All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

propiomazine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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

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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
azlogd74	LogD at pH 7.4	3.266		Moderate	0.71
caco2-efflux	Caco-2 efflux ratio (BA/AB)	0.401		Moderate	0.71
caco2-intrinsic-papp	Caco-2 intrinsic apparent permeability	38.905	10^-6 cm/s	Moderate	0.71
dh-clint	Dog hepatocyte intrinsic clearance	71.450	uL/min/10^6 cells	Moderate	0.71
dppb	Dog plasma protein binding (% unbound)	6.080	%	Moderate	0.71
fcs-ppb	Fetal calf serum protein binding (% unbound)	13.020	%	Moderate	0.71
herg	hERG pIC50	5.730	pIC50	Moderate	0.71
hh-clint	Human hepatocyte intrinsic clearance	24.946	uL/min/10^6 cells	Moderate	0.71
hlm-clint	Human liver microsomal intrinsic clearance	64.863	uL/min/mg protein	Moderate	0.71
hppb	Human plasma protein binding (% unbound)	5.960	%	Moderate	0.71
kinase-safety-class	ACVR2A,ACVR2B,AKT1,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,INSR,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAP4K1,MAPK10,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PDK1,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ZAP70	54
mdck-mdr1-efflux	MDCK-MDR1 efflux ratio	0.520		Moderate	0.71
mh-clint	Mouse hepatocyte intrinsic clearance	185.780		Moderate	0.71
mppb	Mouse plasma protein binding (% unbound)	6.950		Moderate	0.71
nih-mdck-mdr1-efflux	NIH MDCK-MDR1 efflux ratio	1.945		Moderate	0.71
pfas-class	PFAS structural alert (1 = True, 0 = False)	0
pld-class	Phospholipidosis risk class (1 = positive, 0 = negative)	1		Moderate	0.71
pppb	Pig plasma protein binding (% unbound)	17.950	%	Moderate	0.71
rh-clint	Rat hepatocyte intrinsic clearance	252.348	uL/min/10^6 cells	Moderate	0.71
rh-fuinc	Rat hepatocyte fraction unbound in incubation	36.950	%	Moderate	0.71
rppb	Rat plasma protein binding (% unbound)	6.930	%	Moderate	0.71
solubility-dd	Solubility at pH 7.4 in DMSO	535.797	uM	Moderate	0.71

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	5658.99	144.86	997	3400	28337	90595713
Intentional overdose	4934.84	144.86	1073	3324	92761	90531289
Depressed level of consciousness	664.68	144.86	212	4185	72572	90551478
Tachycardia	315.44	144.86	153	4244	157520	90466530
Fatigue	249.38	144.86	290	4107	1153733	89470317
Toxicity to various agents	215.02	144.86	147	4250	287699	90336351
Suicide attempt	183.64	144.86	84	4313	75315	90548735
Snoring	179.02	144.86	43	4354	5083	90618967
Akathisia	177.10	144.86	50	4347	11109	90612941
Mydriasis	170.98	144.86	52	4345	14960	90609090

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	1817.38	96.42	339	1478	14863	42604655
Intentional overdose	1580.33	96.42	372	1445	51084	42568434
Depressed level of consciousness	184.23	96.42	71	1746	47899	42571619
Tachycardia	116.72	96.42	65	1752	101022	42518496

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	4763.19	101.50	873	3629	36556	110548241
Intentional overdose	3881.23	101.50	914	3588	131587	110453210
Depressed level of consciousness	474.42	101.50	176	4326	112102	110472695
Toxicity to various agents	314.51	101.50	211	4291	480344	110104453
Tachycardia	288.23	101.50	153	4349	226492	110358305
Fatigue	232.68	101.50	264	4238	1215694	109369103
Suicide attempt	187.59	101.50	89	4413	103305	110481492
Akathisia	168.94	101.50	51	4451	17062	110567735
Mydriasis	135.99	101.50	46	4456	22111	110562686
Formication	131.24	101.50	33	4469	5615	110579182
Somnolence	121.97	101.50	99	4403	297350	110287447
Suicidal ideation	109.36	101.50	60	4442	93877	110490920
Loss of consciousness	103.69	101.50	76	4426	196230	110388567

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	sedative
CHEBI has role	CHEBI:37930	phenothiazine antipsychotic drug
CHEBI has role	CHEBI:37956	histamine antagonist
CHEBI has role	CHEBI:48279	serotonergic antagonist
CHEBI has role	CHEBI:48561	dopaminergic antagonist
CHEBI has role	CHEBI:48876	muscarinic antagonist

Related Drugs by ATC class:

N05CM Other hypnotics and sedatives 13 drugs

apronalbromisovalcarbromalclomethiazoledexmedetomidineethchlorvynolhexapropymatemethaqualonemethylpentynolniaprazinescopolaminetriclofos show all 13 →

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	Type	Activity value (-log[M])	Mechanism 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
4018031	VANDF
4019914	VANDF
C0033473	UMLSCUI
CHEBI:8491	CHEBI
CHEMBL1201210	ChEMBL_ID
CHEMBL1201068	ChEMBL_ID
DB00777	DRUGBANK_ID
C084591	MESH_SUPPLEMENTAL_RECORD_UI
4940	PUBCHEM_CID
7284	IUPHAR_LIGAND_ID
735	INN_ID
1240-15-9	SECONDARY_CAS_RN
242Z0PM79Y	UNII
227589	RXNORM
1709	MMSL
5371	MMSL
d00914	MMSL
001488	NDDF
001489	NDDF
373493007	SNOMEDCT_US
41324009	SNOMEDCT_US
65868004	SNOMEDCT_US
242Z0PM79Y	INXIGHT DRUGS

Pharmaceutical products:

None