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November 21, 2009
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Pharmacy Author: Omudhome Ogbru, PharmD
Medical Editor: Jay Marks, MD

GENERIC NAME: repaglinide

BRAND NAME: Prandin

DRUG CLASS AND MECHANISM: Repaglinide is an oral medication for lowering blood sugar (glucose) in individuals with diabetes. It is in a class of drugs for treating diabetes type 2 called meglitinides and is chemically unlike other anti-diabetic medication.

Approximately 90% of patients with diabetes have type 2 or non-insulin dependent diabetes mellitus. (Type 2 diabetes usually occurs in adulthood, and is associated with obesity and a strong family history of diabetes.) Glucose intolerance in diabetes type II is caused by reduced insulin secretion from the pancreas after meals and resistance of the body's cells to insulin's effect which is to stimulate the cells to remove glucose from the blood. This leads to high levels of blood glucose.

Like Sulfonylureas, for example, glyburide (Diabeta; Glynase; Micronase), glipizide (Glucotrol), glimepiride (Amaryl), tolbutamide (Orinase), and tolazamide (Tolinase), repaglinide stimulates cells in the pancreas to produce insulin. Glyburide may be more potent than repaglinide at increasing insulin release in persons with low or high blood glucose levels, whereas repaglinide may be more potent in persons with moderate blood glucose levels. Repaglinide is unusual in that it has a rapid onset of action and a short duration of action. When taken just prior to meals, it promotes the release of insulin that normally occurs with meals and is responsible for preventing blood glucose levels from becoming high. It has been shown to lower hemoglobin A1c levels by 1.6% to 1.9%. (Hemoglobin A1c is a blood test which measures the effectiveness of a drug in controlling high blood glucose levels. The lower the hemoglobin A1c, the better the control.) Repaglinide was approved by the FDA in 1997.

GENERIC AVAILABLE: no

PRESCRIPTION: yes

PREPARATIONS: Tablets: 0.5mg, 1mg, 2mg.

STORAGE: Tablets should be stored at room temperature, 15-30 C (59-86 F).

PRESCRIBED FOR: Repaglinide is used in treating type 2 diabetes, together with diet and exercise. It can be used alone (monotherapy) or combined with metformin (Glucophage).

DOSING: Repaglinide is taken immediately before a meal or 15 to 30 minutes before a meal. It should be taken with every meal up to 4 times a day. Doses are adjusted by the physician to achieve the best effect.

DRUG INTERACTIONS: Repaglinide is metabolized (eliminated) in the liver by an enzyme called CYP3A4. Drugs that affect this enzyme may affect the blood levels of repaglinide and thus alter its glucose lowering effect. The metabolism of repaglinide may be prevented by ketoconazole (Nizoral), itraconazole (Sporanox), fluconazole (Diflucan), erythromycin (Ery-Tab), and clarithromycin (Biaxin). As a result, blood levels of repaglinide rise and there is an enhanced glucose-lowering effect. Dangerous hypoglycemic (very low blood glucose) reactions could occur. On the other hand, the elimination of repaglinide may be increased with drugs that increase levels of CYP3A4 in the liver, such as barbiturates, carbamazepine (Tegretol), and rifampin (Rifadin). This can result in lower blood levels of repaglinide and hyperglycemia (high blood glucose).




Report Problems to the Food and Drug Administration

 

You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.


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  • Drug Interactions - Learn about potential drug interactions you may be exposed to. Drug interactions can occur with prescription drugs, OTC medication, vitamins, herbs, and supplements.
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What is hypoglycemia?

Hypoglycemia is the clinical syndrome that results from low blood sugar. The symptoms of hypoglycemia can vary from person to person, as can the severity. Classically, hypoglycemia is diagnosed by a low blood sugar with symptoms that resolve when the sugar level returns to the normal range.

Who is at risk for hypoglycemia?

While patients who do not have any metabolic problems can complain of symptoms suggestive of low blood sugar, true hypoglycemia usually occurs in patients being treated for diabetes (type 1 and type 2). Patients with pre-diabetes who have insulin resistance can also have low blood sugars on occasion if their high circulating insulin levels are further challenged by a prolonged period of fasting. There are other rare causes for hypoglycemia, such as insulin producing tumors (insulinomas) and certain medications. These uncommon causes of hypoglycemia will not be discussed in this ...

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