True statement regarding mechanism of action of sulfonylureas is: March 2008, September 2010
**Core Concept:** Sulfonylureas are a class of medications primarily used in the treatment of type 2 diabetes mellitus by stimulating insulin secretion from beta cells of the pancreas. They bind to a specific receptor (sulfonylurea receptor) found on pancreatic beta cells, leading to insulin release.
**Why the Correct Answer is Right:**
Sulfonylureas exert their effect by binding to the sulfonylurea receptor (SUR) on pancreatic beta cells, which is a member of the ATP-sensitive potassium channel (KATP) family. This binding leads to closure of KATP channels, resulting in membrane depolarization and the opening of voltage-gated calcium channels. The increased calcium influx triggers exocytosis of insulin granules, leading to increased insulin secretion.
**Why Each Wrong Option is Incorrect:**
A. False statement regarding the target receptor: This option incorrectly states that sulfonylureas bind to the glucagon receptor, which is not the primary target for sulfonylureas.
B. False statement regarding the mechanism of action: This option incorrectly suggests that sulfonylureas activate adenylate cyclase, which is not the primary mechanism of action for sulfonylureas.
C. False statement regarding the target receptor: This option incorrectly states that sulfonylureas bind to the somatostatin receptor, while the primary target is the sulfonylurea receptor.
D. False statement regarding the mechanism of action: This option incorrectly suggests that sulfonylureas inhibit glucose-induced insulin secretion, which is not the primary mechanism of action.
**Clinical Pearl:**
The sulfonylurea class of medications is a cornerstone in the management of type 2 diabetes, as they act by increasing insulin secretion and improving glucose homeostasis. However, individual sulfonylureas may have varying pharmacokinetic and pharmacodynamic properties, influencing their efficacy and side effects profile.