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Oral hypoGLYCEMICS
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Classes Sulfonylureas Biguanides Sulfonylureas+biguanide combination
Thiazolidinediones Alpha-glycosidase inhibitors Meglitinides Dipeptidyl Peptidase-4 (DPP-4) Inhibitor
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Sulfonylureas Stimulate β cells to produce more insulin by opening calcium channels
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Sulfonylureas … 1st generation 3rd generation 2nd generation
Tolbutamide (Orinase) Tolazamide (Tolinase) Chlorpropamide (Diabinese) 2nd generation Glyburide (Micronase) Glipizide (Glucotrol) 3rd generation Glimepiride (Amaryl)
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Biguanides Improves insulin sensitivity by increasing peripheral glucose uptake & utilization Metformin (Glucophage) Monotherapy, or combined with sulfonylureas e.g. Glucovance (Glyburide & Metformine) *only anti-diabetic drug that has been proven to reduce the complications of diabetes, as evidenced in a large study of overweight patients with diabetes (UKPDS 1998).
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Thiazolidinediones (Glitazones)
Make cells more sensitive to insulin (esp. fatty cells) Pioglitazone (Avandia)
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Αlpha-Glycosidase Inhibitors
Block enzymes that help digest starches hence delay absorption of complex carbohydrates in the intestine Acarbose (Precose) Miglitol (Glyset)
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Meglitinides Stimulate pancreas to secrete more insulin
Repaglinide (Prandin) Nateglinide (Starlix) [D-phenylalanine derivative]
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Dipeptidyl Peptidase-4 (DPP-4) Inhibitor
Increase and prolongs the action of incretin, a hormone that increases insulin release Vildagliptin (Galvus) Sitagliptin (Januvia)
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Summary Sulfonylureas stimulate β cells
Biguanides improves insulin’s ability to move glucose Sulfonylureas and biguanide combination drugs BOTH Thiazolidinediones cells more sensitive to insulin Alpha-glycosidase inhibitors Block enzymes that help digest starches Meglitinides stimulate β cells (dependant upon glucose conc.) Dipeptidyl Peptidase-4 (DPP-4) Inhibitor increases insulin release
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