Glucocorticoids pharmacological effects

Most of the established pharmacological effects of glucocorticoids are mediated by cytoplasmic glucocorticoid receptors. After binding to the receptor, the steroid-receptor complex binds to chromatin and stimulate the formation of mRNA. The mRNA stimulates the synthesis of enzymes which produce various pharmacological actions. 

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. 

Pharmacology These agents are synthetic adrenocortical steroids with basic glucocorticoid actions and effects. Glucocorticoids may decrease number and activity of inflammatory cells, enhance effect of beta-adrenergic drugs on cyclic AMP production, inhibit bronchoconstrictor mechanisms, or produce direct smooth muscle relaxation. Inhaler use provides effective local steroid activity with minimal systemic effect. 

The reason of effects of fluorine atoms at C-6 and C-9 positions on the pharmacological profile (in particular on the enhancement of the glucocorticoid activity and its dissociation from the mineralocorticoid activity) is not always very clear. Three hypothesis coexist ... 

Glucocorticoids are widely used as drugs to treat arthritis and dermatitis. In pharmacological doses, they are used to suppress various allergic, inflammatory and autoimmune diseases. They are also administered as post-transplant immunosuppressants. Nevertheless, they do not prevent infection and they also inhibit subsequent regenerative processes. Excessive glucocorticoid levels have side effects on many systems, such as the inhibition of bone formation, delayed wound healing, muscle weakness and an increased risk of infection. 

Rheumatoid arthritis and osteoarthritis represent two distinct forms of joint disease that can produce devastating effects on the structure and function of synovial joints. Fortunately, management of these conditions has improved substantially through advancements in drug therapy. Rheumatoid arthritis can be treated pharmacologically with NSAIDs, glucocorticoids, and various DMARDs. NSAIDs, including aspirin, repre-... 

Steroid structure and biosynthesis have been used from a pharmacologic standpoint. Pharmacologists have tried to develop more effective and less toxic synthetic steroids by manipulating the chemical side groups of these compounds. An example is the synthetic glucocorticoid dexamethasone, which is 25 times... 

The primary glucocorticoids used pharmacologically are listed in Table 29-1. These drugs are either chemically identical to the naturally occurring hormones, or they are synthetic analogs of cortisol. The clinical choice of a particular agent depends on the problem being treated and the desired effect in each patient. 

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