LINAGIT 5

Each film coated tablets contains:

(Linagliptin 5 mg)

Tablet for Oral Use

Linagliptin is a competitive, reversible DPP-4 inhibitor. DPP-4, is an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). Inhibition of DPP-4 in turn, increases the plasma concentrations of active incretin hormones, thereby stimulating the release of insulin in a glucose-dependent manner and decreasing circulating levels of glucagon. GLP-1 and GIP are involved in the physiological regulation of glucose homeostasis. Both hormones increase the biosynthesis of insulin and its secretion from pancreatic beta cells in the presence of normal or elevated levels of blood glucose. In addition, GLP-1 reduces glucagon secretion from pancreatic alpha-cells, resulting in a reduction in glucose output in the liver

Absorption: Linagliptin is rapidly absorbed after oral administration, with C (max) occurring after approximately 90 minutes, and reaches steady-state concentrations within 4 days. The oral bioavailability of Linagliptin is approximately 30%.

Distribution: Linagliptin exhibits a V (d) of more than 1000 L, indicating widespread distribution into tissues. Binding to target proteins in plasma and peripheral tissues exerts a major influence upon broadening Linagliptin distribution.

Metabolism & Excretion: Linagliptin is hardly metabolized and approximately 90% of the compound is excreted in an unchanged form by the hepatobiliary route via the feces. 84.7% of Linagliptin is eliminated in the feces and 5.4% is eliminated in the urine.

Half Life: Linagliptin has a long terminal half-life (>100 hours); however, its accumulation half-life is much shorter (approximately 10 hours), accounting for the rapid attainment of steady state.

• Indicated for adults with type 2 diabetes mellitus along with diet and exercise to lower blood sugar

ADVERSE REACTION

The most common side effects of include: runny or stuffy nose, sore throat, cough, and diarrhea

Serious side effects include: severe pain in upper stomach spreading to back, nausea, vomiting, loss of appetite, fast heartbeats, itching, blisters, breakdown of the outer layer of skin, shortness of breath, swelling in legs or feet, rapid weight gain, severe or ongoing pain in joints, fever, sore throat, swelling in  face or tongue, burning in eyes, and skin pain followed by a red or purple skin rash that spreads (especially in the face or upper body) and causes blistering and peeling

DOSAGE AND ADMINISTRATION:

Linagliptin is given as 5mg per oral once daily

CONTRAINDICATIONS

Contraindicated in patient Hypersensitivity to Linagliptin, Diabetic ketoacidosis

WARNINGS AND PRECAUTIONS:

• Discontinue taking Linagliptin if signs and symptoms of Pancreatitis occur
• Use cautiously in patient with heart failure
• Lower dose of the insulin secretagogue or insulin may be required to reduce the risk of hypoglycemia when used in combination with Linagliptin

Pregnancy Category: B

Drug Interaction:

• The efficacy of Linagliptin may be reduced when the drug is coadministered with a strong CYP3A4 or P-glycoprotein inducer (e.g., Rifampin)