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

Stem definition	Drug id	CAS RN
	1745	60-56-0

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: methimazole methylimidazolethiol thyrozol thymidazole thymidazol thycapzol thiamazole tapazole methymazol	A thioureylene antithyroid agent that inhibits the formation of thyroid hormones by interfering with the incorporation of iodine into tyrosyl residues of thyroglobulin. This is done by interfering with the oxidation of iodide ion and iodotyrosyl groups through inhibition of the peroxidase enzyme. Molecular weight: 114.17 Formula: C4H6N2S CLOGP: -0.34 LIPINSKI: 0 HAC: 2 HDO: 1 TPSA: 15.27 ALOGS: -1 ROTB: 0 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

methimazole
methylimidazolethiol
thyrozol
thymidazole
thymidazol
thycapzol
thiamazole
tapazole
methymazol

A thioureylene antithyroid agent that inhibits the formation of thyroid hormones by interfering with the incorporation of iodine into tyrosyl residues of thyroglobulin. This is done by interfering with the oxidation of iodide ion and iodotyrosyl groups through inhibition of the peroxidase enzyme.

Molecular weight: 114.17
Formula: C4H6N2S
CLOGP: -0.34
LIPINSKI: 0
HAC: 2
HDO: 1
TPSA: 15.27
ALOGS: -1
ROTB: 0

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
10	mg	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	93 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
MRTD (Maximum Recommended Therapeutic Daily Dose)	8.76 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
CL (Clearance)	3.70 mL/min/kg	Lombardo F, Berellini G, Obach RS
S (Water solubility)	200 mg/mL	Bocci G, Oprea TI, Benet LZ
t_half (Half-life)	2.40 hours	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Hosey CM, Chan R, Benet LZ
Vd (Volume of distribution)	0.86 L/kg	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
June 21, 1950	FDA

FDA Adverse Event Reporting System (Female)

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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
Agranulocytosis	402.51	14.05	149	9454	24985	63454434
Thyrotoxic crisis	295.04	14.05	58	9545	818	63478601
Hyperthyroidism	231.10	14.05	86	9517	14587	63464832
Antithyroid arthritis syndrome	74.61	14.05	10	9593	4	63479415
Hypothyroidism	69.47	14.05	55	9548	42577	63436842
Choanal atresia	59.65	14.05	9	9594	20	63479399
Exophthalmos	43.80	14.05	14	9589	1502	63477917
Neutropenia	40.81	14.05	85	9518	174920	63304499
Blood thyroid stimulating hormone decreased	38.08	14.05	17	9586	4573	63474846
Drug-induced liver injury	34.14	14.05	36	9567	40186	63439233

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FDA Adverse Event Reporting System (Male)

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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	182.86	18.47	63	4264	10503	34942101
Thyrotoxic periodic paralysis	126.86	18.47	21	4306	128	34952476
Agranulocytosis	86.31	18.47	47	4280	23774	34928830
Thyrotoxic crisis	75.94	18.47	16	4311	399	34952205
Hypothyroidism	61.50	18.47	36	4291	20866	34931738
Polymerase chain reaction	43.55	18.47	8	4319	95	34952509
Kounis syndrome	43.44	18.47	15	4312	2503	34950101
Product administered to patient of inappropriate age	35.95	18.47	14	4313	3277	34949327
Albumin urine present	33.06	18.47	8	4319	376	34952228
Exomphalos	32.01	18.47	7	4320	209	34952395

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FDA Adverse Event Reporting System (Geriatric)

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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
Agranulocytosis	432.45	13.20	187	12430	44843	79686928
Thyrotoxic crisis	339.36	13.20	70	12547	1214	79730557
Hyperthyroidism	318.40	13.20	123	12494	22086	79709685
Thyrotoxic periodic paralysis	120.05	13.20	21	12596	140	79731631
Hypothyroidism	109.86	13.20	80	12537	52312	79679459
Antithyroid arthritis syndrome	74.16	13.20	10	12607	4	79731767
Exophthalmos	49.38	13.20	16	12601	1714	79730057
Drug-induced liver injury	46.82	13.20	55	12562	66062	79665709
Goitre	46.60	13.20	21	12596	5518	79726253
Anti-neutrophil cytoplasmic antibody positive vasculitis	44.13	13.20	18	12599	3711	79728060

