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SULFONYLUREA AGENTS

Mechanism of action: bind to ATP-sensitive potassium-channel receptors on the pancreatic cell surface, thereby reducing potassium conductance and depolarizing the membrane. Depolarization stimulates calcium ion influx through voltage-sensitive calcium channels, raising intracellular concentrations of calcium ions, which induces the secretion, or exocytosis, of insulin.

Major side effects: gastrointestinal discomforts: nausea/vomiting, anorexia, flatulence, constipation, and diarrhea, but generally well tolerated.



SULFONYLUREASBrand NamesDrug InteractionContraindicationDosageCosts per Month
First Generation
Tolbutamide

tolbutamide
OrinaseSulfonyureas
Pheylbutazone
Oxyphenbutazone
MOA Inhibitors
Anabolic steroids
B-blockers
Renal glycosuria
Liver disease
1-2g qd250mg tid: $10.00 - 19.99
1g qd: $10.00 - 19.99
2g qd: $30.00 - 39.99

Chlorpropamide

chlorpropamide
DiabineseNSAIDS, Salicylates
Sulfonamides
Chloramphennicol
MOA Inhibitors
Coumadins
Hypersensitivity
ketoacidoses
250mg qd100mg qd: $5.00 - 9.99
250mg qd: $10.00 - 19.99
Second Generation
Glyburide

glyburide
DiabetaSame as Diabenese
Same as Diabenese
2.5mg qd2.5mg tid: $10.00 - 19.99

Glipizide

glipizide
GlucotrolSame as Diabenese
Same as Diabenese
5mg qd5mg qd: $5.00 - 10.99



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