Nurses Compass
Drug Guide
Linagliptin
Classification
Therapeutic: Antidiabetic agent
Pharmacological: Dipeptidyl peptidase-4 (DPP-4) inhibitor
FDA Approved Indications
- Adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus
Mechanism of Action
Linagliptin inhibits the enzyme DPP-4, increasing levels of incretin hormones, which increase insulin synthesis and release from pancreatic beta cells and decrease glucagon secretion from pancreatic alpha cells, thereby improving glycemic control.
Dosage and Administration
Adult: 5 mg once daily, with or without food
Pediatric: Not approved for pediatric use
Geriatric: No dose adjustment required based on age alone, but monitor renal function
Renal Impairment: No initial dose adjustment needed, but use caution in renal impairment; dose is not recommended in severe renal impairment or ESRD with dialysis
Hepatic Impairment: No dose adjustment recommended for mild to moderate hepatic impairment
Pharmacokinetics
Absorption: Rapidly absorbed, Tmax approximately 1-2 hours
Distribution: High protein binding (~99%)
Metabolism: Minimally metabolized, predominantly excreted unchanged
Excretion: Primarily excreted via the enterohepatic system and feces; minimal urinary excretion (~5%)
Half Life: Approximately 12 hours
Contraindications
- Hypersensitivity to linagliptin or any component
Precautions
- Use with caution in patients with a history of pancreatitis; monitor for pancreatitis symptoms; caution in renal impairment, severe hepatic impairment
Adverse Reactions - Common
- Genital mycotic infections (Uncommon)
- Headache (Uncommon)
- URI symptoms (Uncommon)
Adverse Reactions - Serious
- Pancreatitis (Rare)
- Allergic reactions including anaphylaxis or angioedema (Rare)
Drug-Drug Interactions
- CYP3A4 inhibitors may increase linagliptin levels, but clinical significance is low.
- Other antidiabetic agents may increase hypoglycemia risk
Drug-Food Interactions
- No significant interactions reported
Drug-Herb Interactions
- Limited data, caution advised with herbal supplements
Nursing Implications
Assessment: Monitor blood glucose levels regularly; assess for signs of pancreatitis; check baseline renal and hepatic function.
Diagnoses:
- Risk for unstable blood glucose levels
- Risk for pancreatitis
Implementation: Administer once daily; advise patients to report symptoms of pancreatitis or allergic reactions; educate about hypoglycemia when used with insulin or sulfonylureas.
Evaluation: Blood glucose control goals achieved; no adverse effects observed.
Patient/Family Teaching
- Take medication as prescribed daily, with or without food
- Report symptoms of pancreatitis (severe abdominal pain, nausea, vomiting) or allergic reactions
- Maintain a balanced diet and exercise regimen
- Monitor blood glucose as advised
Special Considerations
Black Box Warnings:
- None currently
Genetic Factors: No specific genetic testing required
Lab Test Interference: May affect some laboratory measurements related to glucose or pancreatic function
Overdose Management
Signs/Symptoms: Hypoglycemia or gastrointestinal symptoms
Treatment: Supportive care; no specific antidote; consider activated charcoal if ingestion recent; monitor blood glucose and provide glucose as needed.
Storage and Handling
Storage: Store at room temperature, 20°C to 25°C (68°F to 77°F)
Stability: Stable when stored properly; discard after expiration.