Oral-Hypoglycemic Agents Flashcards
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Questions and Answers

In what type of patients are oral hypoglycemic agents used?

Type II Diabetics

What are the classes of oral hypoglycemic agents?

Insulin secretagogues, Insulin sensitizers, α glucosidase inhibitors, Incretin-based agents, SGLT-2 Inhibitors

What are the insulin secretagogues?

Sulfonylureas, Meglitinide Analogs, D-Phenylalanine derivative

What is the mechanism of action of sulfonylureas?

<p>Close K+ channel in β cell leading to depolarization --&gt; ⬆︎ in calcium (influx) --&gt; triggers insulin release; ⬇︎ serum glucagon levels</p> Signup and view all the answers

What do insulin secretagogues require to function?

<p>β cells to be intact and functioning</p> Signup and view all the answers

What are the first generation of sulfonylureas?

<p>Tolbutamide, Acetohexamide, Chlorpropamide, Tolazamide</p> Signup and view all the answers

What are the second generation of sulfonylureas?

<p>Glipizide, Glyburide, Glimepiride</p> Signup and view all the answers

What is the difference between 1st and 2nd generation of sulfonylureas?

<p>2nd generation are more potent, more efficacious with fewer adverse effects and less interactions</p> Signup and view all the answers

In which patients should sulfonylureas not be used?

<p>Patients with liver or renal disease</p> Signup and view all the answers

Sulfonylureas should be used in patients with liver or renal disease.

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

Are sulfonylureas absorbed orally?

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

What drugs displace sulfonylureas from protein binding?

<p>Phenylbutazone, Salicylates, Sulfonamides</p> Signup and view all the answers

How much of sulfonylureas are bound to plasma proteins?

<p>99%</p> Signup and view all the answers

What drugs can inhibit the metabolism/excretion of sulfonylureas?

<p>Phenylbutazone, Salicylates, Sulfonamides, Warfarin</p> Signup and view all the answers

What two drugs are used if a patient has impaired renal function?

<p>Glipizide or Tolbutamide</p> Signup and view all the answers

What is the benefit of using biguanides such as metformin compared to sulfonylureas?

<p>Causes modest weight loss, does not cause hypoglycemia, prominent lipid-lowering activity</p> Signup and view all the answers

What are the major adverse effects of metformin?

<p>GI disturbances: metallic taste, diarrhea, Lactic acidosis, Vitamin B12 deficiency</p> Signup and view all the answers

What are the adverse effects of sulfonylureas?

<p>Hypoglycemia, Nausea, Vomiting, Weight Gain, Intolerance to alcohol &amp; disulfiram-like reaction, Can cross the placenta causing fetal hypoglycemia</p> Signup and view all the answers

Who is hypoglycemia most common in as an adverse effect of sulfonylureas?

<p>Elderly patients with impaired hepatic or renal function</p> Signup and view all the answers

What are the short-acting sulfonylureas?

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

What category do Acetohexamide, Tolazamide, Glipizide, and Glyburide fall into?

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

What are the long-acting insulin sulfonylureas?

<p>Chlorpropamide, Glimepiride</p> Signup and view all the answers

What drugs induce the metabolism of sulfonylureas, decreasing their action?

<p>Phenobarbital, Phenytoin, Rifampin, Chronic Alcoholism</p> Signup and view all the answers

What drugs oppose the action of sulfonylureas?

<p>Corticosteroids, Diazoxide, Thiazide, Oral Contraceptives</p> Signup and view all the answers

Which sulfonylurea is long-acting and has more unwanted effects?

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

What is the mechanism of action for meglitinide analogs and D-phenylalanine derivatives?

<p>Close K+ channel in β cell leading to depolarization --&gt; ⬆︎ in calcium (influx) --&gt; triggers insulin release</p> Signup and view all the answers

Do all insulin secretagogues work via the same mechanism?

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

What is the benefit of using repaglinide & nateglinide over sulfonylureas?

<p>Rapid Onset &amp; Short Duration</p> Signup and view all the answers

Flashcards

Oral Hypoglycemic Agents

Oral medications used primarily for Type II Diabetes to help manage blood glucose levels.

Insulin Secretagogue

A medication that stimulates insulin release from the pancreas.

Sulfonylureas

A class of insulin secretagogues that close potassium channels in beta cells, leading to increased insulin release.

First Generation Sulfonylureas

First generation sulfonylureas, less potent with more side effects.

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Second Generation Sulfonylureas

Second generation sulfonylureas, more potent with fewer side effects.

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Sulfonylurea Requirement

Sulfonylureas require functioning beta cells in the pancreas to work effectively.

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Sulfonylurea Metabolism

Sulfonylureas are primarily metabolized by the liver, making them safer for patients with kidney problems.

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Sulfonylurea Displacement

Sulfonylureas can be displaced from their binding sites by other drugs, potentially increasing insulin levels.

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Sulfonylurea Inhibition

Certain medications can inhibit the metabolism of sulfonylureas, increasing their effects and potentially leading to hypoglycemia.

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Sulfonylureas for Impaired Renal Function

Glipizide and tolbutamide are preferred sulfonylureas for patients with impaired renal function.

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Metformin

Metformin is a biguanide, a different class of oral hypoglycemic agent.

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Metformin Mechanism

Metformin can reduce blood sugar without increasing insulin production.

