1. Clinical Overview
Teneligliptin is a potent, long-acting, orally active dipeptidyl peptidase-4 (DPP-4) inhibitor used in the management of type 2 diabetes mellitus. It is characterized by a unique J-shaped structure and a long plasma half-life, allowing for once-daily dosing. It works by increasing the levels of active incretin hormones (GLP-1 and GIP), which stimulate glucose-dependent insulin secretion from pancreatic beta cells and suppress glucagon secretion from alpha cells.
| Onset | Duration | Bioavailability |
|---|---|---|
| Within 1-2 hours for DPP-4 inhibition; peak plasma concentration (Tmax) is reached in approximately 1.5-2.5 hours. | Sustained DPP-4 inhibition for over 24 hours, supporting once-daily administration. | Approximately 35-40%. |
2. Mechanism of Action
Teneligliptin selectively and competitively inhibits the enzyme dipeptidyl peptidase-4 (DPP-4). DPP-4 rapidly degrades the endogenous incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). By inhibiting DPP-4, teneligliptin increases and prolongs the circulating levels of active incretins.
3. Indications & Uses
- Management of Type 2 Diabetes Mellitus in adults as an adjunct to diet and exercise.
- Monotherapy when diet and exercise alone do not provide adequate glycemic control.
- Dual combination therapy with metformin, a sulfonylurea (e.g., glimepiride), pioglitazone, or insulin when single agent therapy is insufficient.
4. Dosage & Administration
Adult Dosage: The recommended dose is 20 mg once daily, with or without food.
Administration: Tablet should be swallowed whole with a glass of water. Can be taken at any time of the day, but preferably at the same time each day to maintain consistent blood levels. Not affected by food.
5. Side Effects
Common side effects may include:
- Headache
- Upper Respiratory Tract Infection
- Constipation
- Nasopharyngitis
6. Drug Interactions
| Drug | Effect | Severity |
|---|---|---|
| Strong CYP3A4 Inducers (e.g., Rifampicin, Carbamazepine, Phenytoin) | May decrease plasma concentration of teneligliptin, reducing its efficacy. | Moderate |
| Strong CYP3A4 Inhibitors (e.g., Ketoconazole, Itraconazole, Clarithromycin) | May increase plasma concentration of teneligliptin. However, due to its wide therapeutic index, dose adjustment is not typically required. | Mild |
| Insulin or Sulfonylureas (e.g., Glimepiride, Glipizide) | Increased risk of hypoglycemia. May require dose reduction of insulin/sulfonylurea. | Moderate to High |
| Digoxin | Teneligliptin may slightly increase digoxin concentration. Monitor digoxin levels. | Mild |
7. Patient Counselling
- DO take the tablet once daily as prescribed, even if you feel well.
- DO continue your diet and exercise plan as advised by your doctor.
- DO monitor your blood glucose levels regularly.
- DO inform all your doctors and pharmacists that you are taking teneligliptin.
- DONT stop taking the medicine without consulting your doctor.
- DONT take a double dose if you miss one. Take the next dose at the usual time.
- DONT use it to treat type 1 diabetes or diabetic ketoacidosis.
8. Toxicology & Storage
Overdose: In clinical trials, doses up to 400 mg (20 times the recommended dose) were not associated with specific severe toxicity. Expected symptoms in massive overdose could include hypoglycemia (if on combination therapy), nausea, and dizziness.
Storage: Store below 30°C. Protect from light and moisture. Keep the blister strips in the outer carton. Keep out of reach of children.