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sitagliptin phosphate


Pharmacologic class: Dipeptidyl peptidase 4 (DPP-4) inhibitor

Therapeutic class: Hypoglycemic

Pregnancy risk category B


Inhibits DPP-4 and slows inactivation of incretin hormones, helping to regulate glucose homeostasis through increased insulin release and decreased glucagon levels


Tablets: 25 mg, 50 mg, 100 mg

Indications and dosages

Adjunct to diet and exercise to improve glycemic control in type 2 diabetes mellitus

Adults: 100 mg P.O. once daily

Dosage adjustment

• Moderate to severe renal insufficiency or end-stage renal disease


• History of serious hypersensitivity to drug (such as anaphylaxis or angioedema)


Use cautiously in:
• concurrent administration of drugs that cause hypoglycemia (such as sulfonylureas or insulin)
• renal impairment, history of pancreatitis
• pregnant or breastfeeding patients
• children younger than age 18 (safety and efficacy not established).


• Assess renal function before starting therapy.

Before starting drug, ask patient about possible risk factors for pancreatitis, such as history of pancreatitis, alcoholism, gallstones, or hypertriglyceridemia. However, it's unknown if these conditions make it more likely that pancreatitis will occur.
• Give with or without food.
• Be aware that drug shouldn't be used to treat type 1 diabetes mellitus or diabetic ketoacidosis.
• Know that when drug is used with a sulfonylurea, a lower dose of sulfonylurea may be required, to reduce risk of hypoglycemia.

Adverse reactions

CNS: headache

EENT: nasopharyngitis

GI: abdominal pain, nausea, vomiting, diarrhea, pancreatitis

GU: acute renal failure

Respiratory: upper respiratory tract infection

Other: hypersensitivity reactions (including anaphylaxis, angioedema, exfoliative skin conditions such as Stevens-Johnson syndrome)


Drug-drug.Digoxin: minimally increased digoxin effect and blood level

Insulin, sulfonylureas: possible increased hypoglycemia risk

Patient monitoring

• Monitor renal function periodically.
• Measure patient's weight and body mass index periodically during therapy.
• Monitor blood glucose and hemoglobin A1c levels periodically during therapy.

Monitor patient for signs and symptoms of hypersensitivity reactions and immediately stop drug and institute emergency measures if such reactions occur.
• Check for diabetes signs and symptoms and disease progression routinely during therapy.

Be aware of postmarketing reports of acute pancreatitis, including fatal and nonfatal hemorrhagic or necrotizing pancreatitis. If pancreatitis is suspected, promptly discontinue drug.

Patient teaching

• Instruct patient to take drug with or without food.
• Teach patient about signs and symptoms of hypoglycemia (such as blurred vision, confusion, tremor, sweating, excessive hunger, drowsiness, and fast heart rate).

Teach patient about signs and symptoms of hypersensitivity reactions (such as rash, throat swelling, or difficulty breathing) and to immediately contact prescriber if these occur.

Instruct patient to immediately discontinue drug and report if signs and symptoms of pancreatitis occur (persistent severe abdominal pain, sometimes radiating to the back, which may or may not be accompanied by vomiting).
• Instruct patient to routinely monitor blood glucose levels at home.
• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs mentioned above.


(sit-a-glip-tin) ,


(trade name)


Therapeutic: antidiabetics
Pharmacologic: enzyme inhibitors
Pregnancy Category: B


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.


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.


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

POrapid1–4 hr24 hr


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


  • pancreatitis (life-threatening)
  • nausea
  • diarrhea


  • acute renal failure


  • upper respiratory tract infection
  • nasopharyngitis


  • arthralgia
  • back pain
  • myalgia


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


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).


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.


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)


  • 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.


A trademark for the drug sitagliptin phosphate.


a trademark for sitagliptin.
References in periodicals archive ?
What our studies discovered was that those patients who were taking Januvia were less likely to suffer from hypoglycemic attacks, than those taking a sulphonylurea.
Q I read about a new drug for diabetes I called Januvia.
Januvia exerts action by inactivating DPP-IV, thereby, increasing active levels of GLP-1 which helps promote the release of insulin.
The 49-year-old controls his blood sugars by taking medication which includes Januvia, a treatment which improves the body's ability to lower blood sugar when it is too high.
Analysts expect Januvia and Janumet to have combined annual sales of $2 billion by 2010.
Januvia is the first diabetes treatment in an emerging class of drugs known as DPP-4 inhibitors that enhance the body's ability to lower elevated blood sugars.
The FDA approved Januvia for use in addition to diet and exercise to improve glucose levels, either by itself or in combination with older drugs.
Unlike many other diabetes drugs, Januvia doesn't cause hypoglycemia (low blood sugar) or weight gain.
The FDA has announced the approval of Januvia (sitagliptin phosphate) Tablets, the first diabetes treatment approved in a new class of drugs known as DPP-4 inhibitors that enhances the body's own ability to lower elevated blood sugar.
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.
The 26-week VERTIS SITA study compared the efficacy and safety of initial combination therapy with ertugliflozin and Merck's DPP-4 inhibitor JANUVIA (sitagliptin) with placebo.