SITASUG-M

Sitagliptin phosphate, an orally-active inhibitor of the dipeptidyl peptidase-4 (DPP-4) enzyme.

Sitagliptin phosphate monohydrate is a white to off-white, crystalline, non-hygroscopic powder. It is soluble in water and N,N-dimethyl formamide; slightly soluble in methanol; very slightly soluble in ethanol, acetone, and acetonitrile; and insoluble in isopropanol and isopropyl acetate.

MEFOMIN SR 500MG TABLET contains Metformin which belongs to the group

of medicines called Anti-diabetic agents. It is used to treat Type II diabetes mellitus when diet and exercise alone does not result in adequate blood sugar control.

Type II diabetes mellitus is a chronic disease characterized by abnormally high levels of glucose in the blood. It is caused due to inadequate production of a hormone called insulin (produced by pancreas to metabolize glucose) in the body or due to inadequate sensitivity of body cells to the actions of insulin

Description

Composition:

Each film coated tablet contains:

Sitagliptin Phosphate Monohydrate IP

Eq. to Sitagliptin 50 mg

Metformin hydrochloride 500 mg

Mechanism:

Sitagliptin is a DPP-4 inhibitor, which is believed to exert its actions in patients with type 2 diabetes by slowing the inactivation of incretin hormones. Incretin hormones, including glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), are released by the intestine throughout the day, and levels are increased in response to a meal. These hormones are rapidly inactivated by the enzyme, DPP-4. The incretins are part of an endogenous system involved in the physiologic regulation of glucose homeostasis. When blood glucose concentrations are normal or elevated, GLP-1 and GIP increase insulin synthesis and release from pancreatic beta cells by intracellular signaling pathways involving cyclic AMP. GLP-1 also lowers glucagon secretion from pancreatic alpha cells, leading to reduced hepatic glucose production. By increasing and prolonging active incretin levels, Sitagliptin increases insulin release and decreases glucagon levels in the circulation in a glucose-dependent manner. Sitagliptin demonstrates selectivity for DPP-4 and does not inhibit DPP-8 or DPP-9 activity in vitro at concentrations approximating those from therapeutic doses.