Adult: As monotherapy or in combination with other hypoglycaemic agents: 20 mg once daily; may increase to 40 mg once daily if effect is inadequate.
Administration
tab: May be taken with or without food. Preferably taken before meals.
Contraindications
Severe ketosis, diabetic coma or precoma, type 1 diabetes mellitus, severe infections, surgery, severe trauma.
Special Precautions
Patient with pituitary or adrenal insufficiency, poor nutritional state, starvation, irregular food intake, history of bowel obstruction or abdominal surgery, heart failure NYHA functional class III-IV, active or history of arrhythmia, bradycardia, low K levels, Torsades de pointes, QT prolongation. Intensive exercise or excessive alcohol intake. Debilitated patients. Severe hepatic impairment. Pregnancy and lactation.
Adverse Reactions
Significant: Hypoglycaemia, hepatic impairment (accompanied by increased AST/ALT), intestinal obstruction, bullous pemphigoid, interstitial pneumonia, prolonged QT interval. Rarely, acute pancreatitis. Gastrointestinal disorders: Abdominal distension, discomfort or pain; constipation, flatulence, nausea, stomatitis, gastric or colonic polyps, duodenal ulcer, reflux oesophagitis, diarrhoea. General disorders and administration site conditions: Malaise. Investigations: Elevated amylase, lipase, γ-GTP, creatine phosphokinase, serum K and uric acid. Metabolism and nutrition disorders: Decreased appetite. Renal and urinary disorders: Proteinuria, presence of ketones in urine, haematuria. Respiratory, thoracic and mediastinal disorders: Allergic rhinitis. Skin and subcutaneous tissue disorders: Eczema, rash, itching, allergic dermatitis.
Patient Counseling Information
This drug may cause dizziness or weakness due to lowering of blood sugar, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor plasma glucose, HbA1c (at least twice yearly in patients who have stable glycaemic control and are meeting treatment goals; quarterly in patients not meeting treatment goals or with therapy change), liver function. Monitor for signs/symptoms of pancreatitis (e.g. severe abdominal pain, anorexia, nausea, vomiting).
Drug Interactions
Increased hypoglycaemic effects with other antidiabetics (e.g. sulfonylureas, insulins, biguanides), β-blockers, MAOIs, salicylic acid. Reduced hypoglycaemic effect with epinephrine, adrenocortical and thyroid hormones. Increased risk of QT prolongation with Class 1A (e.g. procainamide, quinidine) and Class III antiarrhythmics (e.g. amiodarone, sotalol).
Action
Description: Teneligliptin inhibits dipeptidyl peptidase-4 (DPP-4), an enzyme involved in the degradation of the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) leading to increased and prolonged active incretin levels. These incretin hormones enhance insulin release and inhibit glucagon secretion resulting in reduced blood glucose level. Pharmacokinetics: Absorption: Rapidly absorbed. Time to peak plasma concentration: 1-1.3 hours. Distribution: Plasma protein binding: 77.6-82.2%. Metabolism: Metabolised in the liver by CYP3A4 and flavin monooxygenases (FMO) 1 and 3 to several metabolites. Excretion: Via urine (21-34%, as unchanged drug). Elimination half-life: 18.9-26.9 hours.
Chemical Structure
Teneligliptin Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 11949652, Teneligliptin. https://pubchem.ncbi.nlm.nih.gov/compound/Teneligliptin. Accessed Feb. 22, 2022.
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