Aspirin Chemistry. Acetylsalicylic acid. Side effects of the substance Acetylsalicylic acid
Do heroin and aspirin have the same creator?
Friedrich Bayer
Friedrich Bayer was born in 1825. He was the only son in a family of six children. His father was a weaver and dyer, and Bayer followed in his footsteps. In 1848, he opened his own paint business, which quickly became successful. In the past, all dyes were made from organic materials, but in 1856 dyes were discovered that could be made from coal tar derivatives, sparking a revolution in the textile industry. 
Bayer and Friedrich Wescott (chief painter) saw the great potential for the development of this direction, and in 1863 they created their own paint company "Friedrich Bayer et Compagnie".
Aspirin Hoffman.
Bayer died on May 6, 1880, at which time his company was still in the fabric dye business. The company continued to hire chemists to come up with innovative 
e paints and products, and in 1897 luck smiled at one of the chemists. His name was Felix Hoffman.
The persistent chemist was looking for a cure for his father's rheumatism. And as a result of experiments with an unnecessary product of one of the components of the paint, he was able to chemically synthesize a stable form of salicylic acid powder.
The compound has become the active ingredient in many pharmaceutical products called "aspirin". The name comes from "a" from acetyl, and "spir" from the name of the spirea plant, (Filipendula ulmaria, also known as Spiraea ulmaria or meadowsweet), a source of salicin.
Another version of the origin of the name was the name of the patron saint of all those suffering from a headache, St. Aspirinus.
This medicine has been used for 3500 years!
However, Hoffman was not the first to discover and synthesize "aspirin". 40 years earlier, the French chemist Charles Gerhardt had already synthesized acetylsalicylic acid. In 1837, Gerhardt came up with good results, but the procedure was complicated and time consuming. So he decided it was not practical and put the experiments on hold. However, Gerhardt was quite well aware of the potential possibilities of treatment with acetylsalicylic acid, because this has been known for over 3500 years!
In early 1800, German Egyptologist Georg Ebers bought papyri from an Egyptian street vendor.
The Ebers Papyrus is known to have contained a collection of 877 medicinal prescriptions dated to 2500 BC and specifically recommended that an infusion of dried myrtle be used to reduce rheumatic back pain.
As early as 400 BC, Hippocrates, the father of all doctors, recommended extracting tea from the bark of the willow tree to treat fever and pain.
The active ingredient in this juice that actually actually relieves pain, as we know today, is salicylic acid.
Scientists have confirmed that the bitter part of the willow bark is a natural source of the chemical salicin. This chemical can be converted to salicylic acid. Aspirin is a member of this family of chemicals named after salicylic acid esters.
In China and Asia, among the North American Indians and the tribes of South Africa, the beneficial effects of plants containing salicylic acid have been known since early times.
Breakthrough and authorship.
One of the first to try to meet the need for a synthetic substitute for natural antipyretics was the German company Heyden Chemical Co, which built its own salicylic acid factory in 1874.
However, while the salicylic acid extracted from willow bark did reduce pain, its side effect was severe stomach and mouth irritation. Patients of that time were faced with a choice: the harmless expensive salicin (in London in 1877 it cost about 50 pence an ounce) or cheap salicylic acid (5 pence an ounce) with a risk to the stomach.
Hoffmann's breakthrough came on August 10, 1897, when he first produced a 100% chemically pure form of acetylsalicylic acid, i.e. without natural salicylic acid.
On March 6, 1899, Bayer registered aspirin as trademark. But still not without problems.
Deputy Dean of the Faculty of Pharmacy at the University of Strathclyde in Glasgow, Professor Walter Snyder put forward his version of authorship. According to her, the creator of aspirin is Arthur Eichengrün, also a Bayer chemist, but of Jewish origin, unlike Hoffman with Aryan roots. By the time of publication in the history of the sick father and the authorship of Hoffman in 1934 in Germany, this was quite relevant for well-known reasons.
Humanity still uses other inventions of Eichengrün to this day: these are fireproof films, fabrics, plastic furniture and antifreeze.
