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22 Cards in this Set
- Front
- Back
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Sulfonylureas General
(oral hypoglycemic agents) |
Cause insulin release when glucose present BUT NOT in absence
Act by binding to specific R: coupled to inc entry of Ca2+ into B cells; enhance secretion of insulin ADR: HYPOGLYCEMIA, GI, allergic rxn, dermatologic problems, transient leucopenia, CHLOROPROPAMIDE (disulfiram type response; caused fluid retention) |
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Tolbutamide
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1st generation sulfonylurea
onset: 1-4 hours 1/2 life: 3-5 hours duration: 6-10 hours Activity of metabolites: WEAK |
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Tolazamide
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1st generation sulfonylureas
onset: 4-6 hours 1/2 life: 4-7 hours duration: 16-24 hours Activity of metabolites: MODERATE |
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Acetohexamide
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1st generation sulfonylurea
onset: 1-2 hours 1/2 life: 3-11 hours Duration: 12-18 hours Activity of metabolites: MORE ACTIVE |
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Chloropropamide
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1st generation sulfonylurea
onset: 1-3 hours 1/2 life: 24-48 hours duration: 24-72 hours Activity of metabolites: WEAK |
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1st generation sulfonylureas
(spells:TACT) |
Tolbutamide
Acetohexamide Chloropropamide Tolazamide |
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Glyburide
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2nd generation sulfonylurea
onset: 2-4 hours duration: 18-24 hours 1/2 life: 10-16 hours activity of metabolites: MODERATE |
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Glipizide
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2nd generation sulfonylurea
onset: 1-2 hours 1/2 life: 1-5 hours duration: 16-24 hours Activity of metabolites: INACTIVE |
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Metformin
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Biguanide derivatives
onset: 1-2 hours 1/2 life: 2-6 hours duration: 18-24 hours Activity of metabolites: NO METABOLITES Mechanism: does NOT affect insulin secretion, dec hepatic glucose production other mechs: direct stim of glycolysis in peripheral tissues, slowing of glucose ab from GI, inc insulin binding to insulin R important points: RARELY CAUSE HYPOGLYCEMIA, dec hyperlipidemia ADR: CI = hepatic and renal insuff; n/v, anorexia, metallic taste, abd discomfort, DIARRHEA, lactic acidosis, impair B12 absorption |
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Acarbose
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PREVENTS hydrolysis of complex carbs
does NOT stim insulin release does NOT inc insulin action in peripheral tissues does NOT cause hypoglycemia ADR: GI |
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Linogliride
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structurally related to sulfonylureas
appears to act as INSULIN SECRETAGOGUES |
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Troglitazone
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with drawn from market due to liver damage and failure
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Pioglitazone
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IMPROVES PTS ABILITY TO UTILIZE INSULIN
dec insluin resistancde in periphery and liver NOT an insulin secretagogue agonist at PPARgamma Activation of this nuclear R modulates the transcription of insulin responsive genes involved in control of glucose and lipid metabolism |
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Rosiglitazone
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IMPROVES pts ability to utilize insulin
Agonist at PPARgamma |
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Glucagon
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actions are COUTNERREGULATORY to insulin
stims: gluconeogenesis, glycogenolysis, ketogenesis Use: IV, IM, subQ raises [plasma] of glucose in 15 min Tx severe hypOglycemia emergency situations ADR: n/v |
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Bisphosphonates
Etidronate Pamidronate |
clinical utility = INHIBIT BONE RESORPTION
mech: inhibit mineralization this compound incorporated into bone matrix --> imbibed by osteoClasts during resorption --> osteoClasts are incapacitated --> resorption DECREASES |
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Etidronate
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use: paget's dz, post menopausal osteoporosis
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Pamidronate
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use: hypercalcemia for malignancy
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Alendronate
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Use: postmenopausal osteoporosis
Mech: inhibs osteoClasts mediated bone resorption via preferential localization to site of bone resorption bone turnover in postmenopausal women is equal to that in premenopausal women ADR: GI (if used correctly); bone/muscle/joint pain or cramp Metabolism: none; excreted by kidneys |
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Raloxifene (SERM)
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use: postmenopausal osteoporosis
Mech: "selective" estrogenic pathways activated/others blocked; dec bone turnover, LDL levels dec; NO change in total HDL or TG's Metabolized by liver conjugation and excreted in feces Se: flu like symptoms, hot flashes, general GI, arthralgia |
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Calcitonin
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use: metabolic bone dz for renal failure
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Dihydrotrachysterol & ergocalciferol
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Vit D replacement
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