Sulfonylureas: First Generation Hypoglycemic Agents
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Questions and Answers

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

  • Hypoglycemic effects (correct)
  • Increased insulin sensitivity
  • Enhanced insulin secretion
  • Improved glucose tolerance

What is the characteristic of the sulfonyl group in sulfonylureas?

  • Presence of a phosphate group and oxygen atoms for hydrogen bonding
  • Presence of an acidic amine and oxygen atoms for hydrogen bonding (correct)
  • Presence of a hydrophobic group
  • Presence of a basic amine and nitrogen atoms for hydrogen bonding

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

  • It influences the lipophilicity of the drug
  • It has a small lipophilic substituent that enhances activity (correct)
  • It affects the binding to the ATP-sensitive K+ channel
  • It determines the potency of the drug

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

<p>It has little effect on binding to the ATP-sensitive K+ channel (D)</p> Signup and view all the answers

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

<p>Increased risk of adverse effects (B)</p> Signup and view all the answers

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

<p>They stimulate insulin secretion (B)</p> Signup and view all the answers

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

<p>Inhibition of ATP-sensitive K+ channels (C)</p> Signup and view all the answers

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

<p>Glipizide (D)</p> Signup and view all the answers

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

<p>Hypoglycemic reactions (A)</p> Signup and view all the answers

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

<p>Increased potency (C)</p> Signup and view all the answers

Which of the following sulfonylureas has antiplatelet action?

<p>Gliclazide (B)</p> Signup and view all the answers

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

<p>Urine (D)</p> Signup and view all the answers

What is the primary cause of Type 2 diabetes?

<p>Insulin resistance of peripheral tissues (A)</p> Signup and view all the answers

What is a common adverse effect of insulin use?

<p>Hypoglycemia (A)</p> Signup and view all the answers

What is the mechanism of action of Sulfonylureas?

<p>Blocking the action of ATP-sensitive K+ channels (B)</p> Signup and view all the answers

What is the extrapancreatic action of Sulfonylureas?

<p>Sensitizing target tissues to insulin (C)</p> Signup and view all the answers

What is a common cause of Acute Insulin Resistance?

<p>Infection (C)</p> Signup and view all the answers

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

<p>Sulfonylurea receptor (SUR) of the ATP-sensitive K+ channel (A)</p> Signup and view all the answers

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