means of preventing acute myocardial infarction. An undesirable side effect of aspirin's antithrombotic effects is that it can cause excessive bleeding.

Inhibition of COX-1 and COX-2

There are at least two types of cyclooxygenase: COX-1 and COX-2. Aspirin irreversibly inhibits COX-1 and modifies the enzyme activity of COX-2. COX-2 typically produces prostanoids, most of which are proinflammatory. Aspirin-modified PTGS2 produces lipoxins, most of which are anti-inflammatory. New generation NSAIDs, COX-2 inhibitors, have been developed to inhibit PTGS2 alone and reduce the risk of gastrointestinal side effects. However, more recently, newer generation COX-2 inhibitors such as rofecoxib (Vioxx) were withdrawn from the market following evidence that PTGS2 inhibitors increased the risk of heart attack. Endothelial cells express PTGS2, and, by selectively inhibiting PTGS2, reduce prostaglandin production (namely, PGI2; prostacyclin), depending on thromboxane levels. Thus, the protective anticoagulant effect of PGI2 is reduced and the risk of blood clots and heart attacks increases. Because platelets do not have DNA, they cannot synthesize new PTGS. Aspirin irreversibly inhibits the enzyme, which is its most important difference from reversible inhibitors.

Additional mechanisms of action of aspirin

Aspirin has at least three additional mechanisms of action. It blocks oxidative phosphorylation in cartilage (and kidney) mitochondria by diffusion from the proton transport site of the inner membrane back into the mitochondria where it is re-ionized to release protons. In short, aspirin buffers and transports protons. When taken in large doses, aspirin can cause fever due to a temperature surge from the electron transport chain. In addition, aspirin promotes the formation of NO radicals in the body, which has been shown in experiments on mice to be an independent mechanism for reducing inflammation. Aspirin reduces the adhesion of leukocytes, which is important mechanism immune defense from infections; however, these data do not provide conclusive evidence that aspirin is effective against infections. Newer evidence also shows that salicylic acid and its derivatives modulate signaling through NF-κB. NF-κB, a transcription factor complex, plays an important role in many biological processes, including inflammation. In the body, aspirin quickly breaks down into salicylic acid, which itself has anti-inflammatory, anti-temperature and analgesic effects. In 2012, salicylic acid was shown to activate AMP-activated protein kinase, which may be a possible explanation for some of the effects of salicylic acid and aspirin. The acetyl in the aspirin molecule also has a special effect on the body. Acetylation of cellular proteins is an important phenomenon that affects the regulation of protein function at the post-translational level. Recent studies show that aspirin can acetylate more than just COX isoenzymes. These acetylation reactions may explain many of the hitherto unexplained effects of aspirin.

Hypothalamic-pituitary-adrenal activity

Aspirin, like other drugs that affect prostaglandin synthesis, has potent effects on the pituitary gland and indirectly affects certain hormones and physiological functions. The effects of aspirin on growth hormone, prolactin, and thyroid-stimulating hormone (with relative effects on T3 and T4) have been directly demonstrated. Aspirin reduces the effect of vasopressin and increases the effect of naloxone by secreting adrenocorticotropic hormone and cortisol in the hypothalamic-pituitary-adrenal axis, which occurs through interaction with endogenous prostaglandins.

