USMLE First Aid 2016 Pharm: Endocrine – Flashcards
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Lispro, Aspart, Glulisine
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Rapid acting Insulin
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Risks of all insulin:
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Hypoglycemia, lipodystrophy, rare hypersensitivity reaction
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This is the only short acting insulin:
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Regular
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This is the only intermediate acting insulin:
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NPH
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Detemir, glargine:
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long acting insulins
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Diet for Type 1 DM:
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Low carb, insulin replacement
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Treatment plan for Type II DM:
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Dietary modification, exercise for weight loss; oral agents, non-insulin injectables, insulin replacement
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Treatment plan for GDM:
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dietary modifications, exercise, insulin replacement if lifestyle modification fails
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This drug decreases gluconeogenesis, increases glycolysis, increases peripheral glucose reuptake and insulin sensitivity, is the first line therapy in type 2 DM, causing modest weight loss, doesn't need functioning islets
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Metformin (Biguanide)
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Lactic acidosis is the most serious adverse effect of this oral hypoglycemic drug, also seen GI upset and is contraindicated in renal insufficiency
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Metformin (Biguanide)
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Chlorpropamide, tolbutamide are:
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First generation sulfonyureas
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Chlorpropamide and tolbutamide are associated with what unique SE:
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Disulfram like effects (also increase risk of hypoglycemia in renal failure and weight gain)
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Glimepiride, glipizide, glyburide are:
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Second generation sulfonylureas
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These hypoglycemic drugs close K channels in B-cell membrane leading to cell depolarization, insulin release via elevated Ca influx, thus stimulating release of endogenous insulin in type 2 DM, need some islet function in type 1 DM
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Sulfonyureas
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These can be used as mono therapy in 2DM, safe in renal impairment, cause increase in insulin sensitivity in peripheral tissue by binding PPAR-gamma nuclear transcription regulator:
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Glitazones/thiazolidinediones (piglitazone, rosiglitazone)
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The SE of these oral hypoglycemic drugs included weight gain, edema, hepatotoxicity, HF, and increase risk of fracture:
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Glitazones/thiazolidinediones
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This class of oral hypoglycemic drugs can be used as a mono therapy in type 2 or combined with metformin, they stimulate postprandial insulin release by binding to K channels on Beta cell membranes (different site than sulfonylureas)
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Meglitinides (nateglinide, repaglinide)
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Risks of this class of hypoglycemic drug are hypoglycemia increased in renal failure and weight gain
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Meglitinides
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These hypoglycemic drugs are used in type 2 DM and cause increase in glucose-dependent insulin release, decrease in glucagon release, decrease in gastric emptying and elevated satiety:
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GLP-1 analogs (Exenatide, liraglutide sc injection)
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SE of these oral hypoglycemics are nausea, vomiting, pancreatitis and modest weight loss:
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GLP-1 analogs (Exenatide, liraglutide)
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These type 2 DM hypoglycemic drugs inhibit DPP-4 enzyme that deactivates GLP-1 thereby increasing glucose-dependent insulin release, lowering glucagon release, and delaying gastric emptying increasing satiety:
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Linagliptin, saxagliptin, sitagliptin (DPP-4 inhibitors)
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These drugs delay gastric emptying and suppress glucagon, can be used in 1 or 2 DM
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Amylin analogs (pramlintide: sc injection)
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SE of these hypoglycemic drugs include mild urinary or respiratory infections, modest weight change:
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DPP-4 inhibitors (-gliptins)
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SE of these hypoglycemic drugs include hypoglycemia in setting of mistimed prandial insulin, nausea:
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Amylin analogs
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These type 2 DM hypoglycemic drugs block reabsorption of glucose in PCT
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SGLT-2 inhibitors (Canagliflozin, dapagliflozin, empagliflozin)
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SE of these hypoglycemic drugs include Glucosuria, UTI, vaginal yeast infections, hyperkalemia, dehydration, orthostatic hypotension)
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SGLT-2 inhibitors (-gliflozin)
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These type 2 DM hypoglycemic drugs inhibit intestinal brush-border alpha-glucosidases causing delayed hydrolysis and glucose absorption leading to decrease postprandial hyperglycemia
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alpha-glucosidase inhibitors (acarbose, miglitol)
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SE of these hypoglycemic drugs include GI disturbances solely:
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Alpha-glucosidase inhibitors (acabose, miglitol)
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These drugs block thyroid peroxidase, inhibiting the oxidation of iodide and the organification of iodine thereby inhibiting thyroid hormone synthesis
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Thionamides (PTU, methimazole)
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This thionamide also functions in the periphery blocking 5'-deiodinase:
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PTU
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This thionamide cay be used in hyperthyroidism in pregnancy:
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PTU
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Adverse effects of these drugs include: skin rash, rare agranulocytosis, aplastic anemia, hepatotoxicity
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Thionamide (PTU, methimazole)
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This thionamide is a possible teratogen that can cause aplasia cutis:
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Methimazole
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This is a T4 hormone replacement used in hypothyroidism, myxedema, off label weight loss, can cause tachycardia, heat intolerance, tremors, arrhythmias:
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Levothyroxine
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This is a T3 hormone replacement used in hypothyroidism, myxedema, off label weight loss, can cause tachycardia, heat intolerance, tremors, arrhythmias:
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Triiodothyronine (T3)
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These drugs can treat SIADH by blocking action of ADH at V2 receptor:
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Convaptan, tolvaptan (ADH antagonists)
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This is the DOC for central DI (not nephrogenic)
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Desmopressin acetate
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This treats GH deficiency or Turner Syndrome
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GH
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This stimulates labor, uterine contractions, milk let-down: and can control uterine hemorrhage
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Oxytocin
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This can be used for Acromegaly, carcinoid syndrome, gastrinoma, glucagonoma, esophageal varicies:
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Somatostatin (Octreotide)
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This is an ADH antagonist used in SIADH with adverse effects of Nephrogenic DI, photosensitivity, bone and teeth abnormalities:
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Demeclocycline
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These inhibit phospholipase A2, TF-kappa beta, and mediate metabolic, catabolic, antiinflammatory and immunosuppressive effects used in adrenal insufficiency, inflammation, immunosuppression, asthma:
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glucocorticoids
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What happens when you stop long term use glucocorticoids abruptly:
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Adrneal insufficiency
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This is a synthetic analog of aldosterone with little glucocorticoid effect used as a mineralocorticoid replacement in primary adrenal insufficiency:
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Fludrocortisone (SE similar to glucocorticoids, also edema, hyper pigmentation and can exacerbate HF)
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This sensitizes Ca sensing receptor (CaSR) in parathyroid gland to circulating Ca leading to lowered PTH treating primary or secondary hyperparathyroidism:
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cinacalcet (SE of hypocalcemia)