KOMBIGLYZETM XR(Saxagliptin and Metformin XR)沙格列汀和二甲双胍片 KOMBIGLYZE^TM XR

Indications and usage

KOMBIGLYZE XR is a dipeptidyl peptidase-4 inhibitor and a biguanide combination product indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus when treatment with both saxagliptin and metformin is appropriate;

Dosage forms and administration

Tablets: 2.5 mg saxagliptin/1000 mg metformin HCl extended-release, 5 mg saxagliptin/500 mg metformin HCl extended-release, 5 mg saxagliptin/1000 mg metforming HCl extended-release. Administer once daily with evening meal; swallow whole; starting dose based on patient’s current regimen then adjust the dose based on effectiveness and tolerability; limit saxagliptin dose to 2.5 mg daily for patients taking strong cytochrome P450 3A4/5 inhibitors.

Contraindications

Renal impairment; metabolic acidosis, including diabetic ketoacidosis; hypersensitivity to the active substance or to any of the excipients.

Warnings and precautions

• Lactic acidosis: warn patients against excessive alcohol intake;
• not recommended in hepatic impairment;
• temporarily discontinue in patients undergoing radiologic studies with intravascular administration of iodinated contrast materials;
• if pancreatitis is suspected, promptly discontinue;
• metformin might lower vitamin B₁₂ levels in patients with vitamin B₁₂ deficiency;
• when used with an insulin secretagogue or insulin, a lower dose of insulin scretagogue or insulin may be required to minimize risk of hypoglycemia.

Adverse reactions

• Adverse reactions reported in ≥ 5% of patients treated with metformin extended-release and more commonly than in patients treated with placebo are: diarrhea and nausea/vomiting;
• Adverse reactions reported in ≥ 5% of patients treated with saxagliptin and more commonly than in patients treated with placebo are: upper respiratory tract infection, urinary tract infection, and headache;
• Adverse reactions reported in ≥ 5% of treatment-naïve patients treated with coadministered saxagliptin and metform and more commonly than in patients treated with placebo are: headache and nasopharyngitis;
• hypoglycaemia when in combination with SU and insulin;
• hypersensitivity-related events were reported more commonly in patients treated with saxagliptin than in patients with placebo.

Drug interactions

Co-administration with and strong CYP3A4/5 inhibitors (e.g., ketoconazole) increases saxagliptin concentrations; cationic drugs eliminated by renal tubular secretion may reduce metformin elimination.

Use in specific populations

No data in pregnant women; should not be used in treatment of type 1 diabetes mellitus or diabetic ketoacdosis; safety and effective have not been established in children; has not been studied in patients with history of panreatitis.

KOMBIGLYZE XR is a trade mark of the AstraZeneca group of companies.