Glucocorticoids Flashcards
what are the short acting glucocorticoids?
what is considered short acting?
Hydrocrotione
Prednisolone
12 hours
what are the intermediate acting glucocorticoids?
what is considered intermediate acting?
Triamcinolone
Flupresnisolone
12-36 hours
what are the Long Acting Glucocorticoids?
what is considered long acting?
Bethamethasone
Dexamethasone
more than 36 hours
what is the short and rapid acting hydrocortisone?
cortisol
what type of activity does hydrocortisone have?
glucocorticoid and mineralocorticoid
what type of activity does Prednisolone have?
it is the most potent glucocorticoid
what type of activity does Triamcinolone have?
glucocorticoid activity only
what are the most potent glucocorticoids?
Bethamethasone
Dexamethasone
what is one of the most potent glucocorticoids that doesnt retain water?
Dexamethasone
what is the mechanism of action of all glucocorticoids?
they penetrate cells => bind to cytoplasm and activate a receptor, GRE, that goes to the nucleus (glucocorticoid response element) => regulates transcription leading to mRNA and protein synthesis
what effect will glucocorticoids have?
- Carbohydrates: increases glyconeogenesis and glycognesis in fasting (more glucose made from liver)
- Proteins: catabolism of muscle to use amino acids for glucose
- Fat: increases lipolysis for more TAG’s usage, maintaining glucose supply to brain
- Inflammation: inhibits PLA2 => reduces COX 2 (less prostaglandins and leukotrienes)
-
Immunity: decreses Monocytes, Eosinophils, lymphoncytes, except NEUTROPHILS (increases)
- there is less cell mediated response: less IL-1/2, IFN-y
- inducers of cellular immunity
- there is less cell mediated response: less IL-1/2, IFN-y
-
Calcium metabolism: inhibits intestinal absroption of Ca and increases renal excretion of Ca
- loss of Ca from bone (osteoporosis in long use)
what do you use in Addison’s disease (chronic adrenal insufficiency)?
Hydrocortison + Fludrocortisone
what do you use in Addisonian crisis or Acute adrenal insufficiency?
IV Hydrocortisone
Diagnosis of Cushing’s Syndrome is done using what?
Dexamethasone suppression test
in what allergic reactions do you use glucocorticoids?
asthma (decreases # of cytokines and histmaine to supress inflammation)
urticaria
anaphylaxis
allergic drug reaction
in what inflammatory conditions do you use glucocorticoids?
Rheumatoid Arthritis
Osteoarthritis
Gout
name the mineralocorticoids?
Aldosterone
Fludrocortisone
Desoxycortiscosterone
what do the mineralocorticoids do?
- Increase Na+ reabsorption from DCT and CD
- Increase K+ and H+ excretion in urine
What are the Antagonists of Glucocorticoids drugs?
Metyrapone
Ketozonazole
Mifepristone
what does Metyrapone do?
inhibits 11-hydroxylation so it stops the synthesis of cortisol
what is the only glucocorticoid antagonist that can be used in pregnant women?
what is the glucocorticoid antagonist that can be used in Cushing’s syndrome?
what is the glucocorticoid antagonist that is used in testing the adrenal function?
metyrapone
metyrapone
metyrapone
what are 2 side effects of metyrapone?
hirsutism and edema
what does ketoconazole do?
when do you use it?
what can it cause?
it inhibits cholesterol desmolase
the 1st step in steroid synthesis
in cushing syndrome
hepatotoxicity
what does Mifepristone do in high doses?
when is it used?
it blocks glucocorticoid receptors
as a contraceptive and abortifacient when used with misoprostol
also used in cushings syndrome
what is the drug for primary hyperaldosteronism?
what is the drug for Conn’s syndrome?
spironolactone
spironolactone
what mineralocorticoid antagonist drug is used in hypertention?
eplerenone
what drug blocks 17,20 lyase?
what drug blocks conversion of testosterone to estrogen?
ketoconazole
aromatase
what drug blocks the action of aromatase enzyme?
how do you identify cushings disease?
how do you identify addison’s?
anastrazole
central obesity, peripheral thinning, purple striae
high BP, hyperpigmentation, hyperkalemia acidosis
