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100 Cards in this Set
- Front
- Back
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Bisphosphonates: MOA |
Form stable bond w/bone to prevent osteoclast binding and resorption |
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Bisphosphonates: examples |
- dronates (Zoledronic acid = most potent) |
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Bisphosphonates: AEs |
- Esophagitis (PO prep): take on empty stomach w/full glass of water - Transient acute phase reaction (IV prep): flu-like symtoms - Hypocalcemia, cardiac arrhythmias - Osteonecrosis of jaw - Atypical fractures - Contraindicated in renal failure |
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Denosumab: MOA |
Monoclonal antibody against RANK --> inhibit osteoclast activity |
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Denosumab: AEs |
- Hypocalcemia - Eczema - More prone to bacterial infections requiring hospitalization - Neoplastic complications |
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PTH analog: examples |
Teriparatide |
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PTH analog: MOA |
Paradoxically increases bone formation and osteoblast activity when administered at fluctuating levels |
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PTH analog: inications |
Severe ostoeporosis, with: - Severely depleted bone density (T score < -3.5 stdevs) - Multiple risk factors - History multiple osteoporotic fractures |
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PTH analog: AEs |
- Hypercalcemia - Uric acid stones, gout - Headache - Bon cancer: 2 year limit treatment duration - Contraindicated with comorbid bone disease, hypercalcemia gout, renal stones, renal/cardiac/hepatic patients |
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Calcitonin: indications |
Osteoporosis, hypercalcemic crisis |
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Calcitonin: MOA |
Counterregulatory to PTH: - Inhibits osteoclast activation and activity - Increase intestinal calcium excretion in intestine |
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Calcitonin: AEs |
- Epistaxis/rhinorrhea - Nausea/vomiting - Facial swelling - Allergies |
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Selective estrogen receptor modulators (SERMs): examples |
Raloxifene for osteoporosis Tamoxifen for breast cancer |
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Selective estrogen receptor modulators (SERMs): MOA |
Have mixed estrogen antagonism (breast, ovary) and agonism (MSK, adipocytes) |
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Calcimimietics: examples |
Cincalet |
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Calcimimietics: indications |
- Parathyroid cancer - Secondary hyperparathyroidism - Parathyroidectomy is contrainidcated |
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Calcimimietics: MOA |
Increases sensitivity of parathyroid calcium receptor --> decreased PTH secretion |
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Name all the classes of pharmacologic agents for osteoporosis/hyperparathyroidism |
1. Bisphosphonates 2. Denosumab 3. Calcitonin 4. Recombinant PTH 5. Selective estrogen receptor modulator 6. Calcimimetic agent 7. Estrogen (fallen out of favor) |
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Diazoxide: indications |
Insulinoma, congenital hyperinsulinemia |
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Diazoxide: MOA |
Primary mechanism: Maintains open ATP-sensitive K+ channel --> decreased insulin production
Secondary mechanisms: - Increases catecholamine release |
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Diazoxide: adverse effects |
- Fluid retention - Hypertrichosis - Coarse facies |
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Glucagon: indications |
Continuous infusion for newly diagnosed hypoglycemia in newborns |
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Ocreotide: indications |
Bridge for surgery for insulinoma |
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Ocreotide: MOA |
Synthetic somatostatin |
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Streptozocin |
Cytotoxic damage to pancreatic beta-cells for the treatment of hyperinsulinemia |
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List all of the pharmacolgoic agents for hypoglycemia |
1. Glucagon 2. Diazoxide 3. Ocreotide 4. Streptozocin |
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Ocreotide: AEs |
- Inhibits HPA/HPT axes - Decreased splanchnic circulation - Decreased gallbladder contractility, cholecystitis |
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List the pharmacologic options for SIADH |
Vasopressin antagonists: - Lithium - Demeclocycline - Covaptan - Tolvaptan |
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Dopamine agonists: indications, examples and pros/cons of each |
Indications: prolactinoma Bromocriptine: better in pregnancy, #1 choice in infertility Cabergoline: better tolerated, valvular heart disease in higher (Parkinson's) doses |
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Somatostatin agonists: indications |
- Acromegaly - TSH-secreting tumors - GI endocrine tumors |
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Somatostatin agonists: examples |
- reotides |
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Somatostatin agonists: AEs |
Gallstone and gallbladder "sludge" w/chronic use |
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Growth hormone antagonists: indications |
Acromegaly |
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Growth hormone antagonists: examples |
