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 ?
Of the 33 cases of severe arthralgia found in the FDA adverse events reporting database, 28 were associated with the use of sitagliptin (Januvia), with some cases also reported with saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus).
Alogliptin (Nesina), a dipeptidyl peptidase-4 inhibitor, is in the same pharmacologic class as linagliptin (Tradjenta), saxagliptin (Onglyza), and sitagliptin (Januvia).
2008), and of other gliptins, such as alogliptin (Deacon 2008; Pratley 2009) and linagliptin (Rungby 2009; Tiwari 2009) are currently in late phase of development.
This edition includes new drugs, including Azilsartan Medoxomil, Boceprevir, Clobazam, Ezogabine, Fidaxomicin, Linagliptin, Rilpivirine, Rivaroxaban, Telaprevir, Roflumilast, Ticagrelor, and Vilazodone; updated bisphosphonate, antipsychotic, carbapenem, and proton pump inhibitor group monographs; new combinations such as Emtricitabine/Rilpivirine/Tenofovir; and a revised ophthalmic/otic chapter with additions like glaucoma combinations, mast cell stabilizers, ophthalmic antihistamines, and otic corticosteroids.
Washington, July 24 ( ANI ): Study of a drug for people with type 2 diabetes conducted in 32 countries including India has confirmed that the oral DPP-4 inhibitor linagliptin is a safe and effective means of lowering glucose levels for up to 102 weeks, either on its own or in combination with other selected oral anti-diabetic medication.
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).
Contract awarded for linagliptin, coated tablets 5mg.
Those approved in the United States are alogliptin (Nesina), linagliptin (Trajenta), saxagliptin (Onglyza), and sitagliptin (Januvia).
Linagliptin (Tradjenta; B), a dipeptidyl peptidase-4 inhibitor taken orally, is indicated for type 2 diabetes.
The new drug, linagliptin, results in significantly less weight gain and also less hypoglycaemia, experts from Tubingen University Hospital, in Germany, has found.
Phase III studies of Linagliptin, a compound being investigated by Boehringer Ingelheim as a once-daily oral treatment in type 2 diabetes, showed that the drug significantly lowered blood glucose, a report said.