Oral hypoglycemic Flashcards
What are the main classifications of oral hypoglycaemics?
- Insulin secretagogues
- Biguanides
- Insulin sensitizers
- α-glucosidase inhibitors
- GLP-1 analogs
- Dipeptidyl peptidase-IV (DPP-IV) inhibitors
- Amylin antagonists
These classifications help in understanding the different mechanisms of action and therapeutic uses of oral hypoglycaemics.
What are insulin secretagogues?
They are drugs that stimulate insulin secretion from the pancreas.
Examples include sulfonylureas and meglitinides.
Name two examples of sulfonylureas.
- Tolbutamide
- Glibenclamide
Sulfonylureas are used to lower blood glucose levels in type 2 diabetes.
What is the mechanism of action (MOA) of biguanides?
They reduce hepatic glucose production and enhance tissue sensitivity to insulin.
Metformin is the only marketed biguanide.
What is the prototype structure that defines meglitinides?
Meglitinide
Meglitinides are insulin secretagogues that stimulate insulin release.
What distinguishes nateglinide from other meglitinides?
It is a phenylalanine analog of meglitinide and selectively binds to the SUR1 on β-cells.
Nateglinide is used to control blood sugar levels in diabetes.
What is the only clinically used drug in the thiazolidinedione family?
Pioglitazone
It is metabolized mainly through oxidative pathways.
Fill in the blank: Acarbose is a competitive inhibitor for ______.
sucrase
Acarbose is an α-glucosidase inhibitor derived from Actinomyces utahensis.
How do GLP-1 analogs function?
They emulate the function of GLP-1 peptide to control glucose levels by promoting insulin secretion only when glucose level is high.
This mechanism is important for preventing excessive insulin release.
What is required for the activity of DPP-IV inhibitors?
A basic amino function in the structure.
DPP-IV inhibitors are used in managing type 2 diabetes.
True or False: Amylin agonists inhibit gastric emptying and prevent postprandial rise in glucagon.
True
Amylin agonists also help with caloric intake and potential weight gain.
What is the role of a-glucosidase in the body?
It is a membrane-bound enzyme that consists of maltase, sucrase, isomaltase, and glucoamylase.
Inhibiting this enzyme can help manage carbohydrate absorption.
What is the main action of insulin sensitizers?
They enhance insulin sensitivity in tissues.
This class includes drugs like glitazones.
What type of drug is linagliptin?
A DPP-IV inhibitor and xanthine derivative used for type 2 diabetes.
It can be used alone or in combination with other medications.
Fill in the blank: The only marketed biguanide is ______.
Metformin
Metformin is widely used for managing type 2 diabetes.
What is the mechanism of action of amylin agonists?
They modulate gastric emptying, prevent postprandial rise in glucagon, and inhibit caloric intake.
They are administered via subcutaneous route.
What are the two main types of insulin secretagogues?
- Sulfonylureas
- Meglitinides
Both classes stimulate insulin release from the pancreas.
What is the main effect of α-glucosidase inhibitors?
They slow down carbohydrate absorption in the intestines.
This helps in controlling postprandial blood glucose levels.