Pharmacokinetics of aspirin

Salicylic acid is a weak acid and very little of it ionizes in the stomach after oral administration. Acetylsalicylic acid is slightly soluble in acidic environment stomach, due to which its absorption may be delayed by 8-24 hours when taken in high doses. Increased pH and larger coverage area small intestine promotes rapid absorption of aspirin in this area, which, in turn, promotes greater dissolution of salicylate. However, in overdose, aspirin dissolves much more slowly, and its plasma concentrations may increase within 24 hours after administration. About 50–80% of salicylate in the blood is bound to protein, with the remainder remaining in an active ionized form; protein binding is concentration dependent. Saturation of binding sites leads to an increase in the amount of free salicylate and increased toxicity. The volume of distribution is 0.1–0.2 l/kg. Acidosis increases the volume of distribution due to increased cellular penetration of salicylates. 80% of the therapeutic dose of salicylic acid is metabolized in the liver. When bound to, salicyluric acid is formed, and when bound to glucuronic acid, salicylic acid and phenolic glucuronide are formed. These metabolic pathways only have limited opportunities. A small amount of salicylic acid is also hydrolyzed to gentisic acid. When large doses of salicylate are administered, the kinetics shift from first to zero order as metabolic pathways become saturated and the importance of renal excretion increases. Salicylates are excreted from the body by the kidneys in the form of salicyluric acid (75%), free salicylic acid (10%), salicylic phenol (10%) and acyl glucuronides (5%), gentisic acid (< 1%) и 2,3-дигидроксибензойной кислоты. При приеме небольших доз (меньше 250 мг у взрослых), все пути проходят кинетику первого порядка, при этом период полувыведения составляет от 2.0 до 4.5 часов. При приеме больших доз салицилата (больше 4 г), период полураспада увеличивается (15–30 часов), поскольку биотрансформация включает в себя образование салицилуровой кислоты и насыщение салицил фенольного глюкоронида. При увеличении pH мочи с 5 до 8 наблюдается увеличение почечного клиренса в 10-20 раз.

History of the discovery of aspirin

Herbal extracts including willow bark and meadowsweet (spirea), whose active ingredient is salicylic acid, have been used since ancient times to relieve headaches, pain and fever. The father of modern medicine, Hippocrates (460 – 377 BC), described the use of powdered willow bark and leaves to relieve such symptoms. French chemist Charles Frederic Gerhard first prepared acetylsalicylic acid in 1853. While working on the synthesis and properties of various acid anhydrides, he mixed acetyl chloride with the sodium salt of salicylic acid (sodium salicylate). A powerful reaction followed, and the resulting alloy was codified. Gerhard named this compound "salicylic acetyl anhydride" (wasserfreie Salicylsäure-Essigsäure). 6 years later, in 1859, von Gilm obtained analytically pure acetylsalicylic acid (which he called acetylierte Salicylsäure, acetylated salicylic acid) by reacting salicylic acid and acetyl chloride. In 1869, Schroeder, Prinzorn and Kraut repeated the experiments of Gerhard and von Hielm and reported that both reactions lead to the synthesis of the same substance - acetylsalicylic acid. They were the first to describe the correct structure of the substance (in which the acetyl group is attached to the phenolic oxygen). In 1897, chemists at Bayer AG produced a synthetically modified version of salicin, extracted from the plant Filipendula ulmaria (meadowsweet), which causes less stomach irritation than pure salicylic acid. It is still not clear who the main chemist who conceived this project was. Bayer reported that the work was carried out by Felix Hoffmann, but Jewish chemist Arthur Eichengrun later stated that he was the main developer and that records of his contributions were destroyed during the Nazi regime. New drug, formally acetylsalicylic acid, was named "Aspirin" by Bayer AG, after the old botanical name of the plant it contains (meadowsweet), Spiraea ulmaria. The word "Aspirin" is a derivative of the words "acetyl" and "Spirsäure", an old German word for salicylic acid, which in turn comes from the Latin "Spiraea ulmaria". By 1899, Bayer was already selling aspirin throughout the world. Aspirin's popularity increased in the first half of the 20th century due to its supposed effectiveness in treating epidemics. spanish flu 1918. Recent research, however, suggests that the 1918 flu death toll was partly caused by aspirin, but this claim is controversial and not widely accepted in scientific circles. The popularity of aspirin led to intense competition and division of aspirin brands, especially after Bayer's American patent expired in 1917. Since its introduction to the market (acetaminophen) in 1956 and ibuprofen in 1969, aspirin's popularity has waned somewhat. In the 1960s and 1970s, John Wayne and his team discovered the underlying mechanisms of action of aspirin, and clinical trials and other studies conducted between 1960 and 1980 demonstrated that aspirin is an effective drug against blood clots. In the last decades of the 20th century, sales of aspirin increased again, and remain at a fairly high level to this day.

