Example of 1st Gen Sulfonylurea is Chlorpropamide and Tolbutamide 

General MOA 

(1) They act on the so-called ‘sulfonylurea receptors’ (SUR1) on the pancreatic β cell membrane. 

(2) This action causes depolarization by reducing the conductance of ATP-sensitive K+ channels. (Raised ATP production followed by raised Glucose also reduces the conductance of ATP sensitive K+ Channels)

(3) This process enhances Ca2+ influx (Followed by the stimulation of Voltage sensitive Ca++ Channel) and degranulation (followed by calcium dependent translocation), which increases the rate of insulin secretion.


Chlorpropamide

Structure 




Tolbutamide

Structure 


GENERAL USES OF SULFONYLUREAS 

  1. To treat high blood sugar levels caused by type 2 diabetes mellitus
  2. To prevent or delay the complications of diabetes, such as heart disease, kidney disease, nerve damage, and eye problems
  3. To test the function of the pancreas in diagnosing diabetes or other conditions

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