Glucocorticoids anti-inflammatory properties

Since the glucocorticoids have immunosuppressive and anti-inflammatory properties, one would not expect allergic reactions to be a problem, except when excipients act as allergens. Nevertheless, allergic reactions to glucocorticoids themselves have been reported (SEDA-21, 419 291). Immunological reactions to glucocorticoids have... 

Glucocorticoids are prescribed frequently for their immunosuppressive and anti-inflammatory properties. They are administered locally, through topical and intralesional routes, and systemically, through intramuscular, intravenous, and oral routes. 

There are essential structural features that are necessary for glucocorticoid activity. The natural glucocorticoids also interact with the mineralocorticoid receptor and, therefore, will have salt-retaining properties. A large number of synthetic analogues have been prepared to decrease the mineralocorticoid effects in favor of increasing the glucocorticoid (anti-inflammatory) effect of the steroids. In addition, many derivatives are prepared to enhance pharmacokinetic parameters, most notably the synthesis of lipophilic and hydrophilic esters. 

The anti-ulceric properties of Carbenoxolone sodium throw open not only the question of its precise mechanism of action, but also the question of the exact relationship of its activity to the activities of certain other triterpenoids [539]. These include/ -amyrin, which is stated [540] to exhibit anti-inflammatory properties similar to those of the glucocorticoids aescin, the complex glycoside of 16-acetyl-21-tiglyloxyprotoaescigenin (LXX) [541] which exhibits anti-oede-matous properties [542-546] without showing beneficial effects on connective... 

Miscellaneous - Specific amino acids have been studied for anti-inflammatory activity. Thus, the combination of calcium D,L-aspartate/indometha-cin has been repor gd to be effective in primary chronic polyarthritis Dilauroyl-L-lyslne and trans U-aminomethyl-cyclohexane-l-carboxylic acid (tranexamic acid) have anti-inflammatory properties. The activity of tranexamic acid was not attributed to anti-plasmin action. Detailed pharmacology on SKF 17,910-A (X) has been published. This anti-inflammatory and diuretic agent shares some biological properties with glucocorticoids. 

Unlike glucocorticoids, mineralocorticoids have an insignificant effect on carbohydrate volume. They do not exhibit any anti-inflammatory or anti-aUergy properties. They are used for chronic adrenal insufficiency, as well as for raising tonicity and work capacity of muscles. 

Pharmacology The naturally occurring adrenal cortical steroids have both anti-inflammatory (glucocorticoid) and salt-retaining (mineralocorticoid) properties. These compounds are used as replacement therapy in adrenocortical deficiency states and may be used for their anti-inflammatory effects. 

Corticosterone. A natural corticoid with moderate glucocorticoid activity and some mineralocorticoid activity, possessing life-maintaining properties in adrenalectomized animals and several other activities peculiar to the adrenal cortex. Its actions closely resemble those of cortisol, except that it is not anti-inflammatory. 

The glucocorticoids also have powerful anti-inflammatory effects and when first introduced were considered to be the ultimate answer to the treatment of inflammatory arthritis. Although there are increasing data that low-dose corticosteroids have disease-modifying properties,... 

Glucocorticoids have potent anti-inflammatory and immunosuppressive properties. This is particularly evident when they are administered at pharmacological doses. A variety of synthetic glucocorticoids, some far more potent than cortisol, have been created for therapeutic use, such as hydrocortisone, prednisone, prednisolone, dexamethasone and betamethasone. 

Introduction of the 16a-hydroxyl group into 9-fluoro-hydrocortisone and 9-fluoro-prednisolone has been shown by Bernstein et al. [16] to result in complete suppression of the salt-retaining properties of these steroids, without appreciably impairing their glucocorticoid activity. Moreover, studies in man have demonstrated the anti-arthritic activity of 9-fluoro-16a-hydroxy-prednisolone and have confirmed its lack of salt-retaining activity. Subsequently, Lederle reported that the anti-inflammatory potency was lowered, but salt retention was eliminated. 

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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