carbimazole 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	497	22232-54-8

Description:

Molecule

Description

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:

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

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	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 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	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 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	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 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	16.93	16.92	7	4	2737	81930

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	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|

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	P07202	PERT_HUMAN	INHIBITOR				WOMBAT-PK	SCIENTIFIC LITERATURE
Lactoperoxidase	Enzyme	P22079	PERL_HUMAN		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
002140	NDDF
325325006	SNOMEDCT_US
395831005	SNOMEDCT_US

Pharmaceutical products:

None