Adrenal Agents Flashcards
Cortisol (hydrocortisone)
Short Acting Glucocorticoid
Rx: Primary & Secondary adrenal insufficiencies
Cortisone
Prodrug
Activated by 11B-HSD1 –> cortisol
Dexamethasone
Long Acting Glucocorticoid
No mineralcorticoid receptor activation (no salt-retention)
Prednisolone
Intermediate-Acting Glucocorticoid
Prednisone
Prodrug
Activated by 11B-HSD1 –> prednisolone
Fluticasone
Inhaled Glucocorticoid
Rx: asthma (patients who take inhaled B2-receptor agonists > 2x weekly)
MOA: ↑ B2 receptor expression, prevent B2 receptor desensitization
Fludrocortisone
Short Acting Mineralocorticoid
significant salt-retention
Rx: Primary adrenal insufficiency (Addison’s Dz)
Mifepristone
Glucocorticoid receptor antagonist
RU486: Lower doses = anti-progestin
Rx: inoperable patients w/ ectopic ACTH secretion or adrenal carcinoma
Ketoconazole
Corticosteroid synthesis inhibitor
MOA: inhibits 17A-hydroxylase (inhibits 11B-hydroxylase at high levels)
Rx: Cushing’s Syndrome
SE: liver toxicity
Metyrapone
Corticosteroid synthesis inhibitor
MOA: inhibits 11B-hydroxylase (inhibits both aldosterone & cortisol synthesis)
Rx: Cushing’s Syndrome, Diagnostic agent to evaluate ACTH production
Pituitary hypersecretion of ACTH
Decreased CRH
Increased ACTH
Dexamethasone test: 50% reductioin in cortisol
Adrenal adenoma
Decreased CRH
Decreased ACTH
Dexamethasone test: no reduction in cortisol
Ectopic ACTH production
Decreased CRH
Increased ACTH
Dexamethasone test: no reduction in cortisol