COMPOSITION:

Each film-coated tablet contains

  •  Teneligliptin Hemipentahydrobromide Hydrate equivalent to Teneligliptin: 20 mg
  •  Metformin SR: 500 mg

SUMMARY:
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.

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:
Teneligliptin works to competitively inhibit the enzyme dipeptidyl peptidase 4 (DPP-4). This enzyme breaks down the incretins GLP-1 and GIP, gastrointestinal hormones released in response to a meal.[12] By preventing GLP-1 and GIP inactivation, they are able to increase the secretion of insulin and suppress the release of glucagon by the alpha cells of the pancreas. This drives blood glucose levels towards normal. As the blood glucose level approaches normal, the amounts of insulin released and glucagon suppressed diminishes, thus tending to prevent an “overshoot” and subsequent low blood sugar (hypoglycemia) which is seen with some other oral hypoglycemic agents.

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:
Actiglipt 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 Actiglipt 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 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).

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.