Meglitinide
Encyclopedia
Meglitinides, aka "Glinides", are a class of drugs used treat diabetes type 2.
They bind to an ATP
-dependent K
+ (KATP) channel on the cell membrane of pancreatic beta cell
s in a similar manner to sulfonylurea
s but at a separate binding site. This inhibits a tonic, hyperpolarizing outflux of potassium, which causes the electric potential over the membrane to become more positive. This depolarization
opens voltage-gated Ca
2+ channels. The rise in intracellular calcium leads to increased fusion of insulin
granulae with the cell membrane, and therefore increased secretion of (pro)insulin.
's repaglinide
(Prandin), which gained FDA approval in 1997. Another type of drug in this class is nateglinide
(Starlix).
These drugs should be taken 0-30 minutes prior to eating. Follow the instructions given to you by your health-care provider.
. While the potential for hypoglycemia is less than for those on sulfonylurea
s, it is still a serious potential side effect that can be life-threatening. Patients on this medication should know the signs and symptoms of hypoglycemia
and appropriate.
Repaglinide (Prandin) caused an increased incidence in male rats of benign adenomas (tumors) of the thyroid and liver. No such effect was seen with the other drug of its class nateglinide (Starlix).
http://www.accessdata.fda.gov/drugsatfda_docs/label/2010/020741s038lbl.pdf
http://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021204s011lbl.pdf
They bind to an ATP
Adenosine triphosphate
Adenosine-5'-triphosphate is a multifunctional nucleoside triphosphate used in cells as a coenzyme. It is often called the "molecular unit of currency" of intracellular energy transfer. ATP transports chemical energy within cells for metabolism...
-dependent K
Potassium
Potassium is the chemical element with the symbol K and atomic number 19. Elemental potassium is a soft silvery-white alkali metal that oxidizes rapidly in air and is very reactive with water, generating sufficient heat to ignite the hydrogen emitted in the reaction.Potassium and sodium are...
+ (KATP) channel on the cell membrane of pancreatic beta cell
Beta cell
Beta cells are a type of cell in the pancreas located in the so-called islets of Langerhans. They make up 65-80% of the cells in the islets.-Function:...
s in a similar manner to sulfonylurea
Sulfonylurea
Sulfonylurea derivatives are a class of antidiabetic drugs that are used in the management of diabetes mellitus type 2. They act by increasing insulin release from the beta cells in the pancreas.-First generation:* Carbutamide...
s but at a separate binding site. This inhibits a tonic, hyperpolarizing outflux of potassium, which causes the electric potential over the membrane to become more positive. This depolarization
Depolarization
In biology, depolarization is a change in a cell's membrane potential, making it more positive, or less negative. In neurons and some other cells, a large enough depolarization may result in an action potential...
opens voltage-gated Ca
Calcium
Calcium is the chemical element with the symbol Ca and atomic number 20. It has an atomic mass of 40.078 amu. Calcium is a soft gray alkaline earth metal, and is the fifth-most-abundant element by mass in the Earth's crust...
2+ channels. The rise in intracellular calcium leads to increased fusion of insulin
Insulin
Insulin is a hormone central to regulating carbohydrate and fat metabolism in the body. Insulin causes cells in the liver, muscle, and fat tissue to take up glucose from the blood, storing it as glycogen in the liver and muscle....
granulae with the cell membrane, and therefore increased secretion of (pro)insulin.
Drugs
The main branded drug in the meglitinide class is Novo NordiskNovo Nordisk
Novo Nordisk manufactures and markets pharmaceutical products and services. Created in 1989 through a merger of two Danish companies dating back to the 1920s, it has become one of the world's leading companies in diabetes care, where Novo Nordisk pursues research into pulmonary delivery systems;...
's repaglinide
Repaglinide
Repaglinide is for the treatment of type II diabetes. It is supplied by Novo Nordisk...
(Prandin), which gained FDA approval in 1997. Another type of drug in this class is nateglinide
Nateglinide
Nateglinide is a drug for the treatment of type 2 diabetes. Nateglinide was developed by Ajinomoto, a Japanese company and sold by the Swiss pharmaceutical company Novartis....
(Starlix).
These drugs should be taken 0-30 minutes prior to eating. Follow the instructions given to you by your health-care provider.
Side-effects
Side effects include weight gain and hypoglycemiaHypoglycemia
Hypoglycemia or hypoglycæmia is the medical term for a state produced by a lower than normal level of blood glucose. The term literally means "under-sweet blood"...
. While the potential for hypoglycemia is less than for those on sulfonylurea
Sulfonylurea
Sulfonylurea derivatives are a class of antidiabetic drugs that are used in the management of diabetes mellitus type 2. They act by increasing insulin release from the beta cells in the pancreas.-First generation:* Carbutamide...
s, it is still a serious potential side effect that can be life-threatening. Patients on this medication should know the signs and symptoms of hypoglycemia
Hypoglycemia
Hypoglycemia or hypoglycæmia is the medical term for a state produced by a lower than normal level of blood glucose. The term literally means "under-sweet blood"...
and appropriate.
Repaglinide (Prandin) caused an increased incidence in male rats of benign adenomas (tumors) of the thyroid and liver. No such effect was seen with the other drug of its class nateglinide (Starlix).
http://www.accessdata.fda.gov/drugsatfda_docs/label/2010/020741s038lbl.pdf
http://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021204s011lbl.pdf