Glucocorticoids

3 layers of adrenal cortex

zona glomerulosa, zona fasciculata, zona reticularis

Glucocorticoid Effects

Promote normal intermediary metabolism (Hepatic glucose production, lipolysis)

Increase resistance to stress

Alter blood cell levels in plasma (decrease eiosinophils, basophils, lymphocytes - increase RBCs and PLTs

Anti-inflammatory action

name the short acting glucocorticoids

Hydrocortisone

Cortisone

name the intermediate acting glucocorticoids

prednisone

prednisolone

methylprednisolone

triamcinolone

name the long acting glucocorticoids

Betamethasone

Dexamethasone

corticosteroids includes

glucocorticoids and mineralocorticoids

Name the mineralocorticoids

Fludrocortisone

Name the mineralocorticoid antagonists

Spironolactone, Eplerenone

MOA hydrocortisone

Glucocorticoid receptor agonist

Therapeutic use hydrocortisone

Addison disease replacement therapy

ADE hydrocortisone

HPA suppression; Cushingoid effects; hyperglycemia; infection risk; osteoporosis

Pearls hydrocortisone

2/3 AM + 1/3 PM dosing; may need fludrocortisone

MOA betamethasone

Glucocorticoid receptor activation

Therapeutic use betamethasone

Promote fetal lung maturation

ADE betamethasone

Hyperglycemia; infection risk

Pearls betamethasone

Crosses placenta; given IM 48 hours before delivery

MOA dexamethasone

Glucocorticoid receptor agonist

Therapeutic use dexamethasone

Dexamethasone suppression test (Used to diagnose Cushing syndrome); fetal lung maturation; inflammation

ADE dexamethasone

Typical glucocorticoid ADEs

Name the 3 layers of the adrenal glands and what they secrete

zona glomerulosa -> aldosterone

zona fasiculata -> cortisol and androgens

zona reticularis -> NE and Epi

MOA prednisolone

Glucocorticoid receptor agonist

Therapeutic use prednisolone

Inflammatory conditions

ADE prednisolone

Systemic steroid ADEs

what do corticosteroids regulate?

carbohydrate metabolism

MOA fludrocortisone

Mineralocorticoid agonist

Therapeutic use fludrocortisone

Adrenal insufficiency

ADE fludrocortisone

Hypertension; fluid retention; hypokalemia

Pearls fludrocortisone

Titrate based on BP and upright posture; half-life >24 hrs

MOA spironolactone

Mineralocorticoid receptor antagonist; androgen blocker

Therapeutic use spironolactone

CHF; hyperaldosteronism; hirsutism in women

ADE spironolactone

Hyperkalemia; gynecomastia; menstrual irregularities

MOA eplerenone

Selective aldosterone receptor antagonist

Therapeutic use eplerenone

CHF; hyperaldosteronism

ADE eplerenone

Hyperkalemia

Pearls eplerenone

Lower endocrine side effects than spironolactone

ADE of long-term glucocorticoids

HPA suppression; drug-induced Cushing syndrome; osteoporosis; hyperglycemia; infections; mood changes; hypertension; GI ulcers

what do mineralcorticoids regulate?

electrolytes

Signs of Cushingoid appearance

Buffalo hump; moon face; hirsutism; central fat redistribution

which glucocorticoid have mineralocorticoid activity

Fludocortisone

effect of sudden discontinuation of steroids

exogenous steroids suppress the HPA axis, leaving the patient unable to produce endogenous cortisol, which can lead to adrenal crisis and death when supplemental steroids are discontinued

someone taking >20 mg prednisone for more than 3 weeks and/or has a cushingoid appearance likely has:

HPA suppression

how do glucocorticoids promote normal intermediary metabolism?

increase hepatic glucose production

stimulate lipolysis

how do glucocorticoids increase resistance to stress?

improve energy availability (mobilize fuel)

how do glucocorticoids alter blood cells in plasma?

decrease eisinophils, basophils, lymphocytes

increase RBCs and platelets

How do glucocorticoids produce anti-inflammatory actions?

decrease inflammatory cytokines

stablize mast cells

block arachidonic acid

inhibit immune cells

Do glucorticoids improve immunity?

NO. They improve survival during infection by preventing the host from being killed by its own inflammatory response.