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51 Cards in this Set

  • Front
  • Back
Characteristics of glucocorticoid receptors and how it upregulates gene expression
nuclear receptor
receptors are in complexes with heat shock proteins (Hsp90)
free glucocorticoid hormone binds complex in the cytosol and allow conformational change to dissociate heat shock protein
ligand-bound receptor complex is actively transported into the nucleus
this homodimer (two receptor-ligand complex) binds to glucocorticoid receptor elements in the promoter region of genes
why can prednisone be administered to pregnant women without fetal side effects
because the fetal liver is non-functional and does not activate prednisone
Anti-inflammation and immunosuppressive effects of glucocoticoids
decreases circulating lymphocytes, monocytes, eosinophils, and basophils, they move from vascular bed to lymphoid tissue
increase circulating neutrophils
inhibit the function of tissue macrophages
reduce prostaglandins, leukotrienes, and COX-2
vasoconstriction by suppressing mast cell degranulation
decrease capillary permeability by reducing histamine release
inhibits phospholipase A2
glucocorticoids
3 corticosteroids with no topical activity
cortisone
prednisone
fludrocortisone
*oral only
4 corticosteroids no with salt-retaining ability
methyprednisolone - short-acting
triamcinolone - intermediate-acting
betamethasone - long-acting
dexamethasone - long-acting
what should always be given along with synthetic glucocorticoids without salt-retaining activity
fludrocortisone
corticosteroids with most salt-retaining activity
fludrocortisone
what should be given to a pregnant women with high risk for congenital adrenal hyperplasia
dexamethasone to suppress the release of fetal ACTH
Also fludrocortisone to maintain normal blood pressure
what does an overnight dexamethasone test screen for
patients with suppression of plasma cortisol to < 1.8 ug/dL strongly suggests the patient does NOT have Cushing's syndrome
what is done after a patient tests positive during the overnight dexamethasone suppression test
formal dexamethasone test to distinguish between pseudo-cushing's syndrome and actual cushing's syndrome
differentiate the results of the formal dexamethasone suppression test
suppression of cortisol - pseudo-cushing's syndrome (anxiety)
no suppression - cushing's syndrome
what is the high-dose dexamethasone test used to distinguish
whether the cushing's syndrome is pituitary-dependent or ectopic production of ACTH
differentiate the results of the high-dose dexamethasone test
suppression of cortisol - pituitary-dependent cushing's syndrome
no suppression - ectopic production of ACTH
what is used to diagnose primary adrenal insufficiency, diminished response of cortisol to stimulation by this drug
cosyntropin (synthetic ACTH)
synthetic ACTH
cosyntropin
what regulates lung maturation
cortisol
what is given to reduce the incidence of respiratory distress syndrome in infants delivered prematurely
IM betmethasone
3 mechanism of action for corticosteroid inhaler used in asthma
1. anti-inflammation
2. potentiation of B-agonist effects
3. vasoconstriction
what happens to the adrenal cortex during glucocorticoid therapy
atrophy due to suppression of ACTH release
what can abrupt cessation of glucocorticoid therapy result in
acute adrenal insufficiency
common adverse effects of corticosteroids
osteoporosis
infection
hypertension
edema
peptic ulcers
glaucoma
hypokalmia
what two occasions caused increased amounts of deoxycorticosterone (DOC)
adrenocortical carcinoma
17B-hydroxylase deficiency
synthetic mineralcorticoid used to treat adrenocortical insufficiency
fludrocortisone
blocks the conversion of cholesterol to pregnenolone and causes reduction in synthesis of all hormonally active steroids
aminoglutethimide
two indications for aminoglutethimide
1. breast cancer to reduce estrogen
2. malignancy of adrenal cortex to reduce secretion of steroids
associated with increases the clearance of dexamethasone and reducing it's half-life
aminoglutethimide
potent and nonselective inhibitor of adrenal and gonodal steroid synthesis
ketoconazole
used in the treatment of cushing's syndrome
ketoconazole
potent glucocorticoid antagonist and an antiprogestin
mifepristone (RU 486)
mechanism of axn of mifepristone
forms a complex with glucocorticoid receptor
2 indications for mifepristone
1. treats inoperable patients with ectopic ACTH secretion
2. adrenal carcinoma who have failed to respond to other treatments
inhibits aldosterone and testosterone synthesis
spironolactone
indicated for the treatment of primary aldosteronism
spironolactone
indicated for the treatment of hirsuitism in women
spironolactone
mechanism of axn of spironolactone
competes with the mineralcorticoid receptor and possibly interferes with androgen receptor
adverse effects of spironolactone
hyperkalemia
gynecomastia
mineralcorticoid receptor antagonist that only binds to that
eplerenone
long-acting glucocorticoids
betamethasone
dexamethasone
inhibits 11B-hydroxylase activity
metyrapone
used to treat cushing's syndrome in pregnant women
Metyrapone
metryapone adrenal insufficiency test
1. Increased 11-deoxycortisosterone (DOC) along with increased ACTH is normal result
2. Reduced DOC with increased ACT suggests primary adrenal insufficiency
3. No increase in DOC along with no increase in ACTH suggests hypothalamic-pituitary malfunction
treatment of Addison's disease
hydrocortisone + fludrocortisone
treatment of Cushing's syndrome
ketoconazole + hydrocortisone
treatment of congential adrenal hyperplasia
dexamethasone;
then hydrocortisone + fludrocortisone
associated with treatment of breast cancer
aminoglutethimide
used in the treatment of asthma
beclomethasone
inhibits the cyptochome P450 enzymes necessary for the synthesis of all steroids
ketoconazole
antagonist of glucocorticoid receptor by forming a complex with glucocorticoid receptor; also an anti-progestin
mifepristone (RU-486)
indicated uses for mifepristone
medical abortion
very rarely cushing's syndrome
steroid synthesis antagonist associated with hepatic dysfunction as an adverse effect
ketoconazole