Pegvisomant |
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Growth hormone antagonists: MOA |
Prevent dimerization of growth hormone receptor |
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Thionamines: examples and advantages of each |
Methimazole (increased potency and DOA), Propylthiouracil (better in pregnancy |
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Thionamines: MOA |
Primary: interfere with synthesis of thyroid hormone Secondary: may have immunomodulatory functions. Also weakly inhibit T4 --> T3 conversion |
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Thionamines: AEs |
- Mild: GI upset, taste disturbances, skin rash - Hepatitis (PTU) - Birth defects (Methimazole) - Agranulocytosis - Lupus/vasculitis like symptoms |
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Iodine-131: MOA |
Radioactive tissue damage and inflammation to thryoid --> diminished thyroid function |
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Iodine -131: AEs |
- Hypothyroidism - Radiation thyroiditis - Adverse effects on pregnancy/lactation/fertility - Higher risk of cancer |
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Drugs used in hyperthyroid emergencies |
1. T4 2. IV hydrocortisone 3. High dose iodine (Wolff-Chaikoff effect) |
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T4 AKA |
Levothyroxine |
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Levothyroxine: dosing considerations |
1. Increase with weight gain 2. Increase dose with pregnancy (increased requirements) 3. Increase dose w/estrogen (upregulates thyroid binding globulin) 4. Increase dose with Fe, Ca2+, soy (decrease absorption) 5. Increase dose with phenytoin/rifampin (inducers of hepatic metabolism) |
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Outline the treatment approach to pheochromocytoma |
Alpha antagonism (phenoxybenzamine): Alpha-2 antagonism: increases insulin synthesis
Beta antagonism (Propanolol) Beta-1 antagonism: negative chromotrope/inotrope Beta-2 antagonism: adverse effects = vasoconstriction, bronchoconstriction
Alpha before beta always to prevent hypertensive crisis
Supplement w/Metyrosine, which blocks first step in catecholamine synthesis (tyrosine hydroxylase)
Medical treatment for 10 days, followed by surgical resection of pheo |
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Types of human insulin |
1. Regular human insulin 2. NPH |
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Types of analog insulin |
Long-acting (18-24 hrs): Determir, Glargine Short-acting (4 hours -best used post-prandially): Asparat, Lispro, Glulisine |
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Type I DM insulin regimens |
1. 1x or 2x daily long-acting analog insulin + postprandial short-acting analog insulin
2. NPR/insulin mixed x2/day,but leaves lunchtime hyperglycemia uncovered and is generally less predictable/preferable |
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Type II DM insulin regimens |
Begining: single bedtime injection of Glargine |
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Insulin AEs |
1. Hypoglycemia (more common in human insulin than analogs) 2. Weight gain 3. Lipohypertrophy at injection site that impairs absorption; rotate injection sites 4. Development of insulin antibodies --> inactivation , hypersensitivity |
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Most efficacious diabetes pharmacological agents for better glycemic control? |
- Insulin - Metformin - Sulfonylureas |
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Cheapest diabetes medications
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Metformin & Sulfonylureas |
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Combining diabetes meds |
Combine at your leisure - except Sulfonylureas and short-acting insulin secretagoes (same MOA --> severe hypoglycemia) |
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Indications for obesity pharmacotherpay |
BMI > 30 or BMI > 27 w/comorbidities |
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Name the non-insulin DM injectibles |
Pramlintide (TI and severe TII DM) GLP-1 agonists (TII DM) |
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Pramlintide: indications |
TIDM, advanced TIIDM |
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Pramlintide: MOA |
Amylin analog; prevents tendency of endogenous amylin to aggregate and become inactive. Same actions as endogenous amylin: decreases postprandial glucagon and slows gastric empyting. |
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Pramlintide: AEs |
1. Hypoglycemia (decrease insulin by 50%) 2. Nausea (titrate dose) 3. Adds x3/day injections and can't be mixed w/insulin |
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Sulfonylureas: MOA |
Closes ATP-sensitive K+ channel in beta pancreatic cell --> increases insulin secretion |
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Sulfonylureas: examples |
Glyburide, Glipizide, Glimepiride |
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Sulfonylureas: AEs |
1. Weight gain 2. Hypoglycemia (esp. Glyburide) |
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Short-acting secretagogues: MOA |
Close ATP-sensitive K+ channels in pancreatic beta-cells to increase insulin production (same as sulfonylureas, but with shorter binding times) |
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Short-acting secretagogues: indications |
Post-prandial administration for type II diabetes |
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Short-acting secretagogues: AEs |
- Weight gain - Hypoglycemia (less than Sulfonylureas) |
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Biguanides: examples |
