Linagliptin is a potent, selective, competitive dipeptidyl peptidase-4 (DPP-4) inhibitor used for the treatment of type 2 diabetes mellitus. It is a xanthine-based oral anti-diabetic agent that increases the concentration of active incretin hormones (GLP-1 and GIP), thereby increasing insulin secretion and decreasing glucagon secretion in a glucose-dependent manner. Its unique pharmacokinetic profile allows for a once-daily, 5mg dose without adjustment for renal or hepatic impairment.
Adult: 5 mg once daily, with or without food.
Note: Tablet to 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 routine.
Linagliptin selectively and competitively inhibits the enzyme dipeptidyl peptidase-4 (DPP-4). DPP-4 rapidly degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). By inhibiting DPP-4, linagliptin increases and prolongs the activity of these endogenous incretins.
Pregnancy: Category B. Animal studies show no risk, but adequate human studies are lacking. Use only if potential benefit justifies potential risk to fetus. Insulin is preferred for glycemic control in pregnant women.
Driving: Unlikely to affect ability to drive or use machines. However, patients should be alerted to the symptoms of hypoglycemia, especially when used in combination.
| Strong CYP3A4 or P-gp Inducers (e.g., Rifampicin, Carbamazepine, Phenytoin) | May decrease linagliptin plasma concentrations. Monitor glycemic control. | Moderate |
| Sulfonylureas (e.g., Glimepiride, Glipizide) or Insulin | Increased risk of hypoglycemia. May require dose reduction of sulfonylurea/insulin. | Moderate |
| Loop Diuretics (e.g., Furosemide) | Potential pharmacodynamic interaction increasing blood glucose. Monitor. | Minor |
Same composition (Linagliptin (5mg)), different brands: