Sitagliptin

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What is Sitagliptin?

Sitagliptin is a DPP-4 inhibitor used to improve blood sugar control in adults with Type 2 diabetes. It works by blocking the enzyme that breaks down incretin hormones—GLP-1 and GIP—allowing these natural hormones to remain active longer and stimulate insulin release in a glucose-dependent manner. This means Sitagliptin only promotes insulin secretion when blood sugar is elevated, significantly reducing the risk of hypoglycemia compared to older diabetes medications. It's taken once daily as a tablet and is weight-neutral, making it a well-tolerated addition to existing diabetes regimens.

DPP-4 enzyme inhibition

Blocks dipeptidyl peptidase-4, the enzyme that rapidly degrades GLP-1 and GIP incretin hormones, extending their activity and allowing them to stimulate more insulin release and suppress glucagon in a glucose-dependent manner.

Glucose-dependent insulin stimulation

Because it works through incretin hormones that only activate insulin release when blood sugar is elevated, Sitagliptin carries a low risk of hypoglycemia—unlike sulfonylureas that stimulate insulin regardless of current glucose levels.

Weight-neutral profile

Unlike some diabetes medications that cause weight gain, Sitagliptin has a neutral effect on body weight—an important consideration for Type 2 diabetes management where excess weight is often a contributing factor.

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