Dosing and uses of Diabeta, Glynase (glyburide)
Adult dosage forms and 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
Spinal Cord Injury (Orphan)
Orphan designation for treatment of acute spinal cord injury
Sponsor
- Remedy Pharmaceuticals, Inc; 122 W. 27th Street 10th Floor; New York, NY 10001
Subarachnoid Hemorrhage (Orphan)
Orphan designation for treatment of acute subarachnoid hemorrhage
Sponsor
- Remedy Pharmaceuticals, Inc; 122 W. 27th Street 10th Floor; New York, NY 10001
Pediatric dosage forms and strengths
Safety and efficacy not established
Geriatric dosage forms and strengths
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
Diabeta, Glynase (glyburide) adverse (side) 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
Warnings
Contraindications
Hypersensitivity; sulfa allergy
Type 1 diabetes
Diabetic ketoacidosis
Coadministration with bosentan; increased risk of hepatotoxicity
Cautions
Patients with risk of severe hypoglycemia: Elderly, debilitated, or malnourished or with adrenal or pituitary insufficiency
Patients with stress due to infection, fever, trauma, or surgery
Caution in hepatic or renal insufficiency
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
Hemolytic anemia may occur with glucose 6-phosphate dehydrogenase (G6PD) deficiency when treated with sulfonylurea agents
There are no clinical studies establishing conclusive evidence of macrovascular risk reduction with anti-diabetic drugs
All sulfonylureas are capable of producing severe hypoglycemia
Pregnancy and 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 of Diabeta, Glynase (glyburide)
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%)
