Aspirin contraindications side effects

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Contraindications for the use of Aspirin

One of the most famous drugs used in medicine is Aspirin. Like all medications, it has a number of contraindications, and improper use leads to the development of side effects.

Table of contents:

Contraindications for Aspirin cannot be ignored: it should be borne in mind that acetylsalicylic acid, which is part of its composition, is an active component that has an effective effect on all systems and internal organs of the human body.

Contraindications for use

A certain category of patients who feel the need to get rid of pain and inflammation during the development of colds have to look for a replacement for Aspirin. The fact is that this drug is categorically contraindicated for them, and in case of deviation from the rules, instead of benefiting the body, harm will be done. Aspirin should not be taken by people with hypersensitivity to acetylsalicylic acid, as well as in the presence of certain concomitant diseases.

  • stomach and duodenal ulcers;
  • erosive gastritis;
  • combinations of three pathologies: ulcers, nasopharyngeal polyposis, individual intolerance to ASA;
  • hematological syndromes accompanied by diathesis;
  • aortic aneurysm;
  • hypertension;
  • lack of vitamin K in the body;
  • deficiency of glucose-6-phosphate dehydrogenase;
  • endocrine disorders;
  • renal failure;
  • asthma;
  • increased blood pressure;
  • liver pathologies.
In addition, Aspirin is contraindicated for women in the first and third trimester of pregnancy, as well as during lactation. Contraindications for taking Aspirin during pregnancy are due to the fact that these tablets thin the blood and can cause bleeding. An exception in this case is allowed for nursing mothers. They may be allowed to take medication if necessary, but only on condition that they temporarily stop feeding the child. Rules and contraindications for taking Aspirin are indicated in the instructions for use.

Aspirin is contraindicated in children aged 15 to 18 years, as they are more likely to develop Reye's syndrome. The medicine should also not be taken for gout, hyperurencemia and urate nephrourolytis.

What does an overdose lead to when treated with Aspirin?

It is worth noting that aspirin is far from a harmless medicine. Uncontrolled use of acetylsalicylic acid leads to dire consequences. Mild overdose is fraught with the development of complications.

Side effects after Aspirin in this case are as follows:

  • the occurrence of nausea;
  • noise in ears;
  • dizziness;
  • confusion.

If such symptoms occur, it is recommended to either completely eliminate the drug or adjust the dose in accordance with the instructions for use.

The situation is much more complicated in the case of severe overdose. In this situation, the following manifestations may occur:

  • heart failure;
  • respiratory disorder;
  • changes in blood composition, manifested in the form of metabolic acidosis;
  • fever.

In the worst case, the situation can end in cardiac shock. Patients in this condition will require emergency care, which can only be provided in an inpatient setting. After hospitalization, patients are given symptomatic therapy to restore the acid-base balance and normalize cardiac activity.

The occurrence of nausea accompanied by vomiting, pain in the abdomen, gastric bleeding and the development of anemia are clear signs of the consequences of an aspirin overdose from the gastrointestinal tract.

As for dizziness and tinnitus, such signs indicate disorders of the central nervous system.

The most common side effects that occur due to an overdose of Aspirin are bleeding and allergic reactions to the main drug component. Hypersensitivity to aspirin can result in bronchospasms, anaphylactic shock, or the development of Quincke's edema.

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IMPORTANT. The information on the site is provided for informational purposes only. Do not self-medicate. At the first sign of disease, consult a doctor.

Source: http://pillsman.org/24511-aspirin-protivopokazaniya.html

Aspirin - description, instructions, interesting facts

Aspirin is a well-known drug with antipyretic and anti-inflammatory effects. And many simply do not think about possible contraindications and even health hazards when taking a pill “for fever.” In fact, there is constant controversy surrounding the drug in question - it is either considered dangerous or considered almost a panacea for most pathologies.

Aspirin: official instructions for use

The drug in question contains only one active substance - acetylsalicylic acid. Produced in tablet form, aspirin also contains corn starch and microcrystalline cellulose - they are excipients and do not affect the clinical picture.

Aspirin belongs to the group of non-steroidal anti-inflammatory drugs and has antipyretic, anti-inflammatory, and analgesic effects.

Indications for use

Aspirin is effective in the treatment of symptomatic pain in muscles, joints, as well as headaches, dental and menstrual pain.

The drug in question helps reduce body temperature for colds, inflammatory and/or infectious diseases in adults and adolescents.

Recommended dosage

Aspirin can only be taken by adults and children in adolescence.

Please note: clarifications regarding the prescription and use of the drug in question should be made from your attending physician - different restrictions are defined for different countries. For example, in Russia, it is generally strictly forbidden to give aspirin to children under 2 years of age; at the age of 2-12 years, tablets are allowed to be used, but with caution and only after obtaining permission from a specialist. There are countries in which aspirin is strictly prohibited for use by children under 13 years of age. Generally accepted restrictions are up to 15 years of age.

For pain or high body temperature, it is advisable to take 0.5-1 g of aspirin at a time. At least 4 hours should pass between doses of the drug in question. The maximum permissible daily dosage of aspirin is 6 tablets (3 grams).

If aspirin is taken without a doctor’s prescription, then you can only relieve pain with this drug for 7 days in a row - then, if the condition does not improve, you need to visit a doctor, undergo an examination and get an adjustment to the treatment regimen. If aspirin is taken as a drug with an antipyretic effect, then the duration of uncontrolled use should not exceed 3 days.

An aspirin tablet should be taken after meals, washed down with a sufficient amount of water (about 200 ml).

Overdose

There are two degrees of severity of overdose - mild and severe. In the first case, the patient will complain of nausea, tinnitus, short-term dizziness, and rarely, confusion. Correcting the dosage will help normalize the patient’s well-being - when it is reduced, the condition immediately improves. In some cases, it is advisable to exclude aspirin from the treatment regimen.

Severe overdose is manifested by respiratory and cardiac failure, fever, metabolic acidosis, and cardiogenic shock. These conditions require emergency medical care in a hospital setting - fluid loss is compensated, the patient is given activated charcoal, symptomatic therapy is carried out, and blood and urine tests are monitored.

Side effects

Using aspirin without supervision and permission from medical professionals, or incorrectly calculated doses can lead to adverse reactions.

