ACETYLSALICYLIC ACID (Acidum acetylsalicylicum; synonym: aspirin, Acesal, Acetysal, Acylpyrin, Istopirin, Polopiryna) — analgesic means. Salicylic ether acetic to - you; With 9 H 8 O 4 :
Colourless crystals or white crystal powder; in the wet environment it is hydrolyzed with education acetic and salicylic to - you; it is slightly soluble in water, is easily alcohol-soluble, solutions of caustic and carbonic alkalis.
And. to. it is quickly soaked up from a stomach and upper parts of a small bowel; as much as possible collects in fabrics in 1,5 — 2 hours. The greatest number And. to. it is found in a blood plasma, a liver, heart, lungs and adrenal glands; it is less — in synovial and cerebrospinal fluid and in an abdominal cavity. And. to. it is removed from an organism with urine generally in the form of products of biotransformation (salitsilovomochevy, di - and trihydrobenzoic acids, an acylglucuronide, etc.) and partially in not changed look.
At resorptive action And. to. causes analgesic, febrifugal and antiinflammatory effects, raises excretion of urates, stimulating their secretion and reducing a reabsorption in renal tubules. In high doses And. to. has also holeretichesky effect and reduces the level of a prothrombin in a blood plasma.
Analgesic effect And. to., obviously, it is caused as direct action on the thalamic centers of a brain, and reduction under their influence of excitability of receptors in the center of an inflammation. Action And. to. on the Hypothalamic centers of thermal control is followed by increase in a thermolysis due to strengthening of peripheric circulation and increase in sweating therefore body temperature at fever decreases (febrifugal effect).
Antiinflammatory action it is connected with influence And. to. on some processes proceeding in the center of an inflammation. So, And. to. reduces permeability of vessels, reduces activity of hyaluronidase, limits migration of leukocytes, breaks power providing an inflammation by braking of oxidizing phosphorylation and process of transformation of ADF into ATP. Besides, And. to. stabilizes membranes of lysosomes and inhibits a number of enzymes (a 5-oksitriptofandekarboksilaza, a histidinedecarboxylase, alpha chymotrypsin, fibrinolysin) which participate in formation of biologically active agents playing a part in a pathogeny of an inflammation.
Apply And. to. as anesthetic and anti-inflammatory drug at arthritises, neuralgia, mialgiya, a headache. Drug is widely used for treatment of various forms of rheumatism, a pseudorheumatism and other diseases with the phenomena of an inflammation in joints, muscles and internals, and also for decrease in body temperature.
Appoint inside 0,25 — 1 g 3 — 4 times a day (2 — 4 g a day). At good tolerance the daily dose can be increased to 6 — 8 g.
And. to. can make sick, vomiting (reflex and the central origin), a sonitus, easing of hearing, perspiration, allergic reactions, mental disorders. At prolonged use hidden are possible went. - kish. bleedings, formation of ulcers in a stomach and a duodenum. An absolute contraindication to appointment And. to. hypersensitivity (sensitization) to salicylates is, relative — a peptic ulcer of a stomach and duodenum.
Orie acute poisoning And. to. nausea, vomiting, a headache, decrease in hearing and visual acuity, arrhythmia, falling of arterial pressure, excitement of c is noted. the N page, a cut in hard cases is replaced by its oppression. Breath is speeded up in the beginning. Due to the hyperventilation development of a respiratory alkalosis is possible. In case of respiratory depression and blood circulation there is a respiratory and metabolic acidosis. At treatment of acute poisonings And. to., in addition to the actions directed to removal of poison from an organism and reduction of its concentration (a gastric lavage, salt laxatives, introduction to a vein of isotonic solution of sodium chloride, a hemodialysis or peritoneal dialysis, etc.), means of symptomatic therapy apply. Special attention at the same time is paid to elimination of disturbances of acid-base equilibrium, balance of electrolytes, disorders of breath and blood circulation, and also prevention of hypostatic pneumonia.
Forms of release: powder and tablets on 0,25 and 0,5 g. Keep in the dry place in well corked container.
See also Analgesic means .
Bibliography: Mashkovsky M. D. Pharmaceuticals, p.1, page 100, M., 1972; Sigidin Ya. A. Mechanisms of therapeutic influence of antirheumatic means, Vopr. revmat., No. 2, page 46, 1970; In and at 1 es T. Century of Salicylate therapy in rheumatoid arthritis, Med. Clin. N. Amer., y. 52, p. 703, 1968; To u z e 1 1 W.C. Nonsteroid anti-inflammatory agents, Ann. Rev. Pharmacol., v. 8, p. 357, 1968, bib-liogr.; Salter R. H. Aspirin and gastrointestinal bleeding, Amer. J. dig. Dis., v. 13, p. 38, 1968, bibliogr.
V. K. Muratov.