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Active ingredient: Repaglinide - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Hypoglycemic Agents
  • Meglitinides

Dosage Forms

  • Tablet

Brands / Synonyms

AG-EE 388 ZW; AG-EE 623 ZW; Prandimet; Prandin; Repaglinida [Inn-Spanish]; Repaglinide [Usan]; Repaglinidum [Inn-Latin]

Indications

For the treatment of Type II diabetes mellitus.

Pharmacology

Repaglinide 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). Repaglinide 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.

Mechanism of Action

Repaglinide 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.

Absorption

Rapid (bioavailability is 56%)

Toxicity

LD50 >1 g/kg (rat) (W. Grell)

Biotrnasformation / Drug Metabolism

Repaglinide is completely metabolized by oxidative biotransformation and direct conjugation with glucuronic acid after either an IV or oral dose.

Contraindications

PRANDIN is contraindicated in patients with:

1. Diabetic ketoacidosis, with or without coma. This condition should be treated with insulin.

2. Type1 diabetes.

3. Known hypersensitivity to the drug or its inactive ingredients.

Drug 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. See CLINICAL PHARMACOLOGY section, Drug-Drug Interactions.

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. See CLINICAL PHARMACOLOGY section, Drug-Drug Interactions.

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. See CLINICAL PHARMACOLOGY section, Drug-Drug Interactions.

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.

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