Despite the successful cooperation of the scientist with this largest German concern in 1944, the 76-year-old chemist was nevertheless sent to the Theresienstadt concentration camp in the Czech Republic, and his property was confiscated. 
In 1945 he was liberated by the Red Army. And only shortly before his death (“horrified by the very thought that injustice would triumph for another half century”), in his article-testament in Pharmazie, he wrote the true development of events. Eichengrün outlived his article by two weeks. Bayer AG does not support this version of the birth of aspirin.
Initially, the achievement of the company in 1899 received trade certificates only in the United States. In England and Germany, other companies insisted on their own authorship.
However, at that time, Hoffman's written evidence prevailed, in addition, the company patented technological process mass production of aspirin. And she thought of publishing a 200-page catalog of her medicines, among which the novelty stood out especially, and sending it to 30,000 practicing doctors in Europe. .
And when Hoffman retired in 1928, aspirin was known all over the world. Despite this, the chemist lived until his death on February 8, 1946 in Switzerland as an unrecognized author.
Do aspirin and heroin share the same creator?
Aspirin was Bayer's most remarkable success, but not the only one. A few days after Hoffman had succeeded in synthesizing acetylsalicylic acid, he produced another compound for which the Bayer company had big plans. Today, this discovery is of dubious value.
Diacetylmorphine (or heroin), a substance that had also been discovered several decades earlier by the English chemist C.R.A. Wright. Heroin was cautiously recommended by pharmacists during World War I, but by 1931 it had disappeared from the drug lists in almost every country. In 1924, a federal law was passed in the United States that banned its production, sale and consumption.
Additional facts.
Felix Hoffmann was born in Ludwigsburg in 1868. He carried out his pharmaceutical research at the University of Munich. April 1, 1894 joined Friedrich Bayer & Co. After the discovery of pure acetylsalicylic acid, he became the head of the pharmaceutical department.
Friedrich Bayer's company initially produced only anilines. Its founder died in 1880, unaware that Bayer was destined to become a pharmaceutical giant. By 1891, Bayer introduced a different product range. Today, it is more than 10,000 products.
In the 1930s, an employee of the company, (surprisingly) bearing the same last name (Otto Bayer), invented polyurethane.
German microbiologist Gerhard Domagk ("Bayer"), together with colleagues discovered the therapeutic effect of sulfonamides. This discovery revolutionized the chemotherapy of infectious diseases, and Domagku won the Nobel Prize in 1939.
Since 1950 aspirin has become known as a preventative drug in the fight against heart disease, in 37.6% of cases people take aspirin in this capacity (for headaches - only 23.3%).
Aspirin was also used in space as part of the first aid package for the American astronauts of Apollo 11 (lunar module).
The Bayer company is constantly fighting the "leftist" manufacturers of its famous aspirin. That is why the well-known "Soviet" aspirin has long been called acetylsalicylic acid.
Composition and chemical properties of aspirin.
Aspirin tablets contain the active ingredient acetylsalicylic acid, which is the acetic ester of salicylic acid.
The full chemical name of acetylsalicylic acid is as follows:
2-acetoxy-benzoic acid
Physico- Chemical properties
Brief chemical formula: C9H8O4
Molecular mass: 180.2
Melting temperature: 133 - 138 0 С
Dissociation constant: pKa 3.7
Synthesis
Acetylsalicylic acid is produced by heating salicylic acid with acetic anhydride.
Identification
When heated with sodium hydroxide (NaOH) in an aqueous solution, acetylsalicylic acid hydrolyzes to sodium salicylate and sodium acetate. When the medium is acidified, salicylic acid precipitates and can be identified by its melting point (156-160 0 C). Another method for identifying salicylic acid formed during hydrolysis is the coloration of its solution in a dark purple color when iron chloride (FeCl3) is added. The acetic acid present in the filtrate is converted by heating with ethanol and sulfuric acid to ethoxyethanol, which can be easily recognized by its characteristic odour. In addition, acetylsalicylic acid can be identified using various chromatographic methods.
