repaglinide
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repaglinide
[rĕ-pag´lĭ-nīd]repaglinide
Pharmacologic class: Meglitinide
Therapeutic class: Hypoglycemic
Pregnancy risk category C
Action
Inhibits alpha-glucosidases, enzymes that convert oligosaccharides and disaccharides to glucose. This inhibition lowers blood glucose level, especially in postprandial hyperglycemia.
Availability
Tablets: 0.5 mg, 1 mg, 2 mg
Indications and dosages
➣ Adjunct to diet and exercise in type 2 (non-insulin-dependent) diabetes mellitus uncontrolled by diet and exercise alone, or combined with metformin in type 2 diabetes mellitus uncontrolled by diet, exercise, and either repaglinide or metformin alone
Adults: 0.5 to 4 mg P.O. before each meal; may adjust at 1-week intervals based on blood glucose response. Maximum daily dosage is 16 mg.
Contraindications
• Hypersensitivity to drug or its components
• Diabetic ketoacidosis
• Type 1 (insulin-dependent) diabetes mellitus
• Administration with gemfibrozil
Precautions
Use cautiously in:
• renal or hepatic impairment; adrenal or pituitary insufficiency; stress caused by infection, fever, trauma, or surgery
• concurrent use of CYP2C8 inhibitors (such as trimethoprim, gemfibrozil, montelukast)
• concurrent use of CYP3A4 inhibitors (such as ketoconazole, itraconazole, erythromycin)
• concurrent use of CYP3A4 or CYP2C8 inducers (such as rifampin, barbiturates, carbamazepine)
• elderly or malnourished patients
• pregnant or breastfeeding patients
• children.
Administration
• Give 15 to 30 minutes before meals. Administer two, three, or four times daily, if needed, to adapt to patient's meal pattern.
Adverse reactions
CNS: headache, paresthesia
CV: angina, chest pain
EENT: sinusitis, rhinitis
GI: nausea, vomiting, diarrhea, constipation, dyspepsia
GU: urinary tract infection
Metabolic: hyperglycemia, hypoglycemia
Musculoskeletal: joint pain, back pain
Respiratory: upper respiratory infection, bronchitis
Other: tooth disorder, hypersensitivity reaction
Interactions
Drug-drug. Barbiturates, carbamazepine, rifampin: decreased repaglinide blood level
Beta-adrenergic blockers, chloramphenicol, MAO inhibitors, nonsteroidal antiinflammatory drugs, probenecid, sulfonamides, warfarin: potentiation of repaglinide effects
Calcium channel blockers, corticosteroids, estrogens, hormonal contraceptives, isoniazid, phenothiazines, phenytoin, nicotinic acid, sympathomimetics, thyroid preparations: loss of glycemic control
Clarithromycin: increased repaglinide area under the curve and Cmax
Cyclosporine: increased repaglinide plasma concentration
Erythromycin, ketoconazole, miconazole: decreased repaglinide metabolism, increased risk of hypoglycemia
Gemfibrozil, itraconazole: significantly increased repaglinide exposure
Simvastatin: increased repaglinide level
Drug-food. Any food: decreased drug bioavailability
Drug-herbs. Aloe gel (oral), bitter melon, chromium, coenzyme Q10, fenugreek, gymnema sylvestre, psyllium, St. John's wort: additive hypoglycemic effects
Glucosamine: poor glycemic control
Patient monitoring
• Monitor blood glucose and glycosylated hemoglobin levels.
• Monitor patient's meal pattern. Consult prescriber about adjusting dosage if patient adds or misses a meal.
• Assess for angina, shortness of breath, or other discomforts.
• Watch for signs and symptoms of bronchitis and upper respiratory, urinary, and EENT infections.
Patient teaching
• Tell patient to take 15 to 30 minutes before each meal.
• Instruct patient to monitor blood glucose level carefully. Teach him to recognize signs and symptoms of hypoglycemia and hyperglycemia.
• Advise patient to report signs and symptoms of infection.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, foods, and herbs mentioned above.