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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 linagliptin
A10BD11
Forms & Strengths
- Tablet: 500 mg metformin hydrochloride / 2.5 mg linagliptin
- Tablet: 850 mg metformin hydrochloride / 2.5 mg linagliptin
- Tablet: 1000 mg metformin hydrochloride / 2.5 mg linagliptin
Adult Dosing
- Initial dose: One tablet twice daily, individualized based on current regimen, effectiveness, and tolerability
- Maximum recommended daily dose: 2000 mg metformin hydrochloride / 5 mg linagliptin
- Administer with meals to reduce gastrointestinal adverse reactions associated with metformin
Pediatric Dosing
- Safety and efficacy in pediatric patients below 18 years of age have not been established
Indications
- Adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus when treatment with both metformin and linagliptin is appropriate
Mechanism of Action
- Metformin: Decreases hepatic glucose production, decreases intestinal absorption of glucose, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization
- Linagliptin: Competitive inhibitor of dipeptidyl peptidase-4 (DPP-4), slowing the inactivation of incretin hormones GLP-1 and GIP, thereby increasing insulin synthesis/release and decreasing glucagon secretion in a glucose-dependent manner
Contraindications
- Severe renal impairment (eGFR below 30 mL/min/1.73m2) or end-stage renal disease
- Acute or chronic metabolic acidosis, including diabetic ketoacidosis
- History of a serious hypersensitivity reaction to linagliptin (e.g., anaphylaxis, angioedema, urticaria) or metformin
Adverse Reactions
- Diarrhea
- Nausea and vomiting
- Flatulence
- Asthenia
- Hypoglycemia (when used with insulin or insulin secretagogues)
- Pancreatitis
- Severe and disabling arthralgia
- Bullous pemphigoid
Drug Interactions
- Carbonic anhydrase inhibitors: May increase risk of lactic acidosis with metformin
- Cationic drugs eliminated by renal tubular secretion (e.g., cimetidine): May increase metformin concentration
- Strong P-glycoprotein or CYP3A4 inducers (e.g., rifampin): May decrease linagliptin efficacy
- Insulin and insulin secretagogues: Increased risk of hypoglycemia requiring dose reduction
Curated Content: Needs Vetting Before Put to Clinical Use