Properties
Acetylsalicylic acid crystallizes to form colorless monoclinic polyhedra or needles that taste slightly sour. They are stable in dry air but gradually hydrolyze to salicylic acid and acetic acid in humid environments (Leeson and Mattocks, 1958; Stempel, 1961). The pure substance is a white crystalline powder, almost odorless. The smell of acetic acid indicates that the substance has begun to hydrolyze. Acetylsalicylic acid undergoes esterification under the action of alkaline hydroxides, alkaline bicarbonates, and also in boiling water.
Acetylsalicylic acid is poorly soluble in water, soluble in ether and chloroform, and readily soluble in 96% ethanol.
One part of acetylsalicylic acid dissolves in
300 parts of water
20 parts of ether
17 parts of chloroform
7 parts 96% ethanol
The solubility of acetylsalicylic acid in water and aqueous media is highly dependent on the pH level. At pH=2, its solubility in water does not exceed 60 µl/l, however, it rapidly increases as the pH value increases (increase in alkalinity) due to increasing dissociation.
In medical practice, there are several centuries-old medicines that have firmly retained their place in the "golden fund" medicines. One of these drugs, of course, is aspirin (ASA, acetylsalicylic acid), the 100th anniversary of which was celebrated by the German company Bayer in 1999.
Aspirin is one of the most widely used medicines in the world. More than 100 different pain relievers are currently offered in Russia, and almost all of them contain aspirin as the main ingredient.
Indications for the use of ASA in last years significantly expanded, antithrombotic action comes to the fore:
Patients with prosthetic heart valves have to take aspirin for life in order to prevent thrombosis in the area of artificial valves, after coronary artery bypass grafting for coronary heart disease, to prevent recurrent myocardial infarction, patients with transient disorders
cerebral blood supply to prevent ischemic stroke
At least 4.5 million people take aspirin at least once a week, and 500,000 take more than 5 tablets a week. The total scale of aspirin production in the world is thousands of tons per year. In 1994, 11,600 tons of aspirin were consumed in the world, or about 30 therapeutic doses per person per year.
The history of aspirin began about 4,000 years ago. Egyptian papyri that date back to around 1550 BC mention the use of a decoction of white willow leaves for many ailments. Hippocrates (460-377 BC) recommended juice made from the bark of the same tree to treat pain and fever. The healing effect of willow in medicine was also well known in America (before its "discovery" by Columbus). Willow is the first source of aspirin. By the middle of the XVIII century. willow bark was already widely known folk remedy for the treatment of colds.
In 1757, the priest E. Stone from Oxfordshire (Great Britain), became interested in the extreme bitterness of willow bark, similar in taste to cinchona, a rare and expensive remedy for the treatment of malaria.
On June 2, 1763, speaking before the Royal Society, Stone, based on the results of his research, justified the use of willow bark infusion in diseases accompanied by a feverish state.
More than half a century later, intensive research began on the active principle of willow bark. In 1829, the French pharmacist Pierre-Joseph Leroux obtained a crystalline substance from willow bark, which he called salicyl (this name comes from the Latin name "salix" - the name of the plant, first mentioned in the works of the Roman scientist and encyclopedist Varro (116-27 years BC). AD) and related to willow (willow, willow), The content of salicin in willow is approximately 2% by weight of dry matter .. In 1838-1839, the Italian scientist R. Piria split salicyl, showing that this compound is a glycoside, and, having oxidized its aromatic fragment, he obtained a substance which he called salicylic acid.
At first, salicyl was obtained industrially from peeled willow bark, which was a waste from basket industries in Belgium, and this is not a large number of salicin met current needs. However, already in 1874, the first large factory for the production of synthetic salicylates was founded in Dresden.
In 1888, the Bayer company, which until then had been engaged only in the production of aniline dyes, created a pharmaceutical department, and the company was one of the first to be involved in the production of drugs.
The low cost of salicylic acid made it possible to widely use it in medical practice, but treatment with this drug was fraught with many dangers associated with its toxic properties. The toxicity of salicylic acid was the reason that led to the discovery of aspirin.
Felix Hoffmann (1868-1946), a Bayer employee, had an elderly father who suffered from arthritis but was intolerant of sodium salicylates due to chronic acute stomach irritation. A caring chemist son in the chemical literature found data on acetylsalicylic acid,. which was synthesized 30 years earlier by Charles Gerhardt in 1853 and had a lower acidity ..
