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(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.


An oral hypoglycemic drug, C16H15F6N5O, used in its phosphate form to treat type 2 diabetes.


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 ?
However, the Merck Pregnancy Registries (2006-2009) described the outcomes of eight women who were exposed to sitagliptin or sitagliptin/ metformin in the first trimester.
Sam Engel, MD, associate vice president, Merck clinical research, cardiometabolic and women's health, said, 'We are pleased to share these new Phase 3 data with the scientific community that support the product profile of ertugliflozin as add-on therapy to metformin or for first-line use when combined with sitagliptin.
Patients taking ertugliflozin 5 mg or 15 mg, in combination with sitagliptin 100 mg, experienced greater reductions in A1C compared with patients taking placebo alone (1.
The study population included 78,553 adults who initiated saxagliptin and 298,124 who initiated sitagliptin, who were compared with patients who initiated pioglitazone, second-generation sulonyl-ureas, or long-acting insulins.
6 percent of patients (n=695) in both the Sitagliptin and placebo groups in the Per Protocol (PP) analysis (HR=0.
He said the medicine Sitagliptin (brand name Januvia) was put under the TECOS (Trial Evaluating Cardiovascular Outcomes) in 2008.
Objective: To compare combination of metformin and glimepiride with that of metformin and sitagliptin in patients with type 2 diabetes mellitus.
In trials (Aschner et al; Raz I et al), treatment with once-daily 100mg sitagliptin significantly reduced HbA1c by 0.
The aim of the present study is to evaluate the effect of add-on of sitagliptin on blood glucose control or glucose fluctuation as well as the tolerability of this combination therapy in more than 200 Japanese type 2 diabetic patients treated with insulin and/or other OHA in real clinical practice.
While this is less than the reduction typically seen with the diabetes drug metformin (Glucophage, Fortamet), it is slightly better than results seen with some of the newer drugs, such as sitagliptin (Januvia).
CHICAGO -- Canagliflozin outperformed sitagliptin for the treatment of patients with type 2 diabetes in the first randomized head-to-head comparison of drugs representing the two different classes of oral antidiabetic medications.