tolazamide Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antihyperglycaemics 2694 1156-19-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • tolazamide
  • norglycin
  • tolanase
  • tolinase
A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE.
  • Molecular weight: 311.40
  • Formula: C14H21N3O3S
  • CLOGP: 1.34
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 2
  • TPSA: 78.51
  • ALOGS: -3.01
  • ROTB: 2

  • Status: OFM

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.50 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.28 mg/mL Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 53.63 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
July 18, 1966 FDA

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC A10BB05 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Sulfonylureas
FDA CS M0020795 Sulfonylurea Compounds
FDA EPC N0000175608 Sulfonylurea
CHEBI has role CHEBI:35526 hypoglycemic drug
MeSH PA D007004 Hypoglycemic Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Diabetes mellitus type 2 indication 44054006 DOID:9352
Alcoholism contraindication 7200002
Asthenia contraindication 13791008
Uremia contraindication 44730006 DOID:4676
Acidosis contraindication 51387008
Hepatic porphyria contraindication 55056006 DOID:3133
Hypopituitarism contraindication 74728003 DOID:9406
Kidney disease contraindication 90708001 DOID:557
Disease of liver contraindication 235856003 DOID:409
Hypoglycemic disorder contraindication 237630007
Primary adrenocortical insufficiency contraindication 373662000
Surgical procedure contraindication 387713003
Traumatic injury contraindication 417746004
Fever greater than 100.4 Fahrenheit contraindication 426000000
Prolonged-Severe Nausea and Vomiting contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 5.97 acidic
pKa2 3.54 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Sulfonylurea receptor 1, Kir6.2 Ion channel BLOCKER CHEMBL CHEMBL
Arachidonate 15-lipoxygenase Enzyme IC50 5.29 DRUG MATRIX

External reference:

IDSource
4017829 VUID
N0000146187 NUI
D00379 KEGG_DRUG
4017829 VANDF
C3282883 UMLSCUI
CHEBI:9613 CHEBI
CHEMBL817 ChEMBL_ID
D014042 MESH_DESCRIPTOR_UI
1296 INN_ID
DB00839 DRUGBANK_ID
9LT1BRO48Q UNII
5503 PUBCHEM_CID
6847 IUPHAR_LIGAND_ID
10633 RXNORM
1119 MMSL
1138 MMSL
5593 MMSL
d00393 MMSL
000911 NDDF
34393009 SNOMEDCT_US
387186009 SNOMEDCT_US

Pharmaceutical products:

None