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	H03BB02	SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS THYROID THERAPY ANTITHYROID PREPARATIONS Sulfur-containing imidazole derivatives
ATC	H03BB52	SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS THYROID THERAPY ANTITHYROID PREPARATIONS Sulfur-containing imidazole derivatives
CHEBI has role	CHEBI:50671	antithyroid drugs
FDA EPC	N0000175918	Thyroid Hormone Synthesis Inhibitor
FDA MoA	N0000175917	Thyroid Hormone Synthesis Inhibitors
MeSH PA	D013956	Antithyroid Agents
MeSH PA	D006727	Hormone Antagonists

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

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Disease	Relation	SNOMED_ID	DOID
Hyperthyroidism	indication	34486009	DOID:7998
Thyrotoxic crisis	off-label use	29028009	DOID:12837
Agranulocytosis	contraindication	17182001	DOID:12987
Hypothyroidism	contraindication	40930008	DOID:1459
Factor II deficiency	contraindication	73975000
Leukopenia	contraindication	84828003	DOID:615
Pancytopenia	contraindication	127034005	DOID:12450
Liver function tests abnormal	contraindication	166603001
Drug-induced hepatitis	contraindication	235876009
Pregnancy, function	contraindication	289908002

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

Product	Applicant	Ingredients
Felimazole	Dechra, Ltd.	1

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	10.7	acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Thyroid peroxidase	Enzyme	P07202	PERT_HUMAN	INHIBITOR	IC50	5.57	WOMBAT-PK	CHEMBL
Lactoperoxidase	Enzyme	P22079	PERL_HUMAN		IC50	4.93	CHEMBL
Taste receptor type 2 member 38	GPCR	P59533	T2R38_HUMAN	AGONIST	EC50	4.01	IUPHAR
Lactoperoxidase	Enzyme		PERL_BOVIN		IC50	5.08	CHEMBL
Dopamine beta-hydroxylase	Enzyme		DOPO_BOVIN		Ki	4.35	CHEMBL

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External reference:

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ID	Source
MMZ	PDB_CHEM_ID
002139	NDDF
1349907	PUBCHEM_CID
224936	RXNORM
2293	MMSL
31962	MMSL
37656002	SNOMEDCT_US
4017434	VUID
4017434	VANDF
404864000	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Methimazole	HUMAN PRESCRIPTION DRUG LABEL	1	0185-0205	TABLET	5 mg	ORAL	ANDA	19 sections
Methimazole	HUMAN PRESCRIPTION DRUG LABEL	1	0185-0210	TABLET	10 mg	ORAL	ANDA	19 sections
Methimazole	HUMAN PRESCRIPTION DRUG LABEL	1	23155-070	TABLET	5 mg	ORAL	ANDA	19 sections
Methimazole	HUMAN PRESCRIPTION DRUG LABEL	1	23155-070	TABLET	5 mg	ORAL	ANDA	19 sections
Methimazole	HUMAN PRESCRIPTION DRUG LABEL	1	23155-071	TABLET	10 mg	ORAL	ANDA	19 sections
Methimazole	HUMAN PRESCRIPTION DRUG LABEL	1	23155-071	TABLET	10 mg	ORAL	ANDA	19 sections
Methimazole	Human Prescription Drug Label	1	33342-335	TABLET	5 mg	ORAL	ANDA	19 sections
Methimazole	Human Prescription Drug Label	1	33342-336	TABLET	10 mg	ORAL	ANDA	19 sections
Methimazole	HUMAN PRESCRIPTION DRUG LABEL	1	42254-008	TABLET	5 mg	ORAL	ANDA	18 sections
Methimazole	HUMAN PRESCRIPTION DRUG LABEL	1	42254-009	TABLET	10 mg	ORAL	ANDA	18 sections

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