GENERIC NAME: repaglinide
BRAND NAME: Prandin
DRUG CLASS AND MECHANISM: Repaglinide is an oral medication for lowering blood sugar (glucose) in diabetics. 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, e.g. 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 1.6-1.9%.
(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).
Anabolic steroids or androgens can increase the risk of developing
hypoglycemia in diabetic patients taking glucose-lowering medications.
Some drugs increase blood sugar and therefore reverse the effects of
repaglinide. Such drugs include amphetamines, glucorticoids such
as prednisone, estrogens, isoniazid, phenothiazines such as chlorpromazine (Thorazine), phenytoin
(Dilantin), decongestants, and thyroid drugs.
Beta-blockers, e.g. 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 rate, thus making it difficult for patients to
recognize (and treat) hypoglycemic reactions. This not withstanding, 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 because of high blood pressure.)
PREGNANCY: No adequate human studies on the effects of
repaglinide on the fetus have been done; however, there have been no effects in animal studies in which the mother has received repaglinide during pregnancy. Nevertheless, animals given
repaglinide during both lactation (nursing) and gestation have developed skeletal
defects. Therefore, physicians must weight the potential benefits and risks
of this medication when considering its use in pregnant women.
NURSING MOTHERS: 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
breast-feeding.
SIDE EFFECTS: Hypoglycemia (low blood glucose) occurs somewhat
less frequently with repaglinide (1 in 6 persons) than with sulfonylureas such as
glyburide and glipizide (1 in 5 persons). Some symptoms of hypoglycemia
include hunger, nausea, tiredness, perspiration, headache, heart
palpitations, numbness around the mouth, tingling in the fingers, tremors,
muscle weakness, blurred vision, cold temperature, excessive yawning,
irritability, confusion, or loss of consciousness. Headache is reported in
1 in 9 persons. Other possible side effects include nausea, vomiting, diarrhea,
constipation, stomach pain, back pain, and chest pain.
Last Editorial Review: 6/6/1999 6:33:00 PM
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From the Doctors at MedicineNet.com  |
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- Diabetes - Information on Diabetes (Diabetes Mellitus) including types, causes, symptoms of diabetes, medications, and treatment. Produced by the doctors of MedicineNet.com Source:MedicineNet
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