Description
Glipita®
is a preparation of Sitagliptin Phosphate. Sitagliptin Phosphate is an orally-active, potent, and highly selective
inhibitor of the dipeptidyl peptidase-4 (DPP-4) enzyme for the treatment of type 2 diabetes.

Mode of Action
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 ll
diabetes and in normal subjects. Sitagliptin demonstrates high selectivity for DPP-4 and does not inhibit closely-related
enzymes DPP-8 or DPP-9 at therapeutic concentrations.

Indications
Monotherapy
Glipita®
is indicated as an adjunct to diet and exercise to improve glycemic control in patients with type ll diabetes mellitus.
Combination with Metformin
Glipita®
is indicated in patients with type 2 diabetes mellitus to improve glycemic control in combination with Metformin as
initial therapy or when the single agent alone, with diet and exercise, does not provide adequate glycemic control.
Combination with a Sulfonylurea
Glipita®
is indicated in patients with type ll diabetes mellitus to improve glycemic control in combination with a sulfonylurea
when treatment with the single agent alone, with diet and exercise, does not provide adequate glycemic control.
Combination with a Thiazolidinediones
Glipita®
is indicated in patients with type ll diabetes mellitus to improve glycemic control in combination with a thiazolidinedione
when treatment with the single agent alone, with diet and exercise, does not provide adequate glycemic control.
Combination with Metformin and a Sulfonylurea
Glipita®
is indicated in patients with type ll diabetes mellitus to improve glycemic control in combination with Metformin and
a sulfonylurea when dual therapy with these agents, with diet and exercise, does not provide adequate glycemic control.

Dosage and Administration :

The recommended dose of Sitagliptin is 100 mg once daily as monotherapy or as combination therapy with Metformin, a sulfonylurea, a thiazolidinedione, or Metformin plus a sulfonylurea. Sitagliptin can be taken with or without food. Patients with Elderly No dosage adjustment is necessary for elderly patients. Pediatric use There is no data on use of Sitagliptin in patients younger than 18 years of age and therefore not recommended. Renal Insufficiency For patients with mild renal insufficiency (creatinine clearance [CrCl] >50 mL/min, approximately corresponding to serum creatinine levels of >1.7 mg/dL in men and >1.5 mg/dL in women), no dosage adjustment for Sitagliptin is required. In moderate renal insufficiency (CrCl >30 to <50 mL/min, approximately corresponding to serum creatinine levels of >1.7 to <3.0 mg/dL in men and >1.5 to <2.5 mg/dL in women), the dose of Sitagliptin is 50 mg once daily. For patients with severe renal insufficiency (CrCl <30 mL/min, approximately corresponding to serum creatinine levels of > 3.0 mg/dL in men and > 2.5 mg/dL in women) or with end -stage renal disease (ESRD) requiring hemodialysis or peritoneal dialysis, the dose of Sitagliptin is 25 mg once daily. Sitagliptin may be administered without regard to the timing of hemodialysis. Concomitant Use with a Sulfonylurea- When Sitagliptin is used in combination with a sulfonylurea, a lower dose of sulfonylurea may be required to reduce the risk of hypoglycemia.