From the Guidelines
Prandin (repaglinide) works by stimulating insulin release from pancreatic beta cells to lower blood glucose levels, specifically by binding to ATP-dependent potassium channels on beta cell membranes, causing them to close, which leads to membrane depolarization, opening of calcium channels, and increased calcium influx into the cells, triggering insulin secretion. This mechanism of action is characteristic of the meglitinide class of medications, to which Prandin belongs 1. The medication's rapid onset and short duration of action make it particularly effective for controlling postprandial (after-meal) glucose spikes. Some key points about Prandin's use include:
- It should be taken immediately before meals to effectively reduce postprandial blood glucose 1
- It can be used separately or in combination with other antidiabetic medications, such as metformin, although combination therapy may increase the risk of hypoglycemia 1
- Common adverse effects include hypoglycemia and weight gain, but the risk and degree of hypoglycemia are lower with glinides than with sulfonylureas 1
- Prandin can be used in patients with renal insufficiency, making it a versatile option for managing type 2 diabetes in various patient populations 1.
From the FDA Drug Label
Repaglinide lowers blood glucose levels by stimulating the release of insulin from the pancreas. This action is dependent upon functioning beta (ß) cells in the pancreatic islets. Insulin release is glucose-dependent and diminishes at low glucose concentrations Repaglinide closes ATP-dependent potassium channels in the ß-cell membrane by binding at characterizable sites. This potassium channel blockade depolarizes the ß-cell, which leads to an opening of calcium channels. The resulting increased calcium influx induces insulin secretion.
The mechanism of action (MOA) of Prandin (repaglinide) is to stimulate insulin release from the pancreas by:
- Closing ATP-dependent potassium channels in the ß-cell membrane
- Depolarizing the ß-cell, leading to an opening of calcium channels
- Increasing calcium influx, which induces insulin secretion 2
From the Research
Mechanism of Action of Prandin
- Prandin, also known as repaglinide, is a rapid-acting insulin secretagogue that lowers postprandial glucose excursions by targeting early-phase insulin release 3, 4, 5.
- It stimulates insulin secretion from pancreatic beta-cells by closing ATP-dependent potassium channels on the cell membrane of beta-cells 6.
- Repaglinide has a distinct binding site at the beta-cell membrane, which differs from that of sulfonylureas, and corresponds to greater insulinotropic effects with repaglinide than with glibenclamide and/or glimepiride 5.
Therapeutic Use of Prandin
- Prandin is used to improve glycemic control in adults with type 2 diabetes mellitus, and can be used as monotherapy or in combination with other oral antidiabetic agents, such as metformin 3, 4, 7, 6.
- It is typically administered before meals to reduce postprandial glucose levels and improve HbA1c levels 3, 4, 6.
- Prandin has been shown to be effective in reducing postprandial glucose excursions and improving glycemic control in patients with type 2 diabetes, with a reduced risk of hypoglycemia compared to sulfonylureas 3, 4, 5.
Combination Therapy with Metformin
- The combination of repaglinide and metformin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus 6.
- This combination therapy has been demonstrated to be safe and effective in the treatment of type 2 diabetes, and can be used when monotherapy with oral antidiabetic agents fails 6.
- The combination of repaglinide and metformin targets two main defects in type 2 diabetes: insulin resistance and impaired insulin secretion 6.