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ES - Gliclazide

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Gliclazide

GENERAL DRUG CLASSIFICATION: CNS-Neurogenerative disease drugs-Cholinesterase inhibitor


CHEMICAL NAME: 1-(4-methylbenzenesulfonyl)-3-{octahydrocyclopenta[c]pyrrol-2-yl}urea
[1]

GENERIC NAME: Gliclazide[1]


BRAND NAME: Azukon MR [2]
INDICATIONS: For the treatment of NIDDM in conjunction with diet and exercise. (2)
PHARMACOKINETICS: Absorption: Rapidly and well absorbed but may have wide inter-
and intra-individual variability. Peak plasma concentrations occur
within 4-6 hours of oral administration. [1]

Distribution: plasma protein binding approximately 94-95 %. [2]

Metabolism: Extensively metabolized in the liver. Less than 1% of the


orally administered dose appears unchanged in the urine. Metabolites
include oxidized and hydroxylated derivates, as well as glucuronic acid
conjugates. [1]

Excretion: Metabolites and conjugates are eliminated primarily by the


kidneys (60-70%) and also in the feces (10-20%).[1]
PHARMACODYNAMICS: Gliclazide binds to the β cell sulfonyl urea receptor (SUR1). This binding
subsequently blocks the ATP sensitive potassium channels. The binding
results in closure of the channels and leads to a resulting decrease in
potassium efflux leads to depolarization of the β cells. This opens
voltage-dependent calcium channels in the β cell resulting in calmodulin
activation, which in turn leads to exocytosis of insulin containing
secretorty granules. [1]
DRUG INTERACTIONS: May increase hypoglycaemic effect w/ phenylbutazone. [2]

Potentiation of blood glucose lowering effect w/ other antidiabetics


(e.g. acarbose, insulins, metformin), β-blockers, ACE inhibitors, H 2-
receptor antagonists, MAOIs, sulfonamides, clarithromycin and
NSAIDs. [2]

Chlorpromazine, glucocorticoids, ritodrine, salbutamol may cause


increases in blood glucose levels. [2]

Terbutaline may cause increases in blood glucose levels. [2]

May diminish hypoglycaemic effect w/ danazol. May increase


anticoagulant effect of warfarin. [2]
LABORATORY INTERFERENCES: No data available
[1]
REFERENCES: Gliclazide - DrugBank. Drugbank.ca.
https://www.drugbank.ca/drugs/DB01120. Published 2018. Accessed
November 24, 2018.
[2]
Gliclazide: Indication, Dosage, Side Effect, Precaution | MIMS.com
Philippines. Mims.com.
https://www.mims.com/philippines/drug/info/gliclazide?mtype=generic.
Published 2018. Accessed 2018.

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