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Metformin Benefits

Metformin may cause weight loss and has lipid-lowering effects.

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Metformin Side Effects

Metformin can cause gastrointestinal disturbances, lactic acidosis, and vitamin B12 deficiency.

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Sulfonylurea Hypoglycemia Risk

Sulfonylureas are associated with a significant risk of hypoglycemia.

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Sulfonylurea Side Effects

Other potential adverse effects of sulfonylureas include nausea, vomiting, weight gain, intolerance to alcohol, and fetal hypoglycemia.

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Sulfonylurea Hypoglycemia in Elderly

Elderly patients have a higher incidence of hypoglycemia due to sulfonylurea use.

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Sulfonylurea Action Duration

The duration of action of sulfonylureas varies.

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Tolbutamide Duration

Tolbutamide is a short-acting sulfonylurea considered safest for elderly.

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Intermediate-Acting Sulfonylureas

Acetohexamide, Tolazamide, Glipizide, and Glyburide are intermediate-acting sulfonylureas.

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Long-Acting Sulfonylureas

Chlorpropamide and Glimepiride are long-acting sulfonylureas, associated with more adverse effects.

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Sulfonylurea Metabolism Induction

Certain medications can induce sulfonylurea metabolism, reducing their effectiveness.

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Sulfonylurea Opposing Agents

Medications counteracting the effects of sulfonylureas include corticosteroids, diazoxide, thiazides, and oral contraceptives.

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Meglitinide Analogs and D-Phenylalanine Derivatives

Meglitinide analogs and D-Phenylalanine derivatives are insulin secretagogues with a similar mechanism to sulfonylureas.

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Meglitinide Examples

Repaglinide and nateglinide are examples of meglitinide analogs.

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Meglitinide Metabolism

Meglitinide analogs and D-Phenylalanine derivatives are metabolized by the liver.

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Study Notes

Oral Hypoglycemic Agents Overview

  • Oral hypoglycemic agents are primarily used in Type II Diabetics to help manage blood glucose levels.

Classes of Oral Hypoglycemic Agents

  • Five main classes:
    • Insulin secretagogues
    • Insulin sensitizers
    • α glucosidase inhibitors
    • Incretin-based agents
    • SGLT-2 inhibitors

Insulin Secretagogues

  • Include:
    • Sulfonylureas
    • Meglitinide analogs
    • D-Phenylalanine derivatives
  • Mechanism: Close K+ channels in β cells, leading to depolarization, increased calcium influx, and insulin release, while reducing serum glucagon levels.

Sulfonylureas

  • Require intact and functioning β cells to promote insulin release.
  • First generation includes:
    • Tolbutamide
    • Acetohexamide
    • Chlorpropamide
    • Tolazamide
  • Second generation includes:
    • Glipizide
    • Glyburide
    • Glimepiride
  • Second generation are more potent and effective, with fewer adverse effects.

Safety and Pharmacokinetics

  • Not advised for patients with liver or renal disease due to the risk of hypoglycemia.
  • Sulfonylureas are orally absorbed and 99% bound to plasma proteins, making displacement from binding sites a concern.
  • Drugs that can displace sulfonylureas include phenylbutazone, salicylates, and sulfonamides, potentially increasing insulin levels.
  • Phenylbutazone, salicylates, sulfonamides, and warfarin can inhibit sulfonylurea metabolism, risking hypoglycemia.

Alternatives for Impaired Renal Function

  • Glipizide and Tolbutamide are preferred due to their excretion via the liver rather than the kidneys.

Biguanides vs. Sulfonylureas

  • Metformin benefits:
    • Modest weight loss
    • Does not cause hypoglycemia
    • Significant lipid-lowering effects
  • Major adverse effects of metformin:
    • Gastrointestinal disturbances (metallic taste, diarrhea)
    • Lactic acidosis
    • Vitamin B12 deficiency.

Adverse Effects of Sulfonylureas

  • Significant risk of hypoglycemia.
  • Other effects: nausea, vomiting, weight gain, intolerance to alcohol, and potential fetal hypoglycemia when crossing the placenta.
  • Higher incidence of hypoglycemia in elderly patients, especially with longer-acting sulfonylureas.

Sulfonylurea Action Duration

  • Short-acting sulfonylureas: Tolbutamide (safest for elderly).
  • Intermediate-acting: Acetohexamide, Tolazamide, Glipizide, Glyburide.
  • Long-acting: Chlorpropamide, Glimepiride (more adverse effects, not often recommended).

Interactions and Opposing Agents

  • Medications inducing sulfonylurea metabolism (reducing their effectiveness):
    • Phenobarbital, phenytoin, rifampin, chronic alcoholism.
  • Agents opposing sulfonylurea action:
    • Corticosteroids, diazoxide, thiazides, oral contraceptives.

Meglitinide Analogs and D-Phenylalanine Derivatives

  • Similar mechanism of action to sulfonylureas, involving K+ channel closure and increased calcium inflow.
  • Benefits of repaglinide and nateglinide:
    • Rapid onset and short duration.
    • Metabolized by the liver.

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Description

Test your knowledge on oral hypoglycemic agents, their classes, and their uses in patients, specifically for Type II Diabetes. This quiz encompasses various drug classifications and their roles in managing blood sugar levels. Ideal for healthcare professionals and students in medical fields.

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