COMPOSITION

Each tablet contains Teneligliptin Hemipentahydrobromide Hydrate equivalent to Teneligliptin: 20 mg


DESCRIPTION:

Teneligliptin is an orally-active inhibitor of the dipeptidyl peptidase-4 (DPP-4) enzyme. Its chemical name is {(2S,4S)-4-[4-(3-Methyl-1-phenyl-1H-pyrazol-5-yl) piperazin-1-yl] pyrrolidin-2-yl} (1,3-thiazolidin-3-yl) methanone hemipentahydrobromide hydrate. Its molecular formula is C22H30N6OS.2½HBr.xH2O and its molecular weight is 628.86.

MECHANISM OF ACTION:

Teneligliptin 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. Concentrations of the active intact hormones are increased by Teneligliptin, thereby increasing and prolonging the action of these 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 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, Teneligliptin increases insulin release and decreases glucagon levels in the circulation in a glucose-dependent manner.

INDICATIONS:

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

CONTRA-INDICATIONS:

Teneligliptin is contraindicated in the following:

  • Any patient with a known hypersensitivity to Teneligliptin 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 usual adult dosage is 20 mg of Teneligliptin administered orally once daily. If efficacy is insufficient, the dose may be increased up to 40 mg once daily while closely monitoring the clinical course.