Aspirin brand

As part of the 1919 Treaty of Versailles reparations following Germany's defeat in World War I, aspirin (as well as heroin) lost their registered trademark status in France, Russia, the UK and the US, where they became generics. Today, aspirin is considered generic in Australia, France, India, Ireland, New Zealand, Pakistan, Jamaica, Colombia, the Philippines, South Africa, UK and USA. Aspirin, with a capital "A", remains a registered trademark of Bayer in Germany, Canada, Mexico and more than 80 other countries where trademark is the property of Bayer.

Use of aspirin in veterinary medicine

Aspirin is sometimes used for pain relief or as an anticoagulant in veterinary medicine, primarily in dogs and occasionally in horses, although newer medications are now being used with fewer side effects. Dogs and horses exhibit gastrointestinal side effects of aspirin associated with salicylates, but aspirin is often used to treat arthritis in older dogs. Aspirin has demonstrated effectiveness for laminitis (inflammation of the hoof) in horses, but is no longer used for this purpose. Aspirin should only be used in animals under close medical supervision; In particular, cats lack the glucuronide conjugates that promote aspirin excretion, making even small doses potentially toxic to them.

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Medicine based on gender. A couple of years ago, scientists began to examine the studies that had already been conducted. We took 23 tests relating to acetylsalicylic acid. It is popularly known as “Aspirin”.

The studies involved 113,000 people. Scientists set out to find out the dependence of test results on the ratio of men and women in groups of subjects.

It turned out that the effectiveness of the action was higher in male teams. Why? For now, it's a mystery. Let's talk about what acetylsalicylic acid understandable. Let's start with the studied properties of the substance.

Properties of acetylsalicylic acid

Acetylsalicylic acid formula– C 9 H 8 O 4 . The second name of the substance is 2-hydroxybenzoic. The prefix “hydroxy” is given for the presence of hydroxyl OH. , to which it is attached, is the simplest in the class.

Structural formula of acetylsalicylic acid

They have carboxyl groups COOH. In benzoin, like acetylsalicylic acid, there is only one. This is a prerequisite not only for simple ones, but also for fatty ones. For the latter there is one more condition - an open circuit.

This is exactly what the heroine of the article has. In esterified form, that is, the form of ether, fatty acids are present in fats. Acetylsalicylic compound is no exception.

Knowing that acetylsalicylic acid is "Aspirin" It’s easy to guess what she looks like. The substance is crystalline, colorless. It is also known that the compound dissociates in water. The heroine also dissolves easily in ethanol and diester.

The heroine of the article is also identified by its melting point. It is 156 degrees. The substance boils at 211 Celsius. The reaction for determining acetylsalicylic acid takes place in its solution. If chloride is added, the liquid becomes colored.

The heroine of the article may precipitate from solutions. This occurs when the environment becomes acidic. It is at this moment that it is convenient to determine the compound by its melting point, because the experiment requires a crystalline temperature.

By the way, the form is also an identifier for acetylsalicylic acid. Its units are monoclinic, that is, they are built on 3 vectors. They have different lengths. There are 2 right angles between the vectors and one that is not.

Crystals are stable only in dry air. In a humid environment, the powder absorbs water. In this case, two are formed - and salicylic. The first one has a familiar smell.

When he appears, you can understand that the heroine of the article began to fall apart. Chemists call the process hydrolysis. Acetylsalicylic acid itself has almost no smell.

The acetylsalicylic compound is amenable to esterification. This is what chemists call the formation of esters. To form them, they are exposed to alkaline bicarbonates and hydroxides.

The reaction starts in boiling water. By the way, the solubility of aspirin in it depends on the Ph of the liquid. The heroine of the article disintegrates best in alkaline water.

Preparation of acetylsalicylic acid

"Aspirin" is produced by carboxylation of the phenolate. It is taken dry. The phenolate is affected by carbon dioxide. The method is called "Kolbe-Schmitt". It is necessary to withstand a pressure of 0.6 megapascals and a temperature of 185 degrees Celsius. Under these conditions, the reaction proceeds from 8 to 10.

Chemical formula acetylsalicylic acid

An alternative method for the industrial synthesis of the heroine of the article is the oxidation of o-cresol, that is, crude carbolic acid. They act on it with oxide. The reaction occurs when heated. Sometimes, pre-sulfonated cresol is oxidized. In this case, the yield of acetylsalicylic acid increases.

