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- What is repaglinide, and how does it work (mechanism of action)?
- What are the side effects of repaglinide?
- What is the dosage for repaglinide?
- Which drugs or supplements interact with repaglinide?
- Is repaglinide safe to take if I'm pregnant or breastfeeding?
- What else should I know about repaglinide?
What is repaglinide, and how does it work (mechanism of action)?
Repaglinide is an oral medication for lowering blood sugar (glucose) in individuals with type 2 diabetes. It is in a class of drugs for treating diabetes type 2 called meglitinides that are chemically unlike other anti-diabetic medications. Nateglinide (Starlix), is another currently available meglitinide. 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 that causes 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 glucose in the blood.
Like sulfonylureas, for example, glyburide (Diabeta, Glynase), glipizide (Glucotrol, Glucotrol XL), glimepiride (Amaryl), tolbutamide and tolazamide, 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 more moderate abnormalities of 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 over prolonged periods of time; the lower the hemoglobin A1c, the better the control.) Repaglinide was approved by the FDA in 1997.
What brand names are available for repaglinide?
Is repaglinide available as a generic drug?
GENERIC AVAILABLE: Yes
Do I need a prescription for repaglinide?
What are the side effects of repaglinide?
Hypoglycemia (low blood glucose) is the most frequent side effect and it occurs somewhat less frequently with repaglinide than with sulfonylureas such as glyburide and glipizide. Some symptoms of hypoglycemia include:
- heart palpitations,
- numbness around the mouth,
- tingling in the fingers,
- muscle weakness,
- blurred vision,
- cold temperature,
- excessive yawning,
- confusion, or
- loss of consciousness.
Other common side effects include:
- stomach pain,
- back pain,
- upper respiratory infections, and
- chest pain.
Side effects that have been reported post-marketing inlcude:
What is the dosage for repaglinide?
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.
Which drugs or supplements interact with repaglinide?
- 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).
- Some drugs increase blood sugar and therefore reverse the effects of repaglinide. Such drugs include thiazide diuretics (for example, hydrochlorothiazide [Microzide]), loop diuretics (for example, furosemide [Lasix)], amphetamines, glucocorticoids such as prednisone and methylprednisolone (Medrol), estrogens, isoniazid, phenothiazines such as chlorpromazine (Thorazine), phenytoin (Dilantin), somatropin (Genotropin), decongestants and thyroid drugs.
- Anabolic steroids or androgens can increase the risk of developing hypoglycemia in diabetic patients taking glucose-lowering medications.
- MAO inhibitors (for example, isocarboxazid [Marplan] and phenelzine [Nardil], salicylates, and selective serotonin reuptake inhibitors (for example paroxetine (Paxil), fluoxetine (Prozac) and sertraline (Zoloft) also can increase the effects of repaglinide and worsen the chance of developing hypoglycemia.
- Beta blockers, for example, propranolol (Inderal), atenolol (Tenormin), can cause hypoglycemia or hyperglycemia. Also, beta-blockers can blunt some of the body's responses to hypoglycemia such as rapid heart ratea, thus making it difficult for patients to recognize (and treat) hypoglycemic reactions. Nevertheless, beta-blockers have been used successfully in diabetic patients. Treatment with beta-blockers is associated with improved survival in diabetics who are treated with the beta-blocker for high blood pressure.
- Gemfibrozil (Lopid) should not be combined with repaglinide because gemfibrozil may increase blood levels of repaglinide and lead to hypoglycemia.
- Atazanavir (Reyataz) and Trimethoprim (Primsol) can increase the blood levels of repaglinide as well leading to increased risks of hypoglycemia.
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Is repaglinide safe to take if I'm pregnant or breastfeeding?
No adequate human studies on the effects of repaglinide on the fetus have been done. Adverse effects have been reported in some animal studies. Animals given repaglinide during both lactation (nursing) and gestation (pregnancy) have developed skeletal defects. Therefore, physicians must weigh the potential benefits and risks of this medication when considering its use in pregnant women.
It is not known whether repaglinide accumulates in breast milk. However, animals given repaglinide during pregnancy and lactation have developed skeletal defects. Because of the possibility of hypoglycemia in nursing infants and the skeletal effects in nursing animals, it is recommended that repaglinide not be used in women who are breastfeeding.
What else should I know about repaglinide?
What preparations of repaglinide are available?
Tablets: 0.5, 1, and 2 mg.
How should I keep repaglinide stored?
Tablets should be stored at room temperature, below 25 C (77 F).
Repaglinide (Prandin) is a drug prescribed to lower blood sugar levels (glucose) in persons with diabetes. Side effects, drug interactions, warnings and precautions, and patient information should be reviewed prior to taking any medication.
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Related Disease Conditions
Diabetes (Type 1 and Type 2)
Diabetes is a chronic condition characterized by high levels of sugar (glucose) in the blood. The two types of diabetes are referred to as type 1 (insulin dependent) and type 2 (non-insulin dependent). Symptoms of diabetes include increased urine output, thirst, hunger, and fatigue. Treatment of diabetes depends on the type.
