COMPOSITION:
SItapaz M 50/500
Each film-coated tablet contains
Sitagliptin 50 mg + Metformin SR 500 mg
SItapaz M 100/500
Each film-coated tablet contains
Sitagliptin 100 mg + Metformin SR 500 mg
SUMMARY:
Sitagliptin phosphate, is an orally-active, potent, and selective inhibitor of dipeptidyl peptidase 4 (DPP-4), which is described chemically as: 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazine phosphate (1:1) monohydrate.
Category: DPP4 Inhibitors
Metformin Hydrochloride (N, Ndimethylimidodicarbonimidic diamide hydrochloride) is an oral antihyperglycemic drug used in the management of type 2 diabetes. It is a white to off-white crystalline compound with a molecular formula of C4H11N5-HCL and a molecular weight of 165.63 g/mol.
Category: Biguanides
Mechanism of Action:
Sitagliptin is an orally-active, potent, and highly selective inhibitor of the dipeptidyl peptidase 4 (DPP-4) enzyme for the treatment of type 2 diabetes. The DPP-4 inhibitors are a class of agents that act as incretin enhancers. By inhibiting the DPP-4 enzyme, sitagliptin increases the levels of two known active incretin hormones, glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). 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. GLP-1 also lowers glucagon secretion from pancreatic alpha cells, leading to reduced hepatic glucose production.
Metformin is an antihyperglycemic agent that improves glucose tolerance in patients with type 2 diabetes, lowering both basal and postprandial plasma glucose. Metformin decreases hepatic glucose production, decreases intestinal absorption of glucose, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization. Unlike sulfonylureas, metformin does not produce hypoglycemia in either patient with type 2 diabetes or normal subjects and does not cause hyperinsulinemia. With metformin therapy, insulin secretion remains unchanged while fasting insulin levels and day-long plasma insulin response may actually decrease
Indications:
Sitapaz M is a dipeptidyl peptidase-4 (DPP-4) inhibitor and biguanide combination product indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus when treatment with both teneligliptin and metformin is appropriate
Side Effects:
Patients undergoing treatment with Sitapaz M may experience side effects, such as: Nausea, Eczema, Constipation, Pain in the abdomen & accumulation of gas in the gastrointestinal tract, diarrhea, cough or hoarseness, breathing problems, coma, and confusion.
Contraindications:
Any patient with a known hypersensitivity to Sitagliptin or any of the components in the formulation, Severe ketosis, diabetic coma or history of diabetic coma, type 1 diabetic patients, Patients with severe infection, surgery, severe trauma (blood sugar control should preferably be done by insulin).
Severe renal impairment (eGFR below 30 mL/min/1.73 m2), Known hypersensitivity to metformin hydrochloride, Acute or chronic metabolic acidosis, including diabetic ketoacidosis, with or without coma. Diabetic ketoacidosis should be treated with insulin.