Corticosteroids (Iszard) Flashcards
What are the two main effects of glucocorticoids?
- anti-inflammatory effect
- immunosupressive effect
Glucocorticoid agonist
Short-acting: hydrocortisone (cortisol) and cortisol
Intermediate-acting: prednisone, prednisolone, methylprednisolone, and triamcinolone
Long-acting: betamethasone and dexamethasone
Mineralocorticoids agonists
Fludrocortisone; indicated in adrenal insufficiency (Addison’s disease)
Glucocorticoid antagonist
mifepristone; also indicated in medical abortions; very rarely for Cushing’s syndrome
Mineralocorticoid antagonist
spironolactone and eplerenone (more specific); K+ sparing diuretic; most common adverse effect is HYPERkalemia
The mineralocorticoid receptor has equal affinity for what two hormones?
aldosterone and cortisol
MOA of 11-beta HSD2?
converts active cortisol to inactive cortisone
MOA 11-beta HSD1?
converts inactive cortisone to active cortisol
Treatment for Addison’s disease?
combination of glucocorticoid (hydrocortisone) and mineralocorticoid (fludrocortisone)
Treatment for congenital adrenal hyperplasia?
combination of glucocorticoid (hydrocortisone) and mineralocorticoid (fludrocortisone)
Botton line message for corticosteroid use?
cannot be given chronically without the risk for adverse events (mainly immunosuppression); use lowest dose for the shortest possible duration
Corticosteroid use is problematic in which patient populations?
Immunocompromised (HIV/AIDs)
Psychiatric conditions
Osteoporosis
Infections and peptic ulcers
Glycyrrhizin
licorice root extract; inhibitor of 11B-HSD2; cortisol stays active; Na+ and H2O retention; increase K+ loss; increase in BP
Pramlintide
anti-diabetic medication; always used with insulin
short to medium-acting <12 hours corticosteroid drugs
hydrocortisone (cortisol) and cortisol
intermediate-acting 12-36 hours corticosteroid drugs
prednisone
prednisolone
methylprednisolone
triamcinolone
long-acting >36 hours corticosteroid drugs
betamethasone and dexamethasone
Importance of dose-tapering
allows for HPA recovery; w/ chronic use there will be adrenal atrophy; watch for adrenal withdrawal syndrome
What are the 3 ways to test for HPA axis integrity?
morning serum cortisol test
ACTH test
CRH test
Mitotane
can treat cancer of the adrenal glands (adrenal cortical carcinoma)
Ketaconazole
synthesis inhibitor; blocks fungal and human CYP450 enzymes; indicated in inhibition of steroid hormone synthesis; watch for hepatic dysfunction
