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Glibenclamide response

MedGen UID:
1104724
Concept ID:
CN437679
Sign or Symptom
Synonyms: Glybenclamide response; Glyburide response
Drug:
Glibenclamide
MedGen UID:
6612
Concept ID:
C0017628
Pharmacologic Substance
A sulfonamide urea derivative with antihyperglycemic activity that can potentially be used to decrease cerebral edema. Upon administration, glyburide binds to and blocks the sulfonylurea receptor type 1 (SUR1) subunit of the ATP-sensitive inwardly-rectifying potassium (K(ATP)) channels on the membranes of pancreatic beta cells. This prevents the inward current flow of positively charged potassium (K+) ions into the cell, and induces a calcium ion (Ca2+) influx through voltage-sensitive calcium channels, which triggers exocytosis of insulin-containing granules. In addition, glyburide also inhibits the SUR1-regulated nonselective cation (NC) Ca-ATP channel, melastatin 4 (transient receptor potential cation channel subfamily M member 4; (TRPM4)), thereby preventing capillary failure and brain swelling. SUR1-TRPM4 channels are formed by co-assembly of SUR1 with TRPM4 in neurons, astrocytes, and capillary endothelium during cerebral ischemia. Upon ischemia-induced ATP depletion, channels open which results in sodium influx, cytotoxic edema formation, capillary fragmentation and necrotic cell death. SUR1-TRPM4 is not expressed in normal, uninjured tissues. [from NCI]
 
Gene (location): G6PD (Xq28)

Professional guidelines

PubMed

Tomlinson B, Li YH, Chan P
Expert Opin Pharmacother 2022 Dec;23(17):1869-1877. Epub 2022 Nov 10 doi: 10.1080/14656566.2022.2141108. PMID: 36300277
Safouris A, Magoufis G, Tsivgoulis G
Expert Opin Investig Drugs 2021 Oct;30(10):1025-1035. Epub 2021 Oct 13 doi: 10.1080/13543784.2021.1985463. PMID: 34555978
Balsells M, García-Patterson A, Solà I, Roqué M, Gich I, Corcoy R
BMJ 2015 Jan 21;350:h102. doi: 10.1136/bmj.h102. PMID: 25609400Free PMC Article

Curated

Gammal et al, Expanded Clinical Pharmacogenetics Implementation Consortium Guideline for Medication Use in the Context of G6PD Genotype. 2 Sept 2022. Clin Pharmacol Ther.

DailyMed Drug Label, GLYBURIDE, 2019

DailyMed Drug Label, glibenclamide, 2017

Supplemental Content

Table of contents

    Clinical resources

    Practice guidelines

    • PubMed
      See practice and clinical guidelines in PubMed. The search results may include broader topics and may not capture all published guidelines. See the FAQ for details.

    Curated

    • CPIC, 2022
      Gammal et al, Expanded Clinical Pharmacogenetics Implementation Consortium Guideline for Medication Use in the Context of G6PD Genotype. 2 Sept 2022. Clin Pharmacol Ther.
    • DailyMed Drug Label, 2019
      DailyMed Drug Label, GLYBURIDE, 2019
    • DailyMed Drug Label, 2017
      DailyMed Drug Label, glibenclamide, 2017

    Consumer resources

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