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Trade Names:
Starlix
- Tablets 60 mg
- Tablets 120 mg

Mechanism of Action

Pharmacology

Lowers blood glucose levels by stimulating insulin secretion from the pancreas.

Pharmacokinetics

Absorption

Rapidly absorbed immediately prior to a meal. Oral T _max is 1 hr (prior to a meal); bioavailability is approximately 73%. Food delays T _max and C _max .

Distribution

Nateglinide protein binding is 98% (primarily albumin, lesser extent to alpha ₁ -acid glycoprotein). Vd is 10 L (IV).

Metabolism

Hydroxylation followed by glucuronide conjugation via CYP2C9 (70%) and CYP3A4 (30%).

Elimination

Nateglinide is eliminated in urine (83% as metabolites, 16% as parent compound) and feces (10%). The t _{1/ 2} is 1.5 hr.

Special Populations

The peak and total exposure of nateglinide were increased 30% (mild hepatic insufficiency). Use with caution (chronic hepatic insufficiency).

Indications and Usage

As monotherapy to lower blood glucose in patients with type 2 diabetes mellitus (non-insulin-dependent diabetes mellitus) whose hyperglycemia cannot be adequately controlled by diet and exercise and who have not been chronically treated with other antidiabetic agents; in combination with metformin or a thiazolidinedione, in patients whose hyperglycemia is inadequately controlled with metformin, or after a therapeutic response to a thiazolidinedione. Do not use as a substitute for those drugs.

Contraindications

Type 1 diabetes; diabetic ketoacidosis; hypersensitivity to nateglinide or its ingredients.

Dosage and Administration

PO 120 mg tid, 1 to 30 min before meals, alone or in combination with metformin or a thiazolidinedione. The 60 mg dose of nateglinide may be used, alone or in combination with metformin or a thiazolidinedione, in patients whose glycosylated hemoglobin (HbA _1c ) is near goal levels when treatment is initiated.

General Advice

• May be used alone or in combination with metformin or a thiazolidinedione. Not to be used in combination with sulfonylureas or other secretogogues or for the treatment of type 1 diabetes.
• If a meal is skipped, the dose should be skipped to reduce the risk of hypoglycemia.

Storage/Stability

Store tablets at controlled room temperature (59° to 86°F). Keep tightly closed.

Drug Interactions

May reduce the hypoglycemic effects of nateglinide.

May potentiate the hypoglycemic effects of nateglinide.

Laboratory Test Interactions

Uric acid levels may be increased.

Adverse Reactions

CNS

Dizziness (4%).

GI

Diarrhea (3%).

Hypersensitivity

Rash, itching, urticaria (postmarketing).

Metabolic-Nutritional

Hypoglycemia (2%).

Respiratory

Upper respiratory tract infection (11%); bronchitis (3%); coughing (2%).

Miscellaneous

Back pain, flu-like symptoms (4%); arthropathy, accidental trauma (3%).

Precautions

Pregnancy

Category C . Insulin is recommended to maintain blood glucose levels during pregnancy.

Lactation

Undetermined.

Children

Safety and efficacy not established.

Hepatic Function

Use with caution in patients with moderate to severe or chronic liver disease.

Special Risk Patients

Patients with type 2 diabetes and renal failure on dialysis may exhibit reduced overall drug exposure.

Secondary failure

Transient loss of glycemic control may occur in patients with fever, infection, trauma, or surgery. At such times, it may be necessary to discontinue nateglinide and administer insulin.

Overdosage

Symptoms

Exaggerated glucose lowering with hypoglycemic symptoms, coma, seizure, neurological symptoms.

Patient Information

• Explain name, dose, action, and potential side effects of drug.
• Advise patient or caregiver to read Patient Information leaflet before using the first time and with each refill.
• Instruct patient to take prescribed dose immediately before or up to 30 min before each meal.
• Instruct patient if meal is missed, to skip the dose for that meal to reduce risk of hypoglycemia.
• Educate patient or caregiver regarding diabetes and its management, including target ranges for blood sugar control. Instruct patient or caregiver that this medication is not a substitute for diet and exercise and to continue to follow prescribed regimens.
• Educate patient or caregiver regarding potential long-term complications of diabetes and need for regular general physical and eye examinations.
• Ensure patient or caregiver understands how to use home glucose monitor and has a plan for monitoring and recording blood sugar measurements (eg, log). Advise patient to take log to each visit with health care provider.
• Educate patient regarding value of periodic A _1c testing to confirm level of glucose control.
• Review symptoms of hypoglycemia (eg, low blood sugar) and hyperglycemia (eg, high blood sugar), and action plans to undertake in the event either occur.
• Advise patient to discuss with health care provider a plan for managing each of the following situations: medication dosing during intercurrent conditions (eg, vomiting, infection, trauma, stress, sick days); accidental ingestion of too little or too much medication; missed dose of medication; inadequate food intake or a skipped meal; travel across time zones; change in physical activity.
• Instruct patient to notify health care provider if experiencing severe, continuous, or frequent hypoglycemic episodes; hypoglycemic episodes with few or no warning symptoms; or continuous or severe hyperglycemia.
• Advise patient to carry medical identification of diabetes (eg, Medi-Alert ).
• Advise women to notify health care provider if pregnant, planning to become pregnant, or breastfeeding.
• Instruct patient not to take prescription or OTC drugs, dietary supplements, or herbal preparations without consulting health care provider.
• Advise patient that follow-up visits and lab tests will be required to monitor therapy and to keep appointments.