On October 10, 1897, F. Hoffmann described a method for obtaining almost pure acetylsalicylic acid (ASA) and its testing revealed high pharmacological activity. Acetylsalicylic acid was more palatable and did not have an irritating effect.
The name "aspirin" was given to the new drug, taking the letter "a" from the word "acetyl" (acetyl) and the part "spirin" from the German word "Spirsaure", which in turn came from the Latin name of the meadowsweet (Spiraea ulmaria) - a plant containing large amounts of salicylic acid.
In 1899, Bayer began manufacturing a drug called aspirin as an analgesic, antipyretic, and pain reliever.
Over the course of a century, Bayer chemists, as well as others, made numerous attempts to study the effect of changes in the structure of salicylic acid derivatives on their activity, and thus find compounds that are superior to aspirin. The influence of the chain length of the acyl group of aspirin, and various substituents in the cycle, was investigated. We studied various salts of aspirin - calcium, sodium, lithium, as well as lysine acetylsalicylate, which are better soluble in water than acetylsalicylic acid itself.
The presence of an acetyl group in aspirin is a condition for pharmaceutical action. (The molecular basis of the mechanism of action is studied in the course of biochemistry)
Some of the compounds listed above have been introduced into medical practice, and although some drugs have had an advantage over aspirin (especially in the treatment of rheumatism), none of them has ever gained such wide popularity.
Structural formula
True, empirical, or gross formula: C 9 H 8 O 4
The chemical composition of Acetylsalicylic acid
Molecular weight: 180.159
Acetylsalicylic acid(colloquial aspirin; lat. Acidum acetylsalicylicum, salicylic ester of acetic acid) is a drug that has an analgesic (pain reliever), antipyretic, anti-inflammatory and antiplatelet effect. The mechanism of action and safety profile of acetylsalicylic acid are well studied, its effectiveness has been clinically tested, in connection with which this drug is included in the list of essential medicines of the World Health Organization, as well as in the list of vital and essential medicines of the Russian Federation. Acetylsalicylic acid is also widely known under the trade name "Aspirin", patented by Bayer.
Story
Traditional medicine has long recommended the bark of young branches of the white willow as an antipyretic, for example, for preparing a decoction. The bark also received recognition from physicians under the name Salicis cortex. However, all existing willow bark therapeutics have had a very serious side effect - they caused severe abdominal pain and nausea. In a stable form suitable for purification, salicylic acid was first isolated from willow bark by the Italian chemist Rafel Piria in 1838. It was first synthesized by Charles Frederic Gerard in 1853. In 1859, chemistry professor Hermann Kolbe from the University of Marburg revealed the chemical structure of salicylic acid, which made it possible to open the first factory for its production in Dresden in 1874. In 1875, sodium salicylate was used to treat rheumatism and as an antipyretic. Soon its glucosuric effect was established, and salicin began to be prescribed for gout. On August 10, 1897, Felix Hoffman, who worked in the laboratories of Bayer AG, first received samples of acetylsalicylic acid in a form that was possible for medical use; using the acetylation method, he became the first chemist in history to obtain salicylic acid in a chemically pure and stable form. Along with Hoffman, Arthur Eichengrün is also called the inventor of aspirin. The bark of the willow tree served as the raw material for the production of acetylsalicylic acid. Bayer has registered a new drug under the brand name aspirin. Hoffman opened medicinal properties acetylsalicylic acid, trying to find a cure for his father, who suffered from rheumatism. In 1971, pharmacologist John Wayne demonstrated that acetylsalicylic acid inhibits the synthesis of prostaglandins and thromboxanes. For this discovery in 1982, he, as well as Suna Bergström and Bengt Samuelson, were awarded the Nobel Prize in Medicine; in 1984 he was awarded the title of Knight Bachelor.
