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

Brands, Medical Use, Clinical Data

Drug Category

  • Antiarrhythmic Agents
  • Hypoglycemic Agents
  • Sulfonylureas

Dosage Forms

  • Tablet (1.25 mg, 2.5 mg, 5 mg)

Brands / Synonyms

Abbenclamide; Adiab; Apo-Glibenclamide; Azuglucon; Bastiverit; Benclamin; Betanase; Betanese 5; Calabren; Cytagon; Daonil; Debtan; Dia-basan; Diabeta; Diabeta (TN); Diabiphage; Dibelet; Duraglucon; Euclamin; Euglucan; Euglucon; Euglucon 5; Euglykon; GBN 5; Gen-Glybe; Gewaglucon; Gilemal; Glamide; Glibadone; Gliban; Gliben; Gliben-Puren N; Glibenbeta; Glibenclamid AL; Glibenclamid Basics; Glibenclamid Fabra; Glibenclamid Genericon; Glibenclamid Heumann; Glibenclamid Riker M.; Glibenclamid-Cophar; Glibenclamid-Ratiopharm; Glibenclamida [INN-Spanish]; Glibenclamide; Glibenclamide (JP14); Glibenclamidum [INN-Latin]; Glibenil; Glibens; Glibesyn; Glibet; Glibetic; Glibil; Gliboral; Glicem; Glidiabet; Glimel; Glimide; Glimidstata; Glisulin; Glitisol; Glubate; Gluben; Gluco-Tablimen; Glucobene; Glucohexal; Glucolon; Glucomid; Glucoremed; Glucovance; Glucoven; Glyben; Glybenclamide; Glybenzcyclamide; Glyburase; Glyburide; Glyburide (micronized); Glyburide (USP); Glyburide and Metformin; Glyburide [USAN]; Glycolande; Glycomin; Glynase; Hemi-Daonil; Hexaglucon; Humedia; Lederglib; Libanil; Lisaglucon; Malix; Maninil; Med-Glionil; Melix; Micronase; Micronase (TN); Micronized Glyburide; Miglucan; Nadib; Neogluconin; Norglicem 5; Normoglucon; Novo-Glyburide; Orabetic; Pira; Praeciglucon; PresTab; Prodiabet; Renabetic; Semi-daonil; Semi-Euglucon; Semi-Gliben-Puren N; Sugril; Suraben; Tiabet; Yuglucon

Indications

Indicated as an adjunct to diet to lower the blood glucose in patients with non-insulin-dependent diabetes mellitus (Type II) whose hyperglycemia cannot be satisfactorily controlled by diet alone.

Pharmacology

Glyburide, a second-generation sulfonylurea antidiabetic agent, appears to lower the blood glucose acutely by stimulating the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets. With chronic administration in Type II diabetic patients, the blood glucose lowering effect persists despite a gradual decline in the insulin secretory response to the drug. Extrapancreatic effects may be involved in the mechanism of action of oral sulfonyl-urea hypoglycemic drugs. The combination of glyburide and metformin may have a synergistic effect, since both agents act to improve glucose tolerance by different but complementary mechanisms. In addition to its blood glucose lowering actions, glyburide produces a mild diuresis by enhancement of renal free water clearance. Glyburide is twice as potent as the related second-generation agent glipizide.

Mechanism of Action

Sulfonylureas such as glyburide likely bind to ATP-sensitive potassium-channel receptors on the pancreatic cell surface, reducing potassium conductance and causing depolarization of the membrane. Depolarization stimulates calcium ion influx through voltage-sensitive calcium channels, raising intracellular concentrations of calcium ions, which induces the secretion, or exocytosis, of insulin.

Absorption

Significant absorption within 1 hour and peak plasma levels are reached within 4 hours.

Toxicity

Oral rat LD50: > 20,000 mg/kg. Oral mouse LD50: 3250 mg/kg.

Biotrnasformation / Drug Metabolism

Primarily hepatic (mainly cytochrome P450 3A4). The major metabolite is the 4-trans-hydroxy derivative. A second metabolite, the 3-cis-hydroxy derivative, also occurs. These metabolites contribute no significant hypoglycemic action in humans as they are only weakly active.

Contraindications

MICRONASE Tablets are contraindicated in patients with:

1.Known hypersensitivity or allergy to the drug.

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

3.Type I diabetes mellitus, as sole therapy.

Drug Interactions

The hypoglycemic action of sulfonylureas may be potentiated by certain drugs including nonsteroidal anti-inflammatory agents and other drugs that are highly protein bound, salicylates, sulfonamides, chloramphenicol, probenecid, coumarins, monoamine oxidase inhibitors, and beta adrenergic blocking agents. When such drugs are administered to a patient receiving MICRONASE, the patient should be observed closely for hypoglycemia. When such drugs are withdrawn from a patient receiving MICRONASE, the patient should be observed closely for loss of control.

Certain drugs tend to produce hyperglycemia and may lead to loss of control. These drugs include the thiazides and other diuretics, corticosteroids, phe-nothiazines, thyroid products, estrogens, oral contraceptives, phenytoin, nicotinic acid, sympathomimet-ics, calcium channel blocking drugs, and isoniazid. When such drugs are administered to a patient receiving MICRONASE, the patient should be closely observed for loss of control. When such drugs are withdrawn from a patient receiving MICRONASE, the patient should be observed closely for hypoglycemia.

A possible interaction between glyburide and ciprofloxacin, a fluoroquinolone antibiotic, has been reported, resulting in a potentiation of the hypoglycemic action of glyburide. The mechanism for this interaction is not known.

A potential interaction between oral miconazole and oral hypoglycemic agents leading to severe hypoglycemia has been reported. Whether this interaction also occurs with the intravenous, topical or vaginal preparations of miconazole is not known. Metformin: In a single-dose interaction study in NIDDM subjects, decreases in glyburide AUC and Cmax were observed, but were highly variable. The single-dose nature of this study and the lack of correlation between glyburide blood levels and pharmaco-dynamic effects, makes the clinical significance of this interaction uncertain. Coadministration of gly-buride and metformin did not result in any changes in either metformin pharmacokinetics or pharmaco-dynamics.

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