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