nateglinide

Absorption: Well absorbed (73%) following oral administration; absorption is rapid.

Distribution: Unknown.

Protein Binding: 98%.

Metabolism/Excretion: Mostly metabolized by the liver (CYP2C9 [70%] and CYP3A4 [30%]); 16% excreted unchanged in urine.

Half-Life: 1.5 hr.

Time/Action Profile ⬆ ⬇

(effect on blood glucose)

ROUTE	ONSET	PEAK	DURATION
PO	within 20 min	1 hr	4 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Diabetic ketoacidosis;
Type 1 diabetes;
OB: Insulin recommended to control diabetes during pregnancy;
Lactation: Lactation.

Use Cautiously in:

Malnourished patients, patients with pituitary or adrenal insufficiency (↑ susceptibility to hypoglycemia);
Strenuous physical exercise, insufficient caloric intake (↑ risk of hypoglycemia);
Poor metabolizers of CYP2C9 (↑ risk of hypoglycemia);
Autonomic neuropathy (hypoglycemia may be masked);
Moderate to severe liver impairment;
Fever, infection, trauma, or surgery (may lead to transient loss of glycemic control; insulin may be required);
Pedi: Safety and effectiveness not established in children;
Geri: May have sensitivity to drug effects ( risk of hypoglycemia).

Adv. Reactions/Side Effects ⬆ ⬇

Endo: HYPOGLYCEMIA

GI: diarrhea

MS: arthropathy, back pain

Neuro: dizziness

Resp: bronchitis, cough, upper respiratory infection

Misc: flu symptoms

Interactions ⬆ ⬇

Drug-drug:

Concurrent use with beta blockers may mask hypoglycemia.
Alcohol, combination with other antidiabetics, NSAIDs, MAO inhibitors, nonselective beta blockers, amiodarone, fluconazole, miconazole, or oxandrolone may ↑ the risk of hypoglycemia.
Hypoglycemic effects may be ↓ by thiazide diuretics, corticosteroids, thyroid supplements, sympathomimetic (adrenergic) agents, somatropin, rifampin, or phenytoin.

Blood levels and effects are significantly ↓ when administered prior to a liquid meal.

Route/Dosage ⬆ ⬇

PO (Adults ): 120 mg 3 times daily before meals; patients who are approaching glycemic control may be started at 60 mg 3 times daily.

Availability ⬆ ⬇

(Generic available)

Tablets: 60 mg; 120 mg

Assessment ⬆ ⬇

Observe for signs and symptoms of hypoglycemic reactions (sweating, hunger, weakness, dizziness, tremor, tachycardia, anxiety).

Lab Test Considerations:

Monitor serum glucose and HbA_1c periodically during therapy to evaluate effectiveness.
- May cause ↑ uric acid levels.

Toxicity and Overdose:

Overdose is manifested by symptoms of hypoglycemia. Mild hypoglycemia may be treated with administration of oral glucose. Severe hypoglycemia should be treated with IV D50W followed by continuous IV infusion of more dilute dextrose solution at a rate sufficient to keep serum glucose at approximately 100 mg/dL.

Implementation ⬆ ⬇

Patients stabilized on a diabetic regimen who are exposed to stress, fever, trauma, infection, or surgery may require administration of insulin.
PO: Administer 1–30 min prior to meals.
- May be administered concurrently with metformin, or pioglitazone.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take medication at same time each day. Take missed doses as soon as remembered unless almost time for next dose. Do not take if unable to eat.
Explain to patient that this medication controls hyperglycemia but does not cure diabetes. Therapy is long term.
Review signs of hypoglycemia and hyperglycemia with patient. If hypoglycemia occurs, advise patient to take a glass of orange juice or 2–3 tsp of sugar, honey, or corn syrup dissolved in water and notify health care professional.
Encourage patient to follow prescribed diet, medication, and exercise regimen to prevent hypoglycemic or hyperglycemic episodes.
Instruct patient in proper testing of serum glucose and ketones. These tests should be closely monitored during periods of stress or illness and health care professional notified if significant changes occur.
May occasionally cause dizziness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications, especially aspirin and alcohol.
Advise patient to inform health care professional of medication regimen prior to treatment or surgery.
Rep: Insulin is the recommended method of controlling blood glucose during pregnancy. Counsel female patients to use a form of contraception other than oral contraceptives and to notify health care professional promptly if pregnancy is planned or suspected.
Advise patient to carry a form of sugar (sugar packets, candy) and identification describing disease process and medication regimen at all times.
Emphasize the importance of routine follow-up exams.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