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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.

McGraw-Hill Nurse's Drug Handbook, 7th Ed. Copyright © 2013 by The McGraw-Hill Companies, Inc. All rights reserved


(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.
Drug Guide, © 2015 Farlex and Partners


A trademark for the drug sitagliptin phosphate.
The American Heritage® Medical Dictionary Copyright © 2007, 2004 by Houghton Mifflin Company. Published by Houghton Mifflin Company. All rights reserved.
References in periodicals archive ?
Avanir Pharmaceuticals Inc plans to co-promote Merck's type 2 diabetes therapies JANUVIA (sitagliptin) and the sitagliptin family of products in the US.
In the 26-week study, exenatide patients had a 1.55% drop in A1C level compared with a drop of 0.92% for Januvia, known chemically as sitagliptin, and a 1.23% reduction for Actos, known chemically as pioglitazone, according to data presented at the American Diabetes Association scientific meeting in New Orleans.
Merck, which declined to disclose its marketing plans for Janumet and Januvia, said no new clinical data were needed to back the supplemental New Drug Applications for the two label expansions.
The collaboration between the two companies has already been ongoing for a number of years, with both companies developing improved production processes for some of Merck's most important new products, such as Januvia (sitagliptin) for diabetes, asthma drug Singulair (montelukast) and the recently launched hepatitis C therapy Victrelis (boceprevir).
Industrial enzymes company Codexis Inc (NYSE:CDXS) reported on Tuesday the receipt of approval for a new production process for sitagliptin tablets, the active pharmaceutical ingredient in Januvia.
and EMA, including a combo of Zetia and diabetes blockbuster Januvia,
On the positive side, Merck projected strong growth for its relatively new Januvia diabetes franchise, as well as for its HIV drug Isentress and shingles vaccine Zostavax.
So now we procrastinate, and say, "Let's try Januvia or Byetta," or one of the thiazolidinediones we didn't have before.
M2 PHARMA-May 1, 2012-Merck's new environmentally-friendly manufacturing process for Januvia approved by FDA(C)2012 M2 COMMUNICATIONS
Healthcare company Novo Nordisk A/S (NYSE:NVO) announced on Friday that the US Food and Drug Administration (FDA) has approved to update the product label for Victoza (liraglutide [rDNA] injection) to include data showing superior blood sugar control and weight reduction when compared to Januvia (sitagliptin).
Pharma revenues grew 2% to $9.8 billion, led by Singulair (+14% to $1.3 billion), Remicade (+12% to $753 million) and Januvia (+45% to $739 million).
Amylin Pharmaceuticals Inc's (San Diego CA) diabetes treatment Byetta worked better than Merck & Co's (Whitehouse Station NJ) Januvia in tests that measured blood-sugar levels after meals in 61 patients who tried each drug for two weeks.