Corticosteroids glucocorticoid activity

Various synthetic corticosteroids have also been developed. Some display greater potency than the native steroids, while others exhibit glucocorticoid activity with little associated mineralocorticoid effects, or vice versa. The major glucocorticoids used clinically are synthetic. They are usually employed as ... 

Betamethasone Synthetic corticosteroid, displays glucocorticoid activity, lacks mineralocorticoid activity Use mainly as anti-inflammatory and immunosuppressive effect... 

As soon as corticosteroids, such as cortisone, were used in the treatment of rheumatoid arthritis (glucocorticoid activity), important undesirable side effects appeared (sodium retention). In view of lowering the sodium retention, while increasing the anti-inflammatory activity. Fried performed various chemical modifications. Thus, he could observe that introducing a fluorine atom at the 9a position of the hydrocortisone acetate highly enhanced (11 times) the glucocorticoid activity, while the undesired sodium retention was lowered [130]. 

Fluorination of corticosteroids at C-9 or/and C-6 increases glucocorticoid activity, while mineralocorticoid activity, responsible for sodium retention (the main adverse effect of corticoids), is decreased (cf. Chapter 4). Fluorocorticoster-oids were the first fluorinated compounds to be used clinically. They are still major drugs against many inflammatory disorders rheumatoid polyarthritis, ORL (asthma, rhinitis), brain edema, dermatological, allergies, anaphylactic shock, Quincke s edema). 

Cortisone is a natural corticosteroid secreted by the adrenal cortex along with many steroidal hormones. It has mainly glucocorticoidal activity and some degree of mineralo-corticoid activity. 

The adrenal cortex synthesizes corticosteroids (glucocorticoids and mineralocor-ticoids), which differ in activities. In humans, cortisol is the main glucocorticoid, and aldosterone is a main mineralocorticoid. Steroid therapy causes severe potential side effects, hence a careful consideration is always exercised before starting therapy. These are used in variety of disorders such as rheumatic disorder, renal disease, allergic manifestation, bronchial asthma, skin diseases, infectious diseases, malignancy, and hepatic diseases. 

Cortisone is a corticosteroid secreted by the adrenal cortex. It has glucocorticoid activity, as well as appreciable mineralocorticoid activity 25 mg cortisone acetate is equivalent in anti-inflammatory activity to about 5 mg prednisolone. 

Prednisolone is extensively bound to plasma proteins, although less so than hydrocortisone. Prednisolone is a corticosteroid with mainly glucocorticoid activity in fact, 5 mg prednisolone is equivalent in anti-inflammatory activity to ca. 

Beclomethasone dipropionate is a corticosteroid with mainly glucocorticoid activity that is started to exert a topical effect on the lungs, without significant systemic activity. It is used by inhalation, generally from a metered-dose aerosol, for the prophylaxis of asthma. Inhalation of nebulized beclomethasone dipropionate has also been used in the management of asthma in children. 

Flumetasone pivalate is a corticosteroid used topically for its glucocorticoid activity in the treatment of various skin disorders. It is usually employed as a cream, ointment, or lotion. Flumetasone pivalate is also used in ear drops. 

Lamberts S W J, Bruining H A, de Jong F H 1997 Corticosteroid therapy in severe illness. New England Journal of Medicine 337 1285-1292 Lipworth B J 2000 Therapeutic implications of non-genomic glucocorticoid activity. Lancet 356 87-88 Lavin M J et al 1986 Use of steroid eye drops in general practice. British Medical Journal 292 1448... 

Glucocorticoids also have antiallergic properties, as a result of and by an inhibition of the synthesis of histamine by mast cells and basophils. Of the naturally occurring corticosteroids, only cortisol and corticosterone possess glucocorticoid activity, with cortisol the most effective. Cortisone and 11-dehydrocorticosterone lack direct glucocorticoid activity, but have potential glucocorticoid activity because they can be metabolixed to cortisol and corticosterone, respectively. 

Fludrocortisone Synthetic corticosteroid high mineralocorticoid and moderate glucocorticoid activity long duration of action. 

In general, the adrenocortical steroids (or adrenal corticosteroids) distinctly differ in their respective glucocorticoid activities i.e., carbohydrate-regulating), and mineralocorticoid activities (i.e., electrolyte-regulating). It has been observed that in human beings the following two compounds occur commonly ... 

Aldosterone, IIfi,21-dihydroxy-3 0-tBaxo-pregn-4-en-18-al-I8 - II hemiacelal a highly active mineralocorticoid from the adrenal cortex. Unlike other hormones of the adrenal cortex, A. has a carbonyl group on Cl 8, which forms a hemiacetal with the llp-hydroxyl group. It is the most important mineralocorticoid, regulating NaCl resorption and K excretion. It also has some glucocorticoid activity. For structure and biosynthesis, see Adrenal corticosteroids. 

Oral corticosteroids have many properties which may be beneficial in acute and chronic pain relief. They are principally anti-inflammatory or immunosuppressant agents that are derived from adrenal steroids and have primarily glucocorticoid activity with limited or no mineralocorticoid activity. 

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