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Details

Stereochemistry ACHIRAL
Molecular Formula C15H21N3O3S
Molecular Weight 323.411
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of GLICLAZIDE

SMILES

CC1=CC=C(C=C1)S(=O)(=O)NC(=O)NN2C[C@@H]3CCC[C@@H]3C2

InChI

InChIKey=BOVGTQGAOIONJV-BETUJISGSA-N
InChI=1S/C15H21N3O3S/c1-11-5-7-14(8-6-11)22(20,21)17-15(19)16-18-9-12-3-2-4-13(12)10-18/h5-8,12-13H,2-4,9-10H2,1H3,(H2,16,17,19)/t12-,13+

HIDE SMILES / InChI

Molecular Formula C15H21N3O3S
Molecular Weight 323.411
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/mesh/68005907 | https://www.drugs.com/cons/gliclazide.html

Gliclazide (BILXONA®) is an oral sulfonylurea hypoglycemic agent which is used in type 2 diabetes to stimulate insulin production. It differs from other related compounds by an N-containing heterocyclic ring with an endocyclic bond. Gliclazide (BILXONA®) reduces blood glucose levels by stimulating insulin secretion from the beta-cells of the islets of Langerhans. Increase in postprandial insulin and C-peptide secretion persists after two years of treatment. In addition to these metabolic properties, Gliclazide (BILXONA®) has haemovascular properties. It is not available for sale in the United States.

CNS Activity

Curator's Comment: Known to be CNS penetrant in rat. Human data not available.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
3.0 mM [Ki]
50.0 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
BILXONA

Approved Use

Non insulin-dependent diabetes (type 2) in adults when dietary measures, physical exercise and weight loss alone are not sufficient to control blood glucose.

Launch Date

2015
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
2.6 μg/mL
40 mg single, oral
dose: 40 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GLICLAZIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
2.2 μg/mL
40 mg single, oral
dose: 40 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GLICLAZIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1.6 μg/mL
40 mg single, oral
dose: 40 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GLICLAZIDE unknown
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
4.3 μg/mL
80 mg single, oral
dose: 80 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GLICLAZIDE unknown
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
2.8 μg/mL
40 mg single, oral
dose: 40 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GLICLAZIDE serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
4.5 μg/mL
80 mg single, oral
dose: 80 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GLICLAZIDE serum
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
7.7 μg/mL
80 mg 1 times / day multiple, oral
dose: 80 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
GLICLAZIDE serum
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
4 μg/mL
40 mg single, oral
dose: 40 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GLICLAZIDE unknown
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
6.3 μg/mL
80 mg single, oral
dose: 80 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GLICLAZIDE unknown
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
23.6 μg × h/mL
40 mg single, oral
dose: 40 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GLICLAZIDE unknown
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
55.65 μg × h/mL
80 mg single, oral
dose: 80 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GLICLAZIDE unknown
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
37.2 μg × h/mL
40 mg single, oral
dose: 40 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GLICLAZIDE serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
71.8 μg × h/mL
80 mg single, oral
dose: 80 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GLICLAZIDE serum
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
92.5 μg × h/mL
80 mg 1 times / day multiple, oral
dose: 80 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
GLICLAZIDE serum
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
8.6 h
40 mg single, oral
dose: 40 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GLICLAZIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
12.3 h
40 mg single, oral
dose: 40 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GLICLAZIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
9.6 h
40 mg single, oral
dose: 40 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GLICLAZIDE unknown
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
9.1 h
80 mg single, oral
dose: 80 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GLICLAZIDE unknown
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
12.3 h
40 mg single, oral
dose: 40 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GLICLAZIDE serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
11.6 h
80 mg single, oral
dose: 80 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GLICLAZIDE serum
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
11.4 h
80 mg 1 times / day multiple, oral
dose: 80 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
GLICLAZIDE serum
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
11.8 h
40 mg single, oral
dose: 40 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GLICLAZIDE unknown
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
20.5 h
80 mg single, oral
dose: 80 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GLICLAZIDE unknown
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
8%
40 mg single, oral
dose: 40 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GLICLAZIDE serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
9%
80 mg single, oral
dose: 80 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GLICLAZIDE serum
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
7%
80 mg 1 times / day multiple, oral
dose: 80 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
GLICLAZIDE serum
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
6.3%
GLICLAZIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
5%
GLICLAZIDE plasma
Homo sapiens
5%
GLICLAZIDE plasma
Homo sapiens
Doses

