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

Therapeutic class: Hypoglycemic

Pregnancy risk category B


Inhibits DPP-4 and slows inactivation of incretin hormones, thereby increasing blood concentrations and reducing fasting and postprandial glucose concentrations in a glucose-dependent manner in patients with type 2 diabetes mellitus


Tablets: 2.5 mg, 5 mg

Indications and dosages

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

Adults: 2.5 to 5 mg P.O. daily

Dosage adjustment

• Moderate, severe, or end-stage renal disease

• Concurrent use of strong CYP450 inhibitors


• History of serious hypersensitivity to drug (such as anaphylaxis, angioedema, or exfoliative skin conditions)


Use cautiously in:

• renal impairment, history of pancreatitis

• concurrent use of insulin secretagogues or strong CYP450 and CYP3A4/5 inhibitors

• pregnant or breastfeeding patients

• children (safety and efficacy not established).


• Assess renal function before starting therapy.

Before starting drug, identify possible risk factors for pancreatitis, such as history of pancreatitis, alcoholism, gallstones, or hypertriglyceridemia.

• Administer without regard to meals.

• Be aware that drug shouldn't be used for the treatment of type 1 diabetes mellitus or diabetic ketoacidosis.

Adverse reactions

CNS: headache

EENT: sinusitis

GI: vomiting, abdominal pain, gastroenteritis, acute pancreatitis

GU: urinary tract infection

Metabolic: hypoglycemia

Respiratory: upper respiratory tract infection

Skin: urticaria, exfoliative skin conditions

Other: peripheral edema, facial edema, hypersensitivity (including anaphylaxis and angioedema)


Drug-drug. Insulin secretagogues (such as sulfonylureas): possible increased risk of hypoglycemia

Strong CYP3A4/5 inhibitors (such as atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin): significantly increased saxagliptin effect

Drug-diagnostic tests. Lymphocytes: decreased count

Drug-food. Any food: increased saxagliptin area under the curve

Patient monitoring

• Monitor blood glucose and hemoglobin A1C levels and renal function tests periodically during therapy.

• Monitor CBC with differential, particularly lymphocyte count, in patients with unusual or prolonged infection.

Observe patient carefully for signs and symptoms of pancreatitis. If pancreatitis is suspected, promptly discontinue drug and initiate appropriate management.

Patient teaching

• Tell patient to take drug with or without food. Tell patient not to split or cut tablet.

• Teach patient about signs and symptoms of hypoglycemia (blurred vision, confusion, tremor, diaphoresis, excessive hunger, drowsiness, increased heart rate) and how to treat it, especially if taking saxagliptin with other drugs that may cause hypoglycemia.

Instruct patient to discontinue drug and immediately report signs and symptoms of hypersensitivity reaction (such as hives, rash, or swelling of face, lips, or throat) or pancreatitis (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 level at home.

• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs, tests, and food mentioned above.

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


(sax-a-glip-tin) ,


(trade name)


Therapeutic: antidiabetics
Pharmacologic: dipeptidyl peptidase4 ddp4 inhibitors
Pregnancy Category: B


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


Acts as a competitive inhibitor of dipeptidyl peptidase-4 (DPP4), which slows inactivation of incretin hormones, thereby increasing their concentrations and reducing fasting and postprandial glucose concentrations.

Therapeutic effects

Improved control of blood glucose.


Absorption: Well absorbed following oral administration.
Distribution: Unknown.
Metabolism and Excretion: Metabolized by the liver via the P450 3A4/5 (CYP3A4/5) enzyme system, with conversion to 5–hydroxysaxagliptin, a pharmacologically active metabolite; 24% of saxagliptin is excreted unchanged in urine, 36% of hydroxysaxagliptin is excreted unchanged in urine, 22% is eliminated in feces as unabsorbed drug/metabolites excreted in bile.
Half-life: Saxagliptin—2.5 hr; 5–hydroxysaxagliptin—3.1 hr.

Time/action profile (DDP-4 inhibition)

POunknown2 hr (4 hr for 5–hydroxysaxagliptin)†24 hr
† Blood levels


Contraindicated in: Type 1 diabetes;Diabetic ketoacidosis;History of hypersensitivity reaction
Use Cautiously in: Geriatric: May be more sensitive to effects; consider age-related ↓ in renal function; Obstetric: Use only if clearly needed; Lactation: Use cautiously; Pediatric: Safety and effectiveness not established.

