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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.

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

saxagliptin

(săk′sə-glĭp′tn)
n.
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.
References in periodicals archive
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.
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.
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