Application of acetylsalicylic acid

“And a painful sip of aspirin gives you ease of spirit, the good benefits of illness and courage, an unkind chill.” These lines are from a poem by Bella Akhmadulina.

The Silver Age poet included them in “Introduction to the Cold.” We conclude: acetylsalicylic acid has been used in pharmacology for about a century and has been significant from the very beginning.

Aspirin has been proven to block the production of prostaglandins. These are lipids. They are formed in the body enzymatically from fatty acids. Prostaglandins lower blood pressure.

The second action is stimulation of myometrial contractions. This is a layer of cells lining the uterus. We conclude What does acetylsalicylic acid help with?, - from premature labor.

Acetylsalicylic acid is used for colds and headaches

Obstetricians-gynecologists prescribe a quarter of Aspirin to women with a threat of miscarriage or uterine hypertonicity. But, acetylsalicylic acid is known to the general public as an antipyretic.

In this capacity, the drug is approved from the age of 12. In adolescents and adults, the medicine not only reduces fever, but also relieves pain. Respectively, acetylsalicylic acid instructions for use contains a recommended remedy for menstrual cramps, headaches, and aching sensations in the oral cavity.

Aspirin also relieves pain in muscles and joints. Note that Aspirin is available in several forms. Their action varies. Effervescent tablets, for example, are used exclusively for migraines and other pain in the area.

Acetylsalicylic acid is recommended and for a number of cancer diseases, as well as in the role of their prevention. Patients regularly taking aspirin are less likely to be diagnosed with malignant tumors bladder, prostate gland, esophagus.

Aspirin is not included in anticancer drugs. While doctors cannot explain the mechanism of action of the drug, they do not exclude a random factor in the statistics.

At the beginning of the article, we talked about another phenomenon not explained by scientists. We are talking about the different effectiveness of acetylsalicylic acid in relation to the bodies of men and women. There is an exception to the rule.

The heroine of the article blocks Alzheimer's disease mainly in the fairer sex. In theory, the effect of the drug should be the same for everyone. Aspirin thins.

Accordingly, the difficult blood supply to the brain improves. This is the main help in the fight against an illness that takes away memory. Why the method does not work for men with Alzheimer's remains a mystery.

Outside of pharmacology, acetylsalicylic acid is used in everyday life and agriculture. The recommendation is passed on from mouth to mouth to dissolve an Aspirin tablet in a vase of cut flowers.

IN medicinal solution, as in water with potassium permanganate, plants remain fresh longer. In the fields, acid is used to combat fungal infections of the soil. Problematic beds are shed with Aspirin solution at the rate of one tablet per liter of water.

Motorists use the heroine of the article when starting their cars. Aspirin tablets help with dead batteries. The drug reacts with the electrolyte, giving a short-term charge.

The method is relevant for an unexpectedly dead device. Usually, it malfunctions in cold weather. Aspirin, of course, is not suitable as a permanent battery starter.

Housewives know the heroine of the article as a means to remove sweat stains. They remain whitish streaks on clothes. Soaking in a solution for 2 hours helps remove them. acetylsalicylic acid. Price stain remover from the store is many times more expensive. Take 4 Aspirin tablets per glass of water.

The anti-inflammatory effect of Aspirin has made it an acne fighter. used in paste form. The tablets are crushed and mixed with water.

The paste is applied pointwise to inflammation. The drug dries out the lesions and relieves redness. 2-3 minutes is enough. Afterwards, the ointment is washed off with warm, soapy water.

Acetylsalicylic acid for face can also act as an exfoliating agent. True, given the tenderness of the skin on the forehead, cheeks, and near the eyes, the heroine of the article is more often used for the heels.

Acetylsalicylic acid for acne

There the corrosive effect is in place, fights corns. Crushed Aspirin tablets are mixed with juice. Take 5 tablets per teaspoon. You will also need a couple of drops of water.

The mixture is smeared onto rough areas and wrapped with cloth napkins. Afterwards, the feet are wrapped in polyethylene. Remove it after 10-15 minutes. All that remains is to follow in the footsteps of pumice. It will easily remove softened tissue.

