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Drugs Used In Insulin Resistance & Diabetes
PHAR450
7
Pharmacology
Undergraduate 4
04/01/2014

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Term
Insulin
Definition
Injected hypoglycemic
Allows selected cell types to absorb/utilize glucose (liver, skeletal muscle, adipocytes)
Ultrashort-acting: un-complexed, rapidly absorbed
Crystalline zinc insulin: fast acting, short duration
Lente and ultra lente: zinc precipitates
Neutral protamine hagedorn-insulin (NPH): intermediate acting, insulin is released upon degradation of protamine
Term
Glucagon
Definition
Therapeutic use in diabetes to promote breakdown of glycogen or in severe hypoglycemia when IV glucose is not available
Term
Sulfonylureas
Definition
Oral hypoglycemic
Binds to K channel subunit thus decreasing K efflux and depolarizing the beta cell to cause insulin release
Orally bioavailable
Side-effects include hypoglycemia, GI disturbances and drug-drug interactions
Term
Metformin
Definition
Biguanides
Oral hypoglycemic
Activation of AMP-kinase promotes glucose uptake and inhibits gluconeogenesis
No direct insulin actions, low odds of hypoglycemia
Side effects include acidosis and anorexia
Term
Repaglinide
Nateglinide
Definition
Meglitinides
Oral hypoglycemic
Depolarization of beta cell causing insulin release
Short half-life, thus used to control postprandial glucose
Side effects include hypoglycemia
Term
Acarbose
Miglitol
Voglibose
Definition
alpha-Glucosidase inhibitors
Reduce digestion/absorption of complex carbohydrates
Used to control post-prandial glucose levels not controlled by diet or sulfonylureas
Side effects include GI upset and flatulence
Term
Rosiglitazone
Pioglitazone
Definition
Thiazolidinediones (TZDs, glitazones)
Bind a transcription factor (PPAR) and induce selective gene expression
Decrease insulin resistance by increasing glucose uptake and metabolism in muscle/fat
Reduces plasma glucose, lipid and insulin
Chronic therapy leads to reduction in triglyceride and increases HDL:LDL
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