Unit 5-Steroids Flashcards
Cortisol, Cortisone acetate, hydrocortisone, prednisone, prednisolone, methylprednisolone, triamcinolone, dexamethasone
Mechanism
Binds GR, which regulates expression of genes with many effects on carbohydrate metabolism and immune function
Cortisol, Cortisone acetate, hydrocortisone, prednisone, prednisolone, methylprednisolone, triamcinolone, dexamethasone
Side effects
Cushing’s; glucocorticoid-induced osteoporosis; iatrogenic adrenal insufficiency
Hydrocortisone
Uses
Chronic primary adrenal insufficiency (maintenance); CAH
Prednisone
Uses
CAH
Dexamethasone
Uses
Emergency treatment (severe adrenal crisis, PAI); suppression test (Cushing’s); CAH
Fludrocortisone
Drug class
Mineralocorticoid
Fludrocortisone
Mechanism
Binds aldosterone receptor (AR) which increases Na+K+ATPase expression and increase epithelial sodium channel experession
Fludrocortisone
Uses
Chronic primary adrenal insufficiency (maintenance); CAH
Fludrocortisone
Side effects
Primary aldosteronism
Aminoglutethide
Mechanism
Blocks conversion of cholesterol to pregnenolone
Aminoglutethide
Uses
Cushing’s
Ketoconazole
Drug class
Anti-fungal imidazole derivitive
Ketoconazole
Mechanism
Potent, nonselective inhibitor of adrenal and gonadal steroid synthesis
Ketoconazole
Uses
Cushing’s
Mitotane
Drug class
DDT insecticide relative
Mitotane
Mechanism
Nonselective cytotoxic action on adrenal cortex
Mitotane
Uses
Cushing’s
Mitotane
Side effects
Bad side effect profile
Metyrapone
Mechanism
Relatively selective inhibitor of 11-hydroxylation (interferes with cortisol and corticosterone synthesis)
Metyrapone
Uses
Cushing’s
Mifepristone (RU-486)
Mechanism
Progesterone receptor antagonist; GR antagonist at high concentrations
Mifepristone (RU-486)
Uses
Cushing’s (controls hyperglycemia secondary to hypercortisolism)
Mifepristone (RU-486)
Side effects
Fatigue, nausea, headache, hypokalemia, arthralgias
edema and endometrial thickening in women
Pasireotide
Drug class
somatostatin analog