Saxagliptin

Antidiabetic Drug

Drug class: Dipeptidyl peptidase-4 (DPP-4) inhibitor

Saxagliptin (ONGLYZA)（中文：沙格列汀）

Common Strengths of Saxagliptin Tablet

Saxagliptin tablets are available in the following strengths:

• 2.5 mg and 5 mg tablets

Drug Trade Names of Saxagliptin Tablet

Onglyza is the trade name for Saxagliptin

It is also sold under various brand names when combined with other antidiabetic medications, such as:

• KOMBIGLYZE XR TABLET 2.5MG/1000MG: Saxagliptin 2.5mg + Metformin 1000mg
• KOMBIGLYZE XR TABLET 5MG/1000MG: Saxagliptin 5mg + Metformin 1000mg
• KOMBIGLYZE XR TABLET 5MG/500MG: Saxagliptin 5mg + Metformin 500mg

Drug Usage

Treatment of type 2 diabetes mellitus in adults

Mechanism of Action

Inhibits DPP-4 enzyme, increasing levels of incretin hormones (GLP-1 and GIP) which stimulate insulin release and decrease glucagon secretion, thereby lowering blood glucose.

Route of Administration

Oral

Dosages

• 2.5 mg or 5 mg once daily
• No specific dosage adjustments for hypertension or heart failure
• Diabetic kidney disease:
  • eGFR >45 mL/min/1.73 m²: No dosage adjustment
  • eGFR ≤45 mL/min/1.73 m²: 2.5 mg once daily

Side Effects

Frequency	Adverse reactions
Common	Upper respiratory tract infection
	Urinary tract infection
	Headache
Uncommon	Hypoglycemia
	Dyslipidemia
	Gastroenteritis
	Pancreatitis
	Severe cutaneous adverse reactions

Pharmacokinetics

• Absorption
  • Saxagliptin is rapidly absorbed orally. Maximum inhibition of DPP-4 activity is seen approximately 2 hours after a saxagliptin dose.
• Metabolism
  • Saxagliptin is primarily metabolized by cytochrome P450 3A4/5 (CYP3A4/5).
• Elimination
  • 75% of the dose is excreted in urine and 22% in feces.
• Half-life
  • Approximately 2.5 hours
• Sustained effect
  • A single 2.5 mg dose of saxagliptin was associated with plasma DPP-4 activity inhibition of 50% at 24 hours, supporting a once-daily dosing schedule.

Drug Precautions

Pregnancy

Not recommended unless clearly necessary.

Breastfeeding

Not recommended.

Children and Elderly

Not approved for use in children, no dosage adjustment needed for the elderly.

Renal Impairment

Dose adjustment required for moderate to severe renal impairment.

Monitoring Requirements

• Regular blood glucose
• HbA1c
• Signs of pancreatitis

The main symptoms of pancreatitis include:

• Severe abdominal pain, typically in the upper abdomen, that may:
  • Feel worse after eating
  • Be sudden and intense in acute cases
• Nausea and vomiting
• Fever
• Rapid pulse/heart rate

Drug interactions

Strong CYP3A4/5 inhibitors and inducers can alter the pharmacokinetics of saxagliptin.

Strong CYP3A4/5 Inhibitors: Increase the plasma concentration of saxagliptin when taken together
Antifungals	Ketoconazole
	Itraconazole
Antivirals	Ritonavir
Antibiotics	Clarithromycin
	Telithromycin

Strong CYP3A4/5 Inducers: Decrease the plasma concentration of saxagliptin
Anticonvulsants	Carbamazepine
	Phenytoin
	Phenobarbital
Antibiotic	Rifampicin
Glucocorticoid	Dexamethasone

FAQ

How Should I Take the Tablet?

Take once daily with or without food, swallow whole

What Should I Avoid While Taking?

Alcohol consumption

What Happens if I Miss a Dose?

Take as soon as remembered, unless close to the next dose. Do not double dose.