Drug Guide
Repaglinide
Classification
Therapeutic: Antidiabetic agent
Pharmacological: Insulin secretagogue (meglitinide class)
FDA Approved Indications
- Management of type 2 diabetes mellitus to improve glycemic control
Mechanism of Action
Repaglinide stimulates rapid insulin release from pancreatic beta cells by closing ATP-dependent potassium channels, leading to cell depolarization and insulin secretion, thus lowering blood glucose levels.
Dosage and Administration
Adult: Initially 0.5 mg before each meal. Adjust based on response, up to 4 mg per dose.
Pediatric: Not recommended for pediatric use.
Geriatric: Start with lower dose due to potential for increased sensitivity. Monitor closely.
Renal Impairment: Use with caution; starting dose may be lower and titrated carefully.
Hepatic Impairment: Use with caution; dose adjustments may be necessary due to altered metabolism.
Pharmacokinetics
Absorption: Rapidly absorbed with peak concentrations in approximately 1 hour after dosing.
Distribution: Extensively plasma protein-bound.
Metabolism: Primarily metabolized in the liver via CYP3A4 and CYP2C8 pathways.
Excretion: Excreted mainly in feces; minimal renal excretion.
Half Life: Approximately 1 hour; however, its pharmacodynamic effect lasts longer due to insulin secretion.
Contraindications
- Type 1 diabetes mellitus
- Diabetic ketoacidosis
Precautions
- Use with caution in hepatic impairment, and in patients with a history of hypoglycemia. Monitor for hypoglycemia, especially in the elderly.
Adverse Reactions - Common
- Hypoglycemia (Common)
- Headache (Less common)
- Back pain (Less common)
Adverse Reactions - Serious
- Severe hypoglycemia (Rare)
- Allergic reactions (rash, urticaria, angioedema) (Rare)
Drug-Drug Interactions
- Carbamazepine (may decrease effectiveness)
- Gemfibrozil (may increase plasma levels)
- Certain antibiotics and antifungals that inhibit CYP3A4
Drug-Food Interactions
- Alcohol (can potentiate hypoglycemia)
Drug-Herb Interactions
N/ANursing Implications
Assessment: Monitor blood glucose regularly, especially in initial dose adjustment.
Diagnoses:
- Risk for hypoglycemia
- Ineffective tissue perfusion related to hypoglycemia
Implementation: Administer before meals; educate patients to recognize hypoglycemia symptoms.
Evaluation: Assess blood glucose levels to ensure adequate control and absence of hypoglycemia.
Patient/Family Teaching
- Take medication before meals as directed.
- Recognize symptoms of hypoglycemia and how to treat it.
- Maintain regular meal schedule.
- Avoid alcohol and excessive exercise without prior consultation.
Special Considerations
Black Box Warnings:
- None specific, but caution advised due to risk of hypoglycemia.
Genetic Factors: Variations in CYP2C8 may affect drug metabolism.
Lab Test Interference: May falsely elevate some laboratory tests, monitor blood glucose levels directly.
Overdose Management
Signs/Symptoms: Severe hypoglycemia, which can cause confusion, seizure, loss of consciousness, or coma.
Treatment: Administer glucose orally or intravenously; if drinking is possible, give fast-acting carbohydrate. In severe cases, administer glucagon or dextrose infusion under medical supervision.
Storage and Handling
Storage: Store at controlled room temperature, away from moisture and light.
Stability: Stable for designated shelf life when stored appropriately.