Endocrine Pharmacology III - Glucocorticoids and Mineralocorticoids

  1. Adrenal agents
  2. Hypothalamus releases CRH (Corticotropin releasing hormone) causing the anterior pituitary to release adrenocorticotropin, which causes the adrenal glands to release glucocorticoids and mineralocorticoids
  3. Low mineralocorticoids (as seen in Addison's disease) - low blood pressure, salt craving
  4. ACTH (socyntropin) is used clinincally to diagnose whether adrenal insufficiency is central or peripheral
  5. Fludrocortisone is a synthetic glucocorticoid with salt-retaining properties given to patients with mineralocorticoid deficiencies
  6. Desoxycorticosterone acetate has salt-retaining properties but no inflammatory properties; given to treat mineralocorticoid deficiency
  7. Hypertension/edema is a sign of primary aldosteronism or Cushing's syndrome (excess cortisol as a result of hyperadrenalism), as is moonface, purple skin
  8. Spironolactone is used to treat high levels of mineralocorticoids (aldosteronism) by antagonizing aldosterone receptors and androgen receptors
  9. Eplerenone is a more selective aldosterone receptor antagonist
  10. Drospirenone is an aldosterone antagonist
  11. Low glucocorticoids manifests in a large number of ways
  12. Hydrocortisone is most commonly given for patients with low glucocorticoid production
  13. Hydrocortisone is given IV during cases of acute adrenal insufficiency
  14. Dexamethasone is given during pregnancy for patients at a high risk for adrenal hyperplasia
  15. Side-effects of glucocorticoids can include insomnia, peptic ulcers, etc.
  16. Iatrogenic Cushing's syndrome can occur from long-term glucocorticoid use
  17. Adrenal suppression is a consequence of long-term glucocorticoid use
  18. Glucocorticoid use needs to be tapered to avoid withdrawal symptoms (hyponatremia, lethargy, hyperkalemia)
  19. Cushing's syndrome (adrenal hypersecretion) causes thin, fragile skin, obesity, and other symptoms
  20. Low-dose Dexamethasone can determine if patients have Cushing's syndrome (ACTH should decrease)
  21. Aminoglutethimide blocks the conversion of cholesterol and reduces production of all active steroids
  22. Ketoconazole inhibits cholesterol side chain cleavage required for steroid biosynthesis
  23. Etomidate inhibits adrenal steroidogenesis and is the only parenteral agent that can treat Cushing's
  24. Metapyrone can only be given on a compassionate basis - "end-stage" symptoms or resistant to other treatments
  25. Mifepristone (RU-486) is a glucocorticoid receptor antagonist, used for inoperable ectopic ACTH excretion
  26. Mitotane has cytotoxic action on the adrenal cortex to reduce tumors - "compassionate" basis