Repaglinide: A Short Acting Secretagogue with Strategic Advantages
Category: Meglitinide analogue, Oral insulin secretagogue
Available brands: Eurepa and Novonorm 0.5mg, 1mg, 2mg
Indication: Type 2 Diabetes mellitus
Dosing (Oral): HbA1c <8%: 0.5mg and HbA1c >8%: 1-2mg upto 4times/day
Dosing in altered kidney function: CrCl <40ml/min, and on dialysis: 0.5mg OD; gradually increase to 0.5mg before each meal (up to 4 times/day)
Mechanism of action: Meglitinides bind to the sulfonylurea receptor-1 (SUR1) on the pancreatic β-cells, leading to the closure of ATP-sensitive potassium (K-ATP) channels which depolarizes the membrane and facilitates calcium entry through calcium channels thereby stimulating insulin secretion. Repaglinide induced insulin release is glucose-dependent.
Oral administration: Administer within 30 minutes before meals
Food Interactions: With food, repaglinide serum levels is decreased and taking it without eating may cause hypoglycemia.
Drug interactions: Antidiabetics, aspirin and quinolones increases the risk of hypoglycemia. Clopidogrel, statins and spironolactone increases repaglinide concentration and thiazides decreases repaglinide concentration.
Adverse reactions
- Headache
- Hypoglycemia
- Upper respiratory tract infection
- chest pain
- Diarrhea
- Back pain
- Arthralgia
Monitoring parameters: Monitor fasting blood glucose.
Advantages with Repaglinide over other antidiabetics
- It is a potent and lowers HbA1c and early-phase insulin release to lower PPG excursions.
- It has a very short half-life and duration of action allowing flexible meal schedules.
- Severe hypoglycemic episodes are less common with repaglinide compared to sulfonylureas.
- Causes less weight gain compared to sulfonylureas and glitazones.
- Preferred oral agent for diabetics with renal impairment due to its predominant hepatic elimination.
Reference
- Lexicomp drug reference
- Guardado-Mendoza R, Prioletta A & et al. The role of nateglinide and repaglinide, derivatives of meglitinide, in the treatment of type 2 diabetes mellitus. Arch Med Sci. 2013 Oct 31;9(5):936-43
- Mori K, EmotoM,& et al. Potential advantage of repaglinide monotherapy in glycemic control in patients with type 2 diabetes and severe renal impairment. ActaEndocrinol (Buchar). 2017 Apr-Jun;13(2):133-137.
- Moses R. A review of clinical experience with the prandial glucose regulator, repaglinide, in the treatment of type 2 diabetes. Expert OpinPharmacother. 2000 Dec;1(7):1455-67.
