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 diabetes alliance portfolio includes five medications across four different classes of medicines including Onglyza (saxagliptin), part of the innovative class of DPP-4 inhibitors, Komboglyze[TM] (saxagliptin and metformin HCl immediate-release), Byetta [sup.
Outside advisers to the FDA will consider the findings when they meet tomorrow to discuss whether the companies should be allowed to sell the drug, named Onglyza.
Branded agents vying for space in second-line treatment include the DPP-IV inhibitors Januvia (Merck's sitagliptin) and Onglyza (Bristol-Myers Squibb/AstraZeneca's saxagliptin), the PPAR-gamma agonist Actos (Takeda's pioglitazone), the GLP-1 analogues Byetta (Amylin/Eli Lilly's exenatide) and Victoza (Novo Nordisk's liraglutide), and the insulin analogues Lantus (Sanofi-Aventis's insulin glargine) and Levemir (Novo Nordisk's insulin detemir).
Insight and Analysis Provided AstraZeneca Byetta (exenatide) Onglyza (saxagliptin) Farxiga (dapagliflozin) Johnson & Johnson Invokana (canagliflozin) Merck & Co.
11 that it had requested these data from Bristol-Myers Squibb and AstraZeneca, the two companies that together market saxagliptin as Onglyza and Kombiglyze XR.
Onglyza received Marketing Authorisation in 2009 and is indicated in adult patients aged 18 years and older with type 2 diabetes mellitus to improve glycaemic control: in combination with metformin, when metformin alone, with diet and exercise, does not provide adequate glycaemic control; in combination with a sulphonylurea, when the sulphonylurea alone, with diet and exercise, does not provide adequate glycaemic control in patients for whom use of metformin is considered inappropriate; in combination with a thiazolidinedione, when the thiazolidinedione alone with diet and exercise, does not provide adequate glycaemic control in patients for whom use of a thiazolidinedione is considered appropriate.
Bristol-Myers Squibb/AstraZeneca's Onglyza (saxagliptin) will launch in South Korea and China by the end of 2011.
The topic of the Advisory Committee is based on an ongoing review of a previously submitted supplemental New Drug Application to the FDA for ONGLYZA and Kombiglyze XR.
ONGLYZA is indicated in adult patients with type 2 diabetes mellitus to improve glycaemic control in combination with metformin, sulphonylurea, or thiazolidinedione, when each treatment alone, with diet and exercise, does not provide adequate glycaemic control.
ONGLYZA has been submitted for regulatory approval in 93 countries and is approved in 77 countries including the US, Canada, Mexico, EU, India, Brazil and China.
Food and Drug Administration (FDA) that the Agency require a warning on the Onglyza label for a possible increased risk of heart failure in patients using the drug.
With the acquisition, AstraZeneca possess the intellectual property and global rights for the development, manufacture, and commercialization of BMS diabetes business, which comprises Onglyza (saxagliptin), Kombiglyze XR (saxagliptin and metformin HCl extended release), Komboglyze (saxagliptin and metformin HCl), dapagliflozin (marketed as Forxiga outside the US and Farxiga in the US), Xigduo (dapagliflozin and metformin HCl), Byetta (exenatide), Bydureon (exenatide extended-release for injectable suspension), metreleptin, and Symlin (pramlintide acetate).