Linagliptin
Brand Name: Tradjenta
Common Dosage Forms:
Tablets: 5 mg
FDA Indications/Dosages:
As an adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes mellitus: 5 mg taken once daily.
When used with an insulin secretagogue (sulfonylurea) or with insulin, use a lower dose of the insulin secretagogue or insulin to decrease the risk of hypoglycemia.
Monitor: FBG, HbA1C
Pharmacology/Pharmacokinetics: Linagliptin inhibits the dipeptidyl peptidase-4 (DDP-4) enzyme. DDP-4 is responsible for deactivating the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). These hormones are released by the intestine in response to food and are credited with increasing insulin synthesis and release from pancreatic beta cells. GLP-1 also decreases hepatic glucose production by lowering glucagon secretion from pancreatic alpha cells. By inhibiting DDP-4, linagliptin increases insulin and decreases glucagon in response to elevated blood glucose. Inhibition of DDP-4 by sitagliptin lasts for 24 hours. Peak plasma levels are reached in 1.5 hours. Approximately 85% is excreted in the urine as unchanged drug. The terminal half-life after an oral dose is approximately 12 hours.
Drug Interactions: Strong inducers of CYP3A4 or P-gp (rifampin) may decrease effectiveness.
Contraindications/Precautions: Contraindicated in patients with known or suspected hypersensitivity to linagliptin. Increases the risk of acute pancreatitis (upper abdominal pain, nausea and vomiting, fever). Use caution when combining with medications known to cause hypoglycemia. Hypersensitivity reactions have occurred within 3 months of starting therapy. Pregnancy Category B.
Adverse Effects: Adverse effects are uncommon and mild and include nasopharyngitis, diarrhea, and cough. A rare adverse effect seen with other DDP-4 inhibitors is joint pain (arthralgia). Rare but severe cases of hypersensitivity and pancreatitis have been reported.
Patient Consultation:
May be taken without regard to meals.
Closely follow recommended dietary and exercise instructions.
Quarterly HbA1c testing should be performed.
Store in a cool, dry place away from sunlight and children.
If a dose is missed, take it as soon as possible but do not double doses.
Call physician is above side effects are severe or persistent.
