Overview
Repaglinide is a meglitinide-class oral antidiabetic agent used as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. It stimulates insulin secretion from pancreatic beta cells in a glucose-dependent manner, primarily reducing postprandial hyperglycemia. It should not be used in type 1 diabetes or for diabetic ketoacidosis.
Mechanism of Action
Repaglinide is a meglitinide derivative that lowers blood glucose by stimulating insulin release from pancreatic beta cells. It binds to ATP-sensitive potassium channels on beta cell membranes, leading to channel closure, membrane depolarization, calcium influx, and subsequent insulin secretion. This action is glucose-dependent, with minimal effect at low glucose concentrations.
Indications
- Adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus
Common Doses
- 0.5 mg
- 1 mg
- 2 mg
Dosage
Typically administered 15-30 minutes before meals, 2-4 times daily depending on meal patterns. Starting dose is usually 0.5-2 mg before each meal, with maximum recommended dose of 16 mg per day. Dose should be individualized based on glycemic response and adjusted at 1-2 week intervals.
Black Box Warning
Black box warning: Concomitant use with gemfibrozil is contraindicated due to 8.1-fold increase in repaglinide exposure and severe hypoglycemia risk
Contraindications
- Concomitant use with gemfibrozil
- Known hypersensitivity to repaglinide or any inactive ingredients
- Type 1 diabetes mellitus
- Diabetic ketoacidosis
Side Effects
- Hypoglycemia
- Upper respiratory tract infection
- Headache
- Arthralgia
- Back pain
- Diarrhea
- Constipation
- Nausea
- Weight gain
Interactions
- Gemfibrozil: Contraindicated - 8.1-fold increase in repaglinide exposure
- Clopidogrel: Avoid concomitant use - 3.9-5.1-fold increase in exposure
- Cyclosporine: Limit maximum dose to 6 mg daily
- CYP2C8 inhibitors (trimethoprim, montelukast, deferasirox): May require dose reduction
- CYP3A4 inhibitors (ketoconazole, itraconazole, clarithromycin, erythromycin): May require dose reduction
- CYP inducers (rifampin, barbiturates, carbamazepine): May require dose increase
- Other antidiabetic agents: Increased hypoglycemia risk
- Beta-blockers, clonidine: May mask hypoglycemia symptoms
Counseling Points
- Take 15-30 minutes before meals
- Skip dose if meal is skipped
- Monitor blood glucose regularly
- Recognize symptoms of hypoglycemia (sweating, dizziness, confusion)
- Carry glucose source for hypoglycemia treatment
- Inform healthcare providers of all medications
- Maintain regular meal patterns and exercise
- Avoid alcohol which can increase hypoglycemia risk