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?

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

What do insulin secretagogues require to function?

β cells to be intact and functioning Signup and view all the answers

What are the first generation of sulfonylureas?

Tolbutamide, Acetohexamide, Chlorpropamide, Tolazamide Signup and view all the answers

What are the second generation of sulfonylureas?

Glipizide, Glyburide, Glimepiride Signup and view all the answers

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

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

In which patients should sulfonylureas not be used?

Patients with liver or renal disease Signup and view all the answers

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

False Signup and view all the answers

Are sulfonylureas absorbed orally?

True Signup and view all the answers

What drugs displace sulfonylureas from protein binding?

Phenylbutazone, Salicylates, Sulfonamides Signup and view all the answers

How much of sulfonylureas are bound to plasma proteins?

99% Signup and view all the answers

What drugs can inhibit the metabolism/excretion of sulfonylureas?

Phenylbutazone, Salicylates, Sulfonamides, Warfarin Signup and view all the answers

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

Glipizide or Tolbutamide Signup and view all the answers

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

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

What are the major adverse effects of metformin?

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

What are the adverse effects of sulfonylureas?

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

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

Elderly patients with impaired hepatic or renal function Signup and view all the answers

What are the short-acting sulfonylureas?

Tolbutamide Signup and view all the answers

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

Intermediate acting Signup and view all the answers

What are the long-acting insulin sulfonylureas?

Chlorpropamide, Glimepiride Signup and view all the answers

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

Phenobarbital, Phenytoin, Rifampin, Chronic Alcoholism Signup and view all the answers

What drugs oppose the action of sulfonylureas?

Corticosteroids, Diazoxide, Thiazide, Oral Contraceptives Signup and view all the answers

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

Chlorpropamide Signup and view all the answers

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

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

Do all insulin secretagogues work via the same mechanism?

True Signup and view all the answers

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

Rapid Onset & Short Duration Signup and view all the answers

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.