Need 3-keto group, 4-5 double bond and C-17 side
chain for biologic activity.
activity of glucocorticoids.
Also a stronger glucocorticoid
11-B hydroxyl group essential for steroids to bind to
the glucocorticoid receptor. 17-a hydroxyl and
21-hydroxyl greatly enhance activity.
Transported bound to transcortin
Less potent than synthetic
Primary secretory product
of the adrenal gland.
1. Addison's with salt
2. High doses in acute adrenal
insufficiency with IV saline and
3. Secondary adrenal
insufficiency (with no other Rx
because the aldosterone and salt
balance are normal.)
4. Allergic rxns
5. Suppress immune rxn in
6. Neoplasm control
7. Some infections
8. Some non-hypovolumic
Use where inflammation is part
of the pathophysiology.
C-1-2 double bond = delays hepatic metabolism of
the A ring
C-16-a methylation or hydroxylation = delays
metabolism of the D ring and enhances the ratio of
glucocorticoid to mineralocorticoid activity.
C-9 fluorination = increases electro negativity of the
C-11 hydroxyl group. Decreases interaction with 11-
hydroxysteroid dehydrogenase. Both the
glucocorticoid and mineralocorticoid activities are
All absorbed from the GI tract.
Metabolized in the liver and renal excretion by
attachment of glucuronide or sulfate group.
Cushing's syndrome with intensity
related to dose, route, frequency and
exposure. Can inhibit linear growth in
Use K supplementation, restrict Na
intake, H2 blocker to protect upper GI
tract, high calcium diet to minimize
bone loss, vit D supplements,
bisphosphanates to inhibit bone
Daily single dosing as effective as
divided-dosing. Divided dosing = most
likely to cause renal sup