Sitagliptin - DPP-4 inhibitor (Januvia®)
Glucagon-like peptide-1 (GLP-1) is an important incretin hormone in maintaining the glucose homeostatsis in the body. This hormone is secreted from the gastrointestinal tract in response to food intake and exerts it effects via:
- Increased insulin secretion from the beta cells in the pancreas when the blood glucose level is raised
- Blocking glucagon production during the period of elevated blood glucose. Glucagon is a hormone secreted from the alpha cells in the pancreas that causes the release of glucose from the liver during the fasting state.
- Triggering a feeling of satiety, therefore reduces appetite and food intake
- Inhibition of gastric emptying resulting in reducing food absorption from the small intestine.
GLP-1 has a very short half-life of less than 2 minutes. It is rapidly broken down by an enzyme called dipeptidyl peptidase (DPP)-IV. Inhibition of DPP-IV improves the glycemic control by preventing the degradation of GLP-1.
Sitagliptin phosphate tablets (Januvia®, made by Merck and Co, Inc) is the first available orally administered DPP-IV inhibitor. It has been approved by the US Food and Drug Administration (FDA) in October 2006 for use in adult patients with type 2 diabetes mellitus when diet and exercise or current anti-diabetic drugs fail to control blood glucose adequately. It is given as once daily dose, and can be used alone or as a combination with metformin or thiazolidinediones e.g. pioglitazone HCl and rosiglitazone maleate. Side effects of Sitagliptin include runny nose, sore throat, headaches and gastrointestinal effects. However it does not cause weight change or hypoglycemia. |