Endocrine Drugs

jmanderson's version from 2015-11-08 18:42

Section 1

Question Answer
levothyroxineDOC for hypoT4, half life 7 d, take on empty stomach, T3 --> T3 by deiodination
PTUthioamide, PTO inhibitor, deiodinase inhibitor, good for pregnancy, severe hepatitis, rarely fatal agranulocytosis
Methimazolethioamide, PTO inhibitor, more effective, severe hepatitis in fetus + mom (bad for pregnancy), rarely fatal agranulocytosis
Li+ for pre-tx of radioactive iodine for hyperT4 (improves outcomes)
LiuthyronineDOC for myxedema coma, AE of cardiotoxicity
Observation/supportive therapy (BBs, NSAIDs, steroids) tx for subacute viral thyroiditis
Iodide solution inhibit organification of I- (wolff-chaikoff effect), inhibit T4/3 release (inhibit TG proteolysis), decrease size and vascularity of hyperplastic thyroid glands
Iodide solution use prior to surgery or radioablation

Section 2

Question Answer
Fenfen 5HT2B agonist, cardiac valvulopathy, pulmonary HTN, cardiac fibrosis
RimonabantCB1 R antagonist / inverse agonist, anxiety, depression, suicide
Phentermine amphetamine analog (C-IV), increases NE and DA neurotransmission, MWL 2.16-3.6 kg, DI w/ other SSRIs
Orlistatpancreatic lipase inhibitor, wt loss, CV benefits, pt must do low fat diet to lower AEs (flatulence w/ discharge, oily spotting and fecal urgency)
Lorcasserin 5HT2C receptor agonist (C-IV), HA, dizziness, DI serotonin syndrome w/ dextromethorphan and SSRIs
Topiramate (phentermine/topiramate ER) C-IV, 70% pts lose 5% wt loss goal at 1 y, MWL = 9 kg, birth defects, REMS program to prevent birth defects
Topiramate (phentermine/topiramate ER) use in pts with concomitant SZ
bupropion antidepressant, increases dopamine, suicidal ideations, seizures, DI/CI with etOH (excess etOH or abrupt withdrawal  lowers SZ threshold), avoid in SZ pt
bupropion use in concomitant depressed pt
naltrexoneopioid receptor antagonist, nausea, DI w/ opioids
Common Combo for Obesity txbupropion/naltrexone
5HT2C receptor stimulates POMC neuron in arcuate nucleus to stimulate anorexigenic pathway in PVN of hypothalamus
5HTB1Ron arcuate nucleus to inhibit actions at lateral hypothalamus (orexigenic pathway), neuropeptide y from neuron is driven by cannabinoids stimulating back to arcuate nucleus, would cause satiety
fluoxeitineSSRI, use for concomitant depressed pt

Section 3

Question Answer
recombinant GH mimics GH, asphyxiation in severely obese or respiratory impaired pts w/ prader willi syndrome (sx = poor mm tone, low sex hormones, constant hunger)
rhIGF1admin SC, admin 20 min before/after CHO containing meal/snack to avoid hypoglycemia, AE hypoglycemia, use for pts w/ low GH/IGF-1
OctreotideDOC for acromegaly, somotostatin analogue, GI AE (N/D, abd cramps, flatulence, Steatorrhea), AE injection site pain, gallstones w/ LT use, bradyarrhythmias, expensive
Pegvisomant GH receptor antagonist, to normalize IGF-1, expensive, injection site pain, GI AE (N/D), monitor for elevated hepatic aminotransferase levels
bromocriptineDOC for hyperprolactinemia, dopamine receptor agonist, increase GH in healthy pts, decrease GH in acromegaly, not as effective at normalzing GH/IGF-1, but 50% improve in sx, cheaper than somatostatin receptor agonists
dexamethasone/prednisone long-acting synthetic glucocorticoids devoid of NaCl-retaining activity, avoid in Addison’s dz (adrenal insufficiency = low in all adrenocortical hormones)
IV electrolytes and hydrocortisone acute care for congenital adrenal hyperplasia (21-alpha def., hirsutism, irregular menses)
PO hyodrocortisone + fludrocortisone maintenance for congenital adrenal hyperplasia
fludrocortisonemineralocorticoid w/ glucocorticoid effects, HTN, hypoK, HF, monitor serum K and BP
aminoglutethimidelimits all active steroids (at high doses), for Cushing’s syndrome (adrenal adenoma type), AE (antiandrogenic SE  gynecomastia, decrease libido in males), increases hepatic transaminases
Metyraptone decreases cortisol and aldosterone synthesis, for Cushing’s syndrome, androgenic SE (hirsutism, acne), BP and electrolyte abnormalities
MitotaneDOC for cushing’s syndrome (adrenal adenoma etiology), cytotoxic agent, degenerates zona faxciulata and reticularis (adrenal atrophy), AE (N/D, lethargy, and somnolence)
Mifepristone (RU-486) progesterone receptor antagonist, induces abortion in early pregnancy, glucocorticoid receptor antagonist, use for Cushing’s syndrome (ectopic ACTH or adrenal CA etiology) when other therapies don’t work

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