saxagliptin


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saxagliptin

Onglyza

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

Therapeutic class: Hypoglycemic

Pregnancy risk category B

Action

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

Availability

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

Contraindications

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

Precautions

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).

Administration

• 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)

Interactions

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.

saxagliptin

(sax-a-glip-tin) ,

Onglyza

(trade name)

Classification

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

Indications

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

Action

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.

Pharmacokinetics

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)

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

Contraindications/Precautions

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

Cardiovascular

  • peripheral edema (↑ with thiazolidinediones)

Gastrointestinal

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

Hematologic

  • ↓ lymphocyte count

Endocrinologic

  • hypoglycemia (↑ with sulfonylureas)

Miscellaneous

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

Interactions

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.

Route/Dosage

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.

Availability

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)

Implementation

  • 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.

saxagliptin

(săk′sə-glĭp′tn)
n.
An oral hypoglycemic drug, C18H25N3O2, used to treat type 2 diabetes.
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References in periodicals archive ?
The dose of saxagliptin, an oral hypoglycemic agent, may need to be lowered to 2.
The investigation of saxagliptin is part of a broader investigation into the cardiovascular risk of all drugs for type 2 diabetes.
Sitagliptin (Januvia[R]), saxagliptin (Onglyza[R]) and linagliptin (Trajenta[R]) work by inhibiting the enzyme dipeptidyl peptidase IV (DPP-IV), which is responsible for the degradation of the endogenous hormone incretin (also known as glucagon-like peptide-1 or GLP-1).
Recommended dosage: The recommended dose of saxagliptin is 2.
Doctors believe Saxagliptin will improve the care of Type 2 diabetes sufferers.
The FDA statement said that although saxagliptin was "not associated with an increased risk for cardiovascular events in patients who were mainly at low risk for these events, the FDA is requiring a post-market study that will specifically evaluate cardiovascular safety in a higher risk population.
Cardiovascular safety data for the investigational diabetes drug saxagliptin are sufficient to rule out unacceptable excess risk in the population studied, but the manufacturer should conduct longer postmarketing studies in patients at higher risk for cardiovascular events, a federal advisory panel concluded.
Bristol-Myers Squibb Company (NYSE: BMY) and AstraZeneca (NYSE: AZN) today announced results up to 76-weeks from a Phase 3 study of ONGLYZA([TM])(saxagliptin) as initial combination therapy with metformin, which produced long-term glycemic improvement [as measured by glycosylated hemoglobin level (HbA1c)] in treatment-naove adults with type 2 diabetes mellitus inadequately controlled on diet and exercise compared to treatment with an investigational 10 mg dose of saxagliptin or metformin alone.
AstraZeneca today announced it will participate in the US Food and Drug Administration (FDA) Endocrinologic and Metabolic Drugs Advisory Committee meeting on 14 April 2015 to discuss the results of the Saxagliptin Assessment of Vascular Outcomes Recorded in Patients with Diabetes Mellitus (SAVOR) trial for ONGLYZAA (saxagliptin) and KombiglyzeA XR (saxagliptin and metformin HCI extended-release).
Drug Interactions: Because ketoconazole, a strong CYP 3A4/5 inhibitor, increased saxagliptin exposure, the dose of ONGLYZA should be limited to 2.
About the Study: Saxagliptin Added To Metformin Over 102 Weeks The study is an interim analysis of a 42-month long-term extension study designed to assess the safety, tolerability and efficacy of saxagliptin when added to metformin in people with inadequately controlled type 2 diabetes, compared to metformin plus placebo.