Mod 1 lecture 1: corticosteroids and antagonists Flashcards
what are the naturally occuring glucocorticoids
cortisol (hydrocortisone)
cortisone
what is the primary action of cortisol and cortisone
‘stress hormone’
what does cortisol and cortisone cause in the body
gluconeogensis in the liver - increase serum glucose
protein catabolims in extrahepatic tissue
fat catabolims in extrahepatic tissue
inhibits glucose uptake in muscle and adipose
Energy
what are the inflammatory and immune function of cortisol and cortisone
anti-inflammatory effects
immune response suppression
increase catecholamine production and response - increase BP
what releases CRH
hypothalamus
what releases ACTH
anterior pituitary
what releases cortisol
adrenal cortex
what does cortisol inhibit
CRH and ACTH
where is cortisol metabolized
liver
what are the corticosteroids
betamethasone
cortisone
dexamethasone
hydrocortisone
prednisone
methyprednisolone
triamcinalone
what are the mineralocorticoid agnoists and antagonists
fludrocortisone
spironolactone
eplerenone
what are the PK of corticosteroids
bound to corticosteroid bidning protein or albumin. metabolized by the liver and excreted by the kidney.
in CKD - would expect lower plasma protein, increased clearance, decreased t1/2. exception: prednisolone
What are the short acting glucocorticoids
1-12 hours
hydrocortisone and cortisone
have mineralocorticoid activity
liver will convert cortisone to hydrocortisone
kidney will convert hydrocortisone to cortisone
what are the intermediate acting glucocorticoids
12-36 hours
prednisone
prednisiolone
methyprednisiolne
triamcinolone
what are the long acting glucocorticoids
36-55 hours
betamethasone
dexamethasone
what are the key points regarding intermediate acting glucocortioids
have significanly more affinity to glucocortioid receptors
triamicolone has NO mineralocorticoid effects
prednisone is a prodrug that is first convered by the liver to prednisolone which is then metabolized
what are the key points regarding long acting glucocorticoids
only bind to glucocorticoid receptor
used for high dose injections and lung maturation
potency is important to keep in mind
what are the adrenal use for glucocorticoids
replacement therapy (hydrocortisone)
diagnosis of cushings syndrome (dexamethasone)
what are the non-adrenal uses of glucocorticoids
anti - inflammatory
anti-allergy
acceleration of lung maturation (antenatal)
what are the oral glucocoritoids
cortisone
dexamethasone
methyprednisolone
prednisone
what are the intra-articular glucocorticoids
methyprednisolone
tramcinolone
what are the inhaled/nasal glucocorticoids
beclomethasone
budesonide
flunisolids
fluticasone
mometasone
triamcinolone
what are the IV/IM drugs
betamethasone
dexamethasone
hydrocortisone
methyprednisonlone
prednsolone
what is an IM glucocortioid
triamcinolone