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
Images: Related links to external sites (from Bing)
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 |
Ontology: Glyburide (C0017628)
Definition (NCI) | A highly protein bound, longer-acting second-generation sulfonylurea with antihyperglycemic activity. Glyburide, also called glibenclamide, is more likely to cause hypoglycemic episodes due to its longer half-life and possible displacement by other highly protein bound drugs. This agent is metabolized into two inactive metabolites which are excreted in the bile and urine. This agent shows peroxisome proliferator-activated receptor gamma (PPARgamma) agonistic activity. |
Definition (MSH) | An antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide. |
Definition (CSP) | N-4-beta-(2-methoxy-5-chlorobenzamido) -ethylbenzosulfonyl-N'- cyclohexylurea; hypoglycemic used against non-insulin dependent diabetes mellitus; thought to act by increasing insulin receptor expression in target tissues. |
Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
MSH | D005905 |
SnomedCT | 384978002, 80870001, 387466004 |
LNC | LP14720-4, MTHU001812 |
English | Glibenclamide, Glybenclamide, Benzamide, 5-chloro-N-(2-(4-((((cyclohexylamino)carbonyl)amino)sulfonyl)phenyl)ethyl)-2-methoxy-, glyburide, Glyburide, Gyburide, Glyburide (substance), glyburide (medication), GLYBURIDE, Glyburide [Chemical/Ingredient], glybenclamide, glyBURIDE, glibenclamide, Glybenzcyclamide, Glyburide (product), Glibenclamide (substance), GlyBURIDE |
Swedish | Glyburid |
Czech | glibenklamid |
Finnish | Glyburidi |
German | Glyburid, Glibenclamid, Glybencylamid |
Russian | GLIBURID, GLIBENKLAMID, ГЛИБЕНКЛАМИД, ГЛИБУРИД |
Croatian | GLIBURID |
Polish | Euclamin, Glyburide, Glibenklamid |
Japanese | グリベンクラミド, グリブリド |
Spanish | gliburida (sustancia), glibenclamida (producto), glibenclamida (sustancia), glibenclamida, glibenzciclamida, gliburida, Glibenclamida, Gliburida |
French | Glibenclamide |
Italian | Gliburide |
Portuguese | Glibenclamida, Glibureto |