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</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</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</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</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</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</p> Signup and view all the answers

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

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

    Which of the following sulfonylureas has antiplatelet action?

    <p>Gliclazide</p> Signup and view all the answers

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

    <p>Urine</p> Signup and view all the answers

    What is the primary cause of Type 2 diabetes?

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

    What is a common adverse effect of insulin use?

    <p>Hypoglycemia</p> Signup and view all the answers

    What is the mechanism of action of Sulfonylureas?

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

    What is the extrapancreatic action of Sulfonylureas?

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

    What is a common cause of Acute Insulin Resistance?

    <p>Infection</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</p> Signup and view all the answers

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