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

Stem definition	Drug id	CAS RN
	2113	58-39-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: perphenazine perfenazine perfenil perphenan perphenazin thilatazin tranquisan perphanzine	An antipsychotic phenothiazine derivative with actions and uses similar to those of CHLORPROMAZINE. Molecular weight: 403.97 Formula: C21H26ClN3OS CLOGP: 4.01 LIPINSKI: 0 HAC: 4 HDO: 1 TPSA: 29.95 ALOGS: -4.23 ROTB: 6 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

perphenazine
perfenazine
perfenil
perphenan
perphenazin