Gastrointestinal tract

Patients may develop nausea, vomiting and sharp abdominal pain of unclear localization, pronounced signs of gastric bleeding (in some cases they may be hidden), and the development of iron deficiency anemia.

central nervous system

Tinnitus and dizziness - these disturbances in the functioning of the central nervous system usually occur against the background of an overdose.

Please note: the most commonly diagnosed side effect of aspirin use is bleeding.

Allergic reactions with hypersensitivity or individual intolerance to acetylsalicylic acid are also considered a side effect - urticaria, bronchospasm, anaphylactic shock, Quincke's edema.

When does aspirin become dangerous?

The well-known aspirin can be really dangerous not only for health, but also for human life. It is strictly forbidden to take the drug in question on your own - you need to know not only the contraindications, but also the possible risks. It is absolutely contraindicated to take aspirin for the following diseases:

  • acute and chronic gastritis with low/high acidity of gastric juice;
  • peptic ulcer of the duodenum and/or stomach;
  • disorders of the kidneys and urinary system;
  • renal failure;
  • liver pathologies of an inflammatory and/or infectious nature;
  • liver failure;
  • heart failure in severe form;
  • bronchial asthma;
  • hemorrhagic diathesis;
  • persistently elevated blood pressure;
  • enlargement of the thyroid gland;
  • angina pectoris.

Please note : aspirin helps thin the blood - this ability is often used to prevent the formation of blood clots, varicose veins and already diagnosed thrombophlebitis. But as a result of unauthorized use of the drug in question, the number of platelets in the blood may significantly decrease and bleeding will result.

Pregnant women should not use aspirin as an antipyretic, anti-inflammatory or analgesic - this can cause uterine bleeding and miscarriage; aspirin is especially dangerous in the last months of pregnancy. But women who are breastfeeding can take aspirin. But! Only in case of medical necessity and with a temporary refusal to feed the child milk, if it means taking the drug in large doses.

The drug in question is also dangerous for previously diagnosed hay fever, polyps in the nasal passages and sinuses. Aspirin is not recommended for children under 15 years of age, and in some countries it is prohibited for children under 2 years of age.

In addition to categorical contraindications, in medicine there is such a thing as conditional restrictions. For example, if it is necessary to take aspirin, people diagnosed with gout, short-term high blood pressure, or diabetes should consult with specialists or limit their pill intake. And if you have a predisposition to sore throats or have had a heart attack in the recent past, then you definitely shouldn’t decide on your own to use the drug in question.

Please note: when taking an aspirin tablet, you should not wash it down with Coca-Cola or coffee - this combination provokes hyperexcitability, unmotivated irritability, and can lead to causeless hysteria/aggression.

When can aspirin help?

Aspirin has blood-thinning properties - it can really save people's lives. We are talking about people at risk for thrombosis and early heart attacks - daily intake of aspirin in small doses will reduce the risks to zero. But you should understand that you cannot use the drug in question on your own:

  1. Aspirin can cause severe stomach irritation, which can lead to the development of gastritis and/or peptic ulcers. At the very beginning of their development, these diseases are often practically asymptomatic, and continued use of aspirin tablets only aggravates the health situation.
  2. If you have a history of bleeding of varying intensity, then uncontrolled use of aspirin can lead to sudden, severe bleeding - minutes will count.
  3. The drug in question can increase blood pressure - in case of thrombosis or a predisposition to it in a person, this indicator is characterized by a lack of stability, and regular use of aspirin will lead to a sharp increase in it - a hypertensive crisis cannot be avoided.

Aspirin saves you from cancer! This slogan was made by British scientists who conducted an experiment on 25 thousand participants - they took a small dose of aspirin (57 mg) daily for 4 years. The following conclusions were drawn:

  • the likelihood of developing esophageal cancer decreased by 60%;
  • the risk of developing intestinal cancer decreased by 40%;
  • the possibility of malignant tumors in the lungs decreased by 30%;
  • the probability of diagnosing prostate cancer is 10%.

Data were also obtained that regular use of aspirin reduces the likelihood of cancer recurrence, and the drug in question has a particular effect on the dynamics of colon cancer - the number of cancer cells decreases, tumor progression stops.

Another experiment is currently being conducted in England, which will involve 11 thousand people and 100 leading clinics. Patients with already diagnosed cancer of the colon, esophagus, breast, stomach and prostate were selected. The experiment is designed for 12 years, during which the results of taking aspirin for 5 years by one group of patients and placebo will be compared. It is very important to find out the effect of the drug in question on the development of relapses of cancer - it is believed that secondary cancer is much harder and more difficult to treat, so the results of the experiment can significantly alleviate the plight of cancer patients.

Aspirin, so well-known and seemingly safe, could truly become a “discovery” in oncology. But with all its advantages, one cannot exclude a danger to human health/life - this can be caused by uncontrolled use of aspirin, too large daily dosages, or lack of consultation/permission from the attending physician.

Tsygankova Yana Aleksandrovna, medical observer, therapist of the highest qualification category.

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Side effects of the drug Aspirin💊

The drug Aspirin is a type of medicine that has anti-inflammatory and analgesic (pain-relieving) effects. Its composition also has antiplatelet properties, which is reflected in a reduced risk of possible thrombus formation in blood vessels. An equally important advantage of Aspirin is its successful work, if necessary, to eliminate fever and normalize body temperature, as well as its affordable cost. The main active ingredient is acetylsalicylic acid.

Among the indications for the use of the drug it is worth highlighting:

  • migraine (during an acute attack);
  • disturbances in the functioning of the connective tissues of the body (rheumatism);
  • pain syndromes with varying degrees of manifestation and localization;
  • fever, especially as a result of infection with infectious and inflammatory diseases;
  • prevention of recurrence of myocardial infarction;
  • prevention of thrombosis.

As for the rules for taking the drug, it is first important to know whether aspirin has side effects and how much the risk of their occurrence is higher than the expected effect.

Characteristics of side effects that can be caused by Aspirin

If Aspirin was taken in violation of the regimen or dosage, the patient may experience:

  • manifestation of bleeding in the gastrointestinal tract;
  • formation of ulcerative lesions of the gastrointestinal tract;
  • severe nausea;
  • increasing pain in the anterior abdominal wall;
  • thrombocytopenia (pathological decrease in the number of platelets in the blood);
  • anemia;
  • skin rashes with characteristic disturbing itching;
  • hives.

