Linagliptin and Metformin

Hypoglycaemic excluding Insulin · Biguanide/Dipeptidyl peptidase-4 inhibitor

Indications

Type II diabetes inadequately controlled by diet and exercise: when metformin is inadequate in patients who are currently receiving the combination as separate tab or with a sulphonylurea plus metformin is inadequate.

Dosage

Adults: Initially based on current metformin dose, 2.5 mg/850 mg or 2.5 mg/gm twice daily with or after food. Combination therapy, consider lower dose of sulphonylurea, max daily dose of linagliptin, 5 mg. Children: Not recommended.

Adverse Effects

Lactic acidosis.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Contraindications: Moderate to severe renal (CrCl < 60 mL/ min) or hepatic impairment, diabetic ketoacidosis or pre coma. Acute conditions predisposing to renal impairment. Cardiac or respiratory failure, recent MI, acute alcohol intoxication, alcoholism. Precautions: Monitor renal function at least annually (2-4 times years in elderly and patients with serum Creatinine levels = ULN). Discontinue for 48 hours before and after surgery; confirm normal renal function before resuming. Risk of pancreatitis; advise patient of symptoms, discontinue if suspected.

Interactions

Alcohol, cimetidine, iodinated contrast agents, glucocorticoids, insulin, sulphonylurea, diuretics, Beta 2 agonists, potent CYP3A4 and P-gp inducer.

Pharmacokinetics

LINAGLIPTIN: Metabolism: Via minor elimination pathway. A small fraction is converted into an inactive metabolite. Bioavailability: Approx 30%. Time to peak, plasma: 1.5 hrs. Excretion: Faeces (80%). Urine (5%). METFORMIN: Onset of action: Within days, max effects up to 2 wks. Metabolism: Not metabolized by the liver. Bioavailability: Absolute: Fasting: 50%-60%. Half-life elimination: Plasma: 4-9 hrs. Blood: Approx. 17.6 hrs. Time to peak, serum: Immediate release: 2-3 hrs. Extended release: 7 hrs. (Range: 4-8 hrs). Excretion: Urine.

Compiled by Healify Pharmacy from published drug references. How we compile it →

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