COMPOSITION:

SItapaz D 50/5

Each film-coated tablet contains
Sitagliptin 50 mg + Dapagliflozin 5 mg

SItapaz M 100/10

Each film-coated tablet contains
Sitagliptin 100 mg + Dapagliflozin 10 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

Dapagliflozin is an inhibitor of SGLT2. By inhibiting SGLT2, dapagliflozin reduces the reabsorption of filtered glucose and lowers the renal threshold for glucose, and thereby increasing urinary glucose excretion.

Category: SGLT2 Inhibitors

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.

Sodium-glucose cotransporter 2 (SGLT2), expressed in the proximal renal tubules, is responsible for the majority of the reabsorption of filtered glucose from the tubular lumen. Dapagliflozin is an inhibitor of SGLT2. By inhibiting SGLT2, dapagliflozin reduces the reabsorption of filtered glucose and lowers the renal threshold for glucose, and thereby increasing urinary glucose excretion.

Indications:
Sitapaz D is a dipeptidyl peptidase-4 (DPP-4) inhibitor and SGLT-2 inhibitor 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 Sitagliptin and Dapagliflozin is appropriate

Side Effects:
Patients undergoing treatment with Sitapaz D 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).

Patients with a history of serious hypersensitivity reaction to Dapagliflozin. Severe renal impairment, end-stage renal disease, or dialysis.

 

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