Adverse Reactions/Side Effects

Central nervous system

  • headache


  • peripheral edema (↑ with thiazolidinediones)


  • pancreatitis (life-threatening)
  • abdominal pain
  • vomiting


  • ↓ lymphocyte count


  • hypoglycemia (↑ with sulfonylureas)


  • hypersensitivity reactions (anaphylaxis, angioedema, exfoliative skin disorders) (life-threatening)


Drug-Drug interaction

Strong CYP3A4/5 inhibitors, including ketoconazole, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone, nelfinavir, ritonavir, saquinavir, and telithromycin ↑ blood levels; daily dose should not exceed 2.5 mg.↑ risk of hypoglycemia with sulfonylureas or insulin ; may need to ↓ dose of sulfonylureas or insulin.


Oral (Adults) 2.5–5 mg once daily; Strong CYP3A4/5 inhibitors—2.5 mg once daily.

Renal Impairment

Oral (Adults) CCr ≤50 mL/min—2.5 mg once daily.


Tablets: 2.5 mg, 5 mg
In combination with: metformin XR (Kombiglyze 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 saxagliptin 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.
    • Monitor renal function prior to and periodically during therapy.
    • May cause ↓ absolute lymphocyte count.

Potential Nursing Diagnoses

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


  • 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. Swallow tablet whole, do not cut or split.

Patient/Family Teaching

  • Instruct patient to take saxagliptin as directed. If a dose is missed, take the next dose as prescribed; 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 saxagliptin 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 swelling of hands, feet, or ankles; rash; hives; or swelling of face, lips, or throat occur.
  • Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new 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.
Drug Guide, © 2015 Farlex and Partners


An oral hypoglycemic drug, C18H25N3O2, used to treat type 2 diabetes.
The American Heritage® Medical Dictionary Copyright © 2007, 2004 by Houghton Mifflin Company. Published by Houghton Mifflin Company. All rights reserved.
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References in periodicals archive ?
The approval is based on two Phase III trials, which evaluated combinations of dapagliflozin and saxagliptin on a background of metformin over 24 weeks, in patients with inadequately-controlled T2D.
The approval is based on two Phase III trials that assessed combinations of dapagliflozin and saxagliptin on a background of metformin over 24 weeks, in patients with inadequately-controlled T2D.
Reportedly, this approval is based on two phase III trials, which evaluated combinations of dapagliflozin and saxagliptin on a background of metformin over 24 weeks, in patients with inadequately-controlled T2D.
The medical terms (MeSH) used were the following: sodium-glucose cotransporter-2 OR SGLT2 OR empagliflozin OR canagliflozin OR dapagliflozin OR DPP-4 OR dipeptidyl peptidase-4 inhibitors OR sitagliptin OR saxagliptin OR vildagliptin OR linagliptin OR gemigliptin OR canagliptin OR teneligliptin OR alogliptin OR trelagliptin OR omarigliptin OR evogliptin OR dutogliptin OR GLP-1 OR glucagon-like peptide-1 OR exenatide OR lixisenatide OR dulaglutide OR liraglutide OR semaglutide AND endothelial function OR arterial stiffness OR flow-mediated dilation OR pulse wave velocity.
The drugs such as linagliptin, saxagliptin, sitagliptin, and vildagliptin were obtained from pharmaceutical companies as gifted samples in pure powder form of IP grade.
These 4 trials include the simultaneous addition to metformin of exenatide and dapagliflozin, saxagliptin and dapagliflozin, alogliptin and pioglitazone, and empagliflozin and linagliptin.
Patients (n = 12) with both T2DM and stable CAD recruited from the Department of Cardiology, Oslo University Hospital Ullevaal, Oslo, Norway, from 2012-14, were randomized double blinded to placebo or saxagliptin (5mg/day) for 3 months.
While sitagliptin, alogliptin, and saxagliptin were shown to be safe for the cardiovascular system in terms of the MACE, cardiovascular death, and heart failure endpoints, the SAVOR-TIMI 53 trial showed a rather surprising signal for an increased risk for hospitalization of heart failure in the saxagliptin group, especially in the subgroups of impaired renal function and preexisting heart failure [25].
Experts also discuss the positive cardiovascular safety data published for Victoza in the LEADER trial, and shed light on the recent US-FDA issued warnings about heart failure risk to the labels of T2DM medicines containing saxagliptin (Onglyza) and alogliptin (Nesina).
NEITHER SAXAGLIPTIN NOR sitagliptin, the two oral DPP-4 inhibitors most commonly used as antihyperglycemic medications, raised the risk of hospitalization for heart failure in a large population-based cohort study that analyzed data from a Food and Drug Administration surveillance program.
DPP-4 inhibitors (e.g., sitagliptin [Januvia[R]], saxagliptin [Onglyza[R]], linagliptin [Tradjenta[R]], and alogliptin [Nesina[R]]) delay degradation of endogenous GLP-1 and GIP.