Teneligliptin
Indications
Teneligliptin is used for:
Teneligliptin is indicated for the treatment of type 2 diabetes mellitus as monotherapy or in combination with other oral hypoglycemic agents
Adult Dose
Oral
Tablet
20 mg once daily. May be increased to 40 mg once daily.
Child Dose
Renal Dose
Administration
May be taken with or without food.
Contra Indications
Hypersensitivity. Severe ketosis, diabetic coma or history of diabetic coma, type 1 diabetes, severe infection or trauma, surgery.
Precautions
Heart failure NYHA classification III-IV. Pituitary or adrenal insufficiency, poor nutritional state, starvation, irregular food intake or debilitating condition, intensive exercise or excessive alcohol intake. Patients taking medication that may enhance blood glucose lowering effect of teneligliptin (β-blockers, MAOIs) or attenuate blood glucose lowering effect of teneligliptin (steroids, thyroid hormones). History of bowel obstruction or abdominal surgery.
Concomitant use w/ sulfonylureas or insulin. Patients who are prone to QT prolongation, w/ existing or w/ history of arrhythmia, bradycardia, heart failure, low serum K, Torsades de pointes, patients using antiarrhythmic drugs (Class IA & III). Severe hepatic impairment. Pregnancy & lactation.
Pregnancy-Lactation
Interactions
Adverse Effects
Side effects of Teneligliptin :
Hypoglycemia.
Mechanism of Action
Incretin hormones, including glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) are secreted from the gastrointestinal tract in response to a meal. Incretin hormones regulate plasma glucose levels by stimulating glucose-dependent insulin release from pancreatic beta cells and inhibiting glucagon secretion from pancreatic alpha cells. The enzyme Dipeptidyl Peptidase IV (DPP-4) however, rapidly degrades both GLP-1 and GIP within a few minutes. Teneligliptin exerts its hypoglycemic action by suppressing the degradation of GLP-1 via inhibition of dipeptidyl peptidase-4 (DPP-4) enzymes thereby increasing blood concentrations of active GLP-1. Teneligliptin inhibits human plasma DPP-4 activity in a concentration-dependent manner with an in vitro IC50 value (95% confidence interval) of 1.75 (1.62-1.89) nmol/L.