Drug Guide
Linagliptin and Metformin Hydrochloride
Classification
Therapeutic: Antidiabetic agent, combination for type 2 diabetes mellitus
Pharmacological: Dipeptidyl peptidase-4 (DPP-4) inhibitor and biguanide combined
FDA Approved Indications
- Adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus
Mechanism of Action
Linagliptin inhibits DPP-4, increasing incretin levels, which increase insulin secretion and decrease glucagon levels. Metformin decreases hepatic glucose production, decreases intestinal absorption of glucose, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization.
Dosage and Administration
Adult: Typically, one tablet once daily with meals, dosage may vary based on clinical response; physicians should adjust according to the patient's glycemic control.
Pediatric: Not approved for pediatric use.
Geriatric: Use with caution; dose adjustments may be necessary based on renal function.
Renal Impairment: Adjust dosage based on renal function; preferably not used if eGFR <30 mL/min/1.73 m².
Hepatic Impairment: Use with caution; contraindicated in hepatic disease or impairment.
Pharmacokinetics
Absorption: Both drugs are well absorbed orally.
Distribution: Linagliptin has extensive distribution with high protein binding; Metformin is not protein bound.
Metabolism: Linagliptin is minimally metabolized; Metformin is not metabolized and excreted unchanged.
Excretion: Renally excreted; dose adjustments needed for renal impairment.
Half Life: Linagliptin approximately 12 hours; Metformin about 4 to 8.7 hours.
Contraindications
- Severe renal impairment (eGFR <30 mL/min/1.73 m²)
- Acute or chronic metabolic acidosis, including diabetic ketoacidosis
Precautions
- History of pancreatitis, hepatic impairment, congestive heart failure, or lactic acidosis
Adverse Reactions - Common
- Genital candidiasis (Less common)
- Hypoglycemia (when used with other agents) (Relatively rare when used alone)
Adverse Reactions - Serious
- Lactic acidosis (Rare but serious)
- Pancreatitis (Rare)
Drug-Drug Interactions
- Other antihyperglycemic agents, drugs affecting renal function, drugs that affect CYP3A4.
Drug-Food Interactions
N/ADrug-Herb Interactions
N/ANursing Implications
Assessment: Monitor blood glucose levels; assess renal function regularly.
Diagnoses:
- Risk for unstable blood glucose levels
- Risk for lactic acidosis
Implementation: Administer with meals to reduce gastrointestinal side effects; monitor renal function periodically.
Evaluation: Evaluate blood glucose control and renal function; adjust therapy as necessary.
Patient/Family Teaching
- Take medication as prescribed, with meals.
- Report any signs of lactic acidosis (nausea, vomiting, abdominal pain, fatigue).
- Maintain a healthy diet and exercise routine.
- Monitor blood glucose levels regularly.
Special Considerations
Black Box Warnings:
- Lactic acidosis risk associated with metformin, especially in patients with renal impairment.
Genetic Factors: None specific.
Lab Test Interference: None known.
Overdose Management
Signs/Symptoms: Lactic acidosis, hypoglycemia in some cases.
Treatment: Discontinue medication immediately; provide supportive care; consider hemodialysis if indicated.
Storage and Handling
Storage: Store at room temperature away from moisture and heat.
Stability: Stable for shelf life specified by manufacturer.