Xenical use
The beginning of application of glucocorticoids as medical products (ЛС) concerns 40th of the XX-th century. Still in the late thirties of the last century it has been shown that in a bark of adrenal glands hormonal connections of the steroid nature are formed. In 1937 from a bark of adrenal glands has been allocated минералокортикоид дезоксикортикостерон, in 40th — glucocorticoids a cortisone and a hydrocortisone. The wide spectrum of pharmacological effects of a hydrocortisone and a cortisone has predetermined possibility of their use as ЛС. Their synthesis has soon been carried out.
The basic and most active glucocorticoid formed in a human body, the hydrocortisone (cortisol), others, less active is, are presented by a cortisone, кортикостероном, 11-dezoksikortizolom, 11-degidrokortikosteronom.
Development of hormones of adrenal glands is under control ЦНС and is closely connected with hypophysis function. The adrenokortikotropnyj hormone of a hypophysis (АКТГ, кортикотропин) is a physiological stimulator of a bark of adrenal glands. Кортикотропин strengthens formation and allocation of glucocorticoids. The last, in turn, influence a hypophysis, oppressing development кортикотропина and reducing, thus, the further stimulation of adrenal glands (by a principle of negative feedback). Long introduction in an organism of glucocorticoids (a cortisone and its analogs) can lead to oppression and an atrophy of a bark of adrenal glands, and also to oppression of formation not only АКТГ, but also гонадотропных and тиреотропного hypophysis hormones.
Practical application as ЛС from natural glucocorticoids was found by a cortisone and a hydrocortisone. The cortisone, however, more often, than other glucocorticoids, causes by-effects and, in connection with occurrence of more effective and safe preparations now has the limited application. In medical practice use a natural hydrocortisone or its ethers (a hydrocortisone acetate and a hydrocortisone гемисукцинат).
Variety of synthetic glucocorticoids among which allocate not fluorinated (Prednisonum, Prednisolonum, метилпреднизолон) and fluorinated (dexamethasone, бетаметазон, триамцинолон, флуметазон, etc.) is synthesized Glucocorticoids. These connections, as a rule, are more active, than natural glucocorticoids, operate in smaller doses. Action of synthetic steroids is similar to action of natural corticosteroids, but they possess a various parity glucocorticoid and минералокортикоидной activity. More favorable parity between glucocorticoid/anti-inflammatory and минералокортикоидной activity the fluorinated derivatives differ. So, anti-inflammatory activity of dexamethasone (in comparison with that of a hydrocortisone) above in 30 times, бетаметазона — at 25-40 time, триамцинолона — in 5 times, thus influence on a vodno-salt exchange minimum. The fluorinated derivatives differ not only high efficiency, but also low absorption at local application, i.e. smaller probability of development of system by-effects.