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

Stem definition	Drug id	CAS RN
	2298	362-29-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: largon propiomazine propionylpromethazine propiomazine hydrochloride propiomazine HCl	Molecular weight: 340.49 Formula: C20H24N2OS CLOGP: 4.91 LIPINSKI: 0 HAC: 3 HDO: 0 TPSA: 23.55 ALOGS: -4.69 ROTB: 5 Status: OFM Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

largon
propiomazine
propionylpromethazine
propiomazine hydrochloride
propiomazine HCl

Molecular weight: 340.49
Formula: C20H24N2OS
CLOGP: 4.91
LIPINSKI: 0
HAC: 3
HDO: 0
TPSA: 23.55
ALOGS: -4.69
ROTB: 5

Status: OFM

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

Drug dosage:

Dose	Unit	Route
25	mg	O

ADMET properties:

Property	Value	Reference
MRTD (Maximum Recommended Therapeutic Daily Dose)	2.45 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	33 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

Date	Agency	Company	Orphan
Dec. 5, 1960	FDA	HIKMA MAPLE

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
Intentional self-injury	5081.84	182.19	924	2987	24763	63460348
Intentional overdose	4498.43	182.19	994	2917	73158	63411953
Depressed level of consciousness	608.26	182.19	202	3709	61876	63423235
Tachycardia	301.58	182.19	146	3765	118010	63367101
Fatigue	226.86	182.19	273	3638	887755	62597356

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
Intentional self-injury	1766.89	110.83	328	1243	13443	34941917
Intentional overdose	1502.61	110.83	349	1222	43325	34912035
Depressed level of consciousness	163.41	110.83	64	1507	42777	34912583
Tachycardia	113.04	110.83	61	1510	84711	34870649

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
Intentional self-injury	4224.99	108.89	789	2992	31630	79708977
Intentional overdose	3431.38	108.89	815	2966	105145	79635462
Depressed level of consciousness	412.70	108.89	159	3622	96493	79644114
Tachycardia	272.72	108.89	143	3638	177625	79562982
Fatigue	230.14	108.89	248	3533	929479	78811128
Toxicity to various agents	176.65	108.89	151	3630	421389	79319218
Akathisia	169.76	108.89	50	3731	13209	79727398
Mydriasis	119.63	108.89	41	3740	17602	79723005
Somnolence	117.13	108.89	94	3687	238887	79501720

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N05CM06	NERVOUS SYSTEM PSYCHOLEPTICS HYPNOTICS AND SEDATIVES Other hypnotics and sedatives
CHEBI has role	CHEBI:35717	hypnotics
CHEBI has role	CHEBI:37930	phenothiazine antipsychotic drugs
CHEBI has role	CHEBI:37956	antihistamines
CHEBI has role	CHEBI:48279	serotonin antagonists
CHEBI has role	CHEBI:48561	dopaminergic antagonists
CHEBI has role	CHEBI:48876	muscarinic antagonists

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

Disease	Relation	SNOMED_ID	DOID
General anesthesia	indication	50697003
Local anesthesia	indication	386761002
Alcoholism	contraindication	7200002
Organophosphate poisoning	contraindication	8260003
Weight gain finding	contraindication	8943002
Neuroleptic malignant syndrome	contraindication	15244003	DOID:14464
Senile dementia	contraindication	15662003
Chronic disease of respiratory system	contraindication	17097001
Myocardial infarction	contraindication	22298006	DOID:5844
Glaucoma	contraindication	23986001	DOID:1686
Orthostatic hypotension	contraindication	28651003
Torsades de pointes	contraindication	31722008
Parkinsonism	contraindication	32798002
Conduction disorder of the heart	contraindication	44808001
Chronic heart failure	contraindication	48447003
Bradycardia	contraindication	48867003
Extrapyramidal disease	contraindication	76349003
Hyperglycemia	contraindication	80394007	DOID:4195
Epilepsy	contraindication	84757009	DOID:1826
Leukopenia	contraindication	84828003	DOID:615
Stupor	contraindication	89458003
Tardive dyskinesia	contraindication	102449007
Prolonged QT interval	contraindication	111975006
Acute disease of cardiovascular system	contraindication	128487001
Angina pectoris	contraindication	194828000
Disease of liver	contraindication	235856003	DOID:409
Metabolic syndrome X	contraindication	237602007	DOID:14221
Hyperprolactinemia	contraindication	237662005	DOID:12700
Benign prostatic hyperplasia	contraindication	266569009
Retention of urine	contraindication	267064002
Anemia	contraindication	271737000	DOID:2355
Thrombocytopenic disorder	contraindication	302215000	DOID:1588
Neutropenic disorder	contraindication	303011007	DOID:1227
Coma	contraindication	371632003
At risk for aspiration	contraindication	371736008
Visual impairment	contraindication	397540003
Breastfeeding (mother)	contraindication	413712001
Myocardial ischemia	contraindication	414795007	DOID:3393
Obesity	contraindication	414916001	DOID:9970
Congenital long QT syndrome	contraindication	442917000
Carcinoma of female breast	contraindication	447782002

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.19	Basic
pKa2	1.58	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Bioact source	MoA source
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN	ANTAGONIST	WOMBAT-PK	CHEMBL
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN		WOMBAT-PK
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		WOMBAT-PK
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		WOMBAT-PK
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		WOMBAT-PK
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN		WOMBAT-PK
Muscarinic acetylcholine receptor M3	GPCR	P20309	ACM3_HUMAN		WOMBAT-PK
Muscarinic acetylcholine receptor M4	GPCR	P08173	ACM4_HUMAN		WOMBAT-PK
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN		WOMBAT-PK
D(4) dopamine receptor	GPCR	P21917	DRD4_HUMAN		WOMBAT-PK
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		WOMBAT-PK
Alpha-1B adrenergic receptor	GPCR	P35368	ADA1B_HUMAN		WOMBAT-PK

External reference:

ID	Source
4019914	VUID
N0000147999	NUI
D02361	KEGG_DRUG
1240-15-9	SECONDARY_CAS_RN
4018031	VANDF
4019914	VANDF
C0033473	UMLSCUI
CHEBI:8491	CHEBI
CHEMBL252103	ChEMBL_ID
CHEMBL1201210	ChEMBL_ID
CHEMBL1201068	ChEMBL_ID
DB00777	DRUGBANK_ID
C084591	MESH_SUPPLEMENTAL_RECORD_UI
4940	PUBCHEM_CID
7284	IUPHAR_LIGAND_ID
735	INN_ID
242Z0PM79Y	UNII
227589	RXNORM
1709	MMSL
5371	MMSL
d00914	MMSL
001488	NDDF
001489	NDDF
373493007	SNOMEDCT_US
41324009	SNOMEDCT_US
65868004	SNOMEDCT_US

Pharmaceutical products:

None