carbimazole 🐶 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 µM/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 97.65 25.91 39 3013 25295 63460675
Hyperthyroidism 90.94 25.91 32 3020 14641 63471329
Restlessness 78.87 25.91 35 3017 29418 63456552
Dermatitis exfoliative 71.36 25.91 21 3031 5438 63480532
Cholecystitis 67.41 25.91 26 3026 15351 63470619
General physical health deterioration 63.26 25.91 62 2990 201340 63284630
Multiple organ dysfunction syndrome 57.21 25.91 35 3017 56717 63429253
Electrolyte imbalance 54.18 25.91 24 3028 20052 63465918
Autoimmune haemolytic anaemia 52.76 25.91 16 3036 4585 63481385
Respiratory disorder 52.36 25.91 29 3023 39053 63446917
Hypothyroidism 47.37 25.91 28 3024 42604 63443366
Cholestasis 39.85 25.91 22 3030 29412 63456558
Agranulocytosis 37.40 25.91 20 3032 25114 63460856
Hepatocellular injury 35.79 25.91 20 3032 27361 63458609
Cholelithiasis 31.74 25.91 22 3030 43903 63442067
Eye haematoma 31.39 25.91 5 3047 67 63485903
Jaundice 29.34 25.91 18 3034 29233 63456737
Magnetic resonance imaging head abnormal 27.43 25.91 8 3044 2005 63483965
Fluid intake reduced 26.65 25.91 9 3043 3632 63482338

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 63.71 34.82 21 1242 10545 34945123
Diffuse vasculitis 46.59 34.82 7 1256 85 34955583
General physical health deterioration 36.74 34.82 33 1230 128236 34827432

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 133.93 26.79 49 4287 22160 79717892
General physical health deterioration 94.42 26.79 94 4242 275144 79464908
Toxic epidermal necrolysis 69.15 26.79 38 4298 44543 79695509
Dermatitis exfoliative 58.30 26.79 22 4314 10807 79729245
Restlessness 57.01 26.79 34 4302 46458 79693594
Cholecystitis 52.03 26.79 25 4311 22187 79717865
Fluid intake reduced 49.78 26.79 17 4319 6271 79733781
Respiratory disorder 47.82 26.79 30 4306 44826 79695226
Hypothyroidism 43.56 26.79 30 4306 52362 79687690
Agranulocytosis 42.75 26.79 28 4308 45002 79695050
Diffuse vasculitis 41.57 26.79 7 4329 118 79739934
Autoimmune haemolytic anaemia 41.42 26.79 16 4320 8364 79731688
Hepatocellular injury 41.34 26.79 28 4308 47565 79692487
Electrolyte imbalance 38.93 26.79 23 4313 30858 79709194
Acute kidney injury 38.40 26.79 86 4250 519318 79220734
Jaundice 33.98 26.79 26 4310 53323 79686729
Hepatitis cholestatic 33.68 26.79 16 4320 13836 79726216
Multiple organ dysfunction syndrome 32.05 26.79 36 4300 120210 79619842
Cholestasis 30.16 26.79 24 4312 52085 79687967
Cholelithiasis 27.83 26.79 23 4313 52641 79687411
Rhabdomyolysis 27.69 26.79 31 4305 103100 79636952
Nausea 27.09 26.79 113 4223 957083 78782969

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 17.17 17.12 7 4 2802 86979

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 | Suggest Off label Use Form| |View source of the data|

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




🐶 Veterinary Drug Use

None

🐶 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
325325006 SNOMEDCT_US
395831005 SNOMEDCT_US
002140 NDDF

Pharmaceutical products:

None