carbimazole 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,ITK,JAK2,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPK9,MARK4,MET,MTOR,NTRK2,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIM2,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK 44
kinase-selectivity-class AXL,BRAF,CDK9,DDR1,DYRK1B,EPHB4,ERBB2,GRK2,MAP2K6,MAPK12,MAPK7,MARK4,PRKDC,SIK2,STK33,SYK,TEK,TTK 18
pfas-class PFAS structural alert (1 = True, 0 = False) 0

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 119.21 23.53 47 3905 32481 90592014
Hyperthyroidism 98.26 23.53 35 3917 18275 90606220
Restlessness 78.76 23.53 36 3916 35684 90588811
Dermatitis exfoliative 77.57 23.53 22 3930 5514 90618981
Cholecystitis 74.46 23.53 28 3924 17012 90607483
Hypothyroidism 65.22 23.53 36 3916 53091 90571404
Multiple organ dysfunction syndrome 59.33 23.53 37 3915 68299 90556196
Electrolyte imbalance 55.71 23.53 25 3927 23720 90600775
Autoimmune haemolytic anaemia 55.28 23.53 17 3935 5628 90618867
Medical observation 46.71 23.53 8 3944 189 90624306
Respiratory disorder 43.79 23.53 30 3922 64786 90559709
Agranulocytosis 43.72 23.53 24 3928 34978 90589517
General physical health deterioration 41.18 23.53 63 3889 355052 90269443
Cholestasis 40.20 23.53 23 3929 36276 90588219
Hepatocellular injury 36.56 23.53 20 3932 28938 90595557
Hypotension 33.92 23.53 55 3897 325342 90299153
Cholelithiasis 32.41 23.53 23 3929 52483 90572012
Lip erosion 32.05 23.53 8 3944 1230 90623265
Jaundice 29.19 23.53 18 3934 32499 90591996
Eye haematoma 29.04 23.53 5 3947 122 90624373
Circulatory collapse 28.16 23.53 16 3936 24888 90599607
Acquired haemophilia 28.14 23.53 7 3945 1062 90623433
Nausea 27.52 23.53 108 3844 1110208 89514287
Leukopenia 26.49 23.53 27 3925 100683 90523812
Fluid intake reduced 26.35 23.53 9 3943 4143 90620352
Magnetic resonance imaging head abnormal 26.31 23.53 8 3944 2548 90621947
Hyperkalaemia 25.97 23.53 22 3930 64942 90559553
Duodenal polyp 25.72 23.53 5 3947 242 90624253
Cardiac failure 24.62 23.53 27 3925 109469 90515026
Gastrointestinal candidiasis 24.47 23.53 5 3947 312 90624183
Pain 23.84 23.53 7 3945 996334 89628161

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 73.74 29.94 26 1691 14315 42605303
Poisoning deliberate 46.88 29.94 17 1700 10117 42609501
Diffuse vasculitis 45.82 29.94 7 1710 85 42619533
Miosis 42.21 29.94 17 1700 13429 42606189
Rhabdomyolysis 41.04 29.94 30 1687 77989 42541629
Coma 31.36 29.94 22 1695 53532 42566086
Hepatorenal syndrome 30.38 29.94 9 1708 2845 42616773

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 152.12 22.45 57 5612 29204 110554426
Toxic epidermal necrolysis 84.09 22.45 46 5623 56681 110526949
General physical health deterioration 67.11 22.45 95 5574 425200 110158430
Dermatitis exfoliative 62.21 22.45 23 5646 11324 110572306
Hypothyroidism 61.07 22.45 41 5628 72858 110510772
Agranulocytosis 59.71 22.45 38 5631 61722 110521908
Cholecystitis 55.74 22.45 27 5642 25855 110557775
Restlessness 55.34 22.45 35 5634 56224 110527406
Medical observation 50.64 22.45 9 5660 224 110583406
Fluid intake reduced 49.01 22.45 17 5652 6969 110576661
Hepatocellular injury 46.08 22.45 30 5639 50612 110533018
Autoimmune haemolytic anaemia 42.15 22.45 17 5652 10550 110573080
Diffuse vasculitis 41.98 22.45 7 5662 118 110583512
Acute kidney injury 41.79 22.45 97 5572 635333 109948297
Respiratory disorder 38.97 22.45 31 5638 71351 110512279
Electrolyte imbalance 38.83 22.45 24 5645 37004 110546626
Rhabdomyolysis 35.52 22.45 37 5632 120364 110463266
Leukopenia 34.01 22.45 40 5629 148751 110434879
Hepatitis cholestatic 33.87 22.45 17 5652 17549 110566081
Cholestasis 33.05 22.45 27 5642 64491 110519139
Jaundice 32.92 22.45 26 5643 59210 110524420
Thyrotoxic crisis 31.21 22.45 9 5660 2031 110581599
Miosis 30.28 22.45 17 5652 21966 110561664
Multiple organ dysfunction syndrome 30.14 22.45 38 5631 151672 110431958
Nausea 28.68 22.45 132 5537 1235558 109348072
Goitre 28.31 22.45 11 5658 6193 110577437
Lip erosion 27.51 22.45 8 5661 1858 110581772
Coma 27.45 22.45 32 5637 117837 110465793
Poisoning deliberate 27.44 22.45 17 5652 26314 110557316
Cholelithiasis 27.27 22.45 24 5645 63398 110520232
Hepatorenal syndrome 24.03 22.45 9 5660 4588 110579042
Eye haematoma 23.94 22.45 5 5664 295 110583335
Magnetic resonance imaging head abnormal 22.49 22.45 8 5661 3527 110580103

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 16.84 16.83 7 4 3733 110209

Pharmacologic Action:

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

Related Drugs by ATC class:

H03BB Sulfur-containing imidazole derivatives 1 drug
thiamazole

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
8KQ660G60G INXIGHT DRUGS

Pharmaceutical products:

None