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:: Health Conditions - Diabetes - Nateglinide (Starlix)

Nateglinide

diabetes support

Nateglinide (Starlix) is an oral antidiabetic agent is used alone or in combination with other medications to treat type 2 (non-insulin-dependent) diabetes (formerly called 'adult-onset') in people whose diabetes cannot be controlled by diet and exercise alone. Nateglinide belongs to a class of drugs called meglitinides. Nateglinide helps your body regulate the amount of glucose (sugar) in your blood. It decreases the amount of glucose by stimulating the pancreas to release insulin.

 

Starlix® (generic name: Nateglinide) is an oral antidiabetic agent used in the management of Type 2 diabetes mellitus [also known as non-insulin dependent diabetes mellitus (NIDDM) or adult-onset diabetes]. Starlix, (-)-N-[(trans-4-isopropylcyclohexane)carbonyl]-D-phenylalanine, is structurally unrelated to the oral sulfonylurea insulin secretagogues.
Nateglinide is a white powder with a molecular weight of 317.43. It is freely soluble in methanol, ethanol, and chloroform, soluble in ether, sparingly soluble in acetonitrile and octanol, and practically insoluble in water. Starlix biconvex tablets contain 60 mg, or 120 mg, of nateglinide for oral administration.


Inactive Ingredients:

Colloidal silicon dioxide, croscarmellose sodium, hydroxypropyl methylcellulose, iron oxides (red or yellow), lactose monohydrate, magnesium stearate, microcrystalline cellulose, polyethylene glycol, povidone, talc, and titanium dioxide.

Mechanism of action

Nateglinide
is an amino-acid derivative that lowers blood glucose levels by stimulating insulin secretion from the pancreas. This action is dependent upon functioning beta-cells in the pancreatic islets. Nateglinide interacts with the ATP-sensitive potassium (K+ ATP ) channel on pancreatic beta-cells. The subsequent depolarization of the beta cell opens the calcium channel, producing calcium influx and insulin secretion. The extent of insulin release is glucose dependent and diminishes at low glucose levels. Nateglinide is highly tissue selective with low affinity for heart and skeletal muscle.

Metabolism

Nateglinide
is metabolized by the mixed-function oxidase system prior to elimination. The major routes of metabolism are hydroxylation followed by glucuronide conjugation. The major metabolites are less potent antidiabetic agents than nateglinide. The isoprene minor metabolite possesses potency similar to that of the parent compound nateglinide.
In vitro data demonstrate that nateglinide is predominantly metabolized by cytochrome P450 isoenzymes CYP2C9 (70%) and CYP3A4 (30%).

Indications and usage

Starlix (Nateglinide) is indicated as monotherapy to lower blood glucose in patients with Type 2 diabetes (non-insulin dependent diabetes mellitus, NIDDM) whose hyperglycemia cannot be adequately controlled by diet and physical exercise and who have not been chronically treated with other antidiabetic agents.
Starlix is also indicated for use in combination with metformin or a thiazolidinedione. In patients whose hyperglycemia is inadequately controlled with metformin or after a therapeutic response to a thiazolidinedione, Starlix may be added to, but not substituted for, those drugs.
Patients whose hyperglycemia is not adequately controlled with glyburide or other insulin secretagogues should not be switched to Starlix, nor should Starlix be added to their treatment regimen.

Contraindications

Starlix® (Nateglinide) is contraindicated in patients with:
1. Known hypersensitivity to the drug or its inactive ingredients.
2. Type 1 diabetes.
3. Diabetic ketoacidosis. This condition should be treated with insulin.

 

 

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