Acetylsalicylic acid for children and is useful for adults against bee stings. Skin puncture sites are moistened clean water and rub with an Aspirin tablet. You can also rub the hero of the article on your hair.

The product is useful for those who have been painted and have been in contact with bleach. A typical situation for those who go to the pool. Dilute 6 Aspirin tablets into a glass of water, wipe the curls, and after 15 minutes wash off with shampoo.

Dyed hair does not lose color and there is no porosity to speak of. So, acetylsalicylic acid from temperature- just the tip of the iceberg of its application.

The benefits and harms of acetylsalicylic acid

Is it possible to take acetylsalicylic acid? take without a doctor's prescription? It is not allowed inside, and it is not advisable to go outside. Aspirin is still an acid. Having a corrosive effect on the skin, the substance does the same to the mucous membranes. Accordingly, long-term intake of acetylsalicylic compounds orally can lead to gastritis and stomach ulcers.

The irritating effect of the heroine of the article on the stomach is called acedosis. Monitoring by a gastroenterologist is recommended. Internal bleeding may occur.

If you need to constantly take Aspirin, following the instructions will help minimize the risks. The tablets are washed down with a small amount of water and, most importantly, taken with meals.

Acetylsalicylic acid is contraindicated for children under 12 years of age due to the risk of Reye's syndrome. It is also called white liver disease. The disease is rare, but deadly, and occurs specifically in children and adolescents.

The syndrome develops during treatment of febrile illnesses such as acute respiratory viral infections, measles or chickenpox. Not only the liver is affected, but also the brain. Moreover, Reye occurs exclusively in parallel with treatment with Aspirin.

An overdose of acetylsalicylic acid in adults sometimes leads to deafness, skin rashes, and prolonged bleeding from wounds. Actually, circulatory disorders are not only the result of the use of the heroine of the article, but also a contraindication to its use, like hypertension, asthma, chronic diseases liver.

However, in uncontrolled doses everything can be fatal. The newspaper “ZOZH”, for example, describes the death of a man who drank 2 liters daily carrot juice. What is considered an elixir became the reason only because of the volume of alcohol consumed and the consistency of intake.

Aspirin (acetylsalicylic acid) is one of the most famous remedies for fever. But the use of this medicine is more extensive - it even helps against thrombosis and other cardiovascular diseases.

Acetylsalicylic acid - description

Acetyl (acetylsalicylic) acid- substance of the NSAID group, ether acetic acid salicylic. The drug is included in the list of vitally important drugs, has long been known, and has been well studied. He renders a number positive action on the body, of which the most important are antiplatelet, antipyretic, and analgesic. The drug was first patented by Bayer under the brand name Aspirin.

The acid was isolated in 1838 white willow bark- a well-known folk remedy for fever and headache. Initially it was used to treat rheumatism, then gout. Since 1904, the medicine has been sold in tablet form (initially it existed in powder form). Tablets of 0.1, 0.25, 0.5 g are round in shape, with a horizontal stripe in the middle.

Additional components:

The drug is produced by almost all well-known pharmacological companies, for example, Dalkhimfarm, Tatkhimfarmpreparaty, Novasil.

Effect on the body

This drug works as follows - it suppresses the synthesis of prostaglandins and inhibits the production of thromboxanes. The substance acts by inhibiting cyclooxygenase, and this enzyme takes part in the creation prostaglandins(inflammatory mediators) and thromboxanes. Acetylsalicylic acid affects the inflammatory process that occurs in tissues. Also medicine:

  • reduces capillary permeability;
  • reduces hyaluronidase activity;
  • limits the formation of ATP, preventing energy from being provided to inflammatory phenomena.

The drug for internal reception reduces fever - normalizes temperature, which is due to its effect on the thermoregulation centers of the hypothalamus.

The acid also has an analgesic effect by reducing the production of bradycardin and influencing pain centers.

The most important ability of Aspirin is that it thins the blood - therefore the drug is widely used against the formation of blood clots.