Brand name Aspirin
After much debate, they decided to take as a basis the already mentioned Latin name of the plant, from which the Berlin scientist Karl Jakob Lovig first isolated salicylic acid - Spiraea ulmaria. To the four letters "spir" they added "a" to emphasize the special role of the acetylation reaction, and on the right - for euphony and in accordance with the established tradition - "in". It turned out easy to pronounce and easy to remember the name Aspirin. Already in 1899, the first batch of this medicine went on sale. Initially, only the antipyretic effect of aspirin was known, later its analgesic and anti-inflammatory properties were also found out. In the early years, aspirin was sold as a powder, but from 1904 it was sold as a tablet. In 1983, a study appeared in the New England Journal of Medicine, which proved a new important property of the drug - when it is used during unstable angina, the risk of such an outcome of the disease as myocardial infarction or death is reduced by 2 times. Acetylsalicylic acid also reduces the risk of getting cancer, in particular, of the breast and colon.
Mechanism of action
Suppression of the synthesis of prostaglandins and thromboxanes. Acetylsalicylic acid is an inhibitor of cyclooxygenase (PTGS) - an enzyme involved in the synthesis of prostaglandins and thromboxanes. Acetylsalicylic acid acts in the same way as other non-steroidal anti-inflammatory drugs (in particular, diclofenac and ibuprofen), which are reversible inhibitors. Thanks to the remark of the Nobel laureate John Wayne, which he expressed as a hypothesis in one of his articles, it was long believed that acetylsalicylic acid acts as a suicidal inhibitor of cyclooxygenase, acetylation of the hydroxyl group in the active site of the enzyme. Further research has shown that this is not the case.
pharmachologic effect
Acetylsalicylic acid has an anti-inflammatory, antipyretic and analgesic effect, and it is widely used for fever, headache, neuralgia, etc., and as an antirheumatic agent. The anti-inflammatory effect of acetylsalicylic acid (and other salicylates) is explained by its influence on the processes occurring in the inflammation focus: a decrease in capillary permeability, a decrease in hyaluronidase activity, a restriction of the energy supply of the inflammatory process by inhibiting the formation of ATP, etc. In the mechanism of anti-inflammatory action, inhibition of prostaglandin biosynthesis is important. The antipyretic effect is also associated with the effect on the hypothalamic centers of thermoregulation. The analgesic effect is due to the effect on the centers of pain sensitivity, as well as the ability of salicylates to reduce the algogenic effect of bradykinin. The blood-thinning effect of acetylsalicylic acid makes it possible to use it to reduce intracranial pressure in case of headaches. Salicylic acid was the basis for a whole class of drugs called salicylates, an example of such a drug is dihydroxybenzoic acid.
Application
Acetylsalicylic acid is widely used as an anti-inflammatory, antipyretic and analgesic agent. It is used alone and in combination with other drugs. There are a number of finished medicines containing acetylsalicylic acid (tablets "Citramon", "Cofitsil", "Asfen", "Askofen", "Acelizin", etc.). AT recent times injectable preparations were obtained, the main active principle of which is acetylsalicylic acid (see Acelizin, Aspizol). In the form of tablets, acetylsalicylic acid is prescribed orally after meals. Usual doses for adults as an analgesic and antipyretic (for febrile illnesses, headaches, migraines, neuralgia, etc.) 0.25-0.5-1 g 3-4 times a day; for children, depending on age, from 0.1 to 0.3 g per reception. With rheumatism, infectious-allergic myocarditis, rheumatoid arthritis, adults are prescribed for a long time at 2-3 g (less often 4 g) per day, for children at 0.2 g per year of life per day. A single dose for children aged 1 year is 0.05 g, 2 years - 0.1 g, 3 years - 0.15 g, 4 years - 0.2 g. .25 g per reception. Acetylsalicylic acid is an effective, quite affordable tool that is widely used in outpatient practice. It should be borne in mind that the use of the drug should be carried out with the observance of precautionary measures due to the possibility of a number of side effects. Many cases are described when ingestion of even 40 grams of ethanol (100 grams of vodka) in combination with such conventional drugs as aspirin or amidopyrine was accompanied by severe allergic reactions, as well as gastric bleeding. The use of acetylsalicylic acid in everyday life is widespread, as a means of alleviating suffering in the morning after alcohol poisoning (to relieve a hangover). It is an integral component in the well-known Alka-Seltzer drug. According to research by Professor Peter Rothwell (Oxford University), based on an analysis of the health status of 25,570 patients, regular intake of acetylsalicylic acid reduces the 20-year risk of developing prostate cancer by about 10%, lung cancer by 30%, and intestinal cancer - by 40%, cancer of the esophagus and throat - by 60%. Regular intake of acetylsalicylic acid for more than 5 years at a dose of 75 to 100 mg reduces the risk of colorectal cancer by up to 16%.
