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

Stem definition	Drug id	CAS RN
	2284	58-40-2

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: promazine prazin prazine romtiazin promazine hydrochloride promazine HCl	A phenothiazine with actions similar to CHLORPROMAZINE but with less antipsychotic activity. It is primarily used in short-term treatment of disturbed behavior and as an antiemetic. Molecular weight: 284.42 Formula: C17H20N2S CLOGP: 4.60 LIPINSKI: 0 HAC: 2 HDO: 0 TPSA: 6.48 ALOGS: -4.14 ROTB: 4 Status: OFM Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

promazine
prazin
prazine
romtiazin
promazine hydrochloride
promazine HCl

A phenothiazine with actions similar to CHLORPROMAZINE but with less antipsychotic activity. It is primarily used in short-term treatment of disturbed behavior and as an antiemetic.

Molecular weight: 284.42
Formula: C17H20N2S
CLOGP: 4.60
LIPINSKI: 0
HAC: 2
HDO: 0
TPSA: 6.48
ALOGS: -4.14
ROTB: 4

Status: OFM

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

Drug dosage:

Dose	Unit	Route
0.30	g	O
0.10	g	P

ADMET properties:

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Property	Value	Reference
Vd (Volume of distribution)	8.10 L/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	7.90 hours	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	50.23 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
EoM (Fraction excreted unchanged in urine)	2 %	Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability)	16.25 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
CL (Clearance)	14 mL/min/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.11 %	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.02 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

Date	Agency	Company	Orphan
April 13, 1956	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
Sopor	679.73	56.62	152	1762	22012	63465096
Drug abuse	338.27	56.62	113	1801	72405	63414703
Intentional self-injury	189.64	56.62	57	1857	25630	63461478
Intentional overdose	143.84	56.62	61	1853	74091	63413017
Electrocardiogram QT prolonged	105.53	56.62	46	1868	59484	63427624
Suicide attempt	91.71	56.62	42	1872	60876	63426232
Drug interaction	73.01	56.62	58	1856	229073	63258035
Coma	65.57	56.62	34	1880	64330	63422778
Bradyphrenia	62.38	56.62	18	1896	6962	63480146
Overdose	61.62	56.62	40	1874	115038	63372070

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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
Sopor	266.04	45.22	70	1637	12066	34943158
Suicide attempt	139.38	45.22	57	1650	39059	34916165
Intentional self-injury	124.56	45.22	40	1667	13731	34941493
Drug abuse	117.74	45.22	68	1639	99028	34856196
Intentional overdose	116.95	45.22	52	1655	43622	34911602
Somnolence	92.94	45.22	61	1646	111055	34844169
Coma	50.43	45.22	30	1677	45648	34909576
Drug interaction	48.26	45.22	57	1650	225889	34729335

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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
Sopor	913.35	43.38	225	3361	32785	79708017
Drug abuse	401.58	43.38	178	3408	162513	79578289
Intentional self-injury	312.93	43.38	97	3489	32322	79708480
Intentional overdose	174.35	43.38	88	3498	105872	79634930
Suicide attempt	142.56	43.38	71	3515	82861	79657941
Electrocardiogram QT prolonged	128.21	43.38	68	3518	90318	79650484
Drug interaction	110.38	43.38	113	3473	415070	79325732
Bradyphrenia	103.11	43.38	32	3554	10608	79730194
Coma	100.03	43.38	60	3526	100589	79640213
Alcohol interaction	79.68	43.38	22	3564	4852	79735950

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N05AA03	NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Phenothiazines with aliphatic side-chain
CHEBI has role	CHEBI:37930	phenothiazine antipsychotic drugs
CHEBI has role	CHEBI:37955	H1 receptor antagonists
CHEBI has role	CHEBI:48279	serotonin antagonists
CHEBI has role	CHEBI:48561	dopaminergic antagonists
CHEBI has role	CHEBI:48876	muscarinic antagonists
CHEBI has role	CHEBI:50919	antiemetico
CHEBI has role	CHEBI:76779	post-proline endopeptidase inhibitors
MeSH PA	D000932	Antiemetics
MeSH PA	D014150	Antipsychotic Agents

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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
Dermatographic urticaria	indication	7632005	DOID:743
Nausea and vomiting	indication	16932000
Angioedema	indication	41291007	DOID:1558
General anesthesia	indication	50697003
Disruptive behavior disorder	indication	54319003
Schizophrenia	indication	58214004	DOID:5419
Allergic rhinitis	indication	61582004
Nasal discharge	indication	64531003
Nasal congestion	indication	68235000
Psychotic disorder	indication	69322001

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🐶 Veterinary Drug Use

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Species	Use	Relation
Cats	Tranquilization	Indication
Cats	Adjunctive therapy for tetanus	Indication
Cats	Antiemetic prior to worming	Indication
Cats	Preanesthesia	Indication
Cats	Minor operative procedures in conjunction with local anesthesia	Indication
Dogs	Tranquilization	Indication
Dogs	Adjunctive therapy for tetanus	Indication
Dogs	Antiemetic prior to worming	Indication
Dogs	Prevent motion sickness	Indication
Dogs	Preanesthesia	Indication

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🐶 Veterinary products

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Product	Applicant	Ingredients
Ketaset Plus	Zoetis Inc.	3
Promazine Granules	Zoetis Inc.	1
Promazine HCl Injectable	Zoetis Inc.	1
Tranquazine Injection	Bimeda Animal Health Limited	1

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Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.04	Basic
pKa2	3.55	Basic

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
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN	ANTAGONIST	Ki	6.70	WOMBAT-PK	CHEMBL
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	ANTAGONIST	Ki	7.80	WOMBAT-PK	CHEMBL
Sigma non-opioid intracellular receptor 1	Membrane receptor	Q99720	SGMR1_HUMAN		Ki	6.94	DRUG MATRIX
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	7.34	DRUG MATRIX
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	7.89	DRUG MATRIX
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	5.53	DRUG MATRIX
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	6.66	DRUG MATRIX
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	7.28	DRUG MATRIX
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN		Ki	6.90	DRUG MATRIX
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		Ki	8.23	WOMBAT-PK

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External reference:

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ID	Source
P2Z	PDB_CHEM_ID
001471	NDDF
004588	NDDF
142444	RXNORM
2128	MMSL
372741002	SNOMEDCT_US
4018021	VANDF
4019909	VUID
4019909	VANDF
44658005	SNOMEDCT_US

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Pharmaceutical products:

None