Glibenclamide

Glibenclamide, also known as glyburide, is a medication used to treat diabetes mellitus type 2.[1] It is recommended that it be taken together with diet and exercise.[1] It may be used with other antidiabetic medication.[1] It is not recommended for use by itself in diabetes mellitus type 1.[1] It is taken by mouth.[1]

Not to be confused with gliclazide or glipizide.
Glibenclamide
Clinical data
Trade namesDiabeta, Flycron, others[1]
Other namesGlyburide (USAN US)
AHFS/Drugs.comMonograph
MedlinePlusa684058
License data
Pregnancy
category
  • AU: C
  • US: B (No risk in non-human studies)
    Routes of
    administration    		By mouth
    ATC code
    Legal status
    Legal status
    Pharmacokinetic data
    Protein bindingExtensive
    MetabolismLiver hydroxylation (CYP2C9-mediated)
    Elimination half-life10 hours
    ExcretionKidney and biliary
    Identifiers
    CAS Number
    PubChem CID
    IUPHAR/BPS
    DrugBank
    ChemSpider
    UNII
    KEGG
    ChEBI
    ChEMBL
    CompTox Dashboard (EPA)
    ECHA InfoCard100.030.505
    Chemical and physical data
    FormulaC23H28ClN3O5S
    Molar mass494.004 g/mol g·mol−1
    3D model (JSmol)
    Melting point169 to 170 °C (336 to 338 °F)
      (verify)

    Common side effects include nausea and heartburn.[1] Serious side effects may include angioedema and low blood sugar.[1] It is generally not recommended during pregnancy but can be used during breastfeeding.[2] 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.[3][1] It is available as a generic medication.[2] A month supply in the United Kingdom costs the NHS about £3.20 as of 2019.[2] In the United States the wholesale cost of this amount is about $2.50.[4] In 2016, it was the 172nd most prescribed medication in the United States, with more than 3 million prescriptions.[5]

    Medical uses

    It is used in the treatment of type 2 diabetes.

    It is not as good as either metformin or insulin in those who have gestational diabetes.[6]

    Side effects

    Frequently reported side effects include: nausea, heartburn, weight gain, and bloating.[7] The medication is also a major cause of medication-induced hypoglycemia. The risk is greater than with other sulfonylureas.[8] Cholestatic jaundice is noted.

    Glibenclamide may be not recommended in those with G6PD deficiency, as it may cause acute hemolysis.[9]

    Pregnancy and breastfeeding

    It is generally not recommended during pregnancy but can be used during breastfeeding.[2]

    Mechanism of action

    The medication works by binding to and inhibiting the ATP-sensitive potassium channels (KATP) inhibitory regulatory subunit sulfonylurea receptor 1 (SUR1)[10] in pancreatic beta cells. This inhibition causes cell membrane depolarization, opening voltage-dependent calcium channels. This results in an increase in intracellular calcium in the pancreatic beta cell and subsequent stimulation of insulin release.

    After a cerebral ischemic insult, the blood–brain barrier is broken and glibenclamide can reach the central nervous system. Glibenclamide has been shown to bind more efficiently to the ischemic hemisphere.[11] Moreover, under ischemic conditions SUR1, the regulatory subunit of the KATP- and the NCCa-ATP-channels, is expressed in neurons, astrocytes, oligodendrocytes, endothelial cells[12] and by reactive microglia.[11]

    History

    It was developed in 1966 in a cooperative study between Boehringer Mannheim (now part of Roche) and Hoechst (now part of Sanofi-Aventis).[13]

    Trade names

    Glibenclamide is available as a generic, is manufactured by many pharmaceutical companies and is sold in doses of 1.25, 2.5 and 5 mg under many brand names including Gliben-J, Daonil, Diabeta, 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.

    References
    1. "Glyburide Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 18 March 2019.
    2. British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 692. ISBN 9780857113382.
    3. Diabetes in Clinical Practice: Questions and Answers from Case Studies. John Wiley & Sons. 2007. p. 342. ISBN 9780470059135.
    4. "NADAC as of 2019-02-27". Centers for Medicare and Medicaid Services. Retrieved 3 March 2019.
    5. "The Top 300 of 2019". clincalc.com. Retrieved 22 December 2018.
    6. Balsells, M; García-Patterson, A; Solà, I; Roqué, M; Gich, I; Corcoy, R (21 January 2015). "Glibenclamide, metformin, and insulin for the treatment of gestational diabetes: a systematic review and meta-analysis". BMJ (Clinical Research Ed.). 350: h102. doi:10.1136/bmj.h102. PMC 4301599. PMID 25609400.
    7. "Glyburide: MedlinePlus Drug Information". medlineplus.gov. Retrieved 29 October 2019.
    8. Gangji, A. S.; Cukierman, T.; Gerstein, H. C.; Goldsmith, C. H.; Clase, C. M. (1 February 2007). "A Systematic Review and Meta-Analysis of Hypoglycemia and Cardiovascular Events: A comparison of glyburide with other secretagogues and with insulin". Diabetes Care. 30 (2): 389–394. doi:10.2337/dc06-1789. PMID 17259518.
    9. Meloni G, Meloni T (January 1996). "Glyburide-induced acute haemolysis in a G6PD-deficient patient with NIDDM". Br. J. Haematol. 92 (1): 159–60. doi:10.1046/j.1365-2141.1996.275810.x. PMID 8562390.
    10. Serrano-Martín X, Payares G, Mendoza-León A (December 2006). "Glibenclamide, a blocker of K+(ATP) channels, shows antileishmanial activity in experimental murine cutaneous leishmaniasis". Antimicrob. Agents Chemother. 50 (12): 4214–6. doi:10.1128/AAC.00617-06. PMC 1693980. PMID 17015627.
    11. Ortega FJ, Gimeno-Bayon J, Espinosa-Parrilla JF, Carrasco JL, Batlle M, Pugliese M, Mahy N, Rodríguez MJ (May 2012). "ATP-dependent potassium channel blockade strengthens microglial neuroprotection after hypoxia-ischemia in rats" (PDF). Exp. Neurol. 235 (1): 282–96. doi:10.1016/j.expneurol.2012.02.010. hdl:2445/34278. PMID 22387180.
    12. Simard JM, Woo SK, Schwartzbauer GT, Gerzanich V (September 2012). "Sulfonylurea receptor 1 in central nervous system injury: a focused review". J. Cereb. Blood Flow Metab. 32 (9): 1699–717. doi:10.1038/jcbfm.2012.91. PMC 3434627. PMID 22714048.
    13. Marble A (1971). "Glibenclamide, a new sulphonylurea: whither oral hypoglycaemic agents?". Drugs. 1 (2): 109–15. doi:10.2165/00003495-197101020-00001. PMID 4999930.

    This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.