Antiplatelet action
An important feature of acetylsalicylic acid is its ability to have an antiplatelet effect, that is, to prevent spontaneous and induced platelet aggregation. Substances that have an antiplatelet effect are widely used in medicine to prevent the formation of blood clots in people who have had a myocardial infarction, cerebrovascular accident, who have other manifestations of atherosclerosis (for example, angina pectoris, intermittent claudication), as well as at high cardiovascular risk. The risk is considered "high" when the risk of non-fatal myocardial infarction or death due to heart disease in the next 10 years is greater than 20%, or the risk of death from any cardiovascular disease (including stroke) in the next 10 years is greater than 5%. With bleeding disorders, such as hemophilia, the possibility of bleeding increases. Acetylsalicylic acid, as a means of primary prevention of complications of atherosclerosis, can be effectively used at a dose of 75-100 mg / day, this dose is well balanced in terms of efficacy / safety. Acetylsalicylic acid is the only antiplatelet drug whose efficacy when administered in the acute period of ischemic stroke is supported by evidence-based medicine. The studies demonstrated a trend towards a decrease in mortality both during the first 10 days and within 6 months after ischemic stroke, in the absence of severe hemorrhagic complications.
Side effect
Safe daily dose of acetylsalicylic acid: 4 g. Overdose leads to severe pathologies of the kidneys, brain, lungs and liver. Medical historians believe that the massive use of acetylsalicylic acid (10-30 g each) significantly increased mortality during the 1918 flu pandemic. When using the drug, profuse sweating may also develop, tinnitus and hearing loss, angioedema, skin and other allergic reactions . The so-called ulcerogenic (causing the appearance or exacerbation of gastric and / or duodenal ulcers) action is characteristic to one degree or another of all groups of anti-inflammatory drugs: both corticosteroid and non-steroidal (for example, butadione, indomethacin, etc.). The appearance of stomach ulcers and gastric bleeding when using acetylsalicylic acid is explained not only by the resorptive effect (inhibition of blood coagulation factors, etc.), but also by its direct irritant effect on the gastric mucosa, especially if the drug is taken in the form of unground tablets. This also applies to sodium salicylate. With prolonged, without medical supervision, the use of acetylsalicylic acid may experience side effects such as dyspeptic disorders and gastric bleeding. To reduce the ulcerogenic effect and gastric bleeding, acetylsalicylic acid (and sodium salicylate) should be taken only after meals, it is recommended that the tablets be carefully crushed and washed down with plenty of liquid (preferably milk). There is, however, evidence that gastric bleeding can also be observed when taking acetylsalicylic acid after meals. Sodium bicarbonate contributes to a more rapid release of salicylates from the body, however, to reduce the irritating effect on the stomach, they resort to taking mineral alkaline waters or sodium bicarbonate solution after acetylsalicylic acid. Abroad, acetylsalicylic acid tablets are produced in an enteric (acid-resistant) shell in order to avoid direct contact of ASA with the stomach wall. With prolonged use of salicylates, the possibility of developing anemia should be considered and systematically perform blood tests and check for the presence of blood in the feces. Due to the possibility of allergic reactions, caution should be exercised when prescribing acetylsalicylic acid (and other salicylates) to persons with hypersensitivity to penicillins and other "allergenic" drugs. With increased sensitivity to acetylsalicylic acid, aspirin asthma may develop, for the prevention and treatment of which methods of desensitizing therapy have been developed using increasing doses of acetylsalicylic acid. It should be borne in mind that under the influence of acetylsalicylic acid, the effect of anticoagulants (derivatives of coumarin, heparin, etc.), sugar-lowering drugs (derivatives of sulfonylurea), increases the risk of gastric bleeding with the simultaneous use of corticosteroids and non-steroidal anti-inflammatory drugs (NSAIDs), increase side effects methotrexate. The effect of furosemide, uricosuric agents, spironolactone is somewhat weakened.
