Dosing & Uses
Dosage Forms & Strengths
tablet
- 1.25mg
- 2.5mg
- 5mg
tablet, micronized
- 1.5mg
- 3mg
- 5mg
- 6mg
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
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
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
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
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.
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%)
Images
Patient Handout
Formulary
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