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
Hyperthyroidism	223.74	29.81	63	2801	13289	56275914
Toxic epidermal necrolysis	100.78	29.81	39	2825	22003	56267200
Restlessness	80.42	29.81	35	2829	26551	56262652
Dermatitis exfoliative	70.81	29.81	21	2843	5278	56283925
Cholecystitis	67.58	29.81	26	2838	14409	56274794
General physical health deterioration	65.32	29.81	60	2804	169950	56119253
Multiple organ dysfunction syndrome	57.74	29.81	35	2829	52735	56236468
Electrolyte imbalance	55.35	29.81	24	2840	18009	56271194
Respiratory disorder	54.65	29.81	29	2835	33928	56255275
Hypothyroidism	43.48	29.81	26	2838	38170	56251033
Cholestasis	37.77	29.81	21	2843	26892	56262311
Cholelithiasis	32.75	29.81	22	2842	39442	56249761
Hepatocellular injury	30.04	29.81	18	2846	26496	56262707
Agranulocytosis	29.94	29.81	17	2847	22642	56266561

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	95.80	34.74	28	1107	9603	31686606
General physical health deterioration	40.57	34.74	33	1102	113402	31582807
Diffuse vasculitis	39.68	34.74	6	1129	77	31696132
Acute kidney injury	36.29	34.74	47	1088	279667	31416542
Rhabdomyolysis	35.01	34.74	24	1111	63557	31632652

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	278.53	26.05	84	3972	20007	70904381
General physical health deterioration	98.84	26.05	92	3964	235939	70688449
Toxic epidermal necrolysis	71.63	26.05	38	4018	39519	70884869
Restlessness	58.54	26.05	34	4022	42094	70882294
Dermatitis exfoliative	57.78	26.05	22	4034	10529	70913859
Cholecystitis	52.51	26.05	25	4031	20676	70903712
Respiratory disorder	50.21	26.05	30	4026	39093	70885295
Hypothyroidism	41.07	26.05	28	4028	45727	70878661
Electrolyte imbalance	40.84	26.05	23	4033	26838	70897550
Acute kidney injury	37.31	26.05	83	3973	474541	70449847
Hepatocellular injury	36.22	26.05	26	4030	46065	70878323
Diffuse vasculitis	34.86	26.05	6	4050	110	70924278
Hepatitis cholestatic	34.30	26.05	16	4040	12634	70911754
Jaundice	34.27	26.05	26	4030	50082	70874306
Multiple organ dysfunction syndrome	33.61	26.05	36	4020	108479	70815909
Cholelithiasis	28.97	26.05	23	4033	47317	70877071
Cholestasis	28.74	26.05	23	4033	47849	70876539
Rhabdomyolysis	28.30	26.05	31	4025	95729	70828659
Fluid intake reduced	28.22	26.05	11	4045	5596	70918792

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	17.17	17.12	7	4	2802	86979

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