Onglyza (saxagliptin) is a prescription medication indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. As a dipeptidyl peptidase-4 (DPP-4) inhibitor, it functions by enhancing the body’s innate ability to regulate blood sugar through the incretin system. This oral antihyperglycemic agent is designed for use as monotherapy or in combination with other glucose-lowering medications, including metformin, sulfonylureas, or thiazolidinediones, when glycemic targets are not achieved with lifestyle modifications and existing therapies alone. Its mechanism offers a targeted approach to managing postprandial and fasting glucose levels with a favorable tolerability profile.

Features

• Active ingredient: Saxagliptin hydrochloride
• Available in 2.5 mg and 5 mg film-coated tablets
• Once-daily dosing regimen
• DPP-4 enzyme inhibitor class
• Renal dosing adjustment available
• Not associated with weight gain in clinical trials
• Low risk of hypoglycemia when used as monotherapy

Benefits

• Enhances glucose-dependent insulin secretion from pancreatic beta cells
• Suppresses glucagon secretion from pancreatic alpha cells, particularly in hyperglycemic states
• Demonstrates significant reductions in HbA1c levels (average -0.5% to -0.8% in monotherapy)
• Provides 24-hour glycemic control with once-daily administration
• Offers flexible combination therapy options with other antidiabetic agents
• Maintains neutral effect on body weight in most patient populations

Common use

Onglyza is commonly prescribed for adult patients with type 2 diabetes mellitus who have not achieved adequate glycemic control through diet and exercise alone. It is frequently utilized as second-line therapy when metformin monotherapy proves insufficient or when metformin is contraindicated or not tolerated. The medication is particularly valuable for patients who require glycemic control without the risk of weight gain or significant hypoglycemia. Clinical studies have demonstrated its efficacy across various patient demographics, including elderly populations and those with mild to moderate renal impairment (with appropriate dose adjustment). It may be used as part of a comprehensive diabetes management strategy that includes regular glucose monitoring, dietary modifications, and physical activity.

Dosage and direction

The recommended dosage of Onglyza is 5 mg administered once daily, regardless of meals. For patients with moderate or severe renal impairment (creatinine clearance ≤50 mL/min) or end-stage renal disease requiring hemodialysis, the recommended dosage is 2.5 mg once daily. No dosage adjustment is required for patients with hepatic impairment. Tablets should be swallowed whole and not crushed, split, or chewed. Administration timing should be consistent day-to-day to maintain stable drug concentrations. When used in combination with a sulfonylurea, a lower dose of the sulfonylurea may be required to reduce the risk of hypoglycemia.

Precautions

Pancreatitis: Postmarketing reports indicate increased risk of acute pancreatitis. Discontinue promptly if pancreatitis is suspected.
Heart Failure: Increased risk of heart failure hospitalization was observed in clinical trials, particularly in patients with pre-existing cardiovascular disease or renal impairment.
Hypersensitivity Reactions: Serious hypersensitivity reactions including anaphylaxis, angioedema, and exfoliative skin conditions have been reported.
Hepatic Effects: Monitor liver function periodically as hepatic enzyme elevations have been observed.
Macrovascular Outcomes: No clinical studies have established conclusive evidence of macrovascular risk reduction with Onglyza or any other antidiabetic drug.
Renal Impairment: Dose adjustment required for patients with moderate to severe renal impairment.
Laboratory Tests: Periodic assessment of renal function and hematologic parameters recommended during therapy.

Contraindications

• History of serious hypersensitivity reaction to saxagliptin or any component of Onglyza formulations
• Patients with type 1 diabetes mellitus or for the treatment of diabetic ketoacidosis
• Concomitant use with strong CYP3A4/5 inhibitors (e.g., ketoconazole, clarithromycin) in patients with moderate to severe renal impairment
• Pediatric patients under 18 years of age (safety and effectiveness not established)
• Pregnancy unless potential benefit justifies potential risk to fetus (Category B)

Possible side effect

Common (≥5%): Upper respiratory tract infection, urinary tract infection, headache
Less common (1-5%): Peripheral edema, sinusitis, abdominal pain, vomiting, rash
Rare (<1%): Acute pancreatitis, hepatic enzyme elevations, severe joint pain, bullous pemphigoid
Serious but rare: Anaphylaxis, angioedema, severe hypersensitivity reactions, heart failure requiring hospitalization
Hypoglycemia: Incidence increases when used in combination with sulfonylureas or insulin

Drug interaction

Strong CYP3A4/5 inhibitors (e.g., ketoconazole, atazanavir, clarithromycin): May increase saxagliptin exposure—limit Onglyza dose to 2.5 mg daily
Inducers of CYP3A4/5 (e.g., rifampin): May decrease saxagliptin exposure—consider alternative therapy
Insulin secretagogues (e.g., sulfonylureas): Increased risk of hypoglycemia—may require dose reduction of secretagogue
Digoxin: Minimal interaction observed, but monitoring recommended during initiation or discontinuation
Other antidiabetic agents: Additive glycemic effects expected—appropriate monitoring advised

Missed dose

If a dose is missed, it should be taken as soon as remembered on the same day. However, if remembered near the time of the next scheduled dose, the missed dose should be skipped and the regular dosing schedule resumed. Patients should not take two doses of Onglyza on the same day to make up for a missed dose. Consistent daily administration is recommended to maintain optimal glycemic control. Healthcare providers should educate patients on establishing routine administration habits, such as associating dose timing with another daily activity.

Overdose

In clinical trials, doses up to 200 mg daily (40 times the recommended dose) for up to 2 weeks were not associated with significant clinical adverse events. No specific antidote for saxagliptin overdose is known. In the event of overdose, appropriate supportive treatment should be initiated according to the patient’s clinical presentation. Hemodialysis removed approximately 23% of the saxagliptin dose over 4 hours, suggesting hemodialysis may be partially effective in drug removal. Removal of the active metabolite by hemodialysis has not been studied. Contact poison control center for latest recommendations.

Storage

Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C to 30°C (59°F to 86°F). Keep container tightly closed and protect from moisture. Keep out of reach of children and pets. Do not use after expiration date printed on bottle. Tablets should be kept in their original container with the dessicant to maintain stability. Do not transfer to other containers unless specifically designed for medication storage. Protect from light and excessive humidity.

Disclaimer

This information is provided for educational purposes only and does not constitute medical advice. Onglyza is available by prescription only and should be used under the supervision of a qualified healthcare professional. Individual patient responses may vary. Healthcare providers should reference the full prescribing information for complete details regarding administration, warnings, and precautions. Patients should not alter their diabetes management regimen without consulting their healthcare provider. The safety and efficacy of Onglyza in pediatric patients have not been established.

Reviews

Clinical trials demonstrate Onglyza’s consistent efficacy in reducing HbA1c levels with once-daily dosing. The SAVOR-TIMI 53 trial, involving 16,492 patients with type 2 diabetes, showed significant glycemic control though with noted increased risk of heart failure hospitalization. Systematic reviews indicate saxagliptin provides comparable efficacy to other DPP-4 inhibitors with similar safety profiles. Real-world evidence supports its utility in diverse patient populations, particularly those requiring weight-neutral therapy or having renal impairment. Patient satisfaction surveys note convenience of once-daily dosing and generally favorable side effect profile compared to some other antidiabetic regimens.