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14 Cards in this Set
- Front
- Back
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What is the only Sulfonurea that is indicated for combination therapy with with insulin?
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Glimepiride.
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Describe the mechanism of action of the Sulfonylureas.
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These drugs stimulate the endogenous release of insulin. Sulfonylureas close the potassium channels in the pancreatic Beta-cell membrane, and this closure depolarizes the cell, and depolarization triggers insulin release.
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What are the second generation Sulfonylureas? They are more potent than which first generation Sulfonylureas?
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2nd generations are Glyburide, Glipizide, and Glimepiride. The 1st generations are Tolbutamide and Chlorpropamide.
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What class of drugs have the same mechanism of action as the sulfonylureas, but act more quickly? What is the prototypical drug for this class?
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Repaglitinide is the representative drug from the class, meglitinides.
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Which classes of drugs fall under the heading of insulin sensitizers? Can these be used as a monotherapy?
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Biguanides (Metformin), and Thiazolinediones (Rosiglitazone, Pioglitazone). These can be used as a monotherapy for Type II.
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PPAR-y regulates what cellular functions in adipocytes, myocytes, and hepatocytes? Which insulin sensitizing drug is a ligand of PPAR-y?
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PPAR-y regulates the expression of genes involved in lipid and glucose metabolism, insulin transduction, and adipocyte differentiation. Thiazolidinediones are ligands of PPAR-y.
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What are the two main drugs involved in Alpha-Glucosidase inhibition?
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Acarbose and Miglitol.
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Explain the mechanism of action of SItagliptin. What is DPP-4 and why is it important?
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DPP-4 is dipeptidyl peptidase 4 and it is responsible for metabolizing GLP-1 and GIP which are produced by the endocrine cells of the intestine following ingestion of food. Sitagliptin the the first DPP-4 inhibitor. Thus GLP-1 and GIP stick around longer in the blood and can stimulate the release of insulin.
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What are the diabetes medications that act like GLP-1 (GLP-1 analogs)?
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Exenatide and Liraglutide
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What are the effects that GLP-1 and GLP-1 analogs have on the body?
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Stimulate insulin secretion, suppress glucagon secretion, slow GI absorption rate, reduce appetite and reduce liver fat.
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Name the main Amylin analog and what effects it has on the body.
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The main amylin analog is Pramlintide, which promotes satiety via hypothalamic receptors (different than those from GLP-1), suppresses glucagon secretion and slows gastric emptying.
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Glucagon is used to treat what condition?
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Glucagon is a hormone that affects the liver CV system and GI tract, and it can be used to treat severe hypoglycemia in patients.
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Which GLUT transporters are upregulated in the liver in response to insulin?
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GLUT 2
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Which GLUT transporters are upregulated in muscle and adipose tissue in response to insulin?
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GLUT 4
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