Products
Glinides are commercially available in tablet form. Repaglinide (NovoNorm, USA: 1997) was the first to be approved in many countries in 1999, and nateglinide (Starlix) was approved a year later in 2000.
Structure and properties
The glinides differ structurally from the sulfonylureas. They are also referred to as meglitinide analogs. Repaglinide is a carbamoylmethylbenzoic acid derivative. Nateglinide is a cyclohexane derivative of the amino acid phenylalanine.
Effects
The glinides (ATC A10BX) have blood glucose-lowering properties. They promote insulin secretion from pancreatic beta cells. The prerequisite for efficacy is existing endogenous insulin production. Glinides have a short half-life. Like the sulfonylureas, the glinides block the ATP-dependent potassium channels of the beta cell membrane. This leads to a depolarization of the membrane and thus to an opening of the calcium channels. The resulting increased calcium influx induces insulin secretion from the beta cell.
Indications
For the treatment of type 2 diabetes mellitus (type 2 diabetes).
Dosage
According to the SmPC. Tablets are taken within 30 minutes before main meals.
Active ingredients
Two active ingredients are approved in many countries:
- Repaglinide (NovoNorm, generics).
- Nateglinide (Starlix)
Mitiglinide is not registered in many countries.
Contraindications
Contraindications include (selection):
- Hypersensitivity
- Type 1 diabetes
- Diabetic ketoacidosis
- Pregnancy and lactation
Full precautions can be found in the drug label.
Adverse effects
The most common possible adverse effects include hypoglycemia and gastrointestinal symptoms such as abdominal pain and diarrhea.