In children and pregnant women
In connection with the available experimental data on the teratogenic effect of acetylsalicylic acid, it is not recommended to prescribe it and its preparations to women in the first 3 months of pregnancy. The use of non-narcotic painkillers (aspirin, ibuprofen and paracetamol) during pregnancy increases the risk of developmental disorders of the genital organs in newborn boys in the form of cryptorchidism. The results of the study showed that the simultaneous use of two of the three listed drugs during pregnancy increases the risk of having a baby with cryptorchidism by up to 16 times compared with women who did not take these drugs. Currently, there is evidence of the possible danger of using acetylsalicylic acid in children to reduce the temperature in influenza, acute respiratory and other febrile diseases in connection with the observed cases of the development of Reye's syndrome (Reye) (hepatogenic encephalopathy). The pathogenesis of Reye's syndrome is unknown. The disease proceeds with the development of acute liver failure. The incidence of Reye's syndrome among children under 18 years of age in the United States is approximately 1:100,000, while the mortality rate exceeds 36%.
Contraindications
Peptic ulcer of the stomach and duodenum and bleeding are contraindications to the use of acetylsalicylic acid and sodium salicylate. The use of acetylsalicylic acid is also contraindicated in patients with a history of peptic ulcer, portal hypertension, venous congestion (due to a decrease in the resistance of the gastric mucosa), and in violation of blood clotting. Acetylsalicylic acid preparations should not be prescribed to children under 12 years of age to reduce body temperature in viral diseases due to the possibility of developing Reye's syndrome. It is recommended to replace acetylsalicylic acid with paracetamol or ibuprofen. Some people may develop what is called aspirin asthma.
Matter properties
Acetylsalicylic acid is white small needle-shaped crystals or light crystalline powder of slightly acidic taste, slightly soluble in water at room temperature, soluble in hot for 30 minutes. After cooling. Acetylsalicylic acid, when heated above 200 degrees Celsius, becomes an extremely active flux that dissolves oxides of copper, iron and other metals. in the presence of sulfuric acid. The product is recrystallized for purification. The yield is about 80%.
Facts
- In Russia, the traditional household name for acetylsalicylic acid is aspirin. Based on the traditional nature of the term, Bayer was denied registration of the Aspirin brand in Russia.
- More than 80 billion aspirin tablets are consumed annually.
- In 2009, researchers discovered that salicylic acid, of which acetylsalicylic acid is a derivative, can be produced by the human body.
- Acetylsalicylic acid is used as an active acid flux in soldering and tinning with fusible solders.
- Scientists have found that aspirin can help treat many cases of infertility in women, because. it counteracts the inflammation caused by the protein, the increased content of which is the cause of miscarriages. Women can increase their chances of getting pregnant by taking limited doses of aspirin.
Aspirin is the colloquial name for acetylsalicylic acid. Today, this drug is included in the list of essential medicines of the World Health Organization (WHO) and in the list of vital and essential medicines in Russia.
But in the pre-aspirin era most of diseases had no treatment and was often referred to in one word - “heat”, and only not always effective and far from fast-acting herbal decoctions and expensive opiates could alleviate suffering and relieve pain.
willow bark
Only at the end of the 18th century was salicin discovered - an element responsible for the therapeutic effect of a decoction of willow bark, which had a powerful antipyretic effect. But salicin was also expensive due to the complexity of production, and salicylic acid acted worse and had a strong side effect - it destroyed the patient's gastrointestinal tract.
Thus, scientists were faced with the task of creating a universal remedy for fever and pain, the cost of which would be affordable to many.