Doses

DosePopulationAdverse events​
2.1 g single, oral
Overdose
Dose: 2.1 g
Route: oral
Route: single
Dose: 2.1 g
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M
Food Status: UNKNOWN
Sources:
Disc. AE: Metabolic acidosis, Vomiting...
AEs leading to
discontinuation/dose reduction:
Metabolic acidosis (grade 3-4)
Vomiting
Abdominal pain (grade 3)
Hypoglycaemia
Encephalopathy
Acute kidney injury
Haemodynamic instability (grade 3)
Distributive shock (grade 3)
Sources:
1200 mg single, oral
Overdose
Dose: 1200 mg
Route: oral
Route: single
Dose: 1200 mg
Sources:
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: F
Food Status: UNKNOWN
Sources:
Disc. AE: Hepatitis, Hemiplegia...
AEs leading to
discontinuation/dose reduction:
Hepatitis
Hemiplegia (grade 3)
Dysphasia
Lethargy
Tonic-clonic convulsion
Consciousness abnormal
Stupor
Sources:
198 mg 1 times / day multiple, oral
Recommended
Dose: 198 mg, 1 times / day
Route: oral
Route: multiple
Dose: 198 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: FED
Sources:
Other AEs: Hypoglycaemia, Diarrhoea...
Other AEs:
Hypoglycaemia (10.1%)
Diarrhoea (3.4%)
Nausea (5.1%)
Oedema (4.5%)
Dizziness (6.5%)
Headache (8.9%)
Hypertension (3.8%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Acute kidney injury Disc. AE
2.1 g single, oral
Overdose
Dose: 2.1 g
Route: oral
Route: single
Dose: 2.1 g
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M
Food Status: UNKNOWN
Sources:
Encephalopathy Disc. AE
2.1 g single, oral
Overdose
Dose: 2.1 g
Route: oral
Route: single
Dose: 2.1 g
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M
Food Status: UNKNOWN
Sources:
Hypoglycaemia Disc. AE
2.1 g single, oral
Overdose
Dose: 2.1 g
Route: oral
Route: single
Dose: 2.1 g
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M
Food Status: UNKNOWN
Sources:
Vomiting Disc. AE
2.1 g single, oral
Overdose
Dose: 2.1 g
Route: oral
Route: single
Dose: 2.1 g
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M
Food Status: UNKNOWN
Sources:
Metabolic acidosis grade 3-4
Disc. AE
2.1 g single, oral
Overdose
Dose: 2.1 g
Route: oral
Route: single
Dose: 2.1 g
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M
Food Status: UNKNOWN
Sources:
Abdominal pain grade 3
Disc. AE
2.1 g single, oral
Overdose
Dose: 2.1 g
Route: oral
Route: single
Dose: 2.1 g
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M
Food Status: UNKNOWN
Sources:
Distributive shock grade 3
Disc. AE
2.1 g single, oral
Overdose
Dose: 2.1 g
Route: oral
Route: single
Dose: 2.1 g
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M
Food Status: UNKNOWN
Sources:
Haemodynamic instability grade 3
Disc. AE
2.1 g single, oral
Overdose
Dose: 2.1 g
Route: oral
Route: single
Dose: 2.1 g
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M
Food Status: UNKNOWN
Sources:
Consciousness abnormal Disc. AE
1200 mg single, oral
Overdose
Dose: 1200 mg
Route: oral
Route: single
Dose: 1200 mg
Sources:
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: F
Food Status: UNKNOWN
Sources:
Dysphasia Disc. AE
1200 mg single, oral
Overdose
Dose: 1200 mg
Route: oral
Route: single
Dose: 1200 mg
Sources:
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: F
Food Status: UNKNOWN
Sources:
Hepatitis Disc. AE
1200 mg single, oral
Overdose
Dose: 1200 mg
Route: oral
Route: single
Dose: 1200 mg
Sources:
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: F
Food Status: UNKNOWN
Sources:
Lethargy Disc. AE
1200 mg single, oral
Overdose
Dose: 1200 mg
Route: oral
Route: single
Dose: 1200 mg
Sources:
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: F
Food Status: UNKNOWN
Sources:
Stupor Disc. AE
1200 mg single, oral
Overdose
Dose: 1200 mg
Route: oral
Route: single
Dose: 1200 mg
Sources:
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: F
Food Status: UNKNOWN
Sources:
Tonic-clonic convulsion Disc. AE
1200 mg single, oral
Overdose
Dose: 1200 mg
Route: oral
Route: single
Dose: 1200 mg
Sources:
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: F
Food Status: UNKNOWN
Sources:
Hemiplegia grade 3
Disc. AE
1200 mg single, oral
Overdose
Dose: 1200 mg
Route: oral
Route: single
Dose: 1200 mg
Sources:
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: F
Food Status: UNKNOWN
Sources:
Hypoglycaemia 10.1%
198 mg 1 times / day multiple, oral
Recommended
Dose: 198 mg, 1 times / day
Route: oral
Route: multiple
Dose: 198 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: FED
Sources:
Diarrhoea 3.4%
198 mg 1 times / day multiple, oral
Recommended
Dose: 198 mg, 1 times / day
Route: oral
Route: multiple
Dose: 198 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: FED
Sources:
Hypertension 3.8%
198 mg 1 times / day multiple, oral
Recommended
Dose: 198 mg, 1 times / day
Route: oral
Route: multiple
Dose: 198 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: FED
Sources:
Oedema 4.5%
198 mg 1 times / day multiple, oral
Recommended
Dose: 198 mg, 1 times / day
Route: oral
Route: multiple
Dose: 198 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: FED
Sources:
Nausea 5.1%
198 mg 1 times / day multiple, oral
Recommended
Dose: 198 mg, 1 times / day
Route: oral
Route: multiple
Dose: 198 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: FED
Sources:
Dizziness 6.5%
198 mg 1 times / day multiple, oral
Recommended
Dose: 198 mg, 1 times / day
Route: oral
Route: multiple
Dose: 198 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: FED
Sources:
Headache 8.9%
198 mg 1 times / day multiple, oral
Recommended
Dose: 198 mg, 1 times / day
Route: oral
Route: multiple
Dose: 198 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: FED
Sources:
PubMed

