:: Health Conditions - Diabetes
- Nateglinide
 Nateglinide
Nateglinide (brand name: 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® (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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