Metformin + Teneligliptin

Metformin, a biguanide, reduces hepatic glucose production, decreases intestinal glucose absorption, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization. Teneligliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, prolongs the action of incretin hormones (GLP-1 and GIP) by preventing their breakdown. This leads to glucose-dependent enhancement of insulin secretion from pancreatic beta cells and suppression of glucagon secretion from alpha cells, thereby reducing postprandial and fasting glucose levels. The combination provides complementary mechanisms of action to improve glycemic control. Combination rationale: This fixed-dose combination offers improved glycemic control through synergistic mechanisms, targeting different pathways involved in glucose homeostasis. It leverages metformin's ability to reduce insulin resistance and hepatic glucose production, and teneligliptin's enhancement of glucose-dependent insulin secretion. The combination provides greater efficacy than either agent alone, reduces pill burden, and potentially improves patient adherence to therapy.

Adult

Standard adult dosing involves Teneligliptin 20 mg combined with Metformin (typically 500 mg or 1000 mg extended-release, or 500 mg immediate-release). Dosing is usually once or twice daily orally, with meals, depending on the Metformin strength. Common strengths available in India include Teneligliptin 20 mg + Metformin 500 mg (ER/IR) and Teneligliptin 20 mg + Metformin 1000 mg (ER).…

Pediatric

This fixed-dose combination is not indicated for use in pediatric patients.

Renal adjustment

For Metformin: Contraindicated if eGFR <30 mL/min/1.73m2. Not recommended to initiate if eGFR 30-45 mL/min/1.73m2; if already on treatment, consider reducing dose by 50%. No adjustment for eGFR >60 mL/min/1.73m2. For Teneligliptin: No dose adjustment is required for any degree of renal impairment (mild, moderate, or severe), or in patients on hemodialysis.…

Hepatic adjustment

Metformin is contraindicated in severe hepatic impairment due to increased risk of lactic acidosis. Teneligliptin does not require dose adjustment in mild to moderate hepatic impairment, but caution is advised in severe cases. Therefore, the FDC is generally contraindicated or used with extreme caution in severe hepatic dysfunction.

Geriatric

Metformin clearance is reduced in elderly patients. Renal function should be assessed and monitored regularly in older adults. Dosage adjustments for metformin may be necessary based on eGFR. Teneligliptin generally does not require dose adjustment in the elderly based on age alone, but overall renal function dictates the metformin component.

Max dose

Maximum recommended daily dose for Metformin is 2000 mg (though some guidelines permit up to 2550 mg, FDC formulations typically cap at 2000 mg daily). Maximum recommended daily dose for Teneligliptin is 40 mg. Most FDCs contain 20 mg Teneligliptin, allowing for a maximum of 2 tablets (40 mg Teneligliptin + 2000 mg Metformin) per day, if required and tolerated.

• Severe renal impairment (eGFR <30 mL/min/1.73m2)
• Metabolic acidosis, including diabetic ketoacidosis, with or without coma
• Hypersensitivity to metformin, teneligliptin, or any component of the formulation
• Severe hepatic impairment
• Acute or chronic conditions which may cause tissue hypoxia (e.g., cardiac or respiratory failure, recent myocardial infarction, shock)
• Acute alcohol intoxication or alcoholism