PubMed

TitleDatePubMed
Phosphatidylinositol 3-kinase activation is required for sulfonylurea stimulation of glucose transport in rat skeletal muscle.
2004-02
Effects of rosiglitazone maleate when added to a sulfonylurea regimen in patients with type 2 diabetes mellitus and mild to moderate renal impairment: a post hoc analysis.
2003-11
Comparison of repaglinide vs. gliclazide in combination with bedtime NPH insulin in patients with Type 2 diabetes inadequately controlled with oral hypoglycaemic agents.
2003-11
Genetic cause of hyperglycaemia and response to treatment in diabetes.
2003-10-18
[Medication of the month. Gliclazide modified release (Uni Diamicron)].
2003-10
Risk of hypoglycaemia with oral antidiabetic agents in patients with Type 2 diabetes.
2003-10
Monotherapy of type 2 diabetes with once-daily gliclazide modified release in primary care.
2003-10
Effect of rifampin on the pharmacokinetics and pharmacodynamics of gliclazide.
2003-10
Reflex epilepsy and non-ketotic hyperglycemia.
2003-09
Gliclazide modified release: A critical review of pharmacodynamic, metabolic, and vasoprotective effects.
2003-08
Benefits of gliclazide in the atherosclerotic process: decrease in monocyte adhesion to endothelial cells.
2003-08
Pharmacokinetic and pharmacodynamic characterization of gliclazide in healthy volunteers.
2003-07
The application of the convective diffusion model and the film equilibrium model to surfactant-facilitated dissolution of gliclazide.
2003-07
Bioequivalence study of generic gliclazide and Diamicron formulations in healthy Thai male volunteers.
2003-07
Sulfonylureas and cardiovascular effects: from experimental data to clinical use. Available data in humans and clinical applications.
2003-06
Diabetes and vascular disease: a new international trial.
2003-06
Comparison of the micro- and macro-vascular effects of glimepiride and gliclazide in metformin-treated patients with Type 2 diabetes: a double-blind, crossover study.
2003-06
Functional involvement of sulphonylurea receptor (SUR) type 1 and 2B in the activity of pig urethral ATP-sensitive K+ channels.
2003-06
Upregulation of cyclooxygenase-2 is accompanied by increased expression of nuclear factor-kappa B and I kappa B kinase-alpha in human colorectal cancer epithelial cells.
2003-05-19
Spectrofluorimetric and spectrophotometric determination of gliclazide in pharmaceuticals by derivatization with 4-chloro-7-nitrobenzo-2-oxa-1,3-diazole.
2003-05-02
Urinary PC-1 and N-acetyl-beta-D-glucosaminidase activity in patients with type 2 diabetes treated with metformin, gliclazide or glibenclamide.
2003-05
Study of the solubilization of gliclazide by aqueous micellar solutions.
2003-04
Gliclazide protects pancreatic beta-cells from damage by hydrogen peroxide.
2003-03-28
Monocyte matrix metalloproteinase production in Type 2 diabetes and controls--a cross sectional study.
2003-03-10
Diabetic endothelial dysfunction: effect of free radical scavenging in Type 2 diabetic patients.
2003-03-08
Monocyte adhesion in diabetic angiopathy: effects of free-radical scavenging.
2003-03-08
Differential selectivity of insulin secretagogues: mechanisms, clinical implications, and drug interactions.
2003-03-08
Effects of sulfonylureas on K(ATP) channel-dependent vasodilation.
2003-03-08
A simple and sensitive HPLC method for determination of gliclazide in human serum.
2003-03-05
Severe relapsing sulphonylurea-induced hypoglycaemia: a diagnostic and therapeutic challenge.
2003-02
Diabetes mellitus and weight control: differences of respiratory quotient in type 2 diabetic obese subjects receiving sulfonylureas and non-diabetic obese controls.
2003-02
Differential effects of sulphonylureas on the vasodilatory response evoked by K(ATP) channel openers.
2003-02
Population PKPD modelling of the long-term hypoglycaemic effect of gliclazide given as a once-a-day modified release (MR) formulation.
2003-02
Effects of inhibition of ATP-sensitive potassium channels on metabolic vasodilation in the human forearm.
2003-01
[A 50-year history of new drugs in Japan-the development and progress of anti-diabetic drugs and the epidemiological aspects of diabetes mellitus].
2003
Addition of rosiglitazone to existing sulfonylurea treatment in chinese patients with type 2 diabetes and exposure to hepatitis B or C.
2003
The mechanisms of inhibitory actions of gliclazide on neutrophils-endothelial cells adhesion and surface expression of endothelial adhesion molecules mediated by a high glucose concentration.
2002-12-31
Effect of ethanolic extract of Embelia ribes on dyslipidemia in diabetic rats.
2002-12-03
High-frequency insulin pulsatility and type 2 diabetes: from physiology and pathophysiology to clinical pharmacology.
2002-12
[Molecular mechanisms of insulin secretion].
2002-12
Hypoglycaemic activity of Alpinia galanga rhizome and its extracts in rabbits.
2002-12
Combination therapy of alpha-glucosidase inhibitor and a sulfonylurea compound prolongs the duration of good glycemic control.
2002-12
Gliclazide directly inhibits arginine-induced glucagon release.
2002-12
Interaction of the cytosolic domains of the Kir6.2 subunit of the K(ATP) channel is modulated by sulfonylureas.
2002-12
Sulfonylurea stimulation of insulin secretion.
2002-12
Effect of gliclazide on islet transplants.
2002-11
Remodelling of zero-stress state of small intestine in streptozotocin-induced diabetic rats. Effect of gliclazide.
2002-10
Gateways to Clinical Trials.
2002-09
Oral hypoglycaemic agent failure.
2002-07
[Effects of gliclazide on blood rheology of diabetes Wistar rat].
2001-06
Patents