Due to possible complications, the drug is not allowed in the presence of bronchial asthma, peptic ulcers of the stomach and intestinal tract, angina pectoris, as well as arterial hypertension (constantly elevated blood pressure). The use of Aspirin in conditions of an enlarged thyroid gland is extremely dangerous. And also in case of heart failure (at the stage of decompensation).

Under careful medical supervision and compliance with the correct dosages, the drug can be used for hyperuricemia (increased levels of uric acid in the blood), gout, suspected gastric bleeding, and also in the presence of bronchial asthma.

Features of drug overdose

An overdose of a drug is most often chronic, when Aspirin is taken regularly and for an unnecessarily long period. The fact that too much of the drug was taken may also be indicated by an empty package of Aspirin, which was only recently purchased. In chronic forms of poisoning, the effect of the medication may affect:

  • manifestation of tinnitus;
  • dysfunction of the digestive tract;
  • the appearance of acute severe pain in the abdominal area;
  • noticeable hearing loss;
  • frequent headaches;
  • increased sweating;
  • loss of consciousness;
  • manifestation of anemia (pathological decrease in the number of leukocytes and platelets in the blood).

An overdose is extremely dangerous due to complications such as bleeding, worsening existing bronchial asthma, as well as increased symptoms of heart failure.

Dangers of taking Aspirin for the gastrointestinal tract

The ability of the drug to effectively thin the blood and serve as a reliable prevention of thrombosis, as well as relieve pain and fight inflammation, are the main arguments in favor of its choice. But at the same time, taking the drug must be monitored by a doctor, since acetylsalicylic acid can aggravate the problems of ulcerative lesions of the gastrointestinal tract (has an ulcerogenic effect).

It is taking the drug, even in the smallest doses, that can cause new hemorrhages, thereby provoking a complication of an existing disease in the body.

The effect of Aspirin on the central nervous system

Since Aspirin has an analgesic, antipyretic and aggregate effect on the body, many patients consider it absolutely safe and prescribe the required dosage of the drug on their own. This is the main mistake, since incorrect calculations regarding the number of one-time tablets and the duration of the course make the drug a real poison for the body and especially for the central nervous system. In addition to its beneficial functions, Aspirin can also have toxic effects, affecting the central nervous system.

As a rule, this manifests itself in the form of nausea, dizziness, severe headaches, as well as a noticeable deterioration in vision and hearing. It is important to note that after abrupt withdrawal of the drug, a syndrome of so-called reversible deafness may appear, which gradually disappears if the drug is completely discontinued.

When is taking Aspirin most dangerous?

Any use of the drug that is not supervised by a doctor can be dangerous to the body. This is due not only to an overdose and the excessively irritating effect of the drug on the gastric mucosa, but also to the simultaneous use of Aspirin and alcoholic beverages.

It is in the latter case that irritation intensifies, provoking the activity of ulcerative lesions, as well as the manifestation of hemorrhages. Even the most insignificant disease of the body at first glance may be a contraindication for taking the drug.

Features of taking Aspirin during pregnancy and breastfeeding

Taking the product during pregnancy is prohibited. The only exception may be the doctor's decision if there are no alternative treatments for the patient. It is Aspirin, taken at the end of the first trimester at the beginning of the second, that can cause fetal development disorders. This is especially true for the process of myocardial formation - underdevelopment of the cardiac system and organs, as well as cessation of the ductus arteriosus, which leads to pulmonary hypertension and the development of a diaphragmatic hernia. Taking the drug before childbirth contributes to the manifestation of bleeding and hemorrhages in the fetus itself.

It would be a good idea to consult a doctor if a woman took aspirin immediately before pregnancy. The drug should not be taken during lactation due to increased toxic effects.

Features of taking the drug by children

Aspirin is the first thing people think about when a child’s temperature rises. Adults still refuse to understand the advantages and disadvantages of the medication, considering it an effective antipyretic. But you should know that for children under 14 years of age, the drug is completely contraindicated and is not allowed for any purpose.

The reason for the ban lies in the excessively increased risk of Reye's syndrome, which is characterized by acute liver failure and cerebral edema. Signs of the disease include:

  • a sharp deterioration in condition immediately after recovery;
  • manifestation of severe vomiting;
  • difficulty breathing;
  • speech becomes slurred;
  • the appearance of a pronounced odor of ammonia from the mouth;
  • loss of consciousness.

Taking the drug by children with existing chronic diseases of the bronchi and lungs can lead to an increased allergic reaction of the body and to the occurrence of spasms in the bronchi, as well as the appearance of asthma.

Characteristics of the drug when used by elderly patients

The use of Aspirin by older people is usually associated with the need to eliminate bothersome pain or normalize temperature. In this case, the treatment is carried out independently and the dosage is determined without any control from the doctor.

This particular drug is dangerous, since its long-term use provokes macular degeneration (impairments in the functioning of the retina). This in turn leads to loss of vision, primary blindness due to the inability of the retina to function normally.

The dangers of self-medication with Aspirin for liver and kidney diseases

The use of aspirin for antipyretic and analgesic purposes is allowed only after careful consultation with a doctor, as well as the absence of any serious diseases, for example, impaired functionality of the kidneys and liver. Acetylsalicylic acid, which is the main component of the drug, tends to reduce the level of blood clotting inside the vessels, which causes the irreversible process of destruction of the cells of the liver itself to begin. If you add alcohol to Aspirin, the toxic effect and poisoning of the body increases significantly.

If there are disturbances in the functioning of the kidneys, the drug can seriously aggravate an existing problem, causing the emergence of new complications, as well as the development of acute renal failure.

What to watch out for in case of drug overdose

In case of overdose, the body is poisoned with toxic substances. Poisoning can be cumulative (taking the drug regularly over several years), acute (taking a large number of tablets at a time), or taken with any alcoholic drink.

Symptoms of an overdose of Aspirin include:

  • confusion and a distinct disturbance in the thinking process;
  • manifestation of shortness of breath;
  • increased drowsiness;
  • suffocation;
  • depression;
  • disturbance of carbohydrate metabolism;
  • excessive dehydration of the body.

Often, an overdose of the drug leads to death. That is why, at the first signs of nausea, tinnitus and dizziness, a doctor’s consultation is necessary. At your appointment, you should clearly indicate the dosage of the drug taken. If the first symptoms of an overdose are ignored and you continue taking Aspirin, you should expect:

  • manifestations of hallucinations;
  • hearing loss;
  • pathologically increased bleeding;
  • vision problems;
  • excessive sweating;
  • manifestation of convulsions.