Acetylsalicylic acid was first synthesized by a French scientist Charles Frederic Gerard in 1853, the same willow tree bark served as the basis. But acetylsalicylic acid in a form suitable for medical use was created in the laboratories of Bayer. August 10, 1897 German chemist Felix Hoffmann told his colleagues Arthur Eichengrün, doctor Carl Duisberg and professor Heinrich Dreser, who headed the research department of the company - that he managed to get acetylsalicylic acid.
Clinical trials lasted a year and a half. In fact, aspirin became the official trademark of Bayer on March 6, 1899.
According to the laws of the German Empire of that time, chemical compounds were not subject to patenting, but it was possible to register a unique trademark. Therefore, the word "aspirin" was coined to name the new drug. "A" was taken from "acetyl", "spir" - from the Latin name of the herb meadowsweet - spirea, rich in salicin, "in" - as a typical ending for the word for a drug.
At first, aspirin was sold in powder form, and since 1904 - already in the form of tablets, and since 1915 - without a prescription. Aspirin, being inexpensive, effective, and relatively harmless, quickly became the most popular pain reliever.
Stories and fate
Until the 1930s, it was believed that the great medicine was the fruit of collective labor"Bayer specialists". But it is historical justice that Felix Hoffmann's discovery was based on the work of predecessor scientists - the Frenchman Charles Gerhardt and an Englishman Alder Wright. After the triumphant discovery of aspirin, Hoffman worked for Bayer all his life. The fate of his boss, Heinrich Dreser, was sadder.
Working on the process of converting salicylic acid to acetylsalicylic acid, Hoffmann conducts experiments on the acylation of morphine, resulting in the drug heroin. It was supposed to be used as a strong pain reliever, but the side effects of heroin use were immediately apparent. Despite this, it was Heinrich Dreser who became the first official heroin addict, popularizer of the new drug and its first victim: he died of cardiac arrest in 1924.
Arthur Eichengrün ended up in a concentration camp in 1944, and 5 years later, before his death, he published an article dedicated to the 50th anniversary of aspirin, in which he attributed the invention of aspirin to himself. The debate about who exactly was the true inventor of aspirin did not subside after the publication of this article for a long time.
From heat and pain, for the heart and for children
Initially, only the antipyretic effect of aspirin was known, later its analgesic and anti-inflammatory properties were found out. After World War II, California physician Lawrence Craven experimentally discovered that aspirin significantly reduced the risk of heart disease. Today, most of the aspirin is used for this purpose - for the prevention of cardiovascular disease.
In 1952, a sparing concentration of children's aspirin appeared, and in 1969, aspirin tablets were included in the first-aid kits of the Apollo astronauts.
Research activity around the properties of aspirin has not subsided so far. So, according to research by Professor Peter Rothwell from Oxford University, regular intake of acetylsalicylic acid reduces the 20-year risk of developing prostate cancer by 10%, lung cancer by 30%, intestinal cancer by 40%, cancer of the esophagus and throat by 60%. .
According to researchers from the University of Alabama (USA) and the University of Ottawa (Canada), aspirin also reduces the risk of developing liver cancer. Those subjects who took aspirin for 10 years were less likely to suffer from hepatocellular carcinoma and 45% less likely to die from chronic diseases liver.
Researchers at the University of Western Australia in Perth say aspirin helps older people fight depression. And Dutch experts from the Institute of Neurosciences and the Academic Medical Center found that taking aspirin daily to prevent heart disease is fraught with loss of vision for older people. The risk increases by 2 times compared to those who do not take aspirin. But the benefit of aspirin in preventing heart disease is recognized as more significant than the damage it causes to the eyes.
Instructions for use
To date, aspirin is used as an antipyretic and analgesic, as a means of preventing heart attacks and thrombosis, in the complex treatment of certain diseases, for example, in gynecology. Aspirin is widely used as a remedy for hangover symptoms.
Safe daily dose of aspirin: 4 g per day. You can take the drug only after eating and drink it with a sufficient amount of water.
But aspirin should never be used uncontrollably and without a doctor's prescription. An overdose leads to severe pathologies of the kidneys, brain, lungs and liver, the first symptoms of an overdose are sweating, tinnitus and hearing loss, edema, skin and other allergic reactions. Daily intake of aspirin can cause gastrointestinal or even brain bleeding.