Sample Use Guides

The daily dose may vary from 1 to 4 tablets per day, i.e. from 30 to 120 mg taken orally in a single intake at breakfast time.
Route of Administration: Oral
Gliclazide blocked whole-cell murine beta-cell Katp currents with an IC50 of 184 +/- 30 nmol/l (n = 6-10) but was much less effective in rat cardiac and smooth muscle (IC50s of 19.5 +/- 5.4 micromol/l (n = 6-12) and 37.9 +/- 1.0 micromol/l (n = 5-10), respectively). In all three tissues, the action of the drug on whole-cell Katp currents was rapidly reversible. In inside-out patches on beta-cells, gliclazide (1 micromol/l) produced a maximum of 66 +/- 13 % inhibition (n = 5), compared with more than 98 % block in the whole-cell configuration.
Substance Class Chemical
Created
by admin
on Mon Mar 31 19:40:52 GMT 2025
Edited
by admin
on Mon Mar 31 19:40:52 GMT 2025
Record UNII
G4PX8C4HKV
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
DIAMICRON
Preferred Name English
GLICLAZIDE
EP   INN   JAN   MART.   MI   WHO-DD  
INN  
Official Name English
SE 1702
Code English
BENZENESULFONAMIDE, N-(((HEXAHYDROCYCLOPENTA(C)PYRROL-2(1H)-YL)AMINO)CARBONYL)-4-METHYL-
Systematic Name English
SE-1702
Code English
gliclazide [INN]
Common Name English
GLICLAZIDE [MI]
Common Name English
J3.151H
Code English
Gliclazide [WHO-DD]
Common Name English
S-1702
Code English
NSC-758673
Code English
GLICLAZIDE [EP MONOGRAPH]
Common Name English
S-852
Code English
GLICLAZIDE [JAN]
Common Name English
1-(3-AZABICYCLO(3.3.0)OCT-3-YL)-3-(P-TOLYLSULFONYL)UREA
Common Name English
GLIMICRON
Brand Name English
GLICLAZIDE [MART.]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C97936
Created by admin on Mon Mar 31 19:40:52 GMT 2025 , Edited by admin on Mon Mar 31 19:40:52 GMT 2025
WHO-VATC QA10BB09
Created by admin on Mon Mar 31 19:40:52 GMT 2025 , Edited by admin on Mon Mar 31 19:40:52 GMT 2025
WHO-ATC A10BB09
Created by admin on Mon Mar 31 19:40:52 GMT 2025 , Edited by admin on Mon Mar 31 19:40:52 GMT 2025
Code System Code Type Description
ECHA (EC/EINECS)
244-260-5
Created by admin on Mon Mar 31 19:40:52 GMT 2025 , Edited by admin on Mon Mar 31 19:40:52 GMT 2025
PRIMARY
FDA UNII
G4PX8C4HKV
Created by admin on Mon Mar 31 19:40:52 GMT 2025 , Edited by admin on Mon Mar 31 19:40:52 GMT 2025
PRIMARY
MESH
D005907
Created by admin on Mon Mar 31 19:40:52 GMT 2025 , Edited by admin on Mon Mar 31 19:40:52 GMT 2025
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EVMPD
SUB07921MIG
Created by admin on Mon Mar 31 19:40:52 GMT 2025 , Edited by admin on Mon Mar 31 19:40:52 GMT 2025
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PUBCHEM
667431
