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Meglitinide Derivatives

Reviewed by: HU Medical Review Board | Last reviewed: August 2023

Meglitinide derivatives are a class of drugs used to treat people with type 2 diabetes (T2D). They work by triggering cells in the pancreas to release insulin. This helps lower blood sugar levels, especially after eating. Meglitinide derivatives are only useful if your pancreatic beta cells work.

Meglitinide derivatives are usually not the first treatment option for T2D. Your doctor may suggest them if lifestyle changes and other T2D drugs do not control blood sugar. Talk to your doctor about the benefits and risks of meglitinide derivatives.

How do meglitinide derivatives work?

Meglitinide derivatives work by activating “beta cells.” Beta cells are cells in the pancreas that make and release insulin. Meglitinide derivatives bind to proteins on the surface of the beta cells.1,2

This causes changes inside the beta cells that lead to higher calcium levels. Higher calcium levels help insulin granules inside the beta cells fuse more with the surface of those cells.1,2

More fusion with the cell surface increases insulin secretion. This can help lower blood sugar for people with T2D. It is especially useful for lowering blood sugar after you eat.1,2

Sulfonylureas also work like this. But meglitinide derivatives bind to different proteins on the surface of beta cells. Compared to sulfonylureas, meglitinide derivatives:1,3

  • Work as well
  • Work better at higher glucose levels
  • Work quicker but for less time
  • Are less likely to cause low blood sugar (hypoglycemia) or weight gain
  • Cost more


The FDA has approved 2 meglitinide derivatives to treat T2D:1

  • Repaglinide (Prandin®)
  • Nateglinide (Starlix®)

Repaglinide lowers blood sugar slightly better than nateglinide. Both work as well as metformin to reduce blood sugar.2

What are the possible side effects?

Side effects can vary depending on the specific drug you are taking. Common side effects of meglitinide derivatives include:2

  • Runny or stuffy nose
  • Infections of the upper respiratory tract
  • Headache
  • Joint pain
  • Nausea
  • Diarrhea
  • Back pain
  • Weight gain

Some serious side effects are possible. Talk to your doctor about how to spot these side effects. Also talk to your doctor about how to manage these side effects. One serious side effect to look out for is low blood sugar (hypoglycemia).2

These are not all the possible side effects of meglitinide derivatives. Talk to your doctor about what to expect when taking meglitinide derivatives. Call your doctor if you have any changes that concern you when taking meglitinide derivatives.

Other things to know

Before beginning treatment for T2D, tell your doctor about all your health conditions and any other drugs, vitamins, or supplements you take. This includes over-the-counter drugs.

Use meglitinide derivatives exactly as your doctor describes. You will usually take them by mouth as a tablet before each main meal. Your doctor may adjust your dose depending on how well they work.2

Meglitinide derivatives should be used with lifestyle changes, such as regular exercise and a healthy diet. Your doctor may also suggest combining them with other T2D drugs. Do not stop taking any medicines without talking to your doctor first.1

Before taking meglitinide derivatives, tell your doctor your full medical history. Other medicines you take or medical conditions you have may make meglitinide derivatives less safe. Talk to your doctor about:2

  • Other drugs you take, including over-the-counter drugs and supplements
  • Other medical conditions you have, especially liver or kidney disease
  • Any allergies
  • Pregnancy or planned pregnancy

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