Aspirin can be a good pain reliever and antipyretic assistant if you consult a doctor before purchasing it and strictly adhere to the recommended dosage. Otherwise, the drug becomes an extremely dangerous toxic substance, causing many health problems and disruptions in the functioning of major organs.

Source: http://sosudov.net/preparaty/aspirin-4.html

Aspirin - use, contraindications and history of discovery

Aspirin (acetylsalicylic acid) is a salicylate drug that is often used as an analgesic to relieve minor pain and ailments, as an antipyretic to reduce fever, and as an anti-inflammatory drug. Aspirin also has an antiplatelet effect by inhibiting the production of thromboxane, which binds platelet molecules together under normal circumstances to create a patch on damaged blood vessel walls. Because the platelet patch can become too large and also block blood flow, both locally and downstream, aspirin is also used long-term in low dosage to prevent heart attacks, strokes and blood clots in people in the group high risk of blood clots. In addition, it has been found that low-dose aspirin can be given immediately after a heart attack to reduce the risk of death of cardiac tissue or recurrent myocardial infarction. In addition, it may be effective in preventing certain types of cancer, especially colorectal cancer.

. used as an alternative to drugs without causing addiction. The best-known members of this class of drugs include aspirin, ibuprofen and naproxen, which are available without a prescription in most countries. Paracetamol (acetaminophen) is generally not considered an NSAID because.

The main side effects of aspirin are gastrointestinal ulcers, stomach bleeding and tinnitus, especially at high dosages. For children and adolescents, it is not recommended in case of flu-like symptoms or viral illnesses due to the risk of Reye's syndrome.

Aspirin is part of a group of medications called nonsteroidal anti-inflammatory drugs (NSAIDs), but has a different mechanism of action than most other NSAIDs. Although it and other drugs with a similar structure are called salicylates, have similar effects to other NSAIDs (antipyretic, anti-inflammatory, analgesic) and inhibit the same enzyme cyclooxygenase (COX), aspirin (other than other salicylates) does this in an irreversible manner and, unlike others, affects more on the COX-1 variant than the COX-2 variant of the enzyme.

The active ingredient in aspirin was first discovered from willow bark in 1763 by Edward Stone of Wadham College, Oxford University. He discovered salicylic acid, an active metabolite of aspirin. Aspirin was first synthesized in 1897 by chemist Felix Hoffmann with the German company Bayer. Aspirin is among the most widely used medicines in the world, with an estimated ton consumed each year. In countries where aspirin is a registered trademark of Bayer, the generic term is acetylsalicylic acid (ASA). It is included in the WHO List of Essential Medicines, a list of the most important medicines needed in a basic healthcare system.

Medical uses of aspirin

Aspirin is used to treat a number of conditions, including fever, pain, rheumatic fever, and inflammatory conditions such as rheumatoid arthritis, pericarditis, and Kawasaki disease. Lower doses of this drug also reduce the risk of death from a heart attack or the risk of stroke in some circumstances. There is some evidence that it is effective in preventing colorectal cancer, although the mechanisms of this action remain unclear.

Video about aspirin

Aspirin is generally considered inferior to ibuprofen for pain relief because it is more likely to cause gastrointestinal bleeding. It is generally not effective for pain caused by muscle cramps, bloating, stomach distension, or acute skin irritation. As with other NSAIDs, combinations with caffeine provide slightly greater pain relief than aspirin alone. Effervescent aspirin preparations, such as Alka-Seltzer or Blowfish, relieve pain more quickly than tablet formulations, making them useful for treating migraines.

Topical aspirin may be effective in treating some types of neuropathic pain.

Aspirin, either alone or in a combination drug, is effective in treating some types of headaches, but its effectiveness may be questionable for others. A health care professional should promptly treat headaches that are secondary, that is, those caused by another disorder or injury.

The International Classification of Headache Disorders distinguishes between tension-type headaches (the most common type), migraine, and cluster headaches among primary headaches. Aspirin or other over-the-counter analgesics are widely recognized to be effective in the treatment of tension-type headaches. Aspirin, especially when combined with acetaminophen and caffeine, as in Excedrin Migraine, is considered first-line treatment for migraine and is comparable to lower doses of sumatriptan. It is most effective in treating migraines when taken from the beginning.

Like its ability to control pain, aspirin's ability to control fever is related to its effect on the prostaglandin system through its irreversible inhibition of COX. Although the use of aspirin as a fever reducer in adults is well supported, many medical societies and regulatory bodies, including the American Academy of Family Physicians, the American Academy of Pediatrics, and the FDA, strongly recommend against its use for the treatment of fever in adults. children due to the threat of developing Reye's syndrome. This is a rare but often fatal illness associated with the use of aspirin or other salicylates in children during episodes of viral or bacterial infection. Because of the risk of Reye's syndrome in children, in 1986 the FDA required all medications containing aspirin to be labeled with a warning against its use in children and adolescents.

Heart attacks and strokes

The first studies into the effects of aspirin on heart function and stroke prevention were carried out in the early 1970s by Professor Peter Slight, emeritus professor of cardiovascular medicine at the University of Oxford. Professor Slight and his research group at Oxford led and formed a foundation for research into the use of this drug in the prevention of other diseases.

For a subset of the population, aspirin may help prevent heart attacks and strokes. At lower doses, it is known to prevent the progression of existing cardiovascular disease and reduce the incidence of these events for those with a history of them. This is known as secondary prevention.

Aspirin appears to provide little benefit for people with a reduced risk of heart attack or stroke, such as those without a history of them or with pre-existing conditions. This is called primary prevention. Some studies recommended it on a case-by-case basis, while others suggested that the risks of other events, such as gastrointestinal bleeding, were significant enough to outweigh any potential benefits and recommended against using aspirin for primary prevention entirely.

The use of the drug for prevention is complicated by the phenomenon of aspirin resistance. For patients with resistance, the drug's effectiveness is reduced, which may lead to an increased risk of stroke. Some authors have proposed trial regimens to identify patients who are resistant to aspirin or other antithrombotic agents (eg, clopidogrel).

Aspirin has also been proposed as a component in a multidrug for the prevention of cardiovascular diseases.

