Hepatic impairment: Use conservative initial and maintenance doses; avoid use in severe liver disease Show
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Safety and efficacy not established Type 2 DiabetesInitial: 1.25 mg/day if nonmicronized tablets or 0.75 mg/day of micronized tablets Depending on glucose response, may increase dose by no more than 1.25-2.5 mg (regular) or 0.75-1.5 mg (micronized) every week May administer maintenance dose of 1.25-20 mg/day (regular) or 0.75-12 mg/day (micronized); for better satisfactory response may divide dose q12hr for patients taking >10 mg/day (regular) or >6 mg/day (micronized) Dosing considerationsBecause the elderly are susceptible to the hypoglycemic effects of glucose-lowering drugs, the question of how tightly glucose levels should be controlled is controversial Recognizing hypoglycemia in the elderly may be challenging Monitoring other parameters associated with cardiovascular disease, such as blood pressure and cholesterol, may be more important than normalized glycemic control Initial and maintenance dosing should be conservative Use caution in patients with renal insufficiency Next: InteractionsInteraction CheckerEnter a drug nameand glyburide No Results
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Previous Next: Adverse EffectsFrequency Not DefinedAngioedema Urticaria Rash Morbilliform eruptions Pruritus Photosensitivity reaction Heartburn Vasculitis Disulfiram-like reaction Hyponatremia Nocturia Agranulocytosis Hemolytic anemia Pancytopenia Thrombocytopenia Porphyria cutanea tarda Arthralgia Paresthesia Myalgia Blurred vision Diuretic effect (minor) Hypoglycemia Nausea/vomiting Cholestatic jaundice and hepatitis, which occur only rarely, may progress to liver failure Weight gain Bullous reactions, erythema multiforme, and exfoliative dermatitis Previous Next: WarningsContraindicationsHypersensitivity; sulfa allergy Type 1 diabetes Diabetic ketoacidosis with or without coma Coadministration with bosentan; increased risk of hepatotoxicity CautionsRisk of hypoglycemia increases when caloric intake is deficient, when more than one glucose-lowering agent used, when ethanol is ingested, or after severe or prolonged exercise; hypoglycemia is also morelikely to occur in elederly patients, malnourished or debilitated patients, and in patients with adrenal and/or pituitary insufficiency, and patients with severe hepatic and hepatic impairment Concerns for cross-reactivity between agents containing sulfonamide products has been reported for patients with prior allergic reactions to any compound with the sulfonamide structure SO2NH2; an expanding understanding of allergic mechanisms suggest that cross-reactivity between antibiotic sulfonamides and nonantibiotic sulfonamides may not occur or at the very least the potential is extremely low Caution in pregnancy/lactation Administration of oral hypoglycemic drugs has been reported to be associated with increased cardiovascular mortality as compared to treatment with diet alone or diet plus insulin; latest studies, however, do not support association Hemolytic anemia may occur with glucose 6-phosphate dehydrogenase (G6PD) deficiency when treated with sulfonylurea agents; use caution and consider a nonsulfonylurea alternative in patients with G6PD deficiency There are no clinical studies establishing conclusive evidence of macrovascular risk reduction with anti-diabetic drugs Use of glyburide not recommended in chronic kidney disease; metabolism and excretion of glyburide may be slowed in aptients with renal impairment and its active metabolites, causing accumulation in advanced renal insufficiency; prolonged hypoglycemia could occur It may be necessary to discontinue therapy and administer insulin if patient exposed to stress Micronized tablet formulation is not bioequivalent to conventional glyburide tablets; when transferring patient to a different glyburide formulation, retitrate the dose Beta cell destruction may occur following prolonged use of therapy, which may result in loss of treatment efficacy in type 2 diabetes mellitus; discontinue therapy if loss of efficacy occurs in patients who were previously responding to treatment and no contributing factors can be identified All sulfonylureas are capable of producing severe hypoglycemia Previous Next: Pregnancy & LactationPregnancy category: C Lactation: Not known if crosses into breast milk; avoid use in nursing women Pregnancy CategoriesA: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk. B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.NA: Information not available.Previous Next: PharmacologyMechanism of ActionInitial effect is to increase beta-cell insulin secretion May also decrease rate of hepatic glucose production and increase insulin receptor sensitivity AbsorptionBioavailability: Variable, depending on oral dosage form Onset: 15-60 min after a single dose (increase in serum insulin levels) Duration: <24 hr Vd: 9-10 L Peak serum time: 2-4 hr (adults) DistributionProtein bound: 99% MetabolismMetabolized extensively in the liver to less-active metabolites Metabolites: 4-trans-hydroxyglyburide, 3-cis-hydroxyglyburide (active) EliminationHalf-life: 10 hr (DiaBeta); 4 hr (Glynase, PresTab) Excretion: Urine (50%), feces (50%) Previous Next: ImagesBRANDFORM.UNIT PRICEPILL IMAGEglyburide oral - 2.5 mg tablet- 5 mg tablet- 2.5 mg tablet- 1.25 mg tablet- 5 mg tablet- 2.5 mg tablet- 1.25 mg tablet- 2.5 mg tablet- 1.25 mg tablet- 5 mg tablet- 2.5 mg tablet- 1.25 mg tablet- 5 mg tabletCopyright © 2010 First DataBank, Inc. Previous Next: Patient HandoutA Patient Handout is not currently available for this monograph. Previous Next: FormularyFormularyPatient Discounts Adding plans allows you to compare formulary status to other drugs in the same class. To view formulary information first create a list of plans. Your list will be saved and can be edited at any time. Create Your List of Plans Adding plans allows you to:
The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information. View explanations for tiers and restrictions TierDescription1This drug is available at the lowest co-pay. Most commonly, these are generic drugs.2This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.3This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.4This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.5This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.6This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.NCNOT COVERED – Drugs that are not covered by the plan.CodeDefinitionPAPrior Authorization Plans Select State: Done Non-Medicare Plans Medicare Plans Done CLOSE Additional Offers CLOSE Email to Patient From: To: The recipient will receive more details and instructions to access this offer. By clicking send, you acknowledge that you have permission to email the recipient with this information. CLOSE Email Forms to Patient From: To: The recipient will receive more details and instructions to access this offer. By clicking send, you acknowledge that you have permission to email the recipient with this information. Previous Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature. Which mechanism of action explains how glyburide decreases serum glucose?Glyburide is in a class of medications called sulfonylureas. Glyburide lowers blood sugar by causing the pancreas to produce insulin (a natural substance that is needed to break down sugar in the body) and helping the body use insulin efficiently.
What is the mechanism of action for glyburide?Glyburide, along with others in its class of sulfonylureas, exerts its mechanism of action based on increasing insulin secretion from beta cells in the pancreas. [7] Specifically, sulfonylureas bind to the SUR1 receptors in the membranes of the beta cells of potassium ATP-dependent channels.
What mechanism will regulate a decreased amount of blood glucose?Insulin reduces the body's blood sugar levels and provides cells with glucose for energy by helping cells absorb glucose. When blood sugar levels are too low, the pancreas releases glucagon. Glucagon instructs the liver to release stored glucose, which causes the body's blood sugar levels to rise.
What is the mechanism of action for a sulfonylurea such as glyburide used in the treatment of type 2 diabetes?Sulfonylureas and meglitinides directly stimulate release of insulin from pancreatic beta cells and thereby lower blood glucose concentrations. Because they work by stimulating insulin secretion, they are useful only in patients with some beta cell function. Adverse effects may include weight gain and hypoglycemia.
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Which mechanism of action explain how glyburide decreases serum glucose levels?
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