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

Stem definition	Drug id	CAS RN
uracil derivatives used as thyroid antagonists	2308	51-52-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: propylthiouracil 6-n-Propylthiouracil procasil propacil prothiurone	A thiourea antithyroid agent. Propythiouracil inhibits the synthesis of thyroxine and inhibits the peripheral conversion of throxine to tri-iodothyronine. It is used in the treatment of hyperthyroidism. (From Martindale, The Extra Pharmacopeoia, 30th ed, p534) Molecular weight: 170.23 Formula: C7H10N2OS CLOGP: 0.97 LIPINSKI: 0 HAC: 3 HDO: 2 TPSA: 41.13 ALOGS: -2.56 ROTB: 2 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

propylthiouracil
6-n-Propylthiouracil
procasil
propacil
prothiurone

A thiourea antithyroid agent. Propythiouracil inhibits the synthesis of thyroxine and inhibits the peripheral conversion of throxine to tri-iodothyronine. It is used in the treatment of hyperthyroidism. (From Martindale, The Extra Pharmacopeoia, 30th ed, p534)

Molecular weight: 170.23
Formula: C7H10N2OS
CLOGP: 0.97
LIPINSKI: 0
HAC: 3
HDO: 2
TPSA: 41.13
ALOGS: -2.56
ROTB: 2

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.10	g	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	85 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
MRTD (Maximum Recommended Therapeutic Daily Dose)	75.53 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
CL (Clearance)	3.10 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	1.30 hours	Lombardo F, Berellini G, Obach RS
S (Water solubility)	1.20 mg/mL	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
Vd (Volume of distribution)	0.34 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.18 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
July 28, 1947	FDA	DAVA PHARMS INC

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
Anti-neutrophil cytoplasmic antibody positive vasculitis	269.45	30.07	51	2064	2848	63484059
Antineutrophil cytoplasmic antibody positive	152.24	30.07	25	2090	605	63486302
Thyrotoxic crisis	117.29	30.07	21	2094	855	63486052
Hyperthyroidism	106.75	30.07	33	2082	14640	63472267
Vasculitis	99.74	30.07	33	2082	18176	63468731
Exposure during pregnancy	97.84	30.07	62	2053	155485	63331422
Liver transplant	75.05	30.07	17	2098	2274	63484633
Foetal exposure during pregnancy	68.08	30.07	29	2086	31933	63454974
Agranulocytosis	67.78	30.07	27	2088	25107	63461800
Acute hepatic failure	50.48	30.07	20	2095	18307	63468600

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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	67.49	42.56	18	511	10548	34945854
Foetal exposure during pregnancy	66.59	42.56	24	505	38077	34918325
Obstructive pancreatitis	53.12	42.56	9	520	595	34955807

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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
Anti-neutrophil cytoplasmic antibody positive vasculitis	293.03	28.65	56	2329	3673	79738330
Antineutrophil cytoplasmic antibody positive	149.73	28.65	27	2358	1279	79740724
Thyrotoxic crisis	137.13	28.65	25	2360	1259	79740744
Hyperthyroidism	133.19	28.65	42	2343	22167	79719836
Vasculitis	96.63	28.65	34	2351	25068	79716935
Exposure during pregnancy	93.75	28.65	50	2335	101082	79640921
Agranulocytosis	70.92	28.65	32	2353	44998	79697005
Acute hepatic failure	59.11	28.65	25	2360	30088	79711915
Liver transplant	56.14	28.65	15	2370	4408	79737595
Cardiogenic shock	51.19	28.65	25	2360	41889	79700114

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	H03BA02	SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS THYROID THERAPY ANTITHYROID PREPARATIONS Thiouracils
CHEBI has role	CHEBI:22586	antioxidants
CHEBI has role	CHEBI:35221	antimetabolite
CHEBI has role	CHEBI:49020	hormone antagonists
CHEBI has role	CHEBI:50671	antithyroid drugs
CHEBI has role	CHEBI:50903	carcinogen
CHEBI has role	CHEBI:61908	nitric oxide synthase inhibitors
CHEBI has role	CHEBI:74529	antidotes to acetaminophen poisoning
FDA EPC	N0000175918	Thyroid Hormone Synthesis Inhibitor
FDA MoA	N0000175917	Thyroid Hormone Synthesis Inhibitors

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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
Thyrotoxic crisis	indication	29028009	DOID:12837
Hyperthyroidism	indication	34486009	DOID:7998
Necrotizing vasculitis	contraindication	11791001
Hyperbilirubinemia	contraindication	14783006	DOID:2741
Agranulocytosis	contraindication	17182001	DOID:12987
Hypothyroidism	contraindication	40930008	DOID:1459
Interstitial pneumonia	contraindication	64667001
Leukopenia	contraindication	84828003	DOID:615
Pancytopenia	contraindication	127034005	DOID:12450
Liver function tests abnormal	contraindication	166603001

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.52	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	5.06	WOMBAT-PK	CHEMBL
Type I iodothyronine deiodinase	Enzyme	P49895	IOD1_HUMAN	INHIBITOR			CHEMBL	CHEMBL
Myeloperoxidase	Enzyme	P05164	PERM_HUMAN		IC50	5.55	CHEMBL
Taste receptor type 2 member 38	GPCR	P59533	T2R38_HUMAN		EC50	5.70	CHEMBL

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External reference:

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ID	Source
002137	NDDF
2256	MMSL
3814009	SNOMEDCT_US
387203007	SNOMEDCT_US
3CJ	PDB_CHEM_ID
4017432	VUID
4017432	VANDF
4184	INN_ID
5376	MMSL
657298	PUBCHEM_CID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Propylthiouracil	HUMAN PRESCRIPTION DRUG LABEL	1	0228-2348	TABLET	50 mg	ORAL	ANDA	22 sections
Propylthiouracil	Human Prescription Drug Label	1	33342-314	TABLET	50 mg	ORAL	ANDA	22 sections
Propylthiouracil	HUMAN PRESCRIPTION DRUG LABEL	1	42254-010	TABLET	50 mg	ORAL	ANDA	18 sections
Propylthiouracil	HUMAN PRESCRIPTION DRUG LABEL	1	67253-651	TABLET	50 mg	ORAL	NDA	23 sections
Propylthiouracil	HUMAN PRESCRIPTION DRUG LABEL	1	68084-964	TABLET	50 mg	ORAL	NDA	24 sections
Propylthiouracil	HUMAN PRESCRIPTION DRUG LABEL	1	68084-964	TABLET	50 mg	ORAL	NDA	24 sections
PROPYLTHIOURACIL	HUMAN PRESCRIPTION DRUG LABEL	1	70752-171	TABLET	50 mg	ORAL	ANDA	21 sections
PROPYLTHIOURACIL	HUMAN PRESCRIPTION DRUG LABEL	1	70752-171	TABLET	50 mg	ORAL	ANDA	21 sections
PROPYLTHIOURACIL	HUMAN PRESCRIPTION DRUG LABEL	1	72162-2072	TABLET	50 mg	ORAL	ANDA	21 sections

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