Corticosteroids and Antagonists Flashcards
Short to Medium Acting Glucocorticoids
Activates glucocorticoid receptors – altered gene transcription
Suppresses inflammation
Replaces cortisol when deficient
Hydrocortisone (Cortisol) Cortisone Prednisone Prednisolone Methylprednisolone Meprednisolone
Intermediate Acting Glucocorticoids
Triamcinolone
Paramethasone
Fluprednisolone
Long Acting Glucocorticoids
Betamethasone
Dexamethasone
The glucocorticoid with the HIGHEST ANTI-INFLAMMATORY POTENCY
Betamethasone
The mineralocorticoid with the HIGHEST SALT RETAINING POTENCY
Fludrocortisone
Mineralocorticoids
Fludrocortisone
Deoxycorticosterone
Hastens fetal lung maturation
Betamethasone
Dexamethasone
Glucocorticoid Synthesis Inhibitor
Amino-glutethimide
Ketoconazole
Metyrapone
Mifepristone
Inhibits desmolase blocks conversion of cholesterol to pregnenolone
Reduces synthesis of all hormonally active steroids
USES:
breast cancer
Cushing syndrome
DESMOLASE INHIBITOR
Amino-glutethimide
Inhibits cholesterol side chain cleavage, CYP450, and other enzymes necessary for synthesis of all steroids
CYP450 INHIBITOR
Ketoconazole
Selective inhibitor of steroid 11-hydroxylation interfering with cortisol and corticosterone synthesis
Diagnostic testing for adrenal function
Cushing syndrome
DOC - pregnant patients with Cushing syndrome
11-B HYDROXYLASE INHIBITOR
Metyrapone
Competitive inhibitor at the GC receptor and progesterone receptor
USES:
Cushing syndrome
abortifacient for medical abortion
Mifepristone (RU486)
Mineralocorticoid Agonist
Strong agonist of mineralocorticoid receptors and moderate activation of glucocorticoid receptors
Increases Na reabsorption, K and H excretion
USES:
Addison’s disease (Chronic Adrenal Insufficiency)
CAH
Adrenal Replacement Therapy Post Adrenalectomy
MINERALOCORTICOID AGONIST
Fludrocortisone
Deoxycorticosterone
SE: salt and fluid retention hypokalemia CHF muscle wasting osteoporosis glucose intolerance behavioral changes
Mineralocorticoid Antagonist
Blocks aldosterone receptors
USES: HF hypokalemia d.t. other diuretics for post MI hyperaldosteronism
Spironolactone
SE:
hyperkalemia
anti-androgenic effect (i.e. gynecomastia)