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30 Cards in this Set
- Front
- Back
what are the metabolic effects of glucocorticoids?
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stimulate gluconeogenesis, insulin secretion, lipolysis and lipogenesis;
catabolism of muscle proteins, lymphoid tissue, cartilage, bone, fat and skin |
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immune effects of glucocorticoids?
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decrease lymphocytes, eosinophils, basophils, and monocytes;
increase neutrophils; inhibit leukocyte migration |
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other than immune suppression and metabolic effects, what effects do glucocorticoids have on the body?
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aid in renal excretion of water
CNS effects in large doses stimulate gastric acid in large doses |
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at what time of day does cortisol peak in the system?
when is it at its lowest? |
high in AM
lowest around midnight |
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this glucocorticoid has moderate salt-retaining mineralocorticoid effects
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cortisol
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glucocorticoid with longest duration?
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dexamethasone (24-36 h)
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glucocorticoid with most anti-inflammatory effects?
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dexamethasone (30x cortisol)
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benefits of synthetic glucocorticoids?
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less salt-retention, longer half-life, better penetration of lipid barriers for topical activity
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why are glucocorticoids administered in some kinds of CAH?
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suppress ACTH secretion to reduce synthesis of abnormal steroids
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corticosteroid given to pregnant women to help fetal lung maturation?
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betamethasone
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toxic metabolic effects of glucocorticoids?
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growth inhibition, diabetes, muscle wasting, osteoporosis
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how should glucocorticoids be administered to avoid pituitary insufficiency?
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alternate-day therapy, tapering soon after achieving therapeutic response or when discontinuing
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pts on long-term glucocorticoids may need what to avoid adrenal crises?
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additional "stress doses" of glucocorticoids during serious illness or before major surgery
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what is the naturally occuring precursor of aldosterone?
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deoxycorticosterone
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mineralocorticoid given after adrenalectomy d/t its long half-life?
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fludrocortisone
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glucocorticoids aerosolized and used for asthma?
why? |
beclomethasone, budesonide
readily penetrate airway mucosa but very short half-lives after entering blood |
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aldosterone receptor antagonists?
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spironolactone, eplerenone
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clinical use of aldosterone receptor antagonists?
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potassium-sparing diuretics
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competitive inhibitor of glucocorticoid receptors and progesterone receptors?
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Mifepristone (RU-486)
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clinical use of mifepristone?
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treat Cushing's syndrome, emergency contraceptive
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drugs used in treatment of adrenal cancer?
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aminoglutethimide, metyrapone, ketoconazole
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MOA of ketoconazole?
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inhibits P450 enzymes necessary for steroid synthesis
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clinical uses of ketoconazole?
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adrenal carcinoma, hirsutism, breast and prostate cancer
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MOA of aminoglutethimide?
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blocks chol --> pregnenolone (desmolase)
inhibits all steroid synthesis |
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clinical use of aminoglutethimide?
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used with other drugs for tx of steroid-producing adrenocortical cancer
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MOA of metyrapone
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blocks cortisol synthesis by inhibiting 11b-hydroxylase
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clinical use of metyrapone?
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used in diagnostic tests of adrenal fxn
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what is a glucocorticoid response element?
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a specific nucleotide sequence on DNA recognized by steroid hormone receptor-hormone complex
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mineralocorticoid loss in acute adrenal insufficiency can lead to what?
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dehydration
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TxOC for acute adrenal insufficiency?
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cortisol + fludrocortisone
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