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carbimazole 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 497 | 22232-54-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An imidazole antithyroid agent. Carbimazole is metabolized to METHIMAZOLE, which is responsible for the antithyroid activity.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 15 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| 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:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1959 | YEAR INTRODUCED |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Small for dates baby | 16.84 | 16.83 | 7 | 4 | 3733 | 110209 |
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| 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
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Thyroid peroxidase | Enzyme | INHIBITOR | WOMBAT-PK | SCIENTIFIC LITERATURE | |||||
| Lactoperoxidase | Enzyme | IC50 | 4.98 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 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