Sulfonylureas: First Generation Hypoglycemic Agents

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18 Questions

What is the result of modifying the sulfonamide antibacterial with a urea moiety in sulfonylureas?

Hypoglycemic effects

What is the characteristic of the sulfonyl group in sulfonylureas?

Presence of an acidic amine and oxygen atoms for hydrogen bonding

What is the significance of the para position of the phenyl ring in first-generation sulfonylureas?

It has a small lipophilic substituent that enhances activity

What is the effect of having an alkyl or cyclic lipophilic substituent on the non-sulfonyl-attached urea nitrogen in first-generation sulfonylureas?

It has little effect on binding to the ATP-sensitive K+ channel

What is the consequence of requiring high doses of first-generation sulfonylureas for effectiveness?

Increased risk of adverse effects

What is the mechanism of action of sulfonylureas in terms of insulin secretion?

They stimulate insulin secretion

What is the primary mechanism by which second-generation sulfonylureas achieve their therapeutic effect?

Inhibition of ATP-sensitive K+ channels

Which of the following sulfonylureas is preferred in elderly patients due to its faster onset and shorter duration of action?

Glipizide

What is a common adverse effect of sulfonylureas, particularly in elderly patients, liver disease, and renal disease?

Hypoglycemic reactions

What is a characteristic of second-generation sulfonylureas compared to first-generation sulfonylureas?

Increased potency

Which of the following sulfonylureas has antiplatelet action?

Gliclazide

What is the primary route of excretion for sulfonylureas and their metabolites?

Urine

What is the primary cause of Type 2 diabetes?

Insulin resistance of peripheral tissues

What is a common adverse effect of insulin use?

Hypoglycemia

What is the mechanism of action of Sulfonylureas?

Blocking the action of ATP-sensitive K+ channels

What is the extrapancreatic action of Sulfonylureas?

Sensitizing target tissues to insulin

What is a common cause of Acute Insulin Resistance?

Infection

What is the binding site of Sulfonylureas on pancreatic b-cells?

Sulfonylurea receptor (SUR) of the ATP-sensitive K+ channel

This quiz covers the properties and characteristics of sulfonylureas, a class of hypoglycemic agents used to treat diabetes. It includes their structural features, differences between generations, and specific examples like Chlorpropamide and Tolbutamide.

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