The US Agency for Healthcare Research and Quality guidelines recommend taking aspirin indefinitely after percutaneous coronary interventions (PCI), such as coronary artery stent placement. It is often used in combination with an ADP receptor inhibitor, such as clopidogrel, prasugrel or ticagrelor, to prevent blood clots. This is called dual antiplatelet therapy (DAPT). US and European Union guidelines disagree somewhat on the timing and indications for continuing this combination therapy after surgery. US guidelines recommend DAPT for at least 12 months after drug-eluting stent placement, while EU guidelines recommend 6–12 months. However, they agree that aspirin can be continued indefinitely after completion of DAPT.

The effects of aspirin on cancer have been widely studied, particularly its effect on colorectal cancer (CRC). Several meta-analyses and reviews have concluded that regular aspirin use reduces the long-term risk of CRC morbidity and mortality. However, the relationship of drug dose and duration of use for different types of CRC risk, including mortality, progression, and morbidity, has not been clearly defined. Most data on aspirin and the risk of CRC come from observational studies rather than randomized controlled trials (RCTs). However, available RCT data suggest that long-term use at low doses may be effective in preventing some types of CRC. According to the 2007 USPSTF (United States Preventive Services Task Force) guidelines on this topic, the use of aspirin for the prevention of CRC is rated "D" with a recommendation to health care professionals against its routine use for this purpose.

Other uses of aspirin

Aspirin is the first line of therapy for the fever and joint pain symptoms of rheumatic fever. Therapy often lasts one to two weeks, and is rarely indicated for longer. Once the fever and pain have subsided, it is no longer needed as it does not reduce the incidence of cardiac complications or residual rheumatic heart disease. Naproxen is as effective as aspirin and not as toxic, but due to limited clinical experience, naproxen is recommended only as second-line therapy.

Along with rheumatic fever, Kawasaki disease remains one of the few indications for the use of aspirin in children, despite the lack of high-quality evidence of its effectiveness.

Low dose supplementation has moderate benefits when used to prevent preeclampsia.

For some people, aspirin does not have as strong an effect on platelets as it does for others, and this effect is known as resistance or insensitivity. One study suggested that women were more likely to be resistant than men, and another, a pooled study of 2,930 patients, found 28% resistant. A study of 100 Italian patients, on the other hand, found that, of the apparent 31% of subjects resistant to aspirin, only 5% were truly resistant, and the rest were incompatible. Another study of 400 healthy volunteers found no subjects who were truly resistant, but some were pseudo-resistant, reflecting delayed and reduced absorption of the drug.

Adult aspirin tablets are produced in standard sizes that vary slightly between countries, for example 300 mg in the UK and 325 mg in the US. Smaller doses are based on these standards, such as 75 mg and 81 mg tablets. The 81 mg tablets are called "children's" tablets even though they are not intended for administration to infants and children. There is no medical significance in the small difference in dosage between the 75 mg and 81 mg tablets. Historically, an interesting fact is that in the US, a 325 mg dose is equivalent to a historical 5 grain aspirin tablet in pre-metric use.

In general, for adults in cases of fever or arthritis, doses are prescribed 4 times a day, with doses around the maximum daily dose historically used in the treatment of rheumatism. To prevent myocardial infarction in someone with documented or suspected coronary artery disease, much lower single daily doses are prescribed.

USPSTF recommendations for the use of aspirin for the primary prevention of coronary artery disease support its use in older men and older women when the potential benefit of reducing the risk of myocardial infarction (MI) for men or stroke for women outweighs the potential risk of increased risk of gastrointestinal bleeding. . According to the WHI study, regular low-dose (75 or 81 mg) aspirin for women resulted in a 25% reduction in the risk of death from cardiovascular disease and a 14% reduction in the risk of death from any cause. Its low dose has also been associated with a reduced risk of cardiovascular events, and lower dose aspirin (75 or 81 mg/day) may optimize its safety and effectiveness for patients requiring it for long-term prevention.

In children with Kawasaki disease, it is given in weight-based doses, initially 4 times daily for up to two weeks, then at a lower dose once daily for the next six to eight weeks.

Side effects and contraindications of aspirin

Aspirin should not be taken by people who are allergic to ibuprofen or naproxen, or have salicylate intolerance or more general intolerance to NSAIDs, and caution should be used in people with asthma or bronchospasm precipitated by NSAIDs. Due to its effect on the stomach lining, manufacturers recommend that people with peptic ulcers, mild diabetes or gastritis consult a doctor before using it. Even if none of these conditions are present, the risk of stomach bleeding is still increased when aspirin is combined with alcohol or warfarin. Patients with hemophilia or other bleeding tendencies should not take aspirin or other salicylates. It is known to cause hemolytic anemia in people who have the genetic disease glucose-6-phosphate dehydrogenase deficiency, particularly at high doses and depending on the severity of the disease. Due to the increased tendency to bleed, it is not recommended to use aspirin during dengue fever. People with kidney disease, hyperuricemia, or gout should not take aspirin because it inhibits the kidneys' ability to eliminate uric acid, and thus may worsen these conditions. It should not be used in children or teenagers to control cold or flu symptoms because it is associated with Reye's syndrome.

Aspirin use has been shown to increase the risk of gastrointestinal bleeding. Although some of its enteric-coated drugs are advertised as being "gentle on the stomach," in one study, enteric coating did not seem to reduce this risk. Combining aspirin with other NSAIDs also further increased this risk. Its use in combination with clopidogrel or warfarin also increases the risk of upper gastrointestinal bleeding.

It appears that blockade of COX-1 by aspirin results in up-regulation of COX-2 as part of gastric protection. At the same time, simultaneous use of COX-2 inhibitors with aspirin increases erosion of the gastric mucosa. Thus, caution should be exercised when combining it with any “natural” supplements with COX-2 inhibitory properties, such as garlic extracts, curcumin, blueberry, pine bark, ginkgo, fish oil, resveratrol, genistein, quercetin, resorcinol, and others.

In addition to enteric coating, "buffering action" is the other main method used by companies in an attempt to mitigate the problem of gastrointestinal bleeding. Buffering agents are designed to act by preventing aspirin from concentrating in the stomach wall, although the benefits of a buffering agent are controversial. Almost any buffering agent used in antacids can be used. Bufferin, for example, uses MgO. Other drugs use CaCO3.

