Products
Nateglinide is commercially available in the form of film-coated tablets (Starlix, Starlix mite). It has been approved in many countries since 2000.
Structure and properties
Nateglinide (C19H27NO3, Mr = 317.42 g/mol) is a cyclohexane derivative of the amino acid phenylalanine. It is a white powder that is practically insoluble in water.
Effects
Nateglinide (ATC A10BX03) has antidiabetic and insulin secretagogue properties. It promotes endogenous insulin secretion from pancreatic beta cells, thereby lowering glucose levels after meals. The effects are due to the closure of the ATP-dependent potassium channels of the beta cell by binding to the SUR1 receptors. Unlike repaglinide and sulfonylureas, the duration of action is shorter.
Indications
For the treatment of patients with type 2 diabetes mellitus as monotherapy or combination therapy.
Dosage
According to the SmPC. The drug is taken within 1 to 30 minutes before main meals.
Contraindications
- Hypersensitivity
- Diabetes type 1
- Diabetic ketoacidosis
- Pregnancy and lactation
- Severe liver disease
Full precautions can be found in the drug label.
Interactions
Nateglinide is metabolized largely by CYP2C9 (70%) and to a lesser extent by CYP3A4 (30%). An increase in plasma concentrations is observed with concomitant administration of a CYP2C9 inhibitor such as sulfinpyrazone or fluconazole. Furthermore, numerous drugs have an effect on glucose levels.
Adverse effects
Possible adverse effects include hypoglycemia and, rarely, hypersensitivity reactions, elevation of liver enzyme levels, gastrointestinal discomfort, headache, and respiratory infections.
