| Recommended Dose and Dosage Regimen | The recommended dose of linagliptin for adults with type 2 diabetes mellitus is 5 mg orally once daily, with or without food. No dose adjustment is required based on age, gender, race, or renal impairment, including patients with mild to severe renal impairment or end-stage renal disease requiring hemodialysis. Linagliptin can be used alone or in combination with other antidiabetic medications, such as metformin, sulfonylureas, or insulin. Follow your healthcare provider’s instructions regarding dosing and administration. |
| Frequency of Administration | Linagliptin is administered orally once daily. |
| Route of Administration | Linagliptin is available as oral tablets for ingestion. |
| Mechanism of Action (MOA) | Linagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor that enhances glycemic control in patients with type 2 diabetes mellitus. It selectively inhibits the enzymatic activity of DPP-4, an enzyme responsible for degrading incretin hormones such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). By inhibiting DPP-4, linagliptin prolongs the action of endogenous GLP-1 and GIP, leading to increased insulin secretion and decreased glucagon secretion in a glucose-dependent manner. This results in improved glucose homeostasis, reduced fasting and postprandial blood glucose levels, and enhanced glycemic control without causing hypoglycemia when used as monotherapy or in combination with other antidiabetic agents. |
| Pharmacokinetics (PK) | Linagliptin is rapidly absorbed after oral administration, with peak plasma concentrations reached within 1-3 hours. It is primarily eliminated via the enterohepatic route and undergoes minimal renal excretion. The elimination half-life of linagliptin is approximately 12 hours, allowing for once-daily dosing. Linagliptin is highly protein-bound (>99%) and extensively metabolized in the liver via cytochrome P450 (CYP) 3A4-mediated pathways, with metabolites excreted predominantly in the feces. No dosage adjustment is required based on hepatic or renal impairment. |
| Pharmacodynamics (PD) | Linagliptin exerts its pharmacodynamic effects by selectively inhibiting DPP-4 activity, thereby increasing the concentrations of endogenous incretin hormones such as GLP-1 and GIP. Elevated levels of GLP-1 and GIP stimulate glucose-dependent insulin secretion by pancreatic beta cells and inhibit glucagon secretion by pancreatic alpha cells, resulting in enhanced glucose-dependent insulin secretion and suppression of glucagon release. This leads to improved glucose homeostasis, reduced fasting and postprandial blood glucose levels, and enhanced glycemic control in patients with type 2 diabetes mellitus. |
| Pathophysiology | Linagliptin is indicated for the management of type 2 diabetes mellitus as an adjunct to diet and exercise to improve glycemic control in adults. Type 2 diabetes mellitus is characterized by insulin resistance and relative insulin deficiency, leading to hyperglycemia and associated complications such as cardiovascular disease, neuropathy, nephropathy, and retinopathy. Linagliptin helps regulate blood glucose levels by enhancing insulin secretion and suppressing glucagon release in a glucose-dependent manner, thereby improving glycemic control without causing hypoglycemia when used alone or in combination with other antidiabetic medications. |
| Primary Indications | Type 2 diabetes mellitus. |
| Contraindications | Contraindications to linagliptin use include hypersensitivity to linagliptin or any component of the formulation. Linagliptin should not be used in patients with type 1 diabetes mellitus or diabetic ketoacidosis. Use caution in patients with a history of pancreatitis or with severe renal impairment. |
| Purpose of Taking Medication | The purpose of linagliptin therapy is to improve glycemic control |
