sitagliptin


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sitaGLIPtin

(sit-a-glip-tin) ,

Januvia

(trade name)

Classification

Therapeutic: antidiabetics
Pharmacologic: enzyme inhibitors
Pregnancy Category: B

Indications

Adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes mellitus; may be used as monotherapy or combination therapy with metformin, a thiazolidinedione, a sulfonylurea, or insulin.

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 homeostasis. Increased/prolonged incretin levels result in an increase in insulin release and decrease in glucagon levels.

Therapeutic effects

Improved control of blood glucose.

Pharmacokinetics

Absorption: 87% absorbed following oral administration.
Distribution: Unknown.
Metabolism and Excretion: 79% excreted unchanged in urine, minor metabolism.
Half-life: 12.4 hr.

Time/action profile

ROUTEONSETPEAKDURATION
POrapid1–4 hr24 hr

Contraindications/Precautions

Contraindicated in: Type 1 diabetes mellitus;Diabetic ketoacidosis;Hypersensitivity.
Use Cautiously in: Renal impairment (dose ↓ required for CCr <50 mL/min);History of pancreatitis;History of angioedema to another DPP-4 inhibitor Obstetric / Use only if clearly needed. Lactation: Excretion into breast milk unknown; Pediatric: Safety not established; Geriatric: Consider age-related ↓ in renal function when determining dose.

Adverse Reactions/Side Effects

Central nervous system

  • headache

Gastrointestinal

  • pancreatitis (life-threatening)
  • nausea
  • diarrhea

Genitourinary

  • acute renal failure

Respiratory

  • upper respiratory tract infection
  • nasopharyngitis

Musculoskeletal

  • arthralgia
  • back pain
  • myalgia

Miscellaneous

  • allergic reactions including anaphylaxis (life-threatening)
  • angioedema (life-threatening)
  • exfoliative skin conditions (stevens-johnson syndrome) (life-threatening)
  • rash
  • urticaria

Interactions

Drug-Drug interaction

May slightly ↑ serum digoxin levels; monitoring recommended.↑ risk of hypoglycemia when used with insulin, glyburide, glipizide, or glimepiride (may need to ↓ dose of insulin or sulfonylurea).

Route/Dosage

Oral (Adults) 100 mg once daily.

Renal Impairment

Oral (Adults) CCr 30–<50 mL/min—50 mg once daily; CCr <30 mL/min—25 mg once daily.

Availability

Tablets: 25 mg, 50 mg, 100 mg Cost: 25 mg $801.18 / 90, 50 mg $816.93 / 90, 100 mg $816.93 / 90
In combination with: metformin (Janumet), metformin XR (Janumet XR). 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 sitagliptin and monitor serum and urine amylase, amylase/creatinine clearance ratio, electrolytes, serum calcium, glucose, and lipase.
  • Assess for rash periodically during therapy. May cause Stevens-Johnson syndrome. Discontinue therapy if severe or if accompanied with fever, general malaise, fatigue, muscle or joint aches, blisters, oral lesions, conjunctivitis, hepatitis, and/or eosinophilia.
  • Lab Test Considerations: Monitor hemoglobin A1C prior to and periodically during therapy.
    • Monitor renal function prior to and periodically during therapy.

Potential Nursing Diagnoses

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

Implementation

  • Do not confuse sitagliptin with sumatriptan. Do not confuse Januvia (sitagliptin) with Enjuvia (estrogens, conjugated B), Jantoven (warfarin), or Janumet (sitagliptin/metformin).
  • 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 sitagliptin 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 Medication Guide before starting and with each Rx refill in case of changes.
  • Explain to patient that sitagliptin 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 stop taking sitagliptin and notify health care professional promptly if symptoms of hypersensitivity reactions (rash; hives; swelling of face, lips, tongue, and throat; difficulty in breathing or swallowing) or pancreatitis 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.
  • Advise patient to notify health care professional if pregnancy is planned or suspected or if breast feeding. Encourage patients who become pregnant while taking sitagliptin to join the pregnancy registry by calling 1-800-986-8999.

Evaluation/Desired Outcomes

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

sitagliptin

(sĭt′ə-glĭp′tn)
n.
An oral hypoglycemic drug, C16H15F6N5O, used in its phosphate form to treat type 2 diabetes.

sitagliptin

an oral antidiabetic.
indications This drug is used alone or in combination with other antidiabetic agents to treat type 2 diabetes mellitus.
contraindications Diabetic ketoacidosis and known hypersensitivity to this drug prohibit its use.
adverse effects Adverse effects of this drug include hypoglycemia and abdominal pain. Common side effects include headache, nausea, and vomiting.
References in periodicals archive ?
He said the medicine Sitagliptin (brand name Januvia) was put under the TECOS (Trial Evaluating Cardiovascular Outcomes) in 2008.
In two of these studies comparing canagliflozin to current standard treatments, sitagliptin and glimepiride, canagliflozin dosed once-daily at 300 mg provided significantly greater reductions in A1C levels relative to both comparators with similar overall incidence of adverse events.
Low sitagliptin incidence of (Januvia[R]) hypoglycemia in both saxagliptin monotherapy and (Onglyza[R]) combination therapy.
7-fold higher rate of pancreatic cancer in patients on sitagliptin, compared with the other therapies.
Sitagliptin is a member of a potentially new class of oral drugs (DPP-4 inhibitors) that enhances the body's ability to lower blood sugar when it is elevated.
One of the new drugs, sitagliptin, is made by Merck Research Laboratories of Rahway, N.
Merck's first-in-class DPP-IV inhibitor, sitagliptin (Januvia/Xelevia), will remain the leading agent in the class while other agents struggle to differentiate themselves, owing to their lack of significant clinical advantages over Januvia.
Contract awarded for sitagliptin phosphate, metformin hydrochloride, single-coated tablet 50 mg / 1000 mg
06 for sitagliptin, or among those who had been treated with a GLP1 receptor agonist (OR, 0.
In the open-label study, adults with type 2 diabetes (n=659) who participated in one of two 12-week, blinded, dose-finding empagliflozin trials, were treated for an additional 78 weeks with open-label empagliflozin 10 mg or 25 mg (monotherapy or add-on to metformin), metformin alone, or sitagliptin as add-on to metformin.
Efficacy and safety of the dipeptidyl peptidase-4 inhibitor, sitagliptin, compared with the sulfonylurea, glIpizide, in patients with type 2 diabetes inadequately controlled on metformin alone: A randomized, double-blind, non-inferiority trial.
Hillblom Islet Research Centre at UCLA found that sitagliptin, sold in pill form as Januvia, caused abnormalities in the pancreas that are recognized as risk factors for pancreatitis and, with time, pancreatic cancer in humans.