All of these mechanisms of action provide the drug with analgesic, antipyretic, anti-inflammatory, antifever, and antirheumatic effects. Acid also reduces intracranial pressure and reduces headaches.

Indications for use

You can take the medicine for completely different pathologies belonging to different areas of medicine. The best known treatment with Aspirin is for acute conditions accompanied by pain, fever, and inflammation:


Acetyl acid also helps against pericarditis - inflammation in the serous lining of the heart, with Dressler's syndrome(when pericarditis develops in combination with pneumonia, pleurisy). To thin the blood, Aspirin is indicated for many people over 55 who are at risk of heart attack or stroke. It should also be taken in long courses for ischemic heart disease, a stroke or a heart attack that has already occurred.

Other possible indications conditions for which Aspirin should be given:

  • prevention of thromboembolism;
  • heart defects;
  • atrial fibrillation;
  • acute thrombophlebitis;
  • pulmonary infarction;
  • TELA.

Using small doses of medication, tolerance to NSAIDs is formed in the presence of the “aspirin triad” (nasal polyposis, bronchial asthma, allergy to acetyl acid).

Instructions for use

According to the instructions, acetyl acid should be taken orally, at the very beginning of a meal, or at the end of a meal. This will help prevent widespread side effect- the appearance of erosions, irritations on the wall of the stomach and small intestine.

Experts advise drinking Aspirin with milk or alkaline mineral water without gas - this will reduce the irritating effect of acid on the digestive system.

The dosage varies, depending on age and type of disease. Usually enough to drink 0.5 g 2-4 times/day(quantity indicated is for adults). Course duration is up to 12 days, more often - 3-5 days.

Features of therapy in in some cases are:

  1. To prevent problems of the heart and blood vessels, dangerous thrombosis. Take half a tablet in the morning (once a day). The course is up to 2 months without a break. At the same time, blood clotting and platelet count tests are done every 2 weeks.
  2. For rheumatism. Take Aspirin 5-8 g/day for adults, children 100 mg per kg of weight/day. The indicated dose is divided into 5 doses. After a week of such pulse therapy, the dosage is reduced individually, the total duration is 6 weeks. Cancellation is carried out gradually.
  3. For headaches. An adult can take 2 tablets, a child - 10 mg/kg body weight per dose.
  4. Children from 5 years old are usually given 0.25 g of Aspirin per dose, from 2 years old - 0.1 g, from 1 year old - 0.05 g.

The drug is widely used in cosmetology. For example, there is a recipe for a face mask against acne. You need to grind 6 tablets, add lemon juice or honey to a paste. Apply only to inflamed areas of the skin, leave for 15 minutes, rinse.

Side effects and prohibitions

It is strictly forbidden to give acetyl acid to children if they develop a viral infection. In this case, the risk of Reye's syndrome is high, since the drug acts on the structures of the liver and brain that are attacked by the virus. There are other contraindications to therapy:


In many cases, long-term therapy causes a number of side effects. These are nosebleeds, uterine, intestinal, diarrhea, dyspepsia, nausea, vomiting, poor appetite, weakness, dizziness. Short-term visual impairment is possible. The amount of hemoglobin and platelets in the blood may change. With a tendency to kidney pathologies, some people develop kidney failure. From allergic reactions Possible bronchospasm, asthma, rash, anaphylaxis.

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

Release form

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

Pharmacological action

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

Pharmacological group: NSAIDs.

Pharmacodynamics and pharmacokinetics

Acetylsalicylic acid - what is it?

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

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

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

Receiving ASA

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

Pharmacodynamics

The analgesic effect is determined by both central and peripheral action. At feverish conditions reduces temperature by affecting the thermoregulation center.

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

Pharmacokinetics

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

About 80% is in the bound state in plasma. acetylsalicylic and salicylic acids . Biological activity is maintained even when the substance is in protein-bound form.

Metabolized in the liver. Excreted by the kidneys. The pH of urine affects excretion: when it is acidified, it decreases, and when it is alkalized, it increases.

Pharmacokinetic parameters depend on the dose taken. Elimination of a substance is nonlinear. Moreover, in children of the 1st year of life, in comparison with adults, it proceeds much more slowly.