Taking it with vitamin C is a method of protecting the stomach lining that has been researched recently. Taking equal doses of vitamin C and aspirin may reduce the amount of stomach damage that occurs compared to taking the drug alone.

Action on the central nervous system

Based on experiments in rats, it has been established that large doses of salicylate, a metabolite of aspirin, cause temporary tinnitus (tinnitus) through actions on arachidonic acid and the NMDA receptor cascade.

Reye's syndrome, a rare but serious condition characterized by acute encephalopathy and fatty liver, may occur if children or adolescents are given aspirin for fever or other illnesses or infections. According to the US Centers for Disease Control and Prevention, from 1981 to 1997. There were 1207 cases of Reye's syndrome in patients under the age of 18 years. Of these, 93% reported being sick in the three weeks preceding the onset of Reye's syndrome, most commonly with a respiratory infection, chickenpox, or diarrhea. Salicylates were detected in 81.9% of children with reported test results. Since reports of a link between aspirin and Reye's syndrome and the introduction of safety measures to prevent it (including health care warnings and changes in the labeling of drugs containing it), the number of aspirin administrations to children in the United States has decreased significantly, as has the number of reported cases of Reye's syndrome. A similar decline was noted in the UK after warnings were issued against its use in pediatrics. The FDA now recommends that aspirin should not be given to anyone under 12 years of age with a fever, and the UK Medicines and Healthcare Products Regulatory Agency does not recommend that children under 16 years of age take it unless on the advice of a doctor.

Urticaria and swelling

For a small number of people, taking aspirin may cause symptoms similar to an allergic reaction, including hives, swelling and headache. The reaction is caused by salicylate intolerance and is not a true allergy, but rather an inability to absorb even small amounts of aspirin, resulting in an overdose.

Other side effects

Aspirin can cause angioedema (swelling of skin tissue) in some people. In one study, some patients developed angioedema 1-6 hours after taking it. However, after taking aspirin alone, it did not cause angioedema in these patients. It was taken in combination with another NSAID-induced drug when angioedema appeared.

Aspirin causes an increased risk of cerebral microbleeds, which appear as small (5-10 mm or smaller) hypointense lesions on MRI. Such cerebral microbleeds are important because they often occur before ischemic stroke or intracerebral hemorrhage, Binswanger's disease and Alzheimer's disease.

A group study with a mean aspirin dosage of 270 mg per day estimated the mean increase in absolute risk of intracerebral hemorrhage (ICH) of 12 events per person. In comparison, the estimated absolute risk reduction for myocardial infarction was 137 events per person, as well as a reduction of 39 events per person for ischemic stroke. In cases where ICH has already occurred, the use of aspirin leads to higher mortality at a dosage of about 250 mg per day, resulting in a relative risk of death within 3 months after ICH of about 2.5 (confidence interval 1.3 to 4 .6 at 95%).

Aspirin and other NSAIDs can cause hyperkalemia by inducing a state of hyporenin hypoaldosteronism through inhibition of prostaglandin synthesis. However, these substances do not usually cause hyperkalemia on their own under conditions of normal renal function and normal fluid volumes.

Aspirin can cause prolonged bleeding after surgery for up to 10 days. In one study, 30 of 6499 elective surgical patients required repeat surgery to control bleeding. 20 had diffuse bleeding and 10 had localized bleeding. Diffuse, but not discrete, bleeding was associated with preoperative use of the drug alone or in combination with other NSAIDs in 19 of 20 patients with diffuse bleeding.

Laboratory Findings for Various Platelet and Coagulation (VT) Disorders

Partial thromboplastin time

Vitamin K deficiency or warfarin

Normal or slightly enlarged

Increased or not changed

Liver failure, end stage

Factor V deficiency

Factor X deficiency, as in amyloid purpura

Reduced or not changed

Factor XII deficiency

There are acute and chronic aspirin overdose. When we talk about acute poisoning, we mean that one large dose was taken. In the case of chronic poisoning, we are talking about taking doses higher than usual over a certain period of time. The mortality rate for acute overdose is 2%. Chronic overdose is more likely to be fatal, with a mortality rate of 25%. In children, chronic overdose can be particularly severe. Toxicity is treated through a number of potential treatments, including activated charcoal, intravenous dextrose and saline, sodium bicarbonate, and dialysis. The diagnosis of poisoning usually involves measurement of plasma salicylate, the active metabolite of aspirin, by automated spectrophotometric methods. Plasma salicylate levels in the general range: mg/L after usual therapeutic doses, mg/L in patients taking high doses, mg/L after acute overdose. Salicylate is also produced by exposure to bismuth subsalicylate, methyl salicylate, and sodium salicylate.

Aspirin is known to interact with other drugs. For example, acetazolamide and ammonium chloride are known to enhance the effects of salicylate intoxication, and alcohol also increases gastrointestinal bleeding mediated by these types of drugs. Aspirin is known to displace a number of drugs from protein binding sites in the blood, including the antidiabetic drugs tolbutamide and chlorpropamide, warfarin, methotrexate, phenytoin, probenecid, valproic acid (as well as interfering with beta-oxidation, an important part of valproate metabolism), and other NSAIDs. Corticosteroids may also decrease aspirin concentrations. Ibuprofen may antagonize its antiplatelet effects used for cardioprotection and stroke prevention. The pharmacological activity of spironolactone can be reduced by administration of aspirin, which is known to compete with penicillin G for renal tubular secretion. In addition, it may inhibit the absorption of vitamin C.

Chemical properties

Aspirin quickly decomposes in solutions of acetates or ammonium acetate, citrates, carbonates or hydroxides of alkali metals. It is stable in dry air, but gradually hydrolyzes in contact with moisture into acetic and salicylic acids. In a solution with alkalis, hydrolysis proceeds quickly, and the resulting transparent solutions can consist entirely of acetate and salicylate.

Physical properties

Aspirin, an acetyl derivative of salicylic acid, is a white, crystalline, slightly acidic substance with a melting point of 136°C and a boiling point of 140°C. Its acid dissociation constant (pKa) is 3.5 at 25°C.

The synthesis of aspirin is classified as an esterification reaction. Salicylic acid is treated with acetic anhydride, a derivative of the acid, resulting in a chemical reaction in which the hydroxyl group of salicylic acid is transformed into an ester group (R-OH → R-OCOCH3). This reaction produces aspirin and acetic acid, which is considered a byproduct of this process. Sulfuric acid (and sometimes phosphoric acid) is almost always used in small quantities as a catalyst. Typically, this method is used in student teaching laboratories.

