2010/12/12

Acetylsalicylic acid


Acetylsalicylic acid (Latin Acidum acetylsalicylicum, Eng. Acetylsalicylic acid, salicylic ester of acetic acid) - drug has analgetic, antipyretic, antiinflammatory and antiaggregatory action. Small white needle-like crystals or light crystalline powder, slightly soluble in water at room temperature, soluble in hot water, easily soluble in alcohol, caustic and carbonated alkali.

Synthesized by Felix Hoffmann (Bayer AG) in 1897. A patent for his invention of a German chemist, received March 6, 1899. Hoffman opened the medicinal properties of acetylsalicylic acid, trying to find a cure for his father, who suffered from rheumatism.

Aspirin is widely known under the trademark "Aspirin" company "Bayer".

History of creation

Acetylsalicylic acid was first synthesized by Charles Frederic Gerhardt in 1853. August 10, 1897 Arthur Eichengreen, who worked in the laboratories of Bayer in Wuppertal first received samples of acetylsalicylic acid in a form as possible for medical use. Bayer recorded a new drug under the brand name Aspirin.

Already in 1899 the first batch of the drug went on sale. It was originally known only antipyretic effect of aspirin, and later emerged as its analgesic and anti-inflammatory properties. In the early years of aspirin is sold as a powder, and since 1904 in pill form.

In 1987, the medical journal The New England Journal of Medicine published an article [citation needed 230 days], in which the results of years of research confirmed another property of this drug - with its regular use significantly reduced risk of heart attack. According to new data [citation needed 230 days], aspirin also reduces the risk of cancer of the colon.

General Information

Acetylsalicylic acid has anti-inflammatory, antipyretic and analgesic effect, and it is widely used in feverish conditions, headaches, neuralgia, etc., and as antirheumatic.

Anti-inflammatory effect of acetylsalicylic acid (and other salicylates) can be explained by its influence on the processes occurring in the inflammation: a decrease in the permeability of capillaries, decreasing the activity of hyaluronidase, limited power supply of the inflammatory process by inhibition of ATP formation, etc. The mechanism of anti-inflammatory action has a value of inhibition of prostaglandin biosynthesis.

Antipyretic effect is also associated with the effect on the hypothalamic thermoregulatory centers.

Analgesic effect is due to the influence of the centers of pain sensitivity, as well as the ability of salicylates to reduce algogenov action of bradykinin.

Blood-thinning effect of aspirin allows it to reduce intracranial pressure, headaches.

Salicylic acid was the basis for an entire class of drugs called salicylates, an example of such a drug is dihydroxybenzoic acid.

Chemical properties

Acetylsalicylic acid in the hydrolysis breaks down into salicylic and acetic acid. Hydrolysis is carried out by boiling a solution of acetylsalicylic acid in water for 30 seconds. After cooling, salicylic acid, poorly soluble in water, precipitated in the form of fluffy needles.

Application and dosing regimen

Aspirin is widely used as anti-inflammatory, antipyretic and analgesics. Apply it on your own and in combination with other drugs.

There are a number of proprietary medicines containing acetylsalicylic acid (tablets Tsitramon "," Kofitsil "," Asfen "," Askofen "," Atselizin "etc.).

Recently received injectable drugs, the main active principle of which is acetylsalicylic acid (see Atselizin, Aspizol).

In the form of tablets prescribed acetylsalicylic acid orally after meal. Usual dose for adults as an analgesic and antipyretic (for fever diseases, headache, migraine, neuralgia, etc.) 0,25-0,5-1 g 3-4 times a day for children, depending on the age of 0, 1 to 0.3 g per reception.

In rheumatoid arthritis, infectious-allergic myocarditis, rheumatoid arthritis prescribed a long time for adults, 2-3 g (at least 4 grams) per day, children at 0.2 grams per year of life per day. Single dose for children aged 1 year was 0.05 g, 2 years - 0,1 g, 3 years old - 0,15 g, 4 years - 0,2 g. Since the age of 5 can be given in pill form for 0 , 25 g per reception.

Aspirin is effective, very affordable tool that has widespread use in ambulatory practice. Please be aware that drug use should be made with caution due to the possibility of some side effects.

