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
III. Contraindication
- Sulfa Allergy (applies to sulonylureas)
- Renal and liver dysfunction
- Use caution with Sulfonylureas (especially Glyburide)
- Repaglinide or Nateglinide may be preferred here
- Avoid Glyburide in cardiovascular disease (and in general due to Hypoglycemia risk)
- Glimepiride and Glipizide do not appear to increase risk
IV. Mechanism
- Pancreatic beta cell stimulation for Insulin release
- Secretagogues do not burn out the beta cells sooner
V. Dosing Pearls
- Use Long acting agents
- Increase dose every 1-2 weeks until adequate response
- No response in 25-30% of Type II Diabetics
- Never combine secretagogues
- They all have same site of activity
- If one does not work, then all will not work
VI. Preparations: Glimepiride
- Glimepiride (Amaryl)
- Start: 1-2 mg orally daily
- Usual: 4 mg orally daily
- Maximum: 8 mg orally daily (doses above 4 mg daily, are unlikely to offer benefit)
- Advantages
- More rapid onset with longer duration
- Lower Incidence of Hypoglycemia than Glyburide, but greater risk than Glipizide
- Preferred of class for Coronary Artery Disease
VII. Preparations: Glipizide
- Glipizide (Glucotrol)
- Start: 5 mg orally daily
- Usual: 10-20 mg orally daily
- Maximum: 20 mg orally twice daily
- Glipizide Extended Release (Glucotrol XL)
- Start: 5 mg orally daily
- Usual: 5-10 mg orally daily
- Maximum: 20 mg orally daily (doses above 10 mg daily ER, are unlikely to offer benefit)
- Advantages: Least expensive Sulfonylurea
VIII. Preparations: Glyburide
- Precautions
- 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
- Glyburide should be avoided in renal dysfunction where GFR <50 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
- Glyburide (DiaBeta, Micronase)
- Start: 2.5 to 5 mg PO qd
- Usual: 5-20 mg PO qd
- Maximum: 20 mg PO qd
- Glyburide Micronized (Glynase, PresTab)
- Start: 1.5 to 3 mg PO qd
- Usual: 3-12 mg PO qd
- Maximum: 12 mg PO qd
IX. Adverse Effects
- Weight gain
-
Hypoglycemia
- Higher risk of severe Hypoglycemia with Glyburide than other Sulfonylureas
- See Drug Interactions below
X. Drug-interactions: Increased risk of Hypoglycemia with Sulfonylureas
- Chloramphenicol
- Clarithromycin
- Fibrates
- Fluconazole
- Fluoroquinolones (esp. Gatifloxacin)
- H2 Receptor Antagonists
- Miconazole
- Phenylbutazone
- Sulfonamide
- Verapamil
- References
XI. References
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| Glipizide (on 6/18/2017 at Walmart.com) | ||
| Glipizide 10mg | #60 tablets for $4.00 | $0.07 each |
| Glipizide 10mg | #180 tablets for $10.00 | $0.06 each |
| Glipizide 5mg | #30 tablets for $4.00 | $0.13 each |
| Glipizide 5mg | #90 tablets for $10.00 | $0.11 each |
| Glyburide (on 6/18/2017 at Walmart.com) | ||
| Glyburide 2.5mg | #30 tablets for $4.00 | $0.13 each |
| Glyburide 2.5mg | #90 tablets for $10.00 | $0.11 each |
| Glyburide 5mg (blue) | #30 tablets for $4.00 | $0.13 each |
| Glyburide 5mg (blue) | #90 tablets for $10.00 | $0.11 each |
| Glyburide 5mg (green) | #30 tablets for $4.00 | $0.13 each |
| Glyburide 5mg (green) | #90 tablets for $10.00 | $0.11 each |
| Glyburide, micronized (on 6/18/2017 at Walmart.com) | ||
| Glyburide, micronized 3mg | #30 tablets for $4.00 | $0.13 each |
| Glyburide, micronized 3mg | #90 tablets for $10.00 | $0.11 each |
| Glyburide, micronized 6mg | #30 tablets for $4.00 | $0.13 each |
| Glyburide, micronized 6mg | #90 tablets for $10.00 | $0.11 each |
| Glimepiride (on 6/18/2017 at Walmart.com) | ||
| Glimepiride 1mg | #30 tablets for $4.00 | $0.13 each |
| Glimepiride 1mg | #90 tablets for $10.00 | $0.11 each |
| Glimepiride 2mg | #30 tablets for $4.00 | $0.13 each |
| Glimepiride 2mg | #90 tablets for $10.00 | $0.11 each |
| Glimepiride 4mg | #30 tablets for $4.00 | $0.13 each |
| Glimepiride 4mg | #90 tablets for $10.00 | $0.11 each |
| glipizide (on 3/22/2017 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| GLIPIZIDE 10 MG TABLET | Generic | $0.04 each |
| GLIPIZIDE 5 MG TABLET | Generic | $0.03 each |
| GLIPIZIDE ER 10 MG TABLET | Generic | $0.27 each |
| GLIPIZIDE ER 2.5 MG TABLET | Generic | $0.20 each |
| GLIPIZIDE ER 5 MG TABLET | Generic | $0.15 each |