Metformin |
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Biguanides: MOA |
Major: decrease hepatic gluconeogeneis Minor: increase skeletal muscle and adipocyte sensitivity to insulin
Neither is very well understood. |
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Biguanides: AEs & contrainidications |
AEs: - Lactic acidosis (advanced age, renal failure)
Contraindications: - Renal insufficiency - Decompensated heart failure - Hepatic dysfunction/alcohol abuse - Hold for hospitalization and contrast for imaging - Acute/chronic metabolic acidosis, including DKA |
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TZDs: examples |
-glitazones |
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TZDs: MOA |
Bind to PPAR-gamma transcription factor to induce transcription of proteins that promote adipocyte and muscle insulin sensitivity |
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TZDs: AEs |
- Cardiac: fluid retention/edema, congestive heart failure (esp. in conjunction w/insulin) - Increased risk of fractures - Increased risk of bladder cancer |
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Biguanides: indications |
- Type II DM (first-line) - Pre-diabetes - PCOS |
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Alpha-glucosidase inhibitors: examples |
Acarbose, Miglitol |
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Alpha-glucosidase inhibitors: MOA |
Competitively inhibits alpha-glucosidase in the brush border of the intestine, delaying the breakdown of polysaccharides to monosacchardies and thus slowing post-prandial glucose absorption. Also inhibits pancreatic alpha-amylase |
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Alpha-glucosidase inhibitors: AEs |
Flatulence |
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DPP-IV inhibitors: examples |
- gliptins |
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DPP-IV inhibitors: MOA |
Inhibit DPP-IV and thus prevent the breakdown of GLP-1 |
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DPP-IV inhibitors: AEs |
- Increased rate of nasopharyngeal infections/URIs - Pancreatitis |
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Colesevelam: MOA |
Binds bile-acid resins |
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Colesevelam: indication |
TIIDM, high LDLs |
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Colesevelam: AEs |
- Constipation - Hypertriglyceridemia - Decreased absorption of fat-soluble vitamin,s Levothyroxine, and OCPs` |
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Name all DM TII oral agents |
1. Sulfonylureas 2. Short-acting insulin secretagogues 3. Biguanides 4. TZDs 5. Alpha-glucosidase inhibitors 7. Colesevelam 8. Bromocriptine 9. SGLT-2 Inhibitors |
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Bromocriptine: indications |
TIIDM, Prolactinimoa |
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Bromocriptine: MOA |
Dopamine agonist that modulates metabolism through insulin-independent pathways |
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Bromocriptine: AEs |
- Nausea - Dizziness, orthostasis - Somnolence - Aggravation of psychosis - Drug interactions |
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SGLT-2 Inhibitors: Examples |
- glifozins |
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SGLT-2 Inhibitors: MOA |
Encourage glucose excretion by inhibiting sodium glucose linked transporter 2 in PCT of kidneys |
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SGLT-2 Inhibitors: AEs |
- Dehydration w/slight lowering of BP - Increased risk for UTIs - Increased LDL cholesterol - Weight loss |
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GLP-1 Agonists: examples |
Exenatide, Liraglutide |
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GLP-1 Agonists: MOA |
GLP-1 activity w/resistance to DPP-IV |
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GLP-1 Agonists: Aes |
- Nausea (less w/Liraglutide) - 1-2x daily injections - Pancreatitis (Liraglutide) - Contrainidicated in medullary thyroid cancer (Liraglutide) |
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Name the pharmacological agents for treating obesity |
1. Orlistat 2. Locaserin 3. Phentermine 4. Metormin |
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Orlistat: Indications |
Long-term treatment of obesity. Also helps with hyperlipidemia, hypercholesterolemia and type II DM |
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Orlistat: MOA |
Inhibits GI lipase --> malabsorption of fats |
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Orlistat: AEs |
- Flatulence - Incontinence - Increased defecation, steatorrhea - Abdominal cramps - Fat soluble vitamin deficiency |
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Orlistat: Efficacy |
5% more weight loss when compared w/placebo |
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Locaserin: indications |
Long-term treatment of obesity |
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Locaserin: MOA |
Appetite suppression via central serotonin 2C modulation |
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Locaserin: AEs |
- Headache - Dry mouth - Contraindicated in renal insufficiency, mood disorders and pregnancy |
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Phentermine: Indications |
Short term treatment of obesity (max 12 weeks) |
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Phentermine: MOA |
Sympathomimetic NE/dopamine uptake inhibitor |
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Phentermine: AEs |
- Highly addictive, tolerance-building - Overstimulation, euphoria, dysphoria - HTN, tachycardia |
