COMPOSITION:

SITAPAZ 50:
Sitagliptin ……. 50 mg

SITAPAZ 100:
Sitagliptin ……. 100 mg

DESCRIPTION:
tablets contain sitagliptin phosphate, 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.

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. This mechanism is unlike the mechanism seen with sulfonylureas; sulfonylureas cause insulin release even when glucose levels are low, which can lead to sulfonylurea-induced hypoglycemia in patients with type 2 diabetes and in normal subjects. Sitagliptin is a potent and highly selective inhibitor of the enzyme DPP-4 and does not inhibit the closely-related enzymes DPP-8 or DPP-9 at therapeutic concentrations. Sitagliptin differs in chemical structure and pharmacological action from GLP-1 analogues, insulin, sulfonylureas or meglitinides, biguanides, peroxisome proliferator-activated receptor gamma (PPARγ) agonists, alpha-glucosidase inhibitors, and amylin analogues.

INDICATIONS:
Sitagliptin is indicated for the treatment of Type 2 Diabetes Mellitus as a monotherapy, adjunct to diet and exercise.

CONTRA-INDICATIONS:
Sitagliptin is contraindicated in the following:

  • 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).

DOSAGE & ADMINISTRATION:
The recommended dose of Sitagliptin is 100 mg once daily as monotherapy or as combination therapy with metformin, a sulfonylurea, insulin (with or without metformin), a PPARγ agonist (e.g., thiazolidinediones), metformin plus a sulfonylurea, or metformin plus a PPARγ agonist.

For patients with moderate renal impairment (eGFR ≥30 mL/min/1.73 m2 to <45 mL/min/1.73 m2), the dose of Sitagliptin 50 mg once daily is recommended.