Prandin
Prandin - General Information
Prandin is a blood-glucose lowering drug. It lowers blood glucose by stimulating the release of insulin from the pancreas. It achieves this by closing ATP-dependent potassium channels in the membrane of the beta cells. This depolarizes the beta cells, opening the cells' calcium channels, and the resulting calcium influx induces insulin secretion.
Pharmacology of Prandin
Prandin is an oral blood glucose-lowering drug of the meglitinide class used in the management of type 2 diabetes mellitus (also known as non-insulin dependent diabetes mellitus or NIDDM). Prandin lowers blood glucose levels by stimulating the release of insulin from the pancreas. This action is dependent upon functioning beta cells in the pancreatic islets. Insulin release is glucose-dependent and diminishes at low glucose concentrations.
Prandin for patients
Patients should be informed of the potential risks and advantages of Repaglinide (PRANDIN) and of alternative modes of therapy. They should also be informed about the importance of adherence to dietary instructions, of a regular exercise program, and of regular testing of blood glucose and HbA1c. The risks of hypoglycemia, its symptoms and treatment, and conditions that predispose to its development and concomitant administration of other glucose-lowering drugs should be explained to patients and responsible family members. Primary and secondary failure should also be explained.
Patients should be instructed to take Repaglinide before meals (2, 3, or 4 times a day preprandially). Doses are usually taken within 15 minutes of the meal but time may vary from immediately preceding the meal to as long as 30 minutes before the meal. Patients who skip a meal (or add an extra meal) should be instructed to skip (or add) a dose for that meal.
Prandin Interactions
In vitro data indicate that repaglinide metabolism may be inhibited by antifungal agents like ketoconazole and miconazole, and antibacterial agents like erythromycin (cytochrome P-450 enzyme system 3A4 inhibitors). Drugs that induce the cytochrome P450 enzyme system 3A4 may increase repaglinide metabolism; such drugs include rifampin, barbiturates, and carbamezapine.
In vivo data from a study that evaluated the co-administration of a cytochrome P450 enzyme inhibitor, clarithromycin, with PRANDIN resulted in a clinically significant increase in repaglinide plasma levels. This increase in repaglinide plasma levels may necessitate a PRANDIN dose adjustment.
In vivo data from a study that evaluated the co-administration of gemfibrozil with PRANDIN in healthy subjects resulted in a significant increase in repaglinide blood levels. Patients taking PRANDIN should not start taking gemfibrozil; patients taking gemfibrozil should not start taking PRANDIN. Concomitant use may result in enhanced and prolonged blood glucose-lowering effects of repaglinide. Caution should be used in patients already on PRANDIN and gemfibrozil - blood glucose levels should be monitored and PRANDIN dose adjustment may be needed. Rare postmarketing events of serious hypoglycemia have been reported in patients taking PRANDIN and gemfibrozil together. Gemfibrozil and itraconazole had a synergistic metabolic inhibitory effect on PRANDIN. Therefore, patients taking PRANDIN and gemfibrozil should not take itraconazole.
The hypoglycemic action of oral blood glucose-lowering agents may be potentiated by certain drugs including nonsteroidal anti-inflammatory agents and other drugs that are highly protein bound, salicylates, sulfonamides, chloramphenicol, coumarins, probenecid, monoamine oxidase inhibitors, and beta adrenergic blocking agents. When such drugs are administered to a patient receiving oral blood glucose-lowering agents, the patient should be observed closely for hypoglycemia. When such drugs are withdrawn from a patient receiving oral blood glucose-lowering agents, the patient should be observed closely for loss of glycemic control.
Certain drugs tend to produce hyperglycemia and may lead to loss of glycemic control. These drugs include the thiazides and other diuretics, corticosteroids, phenothiazines, thyroid products, estrogens, oral contraceptives, phenytoin, nicotinic acid, sympathomimetics, calcium channel blocking drugs, and isoniazid. When these drugs are administered to a patient receiving oral blood glucose-lowering agents, the patient should be observed for loss of glycemic control. When these drugs are withdrawn from a patient receiving oral blood glucose-lowering agents, the patient should be observed closely for hypoglycemia.
