Glibenclamide

Source: Wikipedia, the free encyclopedia.
Not to be confused with gliclazide or glipizide.

Glibenclamide
Clinical data
Trade namesDiabeta, Glynase, Micronase, others[1]
Other namesGlyburide (USAN US)
AHFS/Drugs.comMonograph
MedlinePlusa684058
License data
Pregnancy
category
  • AU: C
Routes of
administration		By mouth
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)
  • US: ℞-only[2]
  • EU: Rx-only
Pharmacokinetic data
Protein bindingExtensive
MetabolismLiver hydroxylation (CYP2C9-mediated)
Elimination half-life10 hours
ExcretionKidney and bile duct
Identifiers
  • 5-chloro-N-[2-[4-(cyclohexylcarbamoylsulfamoyl)
    phenyl]ethyl]-2-methoxybenzamide
JSmol)
Melting point169 to 170 °C (336 to 338 °F)
SMILES
  • O=C(NC1CCCCC1)NS(=O)(=O)c2ccc(cc2)CCNC(=O)c3cc(Cl)ccc3OC
  • InChI=1S/C23H28ClN3O5S/c1-32-21-12-9-17(24)15-20(21)22(28)25-14-13-16-7-10-19(11-8-16)33(30,31)27-23(29)26-18-5-3-2-4-6-18/h7-12,15,18H,2-6,13-14H2,1H3,(H,25,28)(H2,26,27,29) checkY
  • Key:ZNNLBTZKUZBEKO-UHFFFAOYSA-N checkY
  (verify)

Glibenclamide, also known as glyburide, is an

antidiabetic medication.[1] It is not recommended for use by itself in type 1 diabetes.[1] It is taken by mouth.[1]

Common side effects include nausea and heartburn.

low blood sugar.[1] It is generally not recommended during pregnancy but can be used during breastfeeding.[3] It is in the sulfonylureas class of medications and works by increasing the release of insulin from the pancreas.[1]

Glibenclamide was discovered in 1969 and approved for medical use in the United States in 1984.

generic medication.[3] In 2021, it was the 214th most commonly prescribed medication in the United States, with more than 2 million prescriptions.[5][6]

Medical uses

Glibenclamide is used to lower the blood sugar level in patients with type 2 diabetes mellitus, which is not controlled by diet and exercise alone.

It is not as good as either metformin or insulin in those who have gestational diabetes.[7]


Side effects

Frequently reported side effects include: nausea, heartburn, weight gain, and bloating.[8] The medication is also a major cause of medication-induced hypoglycemia. The risk is greater than with other sulfonylureas.[9]

Contraindications

Glibenclamide may be not recommended in those with

G6PD deficiency, as it may cause acute hemolysis.[10]

Pregnancy and breastfeeding

It is generally not recommended during pregnancy but can be used during breastfeeding.[3]

Mechanism of action

The medication, a

voltage-dependent calcium Channels.[12]

This results in an increase in intracellular calcium in the pancreatic beta cell and subsequent stimulation of insulin release.[13]

After a stroke, the

endothelial cells[15] and by reactive microglia.[14]

According to the research, this and other sulphonylurea drugs also have extra hepatic effects. It works by inhibiting the enzyme Carnityl Acyl Transferase I (CAT-I) indirectly, which is present in the mitochondria. This prevents the transport of long chain fatty acids into the mitochondria for beta-oxidation. This prevents hyperglycemia for which it is prescribed.[16][17]

History

It was developed in 1966 in a cooperative study between

Sanofi-Aventis).[18]

Society and culture

Brand names

Glibenclamide is available as a generic medication, is manufactured by many pharmaceutical companies and is sold under many brand names including Gliben-J, Daonil,[19] Diabeta,[20] Euglucon, Gilemal, Glidanil, Glybovin, Glynase, Maninil, Micronase and Semi-Daonil. It is also available in a fixed-dose combination drug with metformin that is sold under various trade names, e.g. Bagomet Plus, Benimet, Glibomet, Gluconorm, Glucored, Glucovance, Metglib and many others.[21]

References

  1. ^ a b c d e f g h i j "Glyburide Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Archived from the original on 31 March 2019. Retrieved 18 March 2019.
  2. ^ "Glynase- glyburide tablet". DailyMed. 7 October 2017. Archived from the original on 6 October 2022. Retrieved 30 April 2022.
  3. ^
    ISBN 9780857113382
    .
  4. ISBN 9780470059135
    .
  5. ^ "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
  6. ^ "Glyburide - Drug Usage Statistics". ClinCalc. Archived from the original on 12 April 2020. Retrieved 14 January 2024.
  7. PMID 25609400
    .
  8. ^ "Glyburide: MedlinePlus Drug Information". MedlinePlus. Archived from the original on 14 April 2019. Retrieved 29 October 2019.
  9. PMID 17259518
    .
  10. S2CID 41227257
    .
  11. PMID 17015627
    .
  12. S2CID 242029244
    .
  13. ^ "Glyburide". Lexicomp. Wolters Kluwer N.V. Archived from the original on 2 June 2023. Retrieved 3 June 2023.
  14. ^
    S2CID 4828181
    .
  15. PMID 22714048
    .
  16. S2CID 25251669
    .
  17. S2CID 175394
    .
  18. S2CID 13181386
    .
  19. ^ "Daonil". News-Medical.net. Archived from the original on 26 June 2023. Retrieved 26 June 2023.
  20. ^ "DiaBeta (Glyburide Tablets): Uses, Dosage, Side Effects, Interactions, Warning". RxList. Archived from the original on 26 June 2023. Retrieved 26 June 2023.
  21. ^ "Glyburide and metformin". Lexicomp. Wolters Kluwer N.V. Archived from the original on 2 June 2023. Retrieved 3 June 2023.