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ALIMENTARY TRACT AND METABOLISM › DRUGS USED IN DIABETES › BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS › Combinations of oral blood glucose lowering drugs
metformin and alogliptin
A10BD13
Forms & Strengths
- Fixed-dose combination tablet: 12.5 mg alogliptin / 500 mg metformin hydrochloride
- Fixed-dose combination tablet: 12.5 mg alogliptin / 850 mg metformin hydrochloride
- Fixed-dose combination tablet: 12.5 mg alogliptin / 1000 mg metformin hydrochloride
Adult Dosing
- Type 2 diabetes mellitus: One tablet twice daily with meals
- Maximum recommended daily dose: 25 mg alogliptin / 2000 mg metformin hydrochloride
- Titrate dose gradually to reduce gastrointestinal side effects associated with metformin
- Renal adjustment: Contraindicated if eGFR is below 30 mL/min/1.73m2; not recommended to initiate if eGFR is 30-45 mL/min/1.73m2
Pediatric Dosing
- Safety and efficacy have not been established in pediatric patients below 18 years of age
Indications
- Adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus when treatment with both alogliptin and metformin is appropriate
Mechanism of Action
- Alogliptin is a selective dipeptidyl peptidase-4 (DPP-4) inhibitor that slows inactivation of incretin hormones GLP-1 and GIP
- Metformin decreases hepatic glucose production, decreases intestinal absorption of glucose, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization
Contraindications
- Severe renal impairment (eGFR < 30 mL/min/1.73m2) or end-stage renal disease
- Acute or chronic metabolic acidosis, including diabetic ketoacidosis, with or without coma
- History of a serious hypersensitivity reaction to alogliptin or metformin, such as anaphylaxis, angioedema, or severe cutaneous adverse reactions
- History of serious hypersensitivity reaction to any DPP-4 inhibitor
Adverse Reactions
- Nasopharyngitis
- Upper respiratory tract infection
- Headache
- Diarrhea
- Nausea and vomiting
- Hypoglycemia (when used with insulin or insulin secretagogues)
- Acute pancreatitis
- Severe and disabling arthralgia
- Hepatic enzyme elevations and rare cases of hepatic failure
Drug Interactions
- Cationic drugs eliminated by renal tubular secretion (e.g., amiloride, digoxin, morphine, quinidine, quinine, ranitidine, triamterene, trimethoprim, vancomycin) may increase metformin concentration
- Carbonic anhydrase inhibitors (e.g., topiramate, zonisamide, acetazolamide) frequently cause a drop in serum bicarbonate and induce non-anion gap, hyperchloremic metabolic acidosis, increasing risk of lactic acidosis
- Strong CYP3A4/5 inducers or inhibitors generally have minimal effect on alogliptin pharmacokinetics
- Insulin and insulin secretagogues (e.g., sulfonylureas) increase the risk of hypoglycemia, necessitating lower doses of the secretagogue or insulin
Curated Content: Needs Vetting Before Put to Clinical Use