CORTISONE (Cortisonum) — hormone of cortical substance of adrenal glands; represents 11-degidro-17-oxycorticosterone. In 1936 it is allocated from cortical substance almost at the same time by three groups of the researchers headed by E. Kendall, T. Reykhstein, Vintershteyner (O. R. W. Wintersteiner). In 1938 T. Reykhstein established chemical structure To., and Sarr (O. of Sarret) in 1944 its lab carried out. synthesis. Constitutional formula:
To. contains in cortical substance of adrenal glands in small amounts, ways of its allocation from them are extremely difficult; therefore To. receive in generally synthetic way. Biosynthesis To., as well as others corticosteroids (see), comes from cholesterol and AKTG is stimulated; transformation To. in an organism it is similar to transformation of cortisol (see. Hydrocortisone ).
As well as for others glucocorticoid hormones (see), for To. influence on carbohydrate metabolism is characteristic: strengthening of a gluconeogenesis, braking of disintegration of carbohydrates and their transformation into fats, increase in sugar into blood, decrease in sensitivity of an organism to insulin. To. strengthens a catabolism of proteins, increases the content of amino acids in blood, increases release of nitrogen with urine. In much smaller degree, than mineralokortikoidny hormones (see), exerts impact on water mineral metabolism, detaining allocation of ions of sodium and chlorides, and also waters. To. together with cortisol participates in the adaptive reactions of an organism increasing its stability concerning adverse effects.
To. has the regulating effect on the processes happening in connecting fabric and on processes of a hemopoiesis, stimulates assimilation of iron with sideroblasts of marrow that promotes an erythrogenesis. To. possesses strong antiinflammatory, anti-toxic and antiallergenic action.
Determination of content To. in blood and urine it is carried out by the same methods, as other corticosteroids.
Content To. in blood and excretion with urine raise at acromegalias (see), Itsenko's diseases — Cushing (see. Itsenko — Cushing a disease ), at tumors adrenal glands (see), stress (see); contents To. goes down at addisonovy disease (see), hypopituitarism (see), a diffusion toxic craw (see. Craw diffusion toxic ).
Drugs of a cortisone
To. was the first corticosteroid applied F. Henchem (1948) in a wedge, practice. Industrial receiving To. it is carried out from natural steroid substances: sterols (cholesterol, ergosterol, a stigmasterol), bilious to - t (cholic, deoxycholic, thiodeoxycholic), plant substances — saponins, and also the orthotoluidine, an ergosteron (received from yeast), the progesterone (received from the East African type of an aloe).
For a wedge, uses is issued cortisone acetate (Cortisoni acetas; 11-degidro-17-oksikortiko-steron acetate); it is applied hl. obr. at the states demanding bystry therapeutic effect: at anaphylactic, postoperative and other types of shock, at a collapse. It is effective To. at treatment of diseases of connecting fabric (an acute stage of rheumatism, the disseminated lupus erythematosus, a panarteritis, etc.). In gematol, practice To. apply at immunol. conflicts (autoimmune hemolitic anemias, thrombocytopenia, immune agranulocytosis). To. is specific lymphotropic drug, however at a number of diseases preference is given to synthetic drugs of other glucocorticoid hormones (e.g., to Prednisolonum, dexamethasone, a triamsinolon) as they, in comparison with To., cause side effects less often. At impact To. on inflammatory processes activity of hyaluronidase is oppressed, permeability of capillaries and cellular membranes decreases, exudation and emigration of leukocytes is braked (see. Inflammation ); a lysis of lymphocytes and plasmocytes is caused that antigen — an antibody leads to reduction of products of antibodies and oppression of reaction. At use of drugs K. products of fibroblasts and reticular macrophages are suppressed, and also the marrowy reserve of granulocytes in this connection the eosinopenia and a reactive neutrophylic leukocytosis is observed will be mobilized (elimination of granulocytes from marrow increases).
Doses To. are defined strictly individually and vary from 10 — 15 mg a day at hron, diseases to 100 — 200 mg at medical emergencies (shock, immunol. conflicts, etc.); course doses similarly fluctuate (3 — 4 g, sometimes above). At acute diseases use of the most admissible doses is possible (for elimination immunol, the conflict). At intake effect of drug is shown quicker, but continues no more than 6 — 8 hours; at intramuscular introduction action because of slow absorption is shown a little later, but 8 — 12 hour proceed.
Contraindications: diabetes mellitus, severe form of arterial hypertension (idiopathic hypertensia, diseases of kidneys), peptic ulcer, osteoporosis, pregnancy.
Form of release acetate of a cortisone: powder, tablets on 0,025 g and 0,05 g; suspensions for intramuscular injections (on 0,025 g in 1 ml) in bottles on 10 ml. Keep in the cool and protected from light place, in bottles of dark glass; the list B.
See also Corticosteroids, drugs .
Bibliography: See bibliogr, to St. Corticosteroids .
A. I. Vorobyov, Yu. L. Milevskaya.