Onglyza (saxagliptin) is a selective dipeptidyl peptidase-4 (DPP-4) inhibitor indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. It functions by enhancing the body’s innate ability to regulate blood glucose through the incretin system, offering a targeted mechanism that complements existing therapeutic strategies. With its favorable pharmacokinetic profile and once-daily dosing, Onglyza provides clinicians with an effective option for managing hyperglycemia while minimizing certain traditional risks associated with antidiabetic therapies.

Features

• Active ingredient: Saxagliptin (as hydrochloride)
• Pharmacologic class: Dipeptidyl peptidase-4 (DPP-4) inhibitor
• Available strengths: 2.5 mg and 5 mg film-coated tablets
• Administration: Oral, once daily
• Half-life: Approximately 2.5 hours for saxagliptin and 3.1 hours for its active metabolite
• Metabolism: Primarily hepatic via CYP3A4/5
• Excretion: Renal (75%) and fecal (22%)
• FDA-approved: 2009

Benefits

• Enhances glucose-dependent insulin secretion from pancreatic beta cells
• Suppresses glucagon secretion from pancreatic alpha cells
• Demonstrates weight-neutral properties in clinical studies
• Low risk of hypoglycemia when used as monotherapy
• Provides complementary efficacy when combined with metformin, sulfonylureas, or thiazolidinediones
• Offers once-daily dosing convenience with or without food

Common use

Onglyza is primarily prescribed for the management of type 2 diabetes mellitus in adults. It is used as monotherapy or in combination with other antidiabetic agents including metformin, sulfonylureas, thiazolidinediones, and insulin when glycemic control is not achieved with single-agent therapy. The medication is particularly valuable for patients who require additional glycemic control without weight gain or significant hypoglycemia risk. Clinical studies have demonstrated its efficacy across various patient populations, including those with renal impairment (with appropriate dosage adjustment).

Dosage and direction

The recommended dosage of Onglyza is 5 mg once daily, administered orally with or without food. For patients with moderate to 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. Onglyza may be taken at any time of day, but consistency in dosing time is recommended to maintain stable drug levels.

Precautions

Pancreatitis: Postmarketing reports indicate increased risk of acute pancreatitis. Discontinue promptly if pancreatitis is suspected.
Heart Failure: Increased risk of heart failure hospitalization observed in clinical trials, particularly in patients with history of heart failure or renal impairment.
Hypersensitivity Reactions: Serious hypersensitivity reactions including anaphylaxis, angioedema, and exfoliative skin conditions have been reported.
Hepatic Effects: Monitor liver function periodically; rare cases of hepatic dysfunction have been observed.
Macrovascular Outcomes: No clinical studies have established conclusive evidence of macrovascular risk reduction with Onglyza or any other antidiabetic drug.

Contraindications

• History of serious hypersensitivity reaction to saxagliptin or any component of Onglyza tablets
• Patients with type 1 diabetes mellitus or for the treatment of diabetic ketoacidosis
• Concomitant use with strong CYP3A4/5 inhibitors in patients with moderate to severe renal impairment
• Not recommended during pregnancy unless potential benefit justifies potential risk to fetus

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, heart failure, hepatic enzyme elevations, severe joint pain, bullous pemphigoid
Hypoglycemia: Incidence increases when used in combination with sulfonylureas or insulin

Drug interaction

Strong CYP3A4/5 inhibitors (e.g., ketoconazole, clarithromycin): Reduce Onglyza dose to 2.5 mg daily
Insulin secretagogues (e.g., sulfonylureas): May require lower dose of secretagogue to reduce hypoglycemia risk
Other DPP-4 inhibitors: Concurrent use not recommended
ACE inhibitors: Potential interaction requiring blood pressure monitoring
No clinically significant interactions with metformin, pioglitazone, digoxin, simvastatin, or diltiazem observed

Missed dose

If a dose is missed, it should be taken as soon as remembered on the same day. However, if remembered on the following day, 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 important for maintaining optimal glycemic control.

Overdose

In the event of overdose, appropriate supportive measures should be initiated. Hemodialysis may be effective (removes approximately 23% of saxagliptin over 4 hours). During clinical trials, doses up to 400 mg daily for 2 weeks were administered and were generally well-tolerated without dose-related clinical adverse reactions. No specific antidote exists. Symptomatic treatment and monitoring of blood glucose levels are recommended, with particular attention to potential hypoglycemia if taken with other antidiabetic medications.

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 in original container with desiccant to protect from moisture. Keep tightly closed and protect from light. Do not remove desiccant from bottle. Keep out of reach of children and pets. Do not use after expiration date printed on packaging.

Disclaimer

This information is provided for educational purposes only and does not constitute medical advice. Healthcare professionals should exercise their own professional judgment when treating patients. Patients should not make changes to their medication regimen without consulting their healthcare provider. Full prescribing information including boxed warnings should be reviewed before initiating therapy. Individual patient response may vary based on clinical circumstances and concomitant conditions.

Reviews

Clinical trials demonstrate Onglyza 5 mg daily produced significant HbA1c reductions ranging from 0.7% to 0.9% as monotherapy and 0.6% to 0.9% in combination therapy. The medication shows consistent efficacy across various demographic subgroups including elderly patients and those with renal impairment (with appropriate dosing). Real-world evidence supports maintained efficacy over 2 years of treatment with favorable tolerability profile. Healthcare providers report particular satisfaction with its weight-neutral effects and low hypoglycemia risk compared to some other antidiabetic classes.