Created by admin on Mon Mar 31 19:40:52 GMT 2025 , Edited by admin on Mon Mar 31 19:40:52 GMT 2025
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DRUG CENTRAL
1299
Created by admin on Mon Mar 31 19:40:52 GMT 2025 , Edited by admin on Mon Mar 31 19:40:52 GMT 2025
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WIKIPEDIA
GLICLAZIDE
Created by admin on Mon Mar 31 19:40:52 GMT 2025 , Edited by admin on Mon Mar 31 19:40:52 GMT 2025
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RXCUI
4816
Created by admin on Mon Mar 31 19:40:52 GMT 2025 , Edited by admin on Mon Mar 31 19:40:52 GMT 2025
PRIMARY RxNorm
NCI_THESAURUS
C87618
Created by admin on Mon Mar 31 19:40:52 GMT 2025 , Edited by admin on Mon Mar 31 19:40:52 GMT 2025
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EPA CompTox
DTXSID9023095
Created by admin on Mon Mar 31 19:40:52 GMT 2025 , Edited by admin on Mon Mar 31 19:40:52 GMT 2025
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CAS
21187-98-4
Created by admin on Mon Mar 31 19:40:52 GMT 2025 , Edited by admin on Mon Mar 31 19:40:52 GMT 2025
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SMS_ID
100000090151
Created by admin on Mon Mar 31 19:40:52 GMT 2025 , Edited by admin on Mon Mar 31 19:40:52 GMT 2025
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NSC
758673
Created by admin on Mon Mar 31 19:40:52 GMT 2025 , Edited by admin on Mon Mar 31 19:40:52 GMT 2025
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CHEBI
31654
Created by admin on Mon Mar 31 19:40:52 GMT 2025 , Edited by admin on Mon Mar 31 19:40:52 GMT 2025
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DRUG BANK
DB01120
Created by admin on Mon Mar 31 19:40:52 GMT 2025 , Edited by admin on Mon Mar 31 19:40:52 GMT 2025
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INN
3056
Created by admin on Mon Mar 31 19:40:52 GMT 2025 , Edited by admin on Mon Mar 31 19:40:52 GMT 2025
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MERCK INDEX
m5744
Created by admin on Mon Mar 31 19:40:52 GMT 2025 , Edited by admin on Mon Mar 31 19:40:52 GMT 2025
PRIMARY Merck Index
ChEMBL
CHEMBL427216
Created by admin on Mon Mar 31 19:40:52 GMT 2025 , Edited by admin on Mon Mar 31 19:40:52 GMT 2025
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Related Record Type Details
TRANSPORTER -> SUBSTRATE
Compared with the OATP1B1*1a, mutants OATP1B1*5 and OATP1B1*15 showed significantly decreased transport capacity.
TARGET -> INHIBITOR
METABOLIC ENZYME -> SUBSTRATE
Clearance of gliclazide in CYP2C9*2 and *3 was significantly reduced compared to the wild-type.
Related Record Type Details
METABOLITE -> PARENT
METABOLITE -> PARENT
Related Record Type Details
ACTIVE MOIETY