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Chapter: Basic & Clinical Pharmacology : Adrenocorticosteroids And Adrenocortical Antagonists

Synthetic Corticosteroids

Glucocorticoids have become important agents for use in the treat-ment of many inflammatory, immunologic, hematologic, and other disorders.

SYNTHETIC CORTICOSTEROIDS

Glucocorticoids have become important agents for use in the treat-ment of many inflammatory, immunologic, hematologic, and other disorders. This has stimulated the development of many synthetic steroids with anti-inflammatory and immunosuppressive activity.

Pharmacokinetics

A. Source

Pharmaceutical steroids are usually synthesized from cholic acid obtained from cattle or steroid sapogenins found in plants. Further modifications of these steroids have led to the marketing of a large group of synthetic steroids with special characteristics that are pharmacologically and therapeutically important (Table 39–1; Figure 39–3).




B. Disposition

The metabolism of the naturally occurring adrenal steroids has been discussed above. The synthetic corticosteroids (Table 39–1) are in most cases rapidly and completely absorbed when given by mouth. Although they are transported and metabolized in a fashion similar to that of the endogenous steroids, important differences exist.

Alterations in the glucocorticoid molecule influence its affinity for glucocorticoid and mineralocorticoid receptors as well as its protein-binding affinity, side chain stability, rate of elimination, and metabolic products. Halogenation at the 9 position, unsatura-tion of the 1–2 bond of the A ring, and methylation at the 2 or 16 position prolong the half-life by more than 50%. The 1 com-pounds are excreted in the free form. In some cases, the agent given is a prodrug; for example, prednisone is rapidly converted to the active product prednisolone in the body.

Pharmacodynamics

The actions of the synthetic steroids are similar to those of cortisol (see above). They bind to the specific intracellular receptor pro-teins and produce the same effects but have different ratios of glucocorticoid to mineralocorticoid potency (Table 39–1).


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