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?
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What do insulin secretagogues require to function?
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What are the first generation of sulfonylureas?
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What are the second generation of sulfonylureas?
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What is the difference between 1st and 2nd generation of sulfonylureas?
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In which patients should sulfonylureas not be used?
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Sulfonylureas should be used in patients with liver or renal disease.
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Are sulfonylureas absorbed orally?
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What drugs displace sulfonylureas from protein binding?
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How much of sulfonylureas are bound to plasma proteins?
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What drugs can inhibit the metabolism/excretion of sulfonylureas?
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What two drugs are used if a patient has impaired renal function?
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What is the benefit of using biguanides such as metformin compared to sulfonylureas?
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What are the major adverse effects of metformin?
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What are the adverse effects of sulfonylureas?
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Who is hypoglycemia most common in as an adverse effect of sulfonylureas?
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What are the short-acting sulfonylureas?
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What category do Acetohexamide, Tolazamide, Glipizide, and Glyburide fall into?
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What are the long-acting insulin sulfonylureas?
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What drugs induce the metabolism of sulfonylureas, decreasing their action?
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What drugs oppose the action of sulfonylureas?
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Which sulfonylurea is long-acting and has more unwanted effects?
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What is the mechanism of action for meglitinide analogs and D-phenylalanine derivatives?
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Do all insulin secretagogues work via the same mechanism?
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What is the benefit of using repaglinide & nateglinide over sulfonylureas?
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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.
