TRAJENTA 5MG TAB (TABLET)

Administration: Linagliptin: May be taken with or without food. Linagliptin + metformin hydrochloride: Should be taken with food. Special Precautions: Patient w/ history of pancreatitis; angioedema to other DPP-4 inhibitor. Not intended in patients w/ IDDM or for the treatment of diabetic ketoacidosis. Pregnancy and lactation. Monitoring Parameters Monitor HbA1C and serum glucose levels; signs/symptoms of pancreatitis. Adverse Drug Reaction: Hypoglycaemia, severe and disabling arthralgia, nasopharyngitis, rash, mouth ulcer, stomatitis, diarrhoea, cough. Rarely, hypersensitivity reactions. Potentially Fatal: Acute pancreatitis. Drug Interaction: Increased risk of hypoglycaemia when used w/ an insulin secretagogue (e.g. sulfonylurea) or insulin. Plasma concentration of linagliptin may be decreased by strong inducers of P-glycoprotein (e.g. rifampicin) and may be increased by strong P-glycoprotein inhibitors (e.g. ritonavir). Storage :Oral: Store at 25°C. Mechanism of Action: 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: Rapidly absorbed from the GI tract. Bioavailability: Approx 30%. Time to peak plasma concentration: W/in approx 1.5 hr. Distribution: Extensively distributed to body tissues. Plasma protein binding: Concentration dependent: 99% (low concentration); 70-80% (high concentration). Metabolism: Not extensively metabolised. Excretion: Via faeces (approx 80%) and urine (5%). Terminal half-life: >100 hr.