Indications for use: what do Acetylsalicylic acid tablets help with?

Indications for use of Acetylsalicylic acid are:

  • febrile conditions in diseases of an infectious-inflammatory nature;
  • rheumatoid arthritis ;
  • rheumatism ;
  • inflammatory lesion myocardium , the cause of which is an immunopathological reaction;
  • pain syndrome of various origins, including toothache(including headaches associated with alcohol withdrawal syndrome), joint and muscle pain, neuralgia, migraines ,algomenorrhea .

Also aspirin (or acetylsalicylic acid) is used for prophylactic purposes in case of threat thrombosis ,thromboembolism , MI (when the drug is prescribed for secondary prevention).

Contraindications

Taking ASA is contraindicated in:

  • “aspirin” asthma ;
  • during the period of exacerbation erosive and ulcerative lesions of the digestive canal ;
  • stomach/intestinal bleeding ;
  • vitamin deficiency K ;
  • hemophilia , hypoprothrombinemia , hemorrhagic diathesis ;
  • G6PD deficiency;
  • portal hypertension ;
  • renal/liver failure;
  • aortic dissection;
  • during the treatment period (if the weekly dose of the drug exceeds 15/mg);
  • gouty arthritis, gout;
  • (absolute contraindications are the first three and last three months);
  • hypersensitivity to ASA/salicylates.

Side effects

Side effects of ASA treatment may include:

  • nausea;
  • gastralgia;
  • anorexia;
  • thrombocytopenia;
  • erosive and ulcerative lesions of the digestive canal;
  • and/or liver failure.

At long-term use tinnitus appears, hearing acuity decreases, vision is impaired, dizziness occurs and, when taking high doses, headaches. Bleeding is also possible hypocoagulation , vomit, bronchospasm .

Acetylsalicylic acid, instructions for use (Method and dosage)

At active rheumatism adult patients are prescribed 5 to 8 g of ASA per day. For a child, the dose is calculated depending on weight. As a rule, it varies from 100 to 125 mg/kg/day. Frequency of application - 4-5 rubles/day.

1-2 weeks after the start of the course, the dose for a child is reduced to 60-70 mg/kg/day; for adult patients, the dosage remains the same. Treatment should be continued for up to 6 weeks.

According to the instructions for use of Acetylsalicylic acid, the drug should be discontinued gradually over 1-2 weeks.

Acetylsalicylic acid for headaches and as a remedy for fever is prescribed in more low dosages. Yes, when pain syndrome And feverish conditions dose per 1 dose for an adult - from 0.25 to 1 g with a frequency of use from 4 to 6 times per day.

It should be remembered that for headaches, ASA is especially effective if the pain is provoked by an increase in ICP (intracranial pressure).

For children, the optimal dose per dose is 10-15 mg/kg. Frequency of applications - 5 rubles/day.

Treatment should not last more than 2 weeks.

For warning thrombosis And embolism ASA is taken 2-3 times a day. 0.5 g each. To improve the rheological properties (for liquefaction), the drug is taken for a long time at 0.15-0.25 g/day.

For a child over five years of age, a single dosage is 0.25 g, four-year-old children are allowed to give 0.2 g of ASA once, two-year-old children - 0.1 g, one-year-old children - 0.05 g.

It is forbidden to give ASA to children for fever that rises against the background viral infection . The drug acts on the same structures of the brain and liver as some viruses, and in combination with viral infection may cause the child to develop Reye's syndrome .

Application of ASA in cosmetology

A face mask with Acetylsalicylic acid allows you to quickly relieve inflammation, reduce tissue swelling, remove redness, remove the surface layer of dead cells and clean clogged pores.

The drug dries the skin well and is perfectly soluble in fats, which makes it advisable to use it as a remedy for acne : tablets, moistened with water, are applied to inflamed areas on the face or added to face masks.

Acetylsalicylic acid from acne works well in combination with lemon juice or honey. A clay mask is also effective for eliminating skin problems.

To prepare a lemon-aspirin mask, tablets (6 pieces) are simply ground with freshly squeezed juice until smooth. Then the medicine is applied pointwise to inflamed pimples and leave them on until dry.

