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38 Cards in this Set
- Front
- Back
Dopamine agonist treatment for prolactinoma
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Bromocriptine (D2/D1) and Cabergoline (D2)
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Side effects of Cabergoline
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Headache, nausea, orthostatis HTN; discontinue for psychosis
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Treatment for Acromegaly: Octreotide
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Somatostatin analogue (cholesterol gallstones common)
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Treatment for Acromegaly: Bromocriptine
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Dopamine agonist (20% see improvement)
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Treatment for Acromegaly: Pegvisomant
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Competitive GH-receptor antagonist
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Dexamethasone testing for HPA differentiation on cortisol
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Adrenal/ectopic ACTH-production cortisol levels NOT suppressed by negative feedback
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Metyrapone testing
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If ACTH rises, but cortisol precursors don't, signals adrenal insufficency. If neither ACTH or precursors rise, impaired HPA axis. (MOA: blocks conversion of precursors to cortisol)
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Vasopressin receptors
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V1- vasoconstrictor (IP3,Low affinity); V2- antidiuretic (cAMP, high); V3- ACTH stimulation from pituitary
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Desmopressin receptor selectivity
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V2- antidiuretic
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Desmopressin in DI treatment
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Central (eliminates thirst/fluid intake), Dipsogenic (eliminates urination, not thirst/intake)
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Water deprivation test
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Central/polydipsia respond as normal. Central responds with Desmopressin. Nephrogenic never responds.
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Treatment for SIADH
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Cautious infusion of hypertonic saline / furosemide (diuretic) (not too quickly, avoid demyelination); fluid restriction if not severe, V2 receptor antagonists (Aquaretics)
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Somatropin MOA
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Recombinant human GH
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Mecasermin MOA
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Agonist directly at IGF-1 receptor in target tissues if somatropin fails
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Desmopressin MOA
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Selective V2 receptor agonist in kidney (antidiuretic)
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Cellular response to Desmopressin
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Activates G protein in V2 receptor; activation of kinases to receptor coupled aquaporin; increases transport of H2O to reverse hyperosmolality; dilutes concentration of sodium
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Vasopressin
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Non-selective V1/V2 receptor; corrects low bp; may lead to HTN / CNS toxicity
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Octreocide MOA
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Somatostatin receptor to inhibit GH release; injection; gallstones, GI, hyperglycemia, hypoinsulinemia
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Pegvisomant MOA
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Liver GH receptor antagonist; blocks IGF-1 production
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Conivaptan MOA
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Non-seletive vasopressin V1/V2 receptor antagonist (SIADH), reduces hyponatremia
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Tolvaptan MOA
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Oral V2 antagonist (SIADH)
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Common side-effects of dopamine receptor agonists
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Bromocriptine/Cabergoline- orthostatic HTN, ergot-related (burning), CV risk (arrythmia), CNS (delusions, hallucinations, psychosis)
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Mineralocorticoid MOA
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Alters transcription to increase Na+/K+ ATPase expression (inc. blood vol.)
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Glucocorticoid MOA
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Dislodged heat shock protein (HSP), activates receptor, activates glucocorticoid response element (GRE)
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Anti-inflammatory MOA of glucocorticoids
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Cortisol binds GRE, prevents transcription of cytokines and increases anti-inflammatory transcription (PLA2 inhibitor)
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Adrenal steroid agonist with 1:1 ratio
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Hydrocortisone (gluco:mineralo)
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Short-acting, low selectivity corticosteroids
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Prednisone (oral), prednisolone, methyprednisolone
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Intermediate-acting low selectivity corticosteroids
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Triamcinolone
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Long-acting, highly selective corticosteroids
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Betamethasone, dexamethasone, beclomethasone (antiinflammatory effect)
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MOA for corticosteroids
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Increase transcription of lipocortin-1 (inhibits PLA2)
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Long-term effects of corticosteroids
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Catabolic (growth suppression, muscle loss), osteoporosis, cataracts/glaucoma, neurological (hypomania, psychosis, insomnia, anxiety)
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Why must pt ween off of corticosteroids?
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Adrenal suppression
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Tx for Addison's
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Hydrocortisone, androgens, fludrocortisone (selective mineralocorticoid receptor agonist)
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Reason for iatrogenic Cushing's in pt on Ritonavir
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Ritonavir is a CYP3A4 inhibitor, required for corticosteroid metabolism
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Ketoconazole MOA
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Inhibits 17a-hydroxylase and 11B-hydroxylase
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Aminoglutethimide MOA
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Inhibits Cholesterol desmolase and aromatase; nausea, dizziness (decreased T4 -> T3 conversion)
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Major ketoconazole effect
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CYP3A4 inhibitor (drug interactions), hepatotoxicity
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Metyrapone MOA in Cushing's Tx
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11B-hydroxylase inhibitor, causes HTN (precursor build-up), androgenic
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