Metformin Hydrochloride / Linagliptin

What it is and how it works

Mechanism of Action Linagliptin and Metformin Hydrochloride Linagliptin and metformin hydrochloride contains: linagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, and metformin, a biguanide. Linagliptin Linagliptin is an inhibitor of DPP-4, an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). Thus, linagliptin increases the concentrations of active incretin hormones, stimulating the release of insulin in a glucose-dependent manner and decreasing the levels of glucagon in the circulation. Both incretin hormones are involved in the physiological regulation of glucose homeostasis.

Mechanism class: Dipeptidyl Peptidase 4 Inhibitors

Indications

Linagliptin and metformin hydrochloride tablets are indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Limitations of Use Linagliptin and metformin hydrochloride tablets are not recommended in patients with type 1 diabetes mellitus. Linagliptin and metformin hydrochloride tablets have not been studied in patients with a history of pancreatitis. It is unknown whether patients with a history of pancreatitis are at an increased risk for the development of pancreatitis while using linagliptin and metformin hydrochloride tablets . Linagliptin and metformin hydrochloride tablets are a combination of linagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor and metformin hydrochloride (HCl), a biguanide, indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus Limitations of Use • Not recommended in patients with type 1 diabetes mellitus • Has not been studied in patients with a history of pancreatitis

Dosage and administration (summary)

• Individualize the starting dosage of linagliptin and metformin hydrochloride tablets based on the patient's current regimen • The maximum recommended dosage is 2.5 mg linagliptin/1,000 mg metformin HCl twice daily • Take orally twice daily with meals, with gradual dosage escalation to reduce the gastrointestinal effects due to metformin • Prior to initiation, assess renal function with estimated glomerular filtration rate (eGFR) o Do not use in patients with eGFR below 30 mL/min/1.73 m 2 o Initiation is not recommended in patients with eGFR between 30 to 45 mL/min/1.73 m 2 o Assess risk/benefit of continuing if eGFR falls below 45 mL/min/1.73 m 2 o Discontinue if eGFR falls below 30 mL/min…

Contraindications

Linagliptin and metformin hydrochloride are contraindicated in patients with: • severe renal impairment (eGFR below 30 mL/min/1.73 m 2 ) . • acute or chronic metabolic acidosis, including diabetic ketoacidosis . • hypersensitivity to linagliptin, metformin, or any of the excipients in linagliptin and metformin hydrochloride, reactions such as anaphylaxis, angioedema, exfoliative skin conditions, urticaria, or bronchial hyperreactivity have occurred with linagliptin .

Warnings and precautions

Lactic acidosis: See boxed warning Pancreatitis: There have been reports of acute pancreatitis, including fatal pancreatitis. If pancreatitis is suspected, promptly discontinue linagliptin and metformin hydrochloride. Hypoglycemia: Consider lowering the dosage of insulin secretagogue or insulin to reduce the risk of hypoglycemia when initiating linagliptin and metformin hydrochloride Hypersensitivity reactions: Serious hypersensitivity reactions (e.g., anaphylaxis, angioedema, and exfoliative skin conditions) have occurred with linagliptin and metformin hydrochloride.

Pregnancy

Pregnancy Risk Summary The limited data with linagliptin and metformin hydrochloride and linagliptin use in pregnant women are not sufficient to inform a linagliptin and metformin hydrochloride-associated or linagliptin-associated risk for major birth defects and miscarriage.

Storage and supply

Linagliptin and metformin hydrochloride tablets 2.5 mg/500 mg are yellow, oval, biconvex film-coated tablets debossed with “500” on one side and “LM” on the other side, and are supplied as follows: Bottles of 60 (NDC 72205-407-01) Bottles of 180 (NDC 72205-407-02) Linagliptin and metformin hydrochloride tablets 2.5 mg/850 mg are orange, oval, bicon…

Source: Linagliptin And Metformin Hydrochloride (Linagliptin And Metformin Hydrochloride) — US FDA prescribing information, 2025-11-04, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.