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41 Cards in this Set
- Front
- Back
Calcitonin
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opposite of PTH
suppress bone resorption produced by parafollicular cells act via GPCR regulated by Ca and PTH can treat hypercalcemia, osteoporosis, paget disease |
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treatment for hyperthyroidism
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thionamides
radioactive iodine surgery (then L thyroxine for resultant hypothyroidism) |
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Thionamides
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inhibit thyroid peroxidase-mediated iodination of thyroglobulin
methimazole propylthiouracil |
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Methimazole
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thionamide
better choice if 1 treatment chosen |
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propylthiouracil
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blocks peripheral conversion of T4 to T3
treat thyrotoxic crisis |
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thionamide tox
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methimazole can cause cholestatic jaundice
both can cause rash, arthritis, rarely-agranulocytosis |
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5 alpha reductase inhibitors
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treat BPH/MPB
block conversion of testosterone to dihydrotestosterone |
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bisphosphonates
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tx osteoporosis, osteopenia, paget's
MOA- antiresorptive, inhibit osteoclasts by blocking farnesyl pyrophosphate synthesis |
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Alendronate
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most potent bisphosphonate
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Etidronate
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bisphosphonate
give cyclically |
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bisphosphonates tox
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erosive esophagitis
must take on empty stomach, full glass water, remain upright |
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Glucocorticoids effect on bone
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antagonize vit D-mediated absorption of Ca++ and PO4
partially block reabsorption of Ca and PO4 in kidney may enhance PTH-mediated bone resorption |
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Estrogens effect on bone
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adsorb to bone crystals and render them resistant to enzymatic hydrolysis
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Calcitriol
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regulate gene txn
dec PTH stimulate Ca and PO4 absorption from GI stimulates FGF23 release from bone (inhibits VitD production) |
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RANKL + MCSF
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differentiation and activation of osteoclasts
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FGF23 excess
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osteomalacia
(inhibits calcitriol production and dec phosphate levels) |
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Ganirelix
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GnRH antagonist, tx prostate ca
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flutamine
bicalutamine nilutamide |
treat hirsuitism
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Sulfonylureas
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Glipizide
Glyburide Glimepiride inc intracellular Ca= release insulin can cause hypoglycemia |
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Biguanides
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metformin
enhances insulin's suppression of gluconeogenesis enhance glucose uptake by skeletal mm dec TG and LDL no hypoglycemia |
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Thiazolidinediones TZDs
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Pioglitazine
Rosiglitazone reduce insulin's resistance inc glucose utilization in muscle reduce TG, inc HDL no hypoglycemia |
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Glinides
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type 2 DM tx
repaglinide exenatides GLP-1 analog |
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Dipeptidylpeptidase 4 inhibitor (DPP4)
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type 2 DM tx
Sitagliptin Saxagliptin |
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alpha glucosidase inhibitors
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acarbose
miglitol bind jejunal brush border cleave oligo and monsaccharides |
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Insulins
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fast acting: Apart, Lispro, Glulisine
NPH (neutral protamine hagedorn) Glargine- no peak Detemir-no peak |
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Maximum effect on A1C
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metformin>glipizide>glimepiride
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SERMs
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tamoxifen
nonsteroidal estrogen receptor ligand agonist in bone and endometrium antagonist in breast (dec stimulatory GF like TNFalpha and inc inhibitory like TNF beta) |
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tamoxifen metabolism
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CYP2D6 transforms it to endoxifen (100x more potent)
SSRIs dec conc of endoxifen |
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Aromatase MOA and indication
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convert androgens to estrogens
treat locally advanced or metastatic breast ca (not for premenopausal women) |
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premenopausal treatment for breast ca
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premenopause = surg, chemo, then tamoxifen (NEVER chemo+hormonal)
ovarian ablation |
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postmenopausal treatment for breast ca
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surgery
tamoxifen chemo if necessary selective aromatase inhibitor progestins |
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GnRH agonist
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LHRH agonist
treat prostate cancer tumor flare- surge tesosterone before feedback loop inhibits (bone pain, neuropathy, hematuria, urinary obstruction) |
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abiraterone
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treat castration-resistant prostate ca (pts previously treated with docetaxel)
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combined androgen blockade
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GnRH agonist + anti androgenic
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hormones manipulated in oral contraception
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GnRH stimulates FSH and LH
FSH stimulates estradiol secretion and stimulates follicles progesterone is more dominant hormone in 2nd 1/2 of cycle |
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why estrogen in contraceptives?
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negative feedback to pituitary = inhibit FSH and ovulation
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why progestins in contraceptives?
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negative feedback to pituitary= inhibit ovulation (<estrogen)
endometrial atrophy thicken cervical mucus |
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Anastrozole
Exemestane Letrozole |
aromatase inhibitors
prevent conversion to estradiol |
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Goserelin
Leuprolide |
Gonadotropin releasing hormone agonists
suppress FSH and LH to treat ca |
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Bicalutamide
Flutamide Nilutamide Abiraterone |
anti-androgenic agents
nonsteroidal ligands |
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MOA of insulin
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binds tyrosine kinase transmembrane receptor
phosphorylates tissue specific substrates (IRS1, SH2) change gene expression to upregulate lipoprotein lipase, fatty acid synthase, glucokinase |