Glipizide

Glipizide
Clinical data
Trade names Glucotrol
AHFS/Drugs.com Monograph
MedlinePlus a684060
Pregnancy
category
  • AU: C
  • US: C (Risk not ruled out)
    Routes of
    administration
    Oral
    ATC code
    Legal status
    Legal status
    Pharmacokinetic data
    Bioavailability 100% (regular formulation)
    90% (extended release)
    Protein binding 98 to 99%
    Metabolism Hepatic hydroxylation
    Elimination half-life 2 to 5 hours
    Excretion Renal and fecal
    Identifiers
    CAS Number
    PubChem CID
    IUPHAR/BPS
    DrugBank
    ChemSpider
    UNII
    KEGG
    ChEBI
    ChEMBL
    ECHA InfoCard 100.044.919 Edit this at Wikidata
    Chemical and physical data
    Formula C21H27N5O4S
    Molar mass 445.536 g/mol
    3D model (JSmol)
    Melting point 208 to 209 °C (406 to 408 °F)
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    Glipizide is an oral rapid- and short-acting anti-diabetic medication from the sulfonylurea class. It is classified as a second-generation sulfonylurea, which means that it undergoes enterohepatic circulation. Second-generation sulfonylureas are both more potent and have shorter half-lives than the first-generation sulfonylureas.

    Originally available in 1984, it is marketed by Pfizer under the brand name Glucotrol in the USA, where Pfizer sells Glucotrol in doses of 5 and 10 milligrams and Glucotrol XL (an extended release form of glipizide) in doses of 2.5, 5, and 10 milligrams. Other companies also market glipizide, most commonly extended release tablets of 5 and 10 milligrams.

    Mechanism of action

    Glipizide sensitizes the beta cells of pancreatic islets of Langerhans insulin response, meaning that more insulin is released in response to glucose than would be without glipizide ingestion[1]. Glipizide acts by partially blocking potassium channels among beta cells of pancreatic islets of Langerhans. By blocking potassium channels, the cell depolarizes, which results in the opening of voltage-gated calcium channels. The resulting calcium influx encourages insulin release from beta cells. [2]

    See also

    References

    1. Drugs@FDA (the official database of FDA-approved drugs) https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/020329s025lbl.pdf
    2. LH Bösenberg & DG van Zyl (2008) The mechanism of action of oral antidiabetic drugs: A review of recent literature, Journal of Endocrinology, Metabolism and Diabetes of South Africa, 13:3, 80-88, DOI: 10.1080/22201009.2008.1087217
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