Diabetes Treatment (Type 1 and Type 2 Medications and Diet)
The major goal in treating diabetes is controlling elevated blood sugar without causing abnormally low levels of blood sugar. Type 1 diabetes is treated with: insulin, exercise, and a diabetic diet. Type 2 diabetes is first treated with: weight reduction, a diabetic diet, and exercise. When these measures fail to control the elevated blood sugar, oral medications are used. If oral medications are still insufficient, insulin medications are considered.
Low Blood Sugar (Hypoglycemia)
Low blood sugar, or hypoglycemia, is a syndrome in which a person's blood sugar is dangerously low. People with type 1 and type 2 diabetes are at risk for this condition. There are other diseases that can cause a person's blood sugar levels to go too low, for example, pancreatitis, Cushing's syndrome, and pancreatic cancer. Symptoms and signs that your blood sugar levels are too low include palpitations, trembling, intense hunger, sweating, nervousness, and weakness. If your blood sugars become too low, use these nearby as a quick treatment table sugar, soda, juice, and glucose tablets.
High Blood Sugar (Hyperglycemia)
Hyperglycemia or high blood sugar is a serious health problem for diabetics. There are two types of hyperglycemia, 1) fasting, and 2)postprandial or after meal hyperglycemia. Hyperglycemia can also lead to ketoacidosis or hyperglycemic hyperosmolar nonketotic syndrome (HHNS). There are a variety of causes of hyperglycemia in people with diabetes. Symptoms of high blood sugar may include increased thirst, headaches, blurred vision, and frequent urination.Treatment can be achieved through lifestyle changes or medications changes. Carefully monitoring blood glucose levels is key to prevention.
Type 1 vs Type 2 Diabetes (Similarities and Differences)
Diabetes mellitus is a metabolic condition in which a person's blood sugar (glucose) levels are too high. Over 29.1 million children and adults in the US have diabetes. Of that, 8.1 million people have diabetes and don't even know it. Type 1 diabetes (insulin-dependent, juvenile) is caused by a problem with insulin production by the pancreas. Type 2 diabetes (non-insulin dependent) is caused by: Eating a lot of foods and drinking beverages with simple carbohydrates (pizza, white breads, pastas, cereals, pastries, etc.) and simple sugars (donuts, candy, etc.) Consuming too many products with artificial sweeteners (We found out that they are bad for us!) Lack of activity Exercise Stress Genetics While the signs and symptoms of both types of diabetes are the same, which include: Increased urination Increased hunger Increased thirst Unexplained weight loss. However, the treatments are different. Type 1 diabetes is insulin dependent, which means a person with this type of diabetes requires treatment with insulin. People with type 2 diabetes require medication, lifestyle changes like eating a healthy diet, and getting regular exercise.
Type 2 Diabetes
Type 2 diabetes is a chronic condition that may be reversible with diet and lifestyle changes. Symptoms include excessive thirst, frequent urination, weight loss, fatigue, and an unusual odor to your urine. Most people don't know they have type 2 diabetes until they have a routine blood test. Treatment options include medications, a type 2 diabetes diet, and other lifestyle changes.
A diabetic diet, or diabetes diet helps keep blood glucose levels in the target range for patients. Exercise and medication may also help stabilize blood glucose levels. Keeping track of when you take your diabetic medicine, keeping track of food choices, eating the proper amount of fruits, vegetables, carbohydrates, and fats will also help maintain proper blood glucose levels. Foods that raise blood sugar levels are "high glycemic index foods;" examples include: Pumpkin Melons Popcorn Short-grain white rice Foods that help maintain good blood sugar levels are foods that are low on the glycemic index, for example: Rolled or steel-cut oats Many fruits Non-starchy vegetables Beans Legumes Lentils
Diabetes and Kidney Disease
In the United States diabetes is the most common cause of kidney failure. High blood pressure and high levels of blood glucose increase the risk that a person with diabetes will eventually progress to kidney failure. Kidney disease in people with diabetes develops over the course of many years. albumin and eGFR are two key markers for kidney disease in people with diabetes. Controlling high blood pressure, blood pressure medications, a moderate protein diet, and compliant management of blood glucose can slow the progression of kidney disease. For those patients who's kidneys eventually fail, dialysis or kidney transplantation is the only option.
Tips for Managing Type 1 and 2 Diabetes at Home
Managing your diabetes is a full time commitment. The goal of diabetic therapy is to control blood glucose levels and prevent the complications of diabetes. Information about exercise, diet, and medication will help you manage your diabetes better. Blood glucose reagent strips, blood glucose meters, urine glucose tests, tests for urinary ketones, continuous glucose sensors, and Hemoglobin A1C testing information will enable you to mange your diabetes at home successfully.
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