gliclazide indications/contra

Stem definitionDrug idCAS RN
antihyperglycaemics 1299 21187-98-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • gliclazide
  • diabezidum
  • diabrezide
  • diabyl
  • diaprel
  • glimicron
  • glinormax
  • glyzide
  • gliclazid
  • dizalid
  • S 1702
An oral sulfonylurea hypoglycemic agent which stimulates insulin secretion.
  • Molecular weight: 323.41
  • Formula: C15H21N3O3S
  • CLOGP: 1.09
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 2
  • TPSA: 78.51
  • ALOGS: -3.23
  • ROTB: 2

Drug dosage:

DoseUnitRoute
60 mg O

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1972 YEAR INTRODUCED

FDA Adverse Event Reporting System

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MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Hypoglycaemia 976.42 49.74 190 559 14128 3370982
Acute kidney injury 273.55 49.74 89 660 49594 3335516
Diabetes mellitus inadequate control 244.01 49.74 47 702 2972 3382138
Metabolic acidosis 235.96 49.74 55 694 8723 3376387
Intentional overdose 191.64 49.74 52 697 15173 3369937
Lactic acidosis 180.32 49.74 43 706 7457 3377653
Hypoglycaemic coma 102.31 49.74 19 730 968 3384142
Hypotension 93.86 49.74 41 708 49473 3335637
Hyperlactacidaemia 92.92 49.74 16 733 527 3384583
Hyperglycaemia 92.02 49.74 26 723 8642 3376468
Acidosis 88.58 49.74 20 729 2690 3382420
Distributive shock 81.48 49.74 12 737 140 3384970
Shock 69.92 49.74 20 729 6917 3378193
Oxygen saturation decreased 66.67 49.74 21 728 10070 3375040
Condition aggravated 66.18 49.74 30 719 39203 3345907
Malaise 65.56 49.74 35 714 65142 3319968
Vomiting projectile 63.01 49.74 11 738 392 3384718
Diabetic metabolic decompensation 61.66 49.74 9 740 98 3385012
Poisoning deliberate 58.53 49.74 12 737 1019 3384091
Hyperkalaemia 52.40 49.74 18 731 11276 3373834
Dyspnoea 50.75 49.74 35 714 102899 3282211

Pharmacologic Action:

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SourceCodeDescription
ATC A10BB09 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Sulfonylureas
CHEBI has role CHEBI:35526 hypoglycemic agent
MeSH PA D007004 Hypoglycemic Agents

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Diabetes mellitus type 2 indication 44054006 DOID:9352

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 5.97 acidic
pKa2 3.62 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Sulfonylurea receptor 1, Kir6.2 Ion channel BLOCKER Kd 6.22 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Sulfonylurea receptor 2, Kir6.2 Ion channel BLOCKER Ki 5.13 WOMBAT-PK

External reference:

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IDSource
N0000166470 NUI
C0017631 UMLSCUI
D01599 KEGG_DRUG
DB01120 DRUGBANK_ID
4816 RXNORM
325238000 SNOMEDCT_US
395731001 SNOMEDCT_US
N0000166470 NDFRT
003858 NDDF
CHEMBL427216 ChEMBL_ID
3475 PUBCHEM_CID
D005907 MESH_DESCRIPTOR_UI
G4PX8C4HKV UNII
3056 INN_ID
CHEBI:31654 CHEBI
GCZ PDB_CHEM_ID

Pharmaceutical products:

None