How Do Meglitinide Derivatives Work?

Meglitinide derivatives are oral antidiabetic drugs used with a proper diet and exercise to control high blood sugar in people with type 2 diabetes mellitus (T2DM). T2DM is a long-term medical condition in which the body does not use the insulin normally and therefore cannot control the amount of sugar in the blood. Controlling high blood sugar helps prevent kidney damage, blindness, nerve problems, loss of limbs, and sexual function problems and may also lessen the risk of a heart attack or stroke.

Meglitinide derivatives are administered orally three times a day, 1 to 30 minutes before each meal.

Meglitinide derivatives work in the following ways:

• They work by triggering the release of insulin by the beta cells in the pancreas.
• Insulin is a natural substance that allows the body to metabolize sugar from the diet.
• Insulin secretion by pancreatic beta cells is partly controlled by cellular membrane potential regulated through an inverse relationship between the activity of cell membrane adenosine triphosphate (ATP)-sensitive potassium channels and extracellular glucose concentrations.
• Extracellular glucose enters the cell via glucose transporters 2. Once inside the cell, glucose is metabolized to produce ATP (source of energy for use and storage at the cellular level).
• They increase insulin release by inhibiting ATP-sensitive potassium channels that depolarize the beta cells, in turn opening calcium channels that result in the influx of calcium. Increased intracellular calcium induces insulin secretion.
• This can help to lower blood sugar levels, particularly after eating. 

Meglitinide derivatives are used as an adjunct to diet and exercise to improve glycemic control in adults with T2DM either as monotherapy or with metformin.

Some of the common side effects include:

• Diarrhea
• Nausea
• Vomiting
• Stomach upset/pain
• Muscle/joint pain
• Headache
• Weakness

Other rare side effects include:

• Upper respiratory tract infection
• Extreme hunger
• Joint pain or stiffness
• Tremors (an involuntary, rhythmic muscle contraction leading to shaking movements in one or more parts of the body)
• Muscle weakness
• Sinusitis (inflammation or swelling of the tissue lining the sinuses)
• Arthralgia (pain in joints)
• Weight gain
• Dizziness (feeling faint, weak, or unsteady)
• Hypoglycemia (low blood sugar level)
• Sudden sweating
• Fast heartbeat
• Blurred vision
• Tingling in hands/feet

Information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

Generic and brand names of meglitinide derivatives include:

• Nateglinide
• Prandin
• Repaglinide
• Starlix