Pharm

Glyburide

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Glyburide, Glynase, DiaBeta

  • See Also
  1. Second Generation Sulfonylurea
  2. Oral Hypoglycemic Agents
  3. Glipizide
  4. Glimepiride
  1. Better effect in lean patients
  2. Consider when Hemoglobin A1C <9%
  3. Second-line to Metformin in most patients
  4. Consider as first-line in specific cohorts
    1. Consider when post-prandial Glucose 200 to 300 mg/dl
    2. Consider when Type II with Polyuria, polydipsia
  5. Other Sulfonylureas are preferred over Glyburide
    1. Glipizide may be preferred instead due to increased risks of Hypoglycemia associated with Glyburide, Glimepiride
      1. Other agents are generic (no cost advantage to Glyburide)
    2. Glyburide has been associated with worse cardiovascular outcomes in patients presenting for emergent PCI
      1. Jørgensen (2011) Int J Cardiol 152:327-331 [PubMed]
    3. Glyburide appears to predispose to more severe Hypoglycemia than the other Second Generation Sulfonylureas
      1. Avoid in older adults
      2. Glyburide should be avoided in renal dysfunction where GFR <50-60 mL/min (increases hypglycemia risk)
      3. Glyburide should be avoided in severe hepatic dysfunction (increases Hypoglycemia risk)
      4. Gangji (2007) Diabetes Care 30:389-94 [PubMed]
  • Contraindications
  1. Sulfa Allergy (applies to Sulfonylureas)
  2. Renal and liver dysfunction
    1. Use caution with Sulfonylureas (especially Glyburide)
    2. Repaglinide or Nateglinide may be preferred here
    3. Avoid most Sulfonylureas when GFR <60 ml/min (higher risk of Hypoglycemia)
      1. GlipizideHalf-Life is not impacted by lower GFR and is safer to use in low GFR
  3. Avoid Glyburide in cardiovascular disease (and in general due to Hypoglycemia risk)
    1. Glimepiride and Glipizide do not appear to increase risk
  • Mechanism
  1. Sulfonylureas trigger Insulin release from pancreatic beta cells
    1. Sulfonylureas stimulate Potassium channel closure on pancreatic beta cell surface
    2. Secretagogues do NOT burn out the beta cells sooner
  2. Sulfonylureas may also increase tissue Insulin sensitivity
  • Medications
  1. Glyburide (DiaBeta, Micronase) 1.25 mg, 2.5 mg, 5 mg
  2. Glyburide Micronized (Glynase, PresTab) 1.5 mg, 3 mg, 6 mg
  • Dosing
  1. General
    1. Increase dose every 1-2 weeks until adequate response
    2. No response to Sulfonylureas in 25-30% of Type II Diabetics
    3. Long acting Sulfonylureas are preferred
  2. Glyburide (DiaBeta, Micronase)
    1. Start: 2.5 to 5 mg orally daily with breakfast
      1. Start at 1.25 mg orally daily in elderly, renal or hepatic insufficiency, malnourished
    2. Titrate at a maximum of 2.5 mg weekly (or less often)
    3. Usual: 5-20 mg orally daily
    4. Maximum: 20 mg orally daily
      1. Maximum effective dose: 10 mg/day
  3. Glyburide Micronized (Glynase, PresTab)
    1. Start: 1.5 to 3 mg orally daily with breakfast
      1. Start 0.75 mg orally daily in elderly, renal or hepatic insufficiency, malnourished
    2. Titrate at a maximum of 1.5 mg weekly (or less often)
    3. Usual: 3-12 mg orally daily
    4. Maximum: 12 mg orally daily
      1. Consider dividing dose twice daily if >6 mg/day
  • Adverse Effects
  1. See Sulfonylurea Poisoning
  2. Hemolytic Anemia in G6PD Deficiency Risk
  3. Weight gain
  4. Hypoglycemia
    1. See Sulfonylurea Drug Interactions Causing Hypoglycemia
    2. Higher risk of severe Hypoglycemia with Glyburide than other Sulfonylureas
    3. Hypoglycemia risk increases with lower GFR
    4. Glyburide appears to predispose to more severe Hypoglycemia than the other Second Generation Sulfonylureas
      1. Avoid in older adults
      2. Glyburide should be avoided in renal dysfunction where GFR <50-60 mL/min (increases hypglycemia risk)
      3. Glyburide should be avoided in severe hepatic dysfunction (increases Hypoglycemia risk)
      4. Gangji (2007) Diabetes Care 30:389-94 [PubMed]
  5. Cardiovascular Disease
    1. Glyburide has been associated with worse cardiovascular outcomes in patients presenting for emergent PCI
    2. Does not appear to be at increased risk with Sulfonylureas overall
      1. However, avoid Glyburide in cardiovascular disease (and in general due to Hypoglycemia risk)
    3. Glimepiride and Glipizide appear to be neutral in their Cardiovascular Risk effects
      1. Contrast with GLP-1 Agonists and SGLT2 Inhibitors which reduce Cardiovascular Risk
    4. References
      1. (2019) presc lett 26(12): 71
      2. Jørgensen (2011) Int J Cardiol 152:327-331 [PubMed]
  • Safety
  1. Unknown safety in Lactation
  2. Unknown safety in pregnancy
    1. Discontinue at least 2 weeks before delivery (risk of Neonatal Hypoglycemia)
  • Drug Interactions
  1. See Sulfonylurea Drug Interactions Causing Hypoglycemia
  2. Never combine Insulin Secretagogues (Sulfonylureas or Meglitinides)
    1. They all have same site of activity
    2. If one does not work, then all will not work
  • Efficacy
  1. Sulfonylurea effects as a class
    1. Lower Hemoglobin A1C 0.8 to 1.5%
    2. Do not affect all-cause mortality
  • Resources
  1. Glyburide (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=a56f100f-0f42-4188-81ab-04644b824040
  • References
  1. (2017) Presc Lett 25(1): 1-2
  2. Defronzo (1999) Ann Intern Med 131:281-303 [PubMed]
  3. Gangji (2007) Diabetes Care 30:389-94 [PubMed]
  4. Luna (1999) Prim Care 26:895-915 [PubMed]
  5. Vaughan (2024) Am Fam Physician 109(4): 333-42 [PubMed]