A mask with honey is prepared as follows: tablets (3 pieces) are moistened with water, and then, when they dissolve, mixed with 0.5-1 teaspoon (teaspoon) of honey.

To prepare a clay mask, mix 6 crushed ASA tablets and 2 teaspoons of white/blue clay with warm water.

Overdose

Overdose can result from:

  • long-term treatment with ASA;
  • single administration of too high a dose of the drug.

A sign of an overdose is salicylic syndrome , manifested by general malaise, hyperthermia, tinnitus, nausea, vomiting.

Strong accompanied convulsions , stupor, severe dehydration, non-cardiogenic lungs , violations of CBS, shock.

In case of an overdose of ASA, the victim should be immediately hospitalized. They wash out his stomach, give him, and check his CBS.

Depending on the condition of the CBS and the balance of water and electrolytes, the administration of solutions may be prescribed, sodium citrate And sodium bicarbonate (as an infusion).

If the urine pH is 7.5-8.0, and the plasma concentration of salicylates exceeds 300 mg/l (in a child) and 500 mg/l (in an adult), a intensive care alkaline diuretics .

In case of severe intoxication, carry out; replenish fluid loss; symptomatic treatment is prescribed.

Interaction

Increases toxicity barbituric drugs ,valproic acid , methotrexate , effects of oral hypoglycemic drugs, narcotic , sulfa drugs .

Reduces effects diuretics (potassium-sparing and loop), antihypertensive drugs from the ACE inhibitor group, action uricosuric drugs .

When used simultaneously with antithrombotic drugs , thrombolytics , indirect anticoagulants increases the risk of bleeding.

GCS enhance the toxic effect of ASA on the mucous membrane of the digestive canal, increase its clearance and reduce plasma concentration.

When used simultaneously with Li salts, it increases the plasma concentration of Li+ ions.

Strengthens the toxic effect of alcohol on the mucous membrane of the digestive canal.

Terms of sale

Over-the-counter product.

Recipe in Latin (sample):

Rp: Acidi acetylsalicylici 0.5
D.t. d. N 10 in tab.
S. 1 tablet 3 times a day after meals, with plenty of water.

Storage conditions

Tablets should be stored in a dry place at temperatures below 25°C.

Best before date

Four years.

Special instructions

The drug should be used with caution in people with pathologies of the kidneys and liver , with increased bleeding, decompensated CHF, during treatment with anticoagulants, as well as in people with a history of erosive and ulcerative lesions digestive tract and/or stomach/intestinal bleeding .

Even in small doses, ASA reduces excretion uric acid , which in predisposed patients can cause acute attack gout .

When taking high doses of ASA or needing long-term treatment with the drug, it is necessary to regularly monitor the level and see a doctor.

As an anti-inflammatory agent, use ASA at a dose of 5-8 g/day. limited due to increased risk of developing adverse reactions from the gastrointestinal tract.

To reduce bleeding during surgery and in postoperative period, taking salicylates is stopped 5-7 days before surgery.

When taking ASA, you should remember that this drug can be taken for pain relief for no more than 7 days without consulting a doctor. As an antipyretic, ASA is allowed to be taken for no more than 3 days.

Chemical properties of the substance

When ASA crystallizes, colorless needles or monoclinic polyhedra with a slightly sour taste are formed. The crystals are stable in dry air, but with increasing humidity they gradually hydrolyze to salicylic and acetic acids.

The substance in its pure form is a white crystalline powder and practically odorless. The appearance of an acetic acid odor is evidence that the substance has begun to hydrolyze.

viral infection, since such a combination can cause the development of a life-threatening condition for the child - Reye's syndrome .

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

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

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

Acetylsalicylic acid and alcohol

Alcohol is contraindicated during ASA. This combination can cause stomach and intestinal bleeding, as well as severe hypersensitivity reactions.

What is Acetylsalicylic acid used for hangovers?

ASA is a very effective hangover remedy, due to the antiplatelet effect of the drug.

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

Use during pregnancy and breastfeeding

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

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

If a woman is indicated for long-term treatment high doses ASA, you need to stop breastfeeding.