Prandin Contraindications
PRANDIN is contraindicated in patients with:
- Diabetic ketoacidosis, with or without coma. This condition should be treated with insulin.
- Type1 diabetes.
- Known hypersensitivity to the drug or its inactive ingredients.
Additional information about Prandin
Prandin Indication: For the treatment of Type II diabetes mellitus.
Mechanism Of Action: Prandin closes ATP-dependent potassium channels in the b-cell membrane by binding at characterizable sites. This potassium channel blockade depolarizes the b-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.
Drug Interactions: Atenolol The beta-blocker decreases the symptoms of hypoglycemia
Acebutolol The beta-blocker decreases the symptoms of hypoglycemia
Betaxolol The beta-blocker decreases the symptoms of hypoglycemia
Bevantolol The beta-blocker decreases the symptoms of hypoglycemia
Bisoprolol The beta-blocker decreases the symptoms of hypoglycemia
Carteolol The beta-blocker decreases the symptoms of hypoglycemia
Carvedilol The beta-blocker decreases the symptoms of hypoglycemia
Esmolol The beta-blocker decreases the symptoms of hypoglycemia
Labetalol The beta-blocker decreases the symptoms of hypoglycemia
Metoprolol The beta-blocker decreases the symptoms of hypoglycemia
Nadolol The beta-blocker decreases the symptoms of hypoglycemia
Oxprenolol The beta-blocker decreases the symptoms of hypoglycemia
Penbutolol The beta-blocker decreases the symptoms of hypoglycemia
Pindolol The beta-blocker decreases the symptoms of hypoglycemia
Practolol The beta-blocker decreases the symptoms of hypoglycemia
Propranolol The beta-blocker decreases the symptoms of hypoglycemia
Timolol The beta-blocker decreases the symptoms of hypoglycemia
Sotalol The beta-blocker decreases the symptoms of hypoglycemia
Acetohexamide Similar mode of action - questionable association
Chlorpropamide Similar mode of action - questionable association
Gliclazide Similar mode of action - questionable association
Glimepiride Similar mode of action - questionable association
Glipizide Similar mode of action - questionable association
Glisoxepide Similar mode of action - questionable association
Glucosamine Possible hyperglycemia
Glibenclamide Similar mode of action - questionable association
Glycodiazine Similar mode of action - questionable association
Tolbutamide Similar mode of action - questionable association
Tolazamide Similar mode of action - questionable association
Rifampin Rifampin decreases the effect of repaglinide
Erythromycin The macrolide increases the effect of repaglinide
Josamycin The macrolide increases the effect of repaglinide
Clarithromycin Clarithromycin increases the effect of repaglinide
Cyclosporine Cyclosporine increases the effect of repaglinide
Gemfibrozil Gemfibrozil increases the effect and toxicity of repaglinide
Food Interactions: Not Available
Generic Name: Repaglinide
Synonyms: Repaglinida [Inn-Spanish]; Repaglinidum [Inn-Latin]; AG-EE 388 ZW; AG-EE 623 ZW
Drug Category: Hypoglycemic Agents; Meglitinides
Drug Type: Small Molecule; Approved
Other Brand Names containing Repaglinide: Prandin;
Absorption: Rapid (bioavailability is 56%)
Toxicity (Overdose): LD50 >1 g/kg (rat) (W. Grell)
Protein Binding: >98%
Biotransformation: Repaglinide is completely metabolized by oxidative biotransformation and direct conjugation with glucuronic acid after either an IV or oral dose.
Half Life: 1 hour
Dosage Forms of Prandin: Tablet Oral
Chemical IUPAC Name: 2-ethoxy-4-[2-[[(1S)-3-methyl-1-(2-piperidin-1-ylphenyl)butyl]amino]-2-oxoethyl]benzoic acid
Chemical Formula: C27H36N2O4
Repaglinide on Wikipedia: https://en.wikipedia.org/wiki/Repaglinide
Organisms Affected: Humans and other mammals
