Classes
DEA Class; Rx
Common Brand Names; Kombiglyze XR
- Antidiabetics, Biguanides/Dipeptyl Peptidase-IV Inhibitors
Description
Oral combination of a biguanide (metformin) and a dipeptidy-peptidase-4 (DPP-4) inhibitor (saxagliptin)
Used in adults for the treatment of type 2 diabetes mellitus
Per boxed warning the risk of lactic acidosis due to metformin requires care in prescribing and monitoring
Indications
Indicated as adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus who are already treated with sitagliptin or metformin and have inadequate glycemic control on sitagliptin or metformin alone
Individualize starting dose based on patient’s current regimen
Contraindications
History of serious hypersensitivity (eg, anaphylaxis, angioedema, exfoliative skin conditions)
Severe renal disease: eGFR <30 ml/min/1.73 m²
Acute or chronic metabolic acidosis, including diabetic ketoacidosis (should be treated with insulin)
Adverse Effects
Diarrhea (9.6%)
Nausea/vomiting (6.5%)
Headache (6.5%)
Hypoglycemia, saxagliptin (1.6%)
Rash
Lymphopenia
Saxagliptin
- Hypersensitivity reactions including anaphylaxis, angioedema, and exfoliative skin conditions
- Pancreatitis
- Severe and disabling arthralgia
- Bullous pemphigoid
- Rhabdomyolysis
Metformin
- Cholestatic, hepatocellular, and mixed hepatocellular liver injury
Warnings
Gradual increase of metformin dose may reduce GI side effects
Metformin may decrease serum vitamin B12 concentration
Do not exceed saxagliptin 2.5 mg/day when coadministered with strong cytochrome P450 3A4/5 (CYP3A4/5) inhibitors (eg, ketoconazole, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin)
Coadministration of saxagliptin with thiazolidinediones (eg, rosiglitazone, pioglitazone) increases risk for peripheral edema
Inactive tablet ingredients (ie, ghost tablet) may be eliminated in the feces as a soft, hydrated mass
Pancreatitis reported with saxagliptin; monitor for signs and symptoms and discontinue if pancreatitis suspected
Serious hypersensitivity reactions with saxagliptin reported (typically within the first 3 months of therapy)
Caution with history of angioedema
Severe and disabling arthralgia reported in patients taking DPP-4 inhibitors; consider as a possible cause for severe joint pain and discontinue drug if appropriate
Pregnancy and Lactation
Limited available data in pregnant women are not sufficient to determine drug-associated risk for major birth defects and miscarriage
There is no information regarding presence of metformin or alogliptin in human milk, effects on breastfed infant, or effects on milk production
Maximum Dosage
2000 mg/day PO metformin; 5 mg/day PO saxagliptin.
2000 mg/day PO metformin; 5 mg/day PO saxagliptin.
Safety and efficacy have not been established.
Safety and efficacy have not been established.
Safety and efficacy have not been established.
Safety and efficacy have not been established.
How supplied
Saxagliptin/metformin
tablet, extended-release
- 5mg/500mg
- 2.5mg/1000mg
- 5mg/1000mg