glyburide (Rx)

Brand and Other Names:Diabeta, Glynase, more...Glynase PresTab
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

tablet

  • 1.25mg
  • 2.5mg
  • 5mg

tablet, micronized

  • 1.5mg
  • 3mg
  • 5mg
  • 6mg
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Type 2 Diabetes Mellitus

Regular tablets

  • Initial: 2.5-5 mg PO qDay
  • Maintenance: 1.25-20 mg PO qDay or q12hr
  • Not to exceed 20 mg/day
  • Consider administering q12hr for doses >10 mg/day

Micronized tablets

  • Initial: 1.5-3 mg PO qDay
  • Maintenance: 0.75-12 mg PO qDay
  • Not to exceed 12 mg/day
  • Patients at risk for hypoglycemia: 0.75 mg PO qDay initially

Transferring from insulin therapy to glyburide

  • Current insulin dose <20 units: Discontinue insulin and initiate glyburide dose at 2.5-5 mg/day (regular) or 1.5-3 mg/day (micronized)
  • Current insulin dose 20-40 units: Discontinue insulin and initiate glyburide dose at 5 mg/day (regular) or 3 mg/day (micronized)
  • Current insulin dose >40 units: Decrease insulin dose by 50% and initiate glyburide dose at 5 mg/day (regular) or 3 mg/day (micronized); increase glyburide dose by 1.25-2.5 mg (regular) or 0.75-1.5 mg/day (micronized); decrease insulin dose gradually, based on patient’s response as glyburide dose increased

Dosage Modifications

Renal impairment: If CrCl <50 mL/min; caution advised

Hepatic impairment: Use conservative initial and maintenance doses; avoid use in severe liver disease

Orphan Designations

Acute spinal cord injury

Acute subarachnoid hemorrhage

Acute ischemic stroke

Sponsor

  • Remedy Pharmaceuticals, Inc; 122 W. 27th Street 10th Floor; New York, NY 10001

Safety and efficacy not established

Type 2 Diabetes

Initial: 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 considerations

Because 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

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Interactions

Interaction Checker

and glyburide

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            Adverse Effects

            Frequency Not Defined

            Angioedema

            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

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            Warnings

            Contraindications

            Hypersensitivity; sulfa allergy

            Type 1 diabetes

            Diabetic ketoacidosis with or without coma

            Coadministration with bosentan; increased risk of hepatotoxicity

            Cautions

            Risk 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

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            Pregnancy & Lactation

            Pregnancy category: C

            Lactation: Not known if crosses into breast milk; avoid use in nursing women

            Pregnancy Categories

            A: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.

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            Pharmacology

            Mechanism of Action

            Initial effect is to increase beta-cell insulin secretion

            May also decrease rate of hepatic glucose production and increase insulin receptor sensitivity

            Absorption

            Bioavailability: 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)

            Distribution

            Protein bound: 99%

            Metabolism

            Metabolized extensively in the liver to less-active metabolites

            Metabolites: 4-trans-hydroxyglyburide, 3-cis-hydroxyglyburide (active)

            Elimination

            Half-life: 10 hr (DiaBeta); 4 hr (Glynase, PresTab)

            Excretion: Urine (50%), feces (50%)

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            Formulary

            FormularyPatient Discounts

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
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            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
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            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
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            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.