| GLIPIZIDE XL 10 MG TABLET | Generic | $0.27 each |
| GLIPIZIDE XL 2.5 MG TABLET | Generic | $0.20 each |
| GLIPIZIDE XL 5 MG TABLET | Generic | $0.15 each |
| GLIPIZIDE-METFORMIN 2.5-250 MG | Generic | $0.44 each |
| GLIPIZIDE-METFORMIN 2.5-500 MG | Generic | $0.46 each |
| GLIPIZIDE-METFORMIN 5-500 MG | Generic | $0.43 each |
| glyburide (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| GLYBURIDE 1.25 MG TABLET | Generic | $0.11 each |
| GLYBURIDE 2.5 MG TABLET | Generic | $0.11 each |
| GLYBURIDE 5 MG TABLET | Generic | $0.13 each |
| GLYBURIDE MICRO 3 MG TABLET | Generic | $0.06 each |
| GLYBURIDE MICRO 6 MG TABLET | Generic | $0.16 each |
| GLYBURIDE-METFORMIN 1.25 MG-250 MG TABLET | Generic | $0.06 each |
| GLYBURIDE-METFORMIN 2.5-500 MG | Generic | $0.06 each |
| GLYBURIDE-METFORMIN 5-500 MG | Generic | $0.06 each |
| glimepiride (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| GLIMEPIRIDE 1 MG TABLET | Generic | $0.05 each |
| GLIMEPIRIDE 2 MG TABLET | Generic | $0.07 each |
| GLIMEPIRIDE 4 MG TABLET | Generic | $0.10 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 |
Ontology: Glipizide (C0017642)
| Definition (NCI) | A short-acting, second-generation sulfonylurea with hypoglycemic activity. Glipizide is rapidly absorbed, has a very quick onset of action and a short half-life. This agent is extensively metabolized in the liver and the metabolites as well as the unchanged form are excreted in the urine. |
| Definition (MSH) | An oral hypoglycemic agent which is rapidly absorbed and completely metabolized. |
| Definition (CSP) | 1-cyclohexyl-3-(p-(2-(5-methyl pyrazinecarboxamido) ethyl) phenyl) sulfonylurea; a typical member of the sulfonylurea family of type II (NIDDM) antidiabetic drugs. |
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | D005913 |
| SnomedCT | 26124005, 387143009 |
| LNC | LP14719-6, MTHU001811 |
| English | Glidiazinamide, Glipizide, Glydiazinamide, Glypidizine, Pyrazinecarboxamide, N-(2-(4-((((cyclohexylamino)carbonyl)amino)sulfonyl)phenyl)ethyl)-5-methyl-, glipizide, GLIPIZIDE, glipizide (medication), Glipizide [Chemical/Ingredient], glipiZIDE, Glipizide product, Glipizide (product), Glipizide (substance), GlipiZIDE |
| Swedish | Glipizid |
| Czech | glipizid |
| Finnish | Glipitsidi |
| Russian | GLIPIZID, ГЛИПИЗИД |
| Japanese | グリピジジン, グリジアジンアミド, グリピジド |
| Polish | Glipizyd |
| Spanish | glidiacinamida, glidiazinamida, glipicida (sustancia), glipicida, glipizida (producto), glipizida (sustancia), glipizida, Glidiacinamida, Glipidicina, Glipizida |
| French | Glipizide |
| German | Glidiazinamid, Glipizidum, Glipizid, Glydiazinamid, Glypidizin |
| Italian | Glipizide |
| Portuguese | Glidiazinamida, Glipidizina, Glipizida |
Ontology: glimepiride (C0061323)
| Definition (NCI) | A long-acting, third-generation sulfonylurea with hypoglycemic activity. Compared to other generations of sulfonylurea compounds, glimepiride is very potent and has a longer duration of action. This agent is metabolized by CYP2C9 and shows peroxisome proliferator-activated receptor gamma (PPARgamma) agonistic activity. |
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | C057619 |
| SnomedCT | 109079009, 386966003 |
| LNC | LP35577-3, MTHU018302 |
| English | 1-(4-(2-(3-ethyl-4-methyl-2-oxo-3-pyrrolinecarboxamido)ethyl)phenylsulfonyl)-3-(4-methylcyclohexyl)urea, glimepiride, glimepiride (medication), glymepiride, GLIMEPIRIDE, glimepiride [Chemical/Ingredient], Glimepiride, Glimepiride (product), Glimepiride (substance) |
| Spanish | glimepirida (producto), glimepirida (sustancia), glimepirida |
Ontology: Amaryl (C0595112)
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | C057619 |
| English | Amaryl, amaryl, Amarel, Aventis Behring brand of glimepiride, Aventis Pharma brand of glimepiride, Aventis brand of glimepiride, Hoechst brand of glimepiride |
Ontology: Second generation sulfonylurea (C1300198)
| Concepts | Organic Chemical (T109) , Pharmacologic Substance (T121) |
| SnomedCT | 386050002 |
| English | Second generation sulfonylurea (product), Second generation sulfonylurea, Second generation sulphonylurea |
| Spanish | sulfonilurea de segunda generación (producto), sulfonilurea de segunda generación |
