Corticosteroids Flashcards
Explain the CRF-axis
HT→ Corticotropin-Releasing Factor (CRF)
AP→ ACTH
Adrenal Cortex→ Glucocorticoids (ex: cortisol) & Mineralocorticoids (ex: aldosterone)
Endogenous aldosterone secretion primarily controlled by?
Endogenous aldosterone secretion primarily controlled by angiotensin II receptor activation on the adrenal cortex; secondary
control by ACTH from pituitary
Adrenal cortex disorders of hyper-activity
• Hyper-activity
– Cushing’s syndrome
– Hyperaldosteronism
Adrenal cortex disorders of hypo-activity
• Hypo-activity
– Addison’s disease
– Hypothalamic/pituitary issue
Corticorelin
- ) Drug class
- ) Will see ↑ in ?
- ) CRF
2. ) ↑ in ACTH, cortisol, and aldosterone
Cosyntropin
- ) Drug class
- ) Will see ↑ in ?
- ) ACTH
- ) ↑ in cortisol and aldosterone
- possible ↓ in CRF (due to negative feedback loop)
- ) Primary adrenal insufficiency consists of lesions of ?
2. ) Treatment
- ) Adrenal cortex
2. ) Treat with GR and MR agonist (b/c cortex can’t make either steroid)
- ) Secondary adrenal insufficiency consists of lesions of ?
- ) Treatment
- ) pituitary/hypothalmus
2. ) Treat with GR agonist
Therapeutic uses of Glucocorticoids?
-acute/chronic inflammation
-immunosupression
→ prevent organ transplant rejection
-replacement therapy in adrenal insufficiency
-hematologic disorder
Betamethasone
Glucocorticoid Receptor Agonist
Budesonide
Glucocorticoid Receptor Agonist
Clobetasol
Glucocorticoid Receptor Agonist
Cortisone
Glucocorticoid Receptor Agonist
Dexamethasone
Glucocorticoid Receptor Agonist
Fluticasone
Glucocorticoid Receptor Agonist
Hydrocortisone
Glucocorticoid Receptor Agonist
Methylprednisolone
Glucocorticoid Receptor Agonist
Mometasone
Glucocorticoid Receptor Agonist
Prednisolone /Prednisone
Glucocorticoid Receptor Agonist
Triamcinolone
Glucocorticoid Receptor Agonist
ADRs of Glucocorticoid Receptor Agonist
- Hyperglycemia (due to its ↑ GH effect)
- immunosupression
- growth retardation (eventually ↑ GH will diminish)
- HPA axis supression
HPA Axis Suppression
-After about one week of (systemic) GR agonist therapy, endogenous cortisol production is suppressed via negative feedback inhibition
– Takes 2-3 days for HPA axis to turn back on (SO for those 2-3 you don’t have cortisol and you could die)
***Why its important to taper
Mifepristone
Drug classes?
- )
- Glucocorticoid Receptor Antagonist
- Progesterone receptor antagonist
Fludrocortisone
- ) Drug class?
- )Mimics?
- ) Indication?
- ) Mineralcorticoid Receptor Agonist
- ) mimics aldosterone
- ) primary adrenal insufficieny
Aldosterone
MOA?
Binds to mineralocorticoid receptor → INCREASE # of Na channels → more Na/H20 reabsorption and K+ efflux
What drugs antagonize Aldosterone?
- Spironolactone
- Eplerenone