Described many cases where ingestion of even 100 grams of vodka in combination with conventional drugs such as aspirin or Amidopyrine, accompanied by severe allergic reactions and stomach bleeding.

Widespread use of aspirin in the home as a way to remove hangover. Nevertheless, it should be understood that aspirin does not cure a hangover, but only a few removes the pain. It is better to replace it with other analgesics with fewer side effects.

Side effect

Using the drug may develop profuse sweating may occur tinnitus and hearing impaired, angioedema, skin and other allergic reactions.

It is important to note that during long-term (without a doctor's control), use of aspirin may experience side effects such as dyspepsia and stomach bleeding may be amazed at not only the mucosa of the stomach, and duodenum.

The so-called ulcerogenic action inherent in varying degrees to different anti-inflammatory drugs: corticosteroids, phenylbutazone, indomethacin, etc. The appearance of gastric ulcers and gastric bleeding in the application of acetylsalicylic acid, not only due to resorptive activity (inhibition of blood clotting factors, etc.), but it a direct irritating effect on the gastric mucosa, especially if the drug is taken in the form of tablets uncomminuted. This also applies to sodium salicylate.

To reduce the ulcerogenic effect and gastric bleeding should receive acetylsalicylic acid (and sodium salicylate) just after eating, the tablets should carefully grind and drink plenty of fluids (preferably milk). However, there are indications that gastric bleeding may also occur when taking aspirin after a meal. Sodium bicarbonate promotes more rapid release of salicylate from the body, yet to reduce the irritants in the stomach after resorting to receive acetylsalicylic acid alkaline mineral water or sodium bicarbonate.

Overseas tablets of acetylsalicylic acid are produced are often of fine crystalline powder with alkalify (buffer) additions.

With prolonged use of salicylates should consider the possibility of anemia and systematic blood tests and check for blood in the stool.

Due to the possibility of allergic reactions should be cautious about the appointment of acetylsalicylic acid (and other salicylates) individuals with heightened sensitivity to penicillin and other "allergogennym" medicines.

If you are sensitive to acetylsalicylic acid may develop asthma Aspirin for the prevention and treatment methods that are designed desensitizing therapy with increasing doses of aspirin.

In connection with the available experimental data on the teratogenic action of acetylsalicylic acid is recommended not to prescribe it and contain its products to women in the first 3 months of pregnancy.

Currently, aspirin is not recommended for use to reduce temperature in children, especially in cases of suspected viral illness. It is known that the use of aspirin in such patients can cause necrosis of the liver and the development of acute liver failure. This complication known as Reye syndrome (Reye). At the moment pathogenetic mechanism of Reye syndrome is unknown. The disease occurs with the development of acute liver failure. The incidence of Reye syndrome in children under 18 years of age in the United States is approximately 1:100 000, with case fatality rate exceeds 36% [4].

Antiaggregatory action

An important feature of acetylsalicylic acid is its ability to exert antiaggregatory action to inhibit spontaneous and induced platelet aggregation.

Substances that have antiaggregatory action began to receive widespread in medicine for the correction of hemorheological disorders and prevention of thrombotic complications in patients with myocardial infarction, stroke and other cardiovascular diseases.

These substances are sometimes isolated in a separate group antiagregatsionnoe funds (see antiaggregatory agent).

Due to the influence on platelet aggregation, as well as some antikoaguliruyuschey activity should be the treatment of acetylsalicylic acid to conduct periodic blood tests. If bleeding disorders, particularly hemophilia may develop bleeding. For early detection of ulcerogenic action must periodically examine feces for the presence of blood.

Keep in mind that under the influence of acetylsalicylic acid enhances the action of anticoagulants (coumarin derivatives, heparin, etc.), saharoponizhayuschih drugs (sulfonylureas), increases the risk of gastric bleeding during concomitant use of corticosteroids and nonsteroidal anti-inflammatory drugs (NSAIDs) increases the side effects of methotrexate. Weakened by several actions of furosemide, urikozuricheskih funds spironolactone.

Contraindications

Gastric ulcer and duodenal ulcers and bleeding are contraindications to the use of aspirin and sodium salicylate.

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