carbimazole ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
497 22232-54-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • carbimazole
  • athyromazole
  • carbethoxymethimazole
  • carbimazol
  • neomercazole
An imidazole antithyroid agent. Carbimazole is metabolized to METHIMAZOLE, which is responsible for the antithyroid activity.
  • Molecular weight: 186.23
  • Formula: C7H10N2O2S
  • CLOGP: 1.68
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 0
  • TPSA: 32.78
  • ALOGS: -1.77
  • ROTB: 2

Drug dosage:

DoseUnitRoute
15 mg O

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 5.37 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 0 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1959 YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

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
Toxic epidermal necrolysis 100.49 27.90 39 2686 20953 50581446
Hyperthyroidism 77.92 27.90 28 2697 12147 50590252
Restlessness 77.11 27.90 34 2691 25139 50577260
Dermatitis exfoliative 70.26 27.90 21 2704 5121 50597278
General physical health deterioration 67.48 27.90 58 2667 142376 50460023
Cholecystitis 67.16 27.90 26 2699 13845 50588554
Respiratory disorder 55.43 27.90 29 2696 31158 50571241
Multiple organ dysfunction syndrome 54.88 27.90 34 2691 50303 50552096
Electrolyte imbalance 51.94 27.90 23 2702 17146 50585253
Hypothyroidism 42.20 27.90 25 2700 34100 50568299
Cholelithiasis 32.39 27.90 22 2703 37951 50564448
Agranulocytosis 29.94 27.90 17 2708 21404 50580995
Hepatocellular injury 29.45 27.90 18 2707 25929 50576470
Jaundice 29.15 27.90 18 2707 26411 50575988

FDA Adverse Event Reporting System (Male)

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
Hyperthyroidism 59.66 38.08 19 1047 8589 29564872
General physical health deterioration 43.26 38.08 33 1033 102824 29470637
Diffuse vasculitis 39.86 38.08 6 1060 74 29573387

FDA Adverse Event Reporting System (Geriatric)

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
Hyperthyroidism 116.58 27.05 43 3803 18136 64476750
General physical health deterioration 102.92 27.05 90 3756 204335 64290551
Toxic epidermal necrolysis 72.37 27.05 38 3808 37128 64457758
Dermatitis exfoliative 57.29 27.05 22 3824 10330 64484556
Restlessness 56.37 27.05 33 3813 39752 64455134
Cholecystitis 52.77 27.05 25 3821 19611 64475275
Respiratory disorder 51.28 27.05 30 3816 36081 64458805
Hypothyroidism 40.70 27.05 27 3819 40430 64454456
Electrolyte imbalance 38.57 27.05 22 3824 25221 64469665
Acute kidney injury 35.80 27.05 81 3765 449159 64045727
Hepatocellular injury 35.68 27.05 26 3820 45209 64449677
Diffuse vasculitis 34.76 27.05 6 3840 107 64494779
Hepatitis cholestatic 34.27 27.05 16 3830 12139 64482747
Jaundice 34.06 27.05 26 3820 48486 64446400
Multiple organ dysfunction syndrome 32.61 27.05 35 3811 101378 64393508
Cholelithiasis 28.92 27.05 23 3823 45483 64449403
Rhabdomyolysis 28.33 27.05 31 3815 91695 64403191

FDA Adverse Event Reporting System (Pediatric)

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
Small for dates baby 16.93 16.92 7 4 2737 81930

Pharmacologic Action:

SourceCodeDescription
ATC H03BB01 SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
THYROID THERAPY
ANTITHYROID PREPARATIONS
Sulfur-containing imidazole derivatives
MeSH PA D013956 Antithyroid Agents
MeSH PA D006727 Hormone Antagonists
CHEBI has role CHEBI:50266 Prodrugs
CHEBI has role CHEBI:50671 antithyroid drugs

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hyperthyroidism indication 34486009 DOID:7998
Graves' disease indication 353295004 DOID:12361




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

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
Thyroid peroxidase Enzyme INHIBITOR WOMBAT-PK SCIENTIFIC LITERATURE
Lactoperoxidase Enzyme IC50 4.98 CHEMBL

External reference:

IDSource
N0000167064 NUI
D07616 KEGG_DRUG
2020 RXNORM
C0006983 UMLSCUI
CHEBI:617099 CHEBI
CHEMBL508102 ChEMBL_ID
DB00389 DRUGBANK_ID
D002231 MESH_DESCRIPTOR_UI
31072 PUBCHEM_CID
323 INN_ID
8KQ660G60G UNII
002140 NDDF
325325006 SNOMEDCT_US
395831005 SNOMEDCT_US

Pharmaceutical products:

None