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13 Cards in this Set
- Front
- Back
- 3rd side (hint)
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What are corticosteroids? What are the 2 major groups and what secrets them?
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Steroid hormones produced by adrenal cortex: glucocorticoids (cortisol) and mineralocorticoids (aldosterone)
Out (salt-y) to In (sweet) - GFR Zona Glomerulosa (aldosterone), Fasciculata (cortisol), Reticularis (sex hormones) |
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What are the effects of cortisol and glucocorticoids?
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Gluconeogenesis (inc glucose to provide energy), lipolysis (can lead to fat deposition - buffalo hump, moon facies in cushing's)
Increased catabolism (can lead to osteoporosis, decreased growth in children) IMMUNOSUPPRESSIVE: inhibit CMI, decrease lymphocytes, eo's, baso's, mono's, only inc PMNs ANTI-INFLAMMATORY: dec wbc's above, inhibit migration of leukocytes and other effects... |
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Cortisol is highly bound to CBG (corticosteroid binding globulin). What increases CBG and what increases the secretion of cortisol?
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Increase:
Estrogen tx, pregnancy, hyperthyroidism, DM, hematologic, congenital Inc secretion: Exercise, stress, anxiety/depression, anorexia, alcoholism, chronic renal failure |
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What is mitotate? Describe its MOA, AEs, and use.
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Steroidogenic inhibitor: inhibits steroid synthesis, inhibits adrenal cortisol release (slow onset, monitor free cortisol)
AE: LOTS!! GI, Neuromusc, CNS depression Use in adrenalectomy (complete ablation of cortisol production) |
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What is the MOA of KETOCONAZOLE? What are its uses and AEs?
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(adrenal enzyme inhibitor, antifungal)
Inhibits 17-alpha-hydroxylase, 11-beta-hydroxylase, cholesterol desmolase -- potent TESTOSTERONE inhibitor Reduce steroid levels (adrenal carcinoma, hirsutism, breast and prostate cancer), wide use AEs: LFTs (monitor!), GI Gynecomastia/decreased libido/impotence P450 inhibitor |
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What are the MOAs of aminoglutethimide and metyrapone? What are their uses/AEs?
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Aminoglutethimide: inhibits cholesterol desmolase (all steroid synthesis)
AE: BONE MARROW suppression, drug-induced LUPUS Metyrapone: inhibits 11-beta-hydroxylase (dec cortisol) AE: aldosterone effects (hypokalemia, edema), rash, hirsutism Use together for steroid-producing adrenocortical cancer Metyrapone for dx adrenal fcn |
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What is mifepristone? Describe its MOA, AE and use.
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Glucocorticoid antagonist: competitively inhibit at receptor
Tx: Cushing's syndrome, long term effects not known |
(not related)
other antagonists: spironolactone and eplerenone are aldosterone antagonists |
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What is FLUDROCORTISONE acetate and its use?
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Potent synthetic mineralocorticoid
Tx: replacement tx after adrenalectomy, primary adrenal insufficiency (dose based on K level and BP) |
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What are the glucocorticoids or corticosteroid replacement drugs (separated by kinetics)?
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Short-acting, least potent, some antiflamm activity, some mineralocorticoid (salt retention): CORTISONE, Hydrocortisone
Interm-acting, some potency, some anti-inflamm: Triamcinolone, Methylprednisone, PREDNISONE (some mineralocorticoid) Long-acting, Potent, High anti-inflamm, NO mineralo: DEXAMETHASONE, Betamethasone |
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What are the numerous AEs of glucocorticoids?
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Cushing's-like
Aldosterone-like: HTN, hypokalemia Anti-inflamm: infection, less wound healing, less wbcs (except pmns) Bone: osteoporosis, growth inhibition Hyperglycemia Hyperlipidemia PUD, myopathy, behav changes, cataracts Teratogenicity |
Prevent osteoporosis with Ca, VitD, weight bearing exercise, biphosphonates
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What can happen with withdrawal of glucocorticoid tx?
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Disease flare-up
ACUTE ADRENAL INSUFFICIENCY: N/V, fatigue, hypoglycemia, hypotension, myalgia, dizziness, dyspnea, arthralgia |
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How should you administer and withdraw glucocorticoid tx do avoid AEs?
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Alternate day dosing (QOD), start LOW, go SLOW
Taper to physiologic dose at end of tx and switch to short-acting at end Mimic circadian pattern of cortisol, adjust dose under illness, stress, sx |
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What are the uses of glucocorticoid tx?
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Adrenal disorders: Addison's, acute adrenal insufficiency, congenital adrenal hyperplasia to suppress ACTH
Nonadrenal: LOTS. Inflamm/immunologic (asthma: remember beclomethasone and budesonide?), cancers, neuro, hypercalcemia... |
(side note)
Betamethasone: give to pregnant women in premature labor to hasten fetal lung maturation |