Products containing high concentrations of aspirin often smell like vinegar because it can degrade through hydrolysis under humid conditions, producing salicylic and acetic acids.

In the development of pharmaceutical ingredients, polymorphism, that is, the ability of a substance to form multiple crystal structures, plays an important role. Many drugs receive regulatory approval for only one crystalline form or polymorph. For a long time, only one crystal structure of aspirin was known. Since 1960, it has been suspected that it may have a second crystalline form. The elusive second polymorph was first discovered by Vishweshwar and colleagues in 2005, and fine structural details were determined by Bond et al. After attempting to cocrystallize aspirin and levetiracetam from hot acetonitrile, a new type of crystal was discovered. Form II is the only one stable at 100 K and transforms into form I at ambient temperature. The two salicylic molecules in unambiguous Form I form centrosymmetric dimers via acetyl groups with the (acidic) methyl proton to carbonyl hydrogen bonds, and each salicylic molecule in the newly reported Form II forms identical hydrogen bonds with two neighboring molecules instead of one. With respect to hydrogen bonds formed by carboxylic acid groups, both polymorphs form identical dimeric structures.

Mechanism of action of aspirin

In 1971 D.R. Vane, a British pharmacologist who later worked at the Royal College of Surgeons of London, discovered that aspirin suppressed the production of prostaglandins and thromboxanes. For this discovery he was awarded the Nobel Prize in Physiology or Medicine in 1982 together with S.K. Bergstrom and B.I. Samuelson. In 1984 he became the holder of the title of Knight Bachelor.

Inhibition of prostaglandins and thromboxanes

Aspirin's ability to suppress the production of prostaglandins and thromboxanes is due to its irreversible inactivation of the enzyme cyclooxygenase (COX; formally known as prostaglandin endoperoxide synthase, PTGS), required for prostaglandin and thromboxane synthesis. Aspirin acts as an acylating agent, where the acetyl group is covalently attached to a serine residue in the active site of the PTGS enzyme. This makes it different from other NSAIDs (eg, diclofenac and ibuprofen), which are reversible inhibitors.

Low doses of the drug irreversibly block the formation of thromboxane A2 in platelets, producing an inhibitory effect on platelet aggregation during the life of the affected platelets (8-9 days). This antithrombotic property makes aspirin useful in reducing the incidence of heart attacks. A dose of 40 mg per day was able to inhibit most of the maximal release of acutely provoked thromboxane A2, although prostaglandin I2 synthesis was slightly affected. However, to achieve further inhibition, doses of aspirin must be higher.

Prostaglandins, local hormones produced in the body, have a variety of effects, including transmitting pain information to the brain, modulating the hypothalamic thermostat, and inflammation. Thromboxanes are responsible for the aggregation of platelets, which form blood clots. Heart attacks are caused primarily by blood clots, and low-dose aspirin is considered an effective medical intervention for acute myocardial infarction. An undesirable side effect of the drug's antithrombotic effect is that it may cause excessive bleeding.

Inhibition of COX-1 and COX-2

There are at least two different types of cyclooxygenase: COX-1 and COX-2. The action of aspirin is aimed at irreversibly inhibiting COX-1 and changing the enzymatic activity of COX-2. Typically, COX-2 produces prostanoids, most of which are proinflammatory. Aspirin-modified PTGS2 produces lipoxins, most of which are anti-inflammatory. New NSAID drugs, the COX-2 inhibitors (coxibs), have been developed to inhibit only PTGS2, with the goal of reducing the incidence of gastrointestinal side effects.

However, some new COX-2 inhibitors, such as rofecoxib (Vioxx), were withdrawn recently after evidence emerged that PTGS2 inhibitors increase the risk of heart attack and stroke. Endothelial cells lining microvessels in the body are thought to secrete PTGS2, and, through selective inhibition of PTGS2, prostaglandin (specifically PGI2; prostacyclin) production is suppressed relative to thromboxane levels, as PTGS1 in platelets remains intact. Thus, the protective anti-clotting effect of PGI2 is removed, increasing the risk of blood clots and associated heart attacks and other circulatory problems. Because platelets do not have DNA, they are unable to synthesize new PTGS because aspirin irreversibly inhibits the enzyme, an important difference from reversible inhibitors.

Aspirin has been shown to have at least three additional modes of action. It uncouples oxidative phosphorylation in cartilage (and liver) mitochondria by diffusion from the interior of the membrane as a proton carrier back into the mitochondrial matrix, where it ionizes again to release protons. In short, aspirin buffers and transports protons. When high doses are administered, it can actually cause fever due to the heat generated from the electron transport chain, in contrast to its antipyretic effect observed at lower doses. In addition, aspirin causes the formation of NO radicals in the body, which in mice had an independent mechanism to reduce inflammation. This resulted in decreased leukocyte adhesion, an important step in the immune response to infections. Currently, however, there is insufficient evidence to suggest that aspirin helps fight infection. More recent data also suggest that salicylic acid and its derivatives modulate signaling through NF-kB. NF-κB, a transcription factor complex, plays a central role in many biological processes, including inflammation.

Aspirin is easily broken down in the body into salicylic acid, which itself has anti-inflammatory, antipyretic and analgesic effects. In 2012, salicylic acid was found to activate AMP-activated protein kinase, and this has been proposed as a possible explanation for some of the effects of both salicylic acid and aspirin. The acetyl part of the drug molecule is not without its own purposes. Acetylation of cellular proteins is a well-established phenomenon in the regulation of protein function at the post-translational level. Recent studies have shown that aspirin is able to acetylate several other targets in addition to COX isoenzymes. These acetylation reactions may explain its many hitherto unexplained effects.

Like other drugs that affect prostaglandin synthesis, aspirin has profound effects on the pituitary gland, which indirectly affects a number of other hormones and physiological functions. Direct effects were observed on growth hormone, prolactin and TSH (with corresponding effects on T3 and T4). Aspirin reduces the effects of vasopressin and enhances the effects of naloxone on ACTH and cortisol secretion in the hypothalamic-pituitary-adrenal (HPA) axis, which is thought to occur through interactions with endogenous prostaglandins and their role in regulating the HPA axis.

