Drug information of Repaglinide
Repaglinide is an oral diabetes medicine that helps control blood sugar levels by causing the pancreas to produce insulin. Repaglinide is used together with diet and exercise to treat type 2 diabetes. Other diabetes medicines are sometimes used in combination with repaglinide if needed.
Mechanism of effect
Repaglinide closes ATP-dependent potassium channels in the ß-cell membrane by binding at characterizable sites. This potassium channel blockade depolarizes the ß-cell, which leads to an opening of calcium channels. The resulting increased calcium influx induces insulin secretion. The ion channel mechanism is highly tissue selective with low affinity for heart and skeletal muscle.
Repaglinide lowers blood glucose levels by stimulating the release of insulin from the pancreas. This action is dependent upon functioning beta (ß) cells in the pancreatic islets. Insulin release is glucose-dependent and diminishes at low glucose concentrations
After oral administration, repaglinide is rapidly and completely absorbed from the gastrointestinal tract. peak plasma drug levels (Cmax) occur within 1 hour (Tmax). Repaglinide is rapidly eliminated from the blood stream with a half-life of approximately 1 hour. The mean absolute bioavailability is 56% Protein binding and binding to human serum albumin was greater than 98%. epaglinide is rapidly metabolized via oxidation and dealkylation by cytochrome P450 3A4 and 2C9 to form the major dicarboxylic acid derivative (M2) 90% eliminated in feces (<2% as unchanged drug), 8% in urine (0.1% as unchanged drug)
Drug indicationsdiabetes mellitus type2
Usual Adult Dose for Diabetes Type 2 Individualize therapy: Dose preprandially 2, 3, or 4 times a day -For patients not previously treated with antidiabetic agents or whose glycosylated hemoglobin (HbA1c) is less than 8%: Initial dose: 0.5 mg orally with each meal -For patients previously treated with antidiabetic agents or whose HbA1c is 8% or higher: Initial dose: 1 or 2 mg orally with each meal Dose Adjustments: Based upon blood glucose response, double the preprandial dose up to a maximum meal time dose of 4 mg until satisfactory glycemic response is achieved; allow at least 1 week to assess response after each dose adjustment. Recommended Dose Range: 0.5 to 4 mg orally with each meal Maximum Daily Dose: 16 mg per day
Drug contraindicationshypersensitivity to drug or its components. , diabetic ketoacidosis , Coadministration of gemfibrozil , Type 1 diabetes
Side effectsnausea , Headache , chest pain , constipation , vomiting , allergic reaction , Diarrhea , paresthesia , Rhinitis , dyspepsia , Urinary tract infection , sinusitis , Arthralgia , back pain , bronchitis , Hypoglycemia
InteractionsErythromycin , Oxymetholone , Propranolol , Gemfibrozil , Simvastatin , Fenofibrate , Nifedipine , Ketoconazole , Clarithromycin , Ethinyl Estradiol , Sotalol , Cyclosporine , Glibenclamide , Metoprolol , Carvedilol , Thyrotropin alfa , Rifabutin , fluvastatin , teriflunomide , Canagliflozin , lumacaftor and Ivacaftor , Grepafloxacin , Cannabidiol , tecovirimat , Alclometasone
1-All oral blood glucose-lowering drugs including repaglinide are capable of producing hypoglycemia. 2-Repaglinide is not indicated for use in combination with NPH-insulin
Points of recommendation
Patients should be informed about the importance of adherence to dietary instructions, of a regular exercise program, and of regular testing of blood glucose and HbA1c.