linagliptin


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linagliptin

(lin-a-glip-tin) ,

Tradjenta

(trade name),

Trajenta

(trade name)

Classification

Therapeutic: antidiabetics
Pharmacologic: dipeptidyl peptidase4 ddp4 inhibitors
Pregnancy Category: B

Indications

Adjunct to diet and exercise in the management of type 2 diabetes mellitus.

Action

Inhibits the enzyme dipeptidyl peptidase-4 (DPP-4), which slows the inactivation of incretin hormones, resulting in increased levels of active incretin hormones. These hormones are released by the intestine throughout the day, and are involved in regulation of glucose. Increased/prolonged incretin levels increase insulin release and decrease glucagon levels.

Therapeutic effects

Improved control of blood glucose.

Pharmacokinetics

Absorption: 30% absorbed following oral administration.
Distribution: Extensively distributed to tissues.
Metabolism and Excretion: Approximately 90% excreted unchanged in urine; mininally metabolized.
Half-life: >100 hr (due to saturable binding to DPP-4).

Time/action profile

ROUTEONSETPEAKDURATION
POunknown1.5 hr†24 hr
† Blood level.

Contraindications/Precautions

Contraindicated in: Hypersensitivity. Cross-sensitivity may occur with sitagliptin;Type 1 diabetes mellitus;Diabetic ketoacidosis.
Use Cautiously in: History of pancreatitis; Geriatric: Elderly may have greater sensitivity to drug effects; Obstetric: Use during pregnancy only if clearly needed; Lactation: Excretion in breast milk unknown, use cautiously; Pediatric: Safety and effectiveness not established.

Adverse Reactions/Side Effects

Respiratory

  • bronchial hyperreactivity

Gastrointestinal

  • pancreatitis (life-threatening)

Dermatologic

  • localized exfoliation
  • urticaria

Metabolic

  • hypoglycemia
  • hypertriglyceridemia

Miscellaneous

  • hypersensitivity reactions including angioedema

Interactions

Drug-Drug interaction

↑ risk of hypoglycemia with sulfonylureas or insulin ; dose ↓ of sulfonylurea or insulin may be necessary.Concurrent use of P-glycoprotein or CYP3A4 inducers, including rifampin may ↓ blood levels and effectiveness and should be avoided.

Route/Dosage

Oral (Adults) 5 mg once daily.

Availability

Tablets: 5 mg
In combination with: metformin (Jentadueto). See combination drugs.

Nursing implications

Nursing assessment

  • Observe patient for signs and symptoms of hypoglycemic reactions (abdominal pain, sweating, hunger, weakness, dizziness, headache, tremor, tachycardia, anxiety).
  • Monitor for signs of pancreatitis (nausea, vomiting, anorexia, persistent severe abdominal pain, sometimes radiating to the back) during therapy. If pancreatitis occurs, discontinue linagliptin and monitor serum and urine amylase, amylase/creatinine clearance ratio, electrolytes, serum calcium, glucose, and lipase.
  • Lab Test Considerations: Monitor hemoglobin A1C prior to and periodically during therapy.
    • May cause ↑ uric acid levels.

Potential Nursing Diagnoses

Imbalanced nutrition: more than body requirements (Indications)
Noncompliance (Patient/Family Teaching)

Implementation

  • Patients stabilized on a diabetic regimen who are exposed to stress, fever, trauma, infection, or surgery may require administration of insulin.
  • Oral: May be administered without regard to food.

Patient/Family Teaching

  • Instruct patient to take linagliptin as directed. Take missed doses as soon as remembered, unless it is almost time for next dose; do not double doses. Advise patient to read the Patient Package Insert before starting and with each Rx refill; new information may be available.
  • Explain to patient that linagliptin helps control hyperglycemia but does not cure diabetes. Therapy is usually long term.
  • Instruct patient not to share this medication with others, even if they have the same symptoms; it may harm them.
  • Encourage patient to follow prescribed diet, medication, and exercise regimen to prevent hyperglycemic or hypoglycemic episodes.
  • Review signs of hypoglycemia and hyperglycemia with patient. If hypoglycemia occurs, advise patient to take a glass of orange juice or 2–3 tsp of sugar, honey, or corn syrup dissolved in water, and notify health care professional.
  • Instruct patient in proper testing of blood glucose and urine ketones. These tests should be monitored closely during periods of stress or illness and health care professional notified if significant changes occur.
  • Advise patient to notify health care professional promptly if signs and symptoms of pancreatitis or if rash; hives; or swelling of face, lips, or throat occur.
  • Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications, especially other oral hypoglycemic medications.
  • Advise patient to notify health care professional if pregnancy is planned or suspected or if breast feeding.

Evaluation/Desired Outcomes

  • Improved hemoglobin A1C, fasting plasma glucose and 2–hr post-prandial glucose levels.

linagliptin

(lĭn′ə-glĭp′tn)
n.
An oral hypoglycemic drug, C25H28N8O2, used to treat type 2 diabetes.
References in periodicals archive ?
In conjunction, Linagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, works by increasing hormones that stimulate the pancreas to produce more insulin and the liver to produce less glucose.
Those subjects who had previously received linagliptin (1,532) continued to do so and those who had received the placebo during the earlier trials (589) were also given the drug during the 78-week trial extension.
The new tablet combines the dipeptidyl peptidase-4 (DPP-4) inhibitor, linagliptin and metformin, said a statement from Boehringer Ingelheim Pharmaceuticals and Eli Lilly and Company.
Sitagliptin (Januvia[R]), saxagliptin (Onglyza[R]) and linagliptin (Trajenta[R]) work by inhibiting the enzyme dipeptidyl peptidase IV (DPP-IV), which is responsible for the degradation of the endogenous hormone incretin (also known as glucagon-like peptide-1 or GLP-1).
Summary: Linagliptin continues to differentiate itself as potential future option for patients with type 2 diabetes, regardless of stage of the condition or kidney function
Limited Tenders are invited for Supply of Medicine: Tab Linagliptin 5mg QTY 2500 Pen
2-year efficacy and safety of linagliptin compared with glimepiride in patients with type 2 diabetes inadequately controlled on metformin: a randomised, double-blind, non-inferiority trial.
Jentadueto XR is a prescription medicine that contains two diabetes medicines, linagliptin and metformin.
CV outcomes trials for the two other approved DPP-4 inhibitors--sitagliptin (Januvia) and linagliptin (Tradjenta)--are ongoing.
Cardiovascular Outcome Study of Linagliptin versus Glimepiride in Patients with Type 2 Diabetes (CAROLINA) an ongoing large head-to- head CV outcome trial comparing a SU (glimepiride) with a dipeptidyl peptidase-4 (DPP-4) inhibitor (linagliptin) will provide much needed information related to SU safety.
Alogliptin (Nesina), a dipeptidyl peptidase-4 inhibitor, is in the same pharmacologic class as linagliptin (Tradjenta), saxagliptin (Onglyza), and sitagliptin (Januvia).
The new drug, linagliptin, results in significantly less weight gain and also less hypoglycaemia, experts from Tubingen University Hospital, in Germany, has found.