INCRET M

INCRET-M combines 2 antihyperglycemic agents with complementary mechanisms of action to improve glycemic control in patients with type 2 diabetes mellitus: linagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, and metformin, a member of the biguanide class. Metformin is a biguanide w/ antihyperglycaemic effects, lowering both basal and postprandial plasma glucose. It decreases hepatic glucose production by inhibiting gluconeogenesis and glycogenolysis; delays intestinal absorption of glucose; and enhances insulin sensitivity by increasing peripheral glucose uptake and utilisation. Linagliptin inhibits dipeptidyl peptidase-4 (DPP-4), an enzyme which is involved in the inactivation of the incretin hormones GLP-1 (glucagon-like peptide-1) and GIP (glucose-dependent insulinotropic polypeptide). Both incretin hormones are involved in the physiological regulation of glucose homeostasis. Inhibition of DPP-4 leads to increased and prolonged active incretin levels.

Absorption: Slowly and incompletely absorbed from the GI tract. Absolute bioavailability: Approx 50-60% (fasting); reduced if taken w/ food. Time to peak plasma concentration: 2-3 hr (immediate-release); 4-8 hr (extended-release). Distribution: It crosses the placenta and distributed in breast milk (small amounts). Volume of distribution: 654 ± 358 L.Plasma protein binding is negligiable. Metabolism: Not metabolised. Excretion: Via urine (90% as unchanged drug). Elimination half-life: Approx 2-6 hr.

The dosage of INCRET-M should be individualized on the basis of both effectiveness and tolerability, while not exceeding the maximum recommended dose of 2.5 mg linagliptin/1000 mg metformin hydrochloride twice daily. INCRET-M should be given twice daily with meals. Dose escalation should be gradual to reduce the gastrointestinal (GI) side effects associated with metformin use. Recommended starting dose: • In patients currently not treated with metformin, initiate treatment with 2.5 mg linagliptin/500 mg metformin hydrochloride twice daily • In patients already treated with metformin, start with 2.5 mg linagliptin and the current dose of metformin taken at each of the two daily meals (e.g., a patient on metformin 1000 mg twice daily would be started on 2.5 mg linagliptin/1000 mg metformin hydrochloride twice daily with meals). • Patients already treated with linagliptin and metformin individual components may be switched to INCRET-M containing the same doses of each component.

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