repaglinide, 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 that are chemically unlike other anti-diabetic medications. 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 2 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 different because 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 (HbA1c) 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: 0.5, 1, and 2 mg.

STORAGE: Tablets should be stored at room temperature below 25 C (77 F).

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

DOSING: Repaglinide is taken 15 to 30 minutes before a meal. It should be taken with meals and may be administered 2, 3, or 4 times a day.

For patients with HbA1c < 8% who are receiving treatment for the first time the starting dose is 0.5 mg with each meal.

Patients who have been treated with other diabetes drugs and whose HbA1c is = 8% should start with 1 or 2 mg with each meal. The initial dose may be doubled at weekly intervals until the desired response is achieved or the maximum dose of 4 mg with each meal (16 mg daily) is achieved.

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).

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