Generic
Repaglinide
23 brands available in the market
At a glance
Repaglinide is a meglitinide analog used as an adjunct to diet and exercise to lower blood glucose in patients with type 2 diabetes mellitus. It stimulates insulin release from pancreatic beta-cells with rapid onset and rapid elimination.
Description
Repaglinide binds to specific receptors on pancreatic beta-cell membranes, closing ATP-dependent K+ channels and causing cell membrane depolarization, which increases Ca²⁺ influx and stimulates insulin secretion. It has rapid onset and rapid elimination, helping control postprandial glucose spikes.
Indications
- Type 2 diabetes mellitus (not controlled by diet and exercise alone)
- In combination with metformin (when not controlled by either agent alone)
Therapeutic class
Meglitinide Analogues
Pharmacological class
Insulin Secretagogue (Meglitinide)
Pharmacology
Repaglinide closes ATP-dependent K+ channels on pancreatic beta-cells, causing depolarization, increased Ca²⁺ influx, and insulin secretion. It has rapid onset and rapid elimination, helping control glucose spikes associated with meals.
Mechanism of action
Lowers blood sugar by stimulating insulin release from pancreatic beta-cells.
Dosage
Adult Dose (Oral):
- No prior treatment or HbA1c <8%: 0.5 mg before each meal
- Prior treatment or HbA1c >8%: 1-2 mg before each meal
- Take immediately or up to 30 minutes before each meal
- Adjust dose at 1-2 week intervals; single dose max 4 mg; max 16 mg/day
- Hepatic impairment: May require longer intervals between adjustments
- Renal impairment (CrCl 20-40): 0.5 mg with meals; titrate slowly
Administration
- Take 15-30 minutes before meals
- Swallow tablet whole; do not chew, crush, or break
- Skip the dose if a meal is skipped
Missed dose
If you miss a dose, skip it and continue with your normal schedule; do not double the dose.
Side effects
Common Side Effects:
- Hypoglycemia (low blood sugar)
- Upper respiratory tract infection
- Diarrhea
- Constipation
- Nausea
- Vomiting
- Joint pain
- Dizziness
- Back pain
Precautions & warnings
- May affect driving ability (hypoglycemia or hyperglycemia)
- Risk of hypoglycemia: delayed/missed meals, alcohol, other antidiabetic medications
- Carry sugar or fruit juice
- Caution in liver and kidney disease
Contraindications
- Diabetic ketoacidosis
- Severe hepatic impairment
- Type 1 diabetes
- Pregnancy
- Lactation
- Hypersensitivity to repaglinide or any ingredient
Drug interactions
- CYP3A4 inducers (rifampicin, barbiturates, carbamazepine): Increased repaglinide metabolism
- NSAIDs, salicylates, sulphonamides, phenylbutazone, oral anticoagulants, hydantoins: Potentiated action
- Ketoconazole, fluconazole, itraconazole, erythromycin: Increased plasma concentrations
- Gemfibrozil: Enhanced and prolonged glucose-lowering effect
- Potentially fatal: Increased risk of myocardial infarction with isophane insulin
Food interactions
Alcohol consumption with Repaglinide is unsafe.
Use in pregnancy
Use in Pregnancy: May be unsafe during pregnancy; animal studies have shown harmful effects; use only if clearly needed.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Probably safe; limited human data suggests no significant risk; monitor breastfed baby's blood sugar.
Pediatric use
Safety and efficacy not established in pediatric patients.
Geriatric use
Caution required in elderly patients; dose adjustment may be needed.
Renal / hepatic impairment
Renal Impairment: Caution in severe kidney disease; CrCl 20-40: 0.5 mg with meals; titrate slowly; CrCl <20: data not available; consult your doctor.
Hepatic Impairment: Caution in liver disease; may require longer intervals between adjustments; not recommended in severe liver disease; consult your doctor.
Overdose effects
Overdose (up to 80 mg): Few adverse effects other than lowering of blood glucose; hypoglycemia did not occur when meals were given; severe hypoglycemic reactions (coma, seizure) are infrequent; treatment: glucose administration, symptomatic supportive care.
Storage conditions
Do not store above 30°C; keep away from light; keep out of reach of children.
Chemical structure
Repaglinide