II. Indications: Type II Diabetes Mellitus (early, phase 1-2)
- Better effect in lean patients
- Consider when Hemoglobin A1C <9%
- Second-line to Metformin in most patients
- Consider as first-line in specific cohorts
- Other Sulfonylureas are preferred over Glyburide
- Glipizide may be preferred instead due to increased risks of Hypoglycemia associated with Glyburide, Glimepiride
- Other agents are generic (no cost advantage to Glyburide)
- Glyburide has been associated with worse cardiovascular outcomes in patients presenting for emergent PCI
- Glyburide appears to predispose to more severe Hypoglycemia than the other Second Generation Sulfonylureas
- Avoid in older adults
- Glyburide should be avoided in renal dysfunction where GFR <50-60 mL/min (increases hypglycemia risk)
- Glyburide should be avoided in severe hepatic dysfunction (increases Hypoglycemia risk)
- Gangji (2007) Diabetes Care 30:389-94 [PubMed]
- Glipizide may be preferred instead due to increased risks of Hypoglycemia associated with Glyburide, Glimepiride
III. Contraindications
- Sulfa Allergy (applies to Sulfonylureas)
- Renal and liver dysfunction
- Use caution with Sulfonylureas (especially Glyburide)
- Repaglinide or Nateglinide may be preferred here
- Avoid most Sulfonylureas when GFR <60 ml/min (higher risk of Hypoglycemia)
- Avoid Glyburide in cardiovascular disease (and in general due to Hypoglycemia risk)
- Glimepiride and Glipizide do not appear to increase risk
IV. Mechanism
-
Sulfonylureas trigger Insulin release from pancreatic beta cells
- Sulfonylureas stimulate Potassium channel closure on pancreatic beta cell surface
- Secretagogues do NOT burn out the beta cells sooner
- Sulfonylureas may also increase tissue Insulin sensitivity
V. Medications
- Glyburide (DiaBeta, Micronase) 1.25 mg, 2.5 mg, 5 mg
- Glyburide Micronized (Glynase, PresTab) 1.5 mg, 3 mg, 6 mg
VI. Dosing
-
General
- Increase dose every 1-2 weeks until adequate response
- No response to Sulfonylureas in 25-30% of Type II Diabetics
- Long acting Sulfonylureas are preferred
- Glyburide (DiaBeta, Micronase)
- Start: 2.5 to 5 mg orally daily with breakfast
- Start at 1.25 mg orally daily in elderly, renal or hepatic insufficiency, malnourished
- Titrate at a maximum of 2.5 mg weekly (or less often)
- Usual: 5-20 mg orally daily
- Maximum: 20 mg orally daily
- Maximum effective dose: 10 mg/day
- Start: 2.5 to 5 mg orally daily with breakfast
- Glyburide Micronized (Glynase, PresTab)
- Start: 1.5 to 3 mg orally daily with breakfast
- Start 0.75 mg orally daily in elderly, renal or hepatic insufficiency, malnourished
- Titrate at a maximum of 1.5 mg weekly (or less often)
- Usual: 3-12 mg orally daily
- Maximum: 12 mg orally daily
- Consider dividing dose twice daily if >6 mg/day
- Start: 1.5 to 3 mg orally daily with breakfast
VII. Adverse Effects
- See Sulfonylurea Poisoning
- Hemolytic Anemia in G6PD Deficiency Risk
- Weight gain
-
Hypoglycemia
- See Sulfonylurea Drug Interactions Causing Hypoglycemia
- Higher risk of severe Hypoglycemia with Glyburide than other Sulfonylureas
- Hypoglycemia risk increases with lower GFR
- Glyburide appears to predispose to more severe Hypoglycemia than the other Second Generation Sulfonylureas
- Avoid in older adults
- Glyburide should be avoided in renal dysfunction where GFR <50-60 mL/min (increases hypglycemia risk)
- Glyburide should be avoided in severe hepatic dysfunction (increases Hypoglycemia risk)
- Gangji (2007) Diabetes Care 30:389-94 [PubMed]
- Cardiovascular Disease
- Glyburide has been associated with worse cardiovascular outcomes in patients presenting for emergent PCI
- Does not appear to be at increased risk with Sulfonylureas overall
- However, avoid Glyburide in cardiovascular disease (and in general due to Hypoglycemia risk)
- Glimepiride and Glipizide appear to be neutral in their Cardiovascular Risk effects
- Contrast with GLP-1 Agonists and SGLT2 Inhibitors which reduce Cardiovascular Risk
- References
- (2019) presc lett 26(12): 71
- Jørgensen (2011) Int J Cardiol 152:327-331 [PubMed]
VIII. Safety
- Unknown safety in Lactation
- Unknown safety in pregnancy
- Discontinue at least 2 weeks before delivery (risk of Neonatal Hypoglycemia)
IX. Drug Interactions
- See Sulfonylurea Drug Interactions Causing Hypoglycemia
- Never combine Insulin Secretagogues (Sulfonylureas or Meglitinides)
- They all have same site of activity
- If one does not work, then all will not work
X. Efficacy
-
Sulfonylurea effects as a class
- Lower Hemoglobin A1C 0.8 to 1.5%
- Do not affect all-cause mortality
XI. Resources
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Related Studies
| glyburide (on 6/21/2023 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| GLYBURIDE 1.25 MG TABLET | Generic | $0.07 each |
| GLYBURIDE 2.5 MG TABLET | Generic | $0.09 each |
| GLYBURIDE 5 MG TABLET | Generic | $0.06 each |
| GLYBURIDE MICRO 3 MG TABLET | Generic | $0.15 each |
| GLYBURIDE MICRO 6 MG TABLET | Generic | $0.20 each |
| GLYBURIDE-METFORMIN 2.5-500 MG | Generic | $0.04 each |
| GLYBURIDE-METFORMIN 5-500 MG | Generic | $0.05 each |