Pharmacokinetics of aspirin

Salicylic acid is a weak acid and very little of it ionizes in the stomach after oral administration. Acetylsalicylic acid is poorly soluble in acidic gastric conditions, which may delay the absorption of large doses for 8-24 hours. The increased pH and larger surface area of ​​the small intestine causes aspirin to be absorbed more quickly into the small intestine, which in turn allows more salicylate to dissolve. Due to this solubility problem, however, it is absorbed much more slowly in overdose, and plasma concentrations may continue to rise for up to 24 hours after administration.

About 50-80% of salicylic acid in the blood is bound to the albumin protein, while the rest remains in an active, ionized state; protein binding is concentration dependent. Saturation of binding sites results in more free salicylate and increased toxicity. The volume of distribution is 0.1-0.2 l/g. Due to acidosis, the volume of distribution increases due to increased penetration of salicylates into tissues.

Up to 80% of therapeutic doses of salicylic acid are metabolized in the liver. Combined with glycine it forms salicyluric acid, and with glucuronic acid it forms salicylic acyl and phenolic glucuronide. These metabolic pathways have only limited capabilities. Salicylic acid is also hydroxylated to gentisic acid in small amounts. At high doses of salicylate, the kinetics switch from first order to zero order as metabolic pathways become saturated and renal excretion becomes increasingly important.

Salicylates are excreted from the body mainly by the kidneys in the form of salicyluric acid (75%), free salicylic acid (10%), salicylic phenol (10%) and acyl glucuronides (5%), gentisic acid (<1%) and 2,3- dihydroxybenzoic acid. When absorbed in small doses (less than 250 mg for an adult), all pathways are reactivated by first-order kinetics, with a half-life of approximately 2-4.5 hours. Upon absorption of higher doses of salicylate (more than 4 g), the half-life becomes much longer (15-30 hours) as the biotransformation pathways associated with the formation of salicyluric acid and salicylic phenolic glucuronide become saturated. Renal excretion of salicylic acid becomes increasingly important when metabolic pathways become saturated because it is extremely sensitive to changes in urinary pH. When urine pH increases from 5 to 8, there is an immediate increase in renal clearance. The use of urinary alkalinization exploits this aspect of salicylate elimination.

History of aspirin

Since ancient times, plant extracts including willow bark and spirea, whose active ingredient is salicylic acid, have been known to help relieve headaches, aches and fevers. The father of modern medicine, Hippocrates (c. BC), left historical records describing the use of a powder made from willow bark and leaves to help with these symptoms.

French chemist, Charles Frederic Gerhardt, was the first to prepare acetylsalicylic acid in 1853. In the course of his work on the synthesis and properties of various acid anhydrides, he mixed acetyl chloride with the sodium salt of salicylic acid (sodium salicylate). A violent reaction followed, and the resulting melt soon solidified. Since a structural theory did not exist at the time, Gerhardt named his compound "salicylic acetic anhydride." This aspirin preparation was one of many reactions Gerhardt carried out for his reports on anhydrides and which he did not pursue further.

6 years later, in 1859, Von Gilm obtained analytically pure acetylsalicylic acid (which he called acetylated salicylic acid) using the reaction of salicylic acid and acetyl chloride. In 1869, Schröder, Prinzhorn and Kraut repeated the synthesis of Gerhardt (from sodium salicylate) and Von Gtlm (from salicylic acid) and concluded that both reactions gave the same compound, acetylsalicylic acid. They were the first to assign it the correct structure with an acetyl group attached to a phenolic oxygen.

In 1897, chemists working for Bayer AG produced a synthetically modified version of salicin, derived from the meadowsweet species Filipendula ulmaria (meadowsweet), which caused less digestive upset than pure salicylic acid. The identity of the lead chemist on this project is a matter of debate. Bayer claims that the work was done by Felix Hoffmann, but Jewish chemist Arthur Eichengrun later claimed that he was the lead researcher and that records of his contributions were destroyed under the Nazi regime. The new drug, officially acetylsalicylic acid, was named aspirin by Bayer AG after the old botanical name for meadowsweet, Spiraea ulmaria . By 1899 Bayer was selling it worldwide. The name "aspirin" is derived from "acetyl" and "Spirsäure", the old German name for salicylic acid. Aspirin grew in popularity in the first half of the 20th century due to its supposed effectiveness as a result of the 1918 Spanish flu pandemic. However, recent research suggests that the high death rate from the 1918 influenza was partly due to aspirin, although this is highly controversial and is not widely accepted. The profitability of aspirin led to intense competition and proliferation of aspirin brands and products, especially after Bayer's American patent expired in 1917.

Aspirin's popularity declined following the market introduction of paracetamol (acetaminophen) in 1956 and ibuprofen in 1969. In the 1960s and 1970s, John Wayne and others discovered the underlying mechanism of action of aspirin, and clinical trials and other studies from the 1960s to the 1980s. have established the effectiveness of aspirin as an anticoagulant agent that reduces the risk of clotting disorders. Sales of aspirin increased significantly in the last decades of the 20th century, and remain strong into the 21st century due to its widespread use as a preventative treatment for heart attacks and strokes.

As part of war reparations specified in the 1919 Treaty of Versailles following Germany's surrender after World War I, aspirin (along with heroin) lost its registered trademark status in France, Russia, the UK and the US, where it became a generic name. Today, aspirin is the generic name in Australia, France, India, Ireland, New Zealand, Pakistan, Jamaica, Colombia, the Philippines, South Africa, the UK and the USA. Aspirin, with a capital "A", remains a registered trademark of Bayer in Germany, Canada, Mexico and over 80 other countries where the trademark is owned by Bayer, using acetylsalicylic acid in all markets, but using different packaging and physical aspects for each .

Veterinary uses of aspirin

Aspirin is sometimes used for pain relief or as an anticoagulant in veterinary medicine, primarily in dogs and sometimes in horses, although newer medications with fewer side effects are usually used instead.

Both dogs and horses are susceptible to developing gastrointestinal side effects associated with salicylates, but it is a useful treatment for arthritis in older dogs, and is somewhat reassuring in cases of laminitis in horses. It is no longer commonly used for cases of laminitis as it may be counterproductive to treatment.

Aspirin should only be used in animals under the direct supervision of a veterinarian. In particular, cats lack the glucuronide conjugates that aid in the excretion of aspirin, making even low doses potentially toxic.

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