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 once-daily dosing and favorable tolerability profile, Onglyza represents a rational choice for clinicians seeking to optimize glucose-lowering regimens while minimizing risks of weight gain and hypoglycemia.

Features

• Contains saxagliptin hydrochloride as the active pharmaceutical ingredient
• Available in 2.5 mg and 5 mg film-coated tablets
• Once-daily oral administration, with or without food
• Selective and reversible inhibition of DPP-4 enzyme
• Renal dosing adjustments available for impaired kidney function
• Manufactured under current Good Manufacturing Practices (cGMP)

Benefits

• Enhances glucose-dependent insulin secretion from pancreatic beta cells
• Suppresses glucagon secretion from pancreatic alpha cells, particularly in hyperglycemic states
• Low inherent risk of hypoglycemia when used as monotherapy
• Weight-neutral profile, supporting long-term adherence and metabolic goals
• Provides sustained HbA1c reduction as part of a comprehensive diabetes management plan
• Compatible with other antihyperglycemic agents, including metformin, sulfonylureas, and thiazolidinediones

Common use

Onglyza is commonly prescribed for adult patients with type 2 diabetes mellitus whose hyperglycemia remains inadequately controlled despite lifestyle modifications and/or other antihyperglycemic therapies. It is frequently utilized in combination regimens, particularly when additional glycemic control is needed without introducing significant risks of hypoglycemia or weight gain. Clinical scenarios often include its use after metformin monotherapy failure, as an alternative to sulfonylureas in patients prone to hypoglycemia, or as part of triple therapy in complex cases requiring multiple mechanisms of action.

Dosage and direction

The recommended dosage of Onglyza is 5 mg taken orally once daily, with or without food. For patients with moderate or severe renal impairment (creatinine clearance ≤50 mL/min) or with end-stage renal disease requiring hemodialysis, the dosage should be reduced to 2.5 mg once daily. Hemodialysis patients should administer Onglyza after the dialysis session. Tablets should be swallowed whole and not crushed, chewed, or split. Dosage adjustments may be necessary when used concomitantly with strong CYP3A4/5 inhibitors.

Precautions

Pancreatitis: Postmarketing reports indicate increased risk of acute pancreatitis; discontinue promptly if pancreatitis is suspected.
Hypersensitivity reactions: Cases of anaphylaxis, angioedema, and exfoliative skin conditions have been reported.
Hepatic impairment: Use with caution in patients with liver disease; monitor liver enzymes periodically.
Macrovascular outcomes: No clinical studies have established conclusive evidence of reduced macrovascular risk.
Renal impairment: Dose adjustment required as specified in dosing guidelines.
Concomitant insulin secretagogues: May require lower doses of secretagogues to reduce hypoglycemia risk.

Contraindications

History of serious hypersensitivity reactions to saxagliptin or any component of Onglyza formulations. This includes anaphylaxis, angioedema, or severe cutaneous adverse reactions. The presence of type 1 diabetes mellitus or diabetic ketoacidosis, as Onglyza is not indicated for these conditions. Concomitant use with alogliptin, linagliptin, sitagliptin, or vildagliptin is contraindicated due to therapeutic duplication.

Possible side effects

Common (≥5%): Upper respiratory tract infection, urinary tract infection, headache
Less common (1-5%): Peripheral edema, sinusitis, abdominal pain, gastroenteritis, vomiting
Rare (<1%): Acute pancreatitis, hepatic enzyme elevations, hypersensitivity reactions (including urticaria and facial edema)
Postmarketing reports: Severe joint pain, bullous pemphigoid, heart failure (particularly when used with thiazolidinediones)

Drug interaction

Strong CYP3A4/5 inhibitors (e.g., ketoconazole, clarithromycin): May increase saxagliptin exposure; reduce Onglyza dose to 2.5 mg daily.
Insulin secretagogues (e.g., sulfonylureas): Increased risk of hypoglycemia; consider lower secretagogue dose.
ACE inhibitors: Potential increased risk of angioedema, though causal relationship not established.
Other DPP-4 inhibitors: Contraindicated due to mechanism duplication.
No clinically significant interactions with metformin, pioglitazone, digoxin, simvastatin, or diltiazem observed in clinical studies.

Missed dose

If a dose of Onglyza is missed, it should be taken as soon as remembered on the same day. However, if the missed dose is not remembered until the following day, the patient should skip the missed dose and resume the regular dosing schedule. Do not double the dose to make up for a missed dose. Consistent daily administration is recommended to maintain stable DPP-4 inhibition and glycemic control.

Overdose

In the event of overdose, supportive measures should be initiated with regular monitoring of vital signs and clinical status. Reported overdoses up to 200 mg were associated with increased incidence of headache, dizziness, fatigue, and hypoglycemia. Hemodialysis may remove saxagliptin (approximately 23% removal over 4 hours), though clinical experience with dialysis in overdose is limited. There is no specific antidote for saxagliptin overdose; blood glucose monitoring and appropriate management of hypoglycemia are recommended.

Storage

Store Onglyza tablets 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 the original container with the lid tightly closed to protect from moisture. Dispense in original container with desiccant. Do not remove desiccant from the bottle. Keep out of reach of children and pets. Do not use beyond the expiration date printed on the 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 considering the use of Onglyza. Prescribing decisions must be based on the individual patient’s medical history, current medications, and overall clinical status. Please refer to the full prescribing information for complete details regarding indications, dosing, warnings, and precautions. Patients should not initiate or discontinue Onglyza without consulting their healthcare provider.

Reviews

Clinical trials demonstrate Onglyza 5 mg daily produces mean HbA1c reductions of 0.6-0.8% as monotherapy and 0.7-0.9% when added to metformin therapy. Extension studies show maintained efficacy over 102 weeks with sustained safety profile. Real-world evidence supports its utility in diverse patient populations, particularly those requiring renal dose adjustments. The cardiovascular outcomes trial (SAVOR-TIMI 53) showed saxagliptin did not increase or decrease major adverse cardiovascular events compared to placebo in patients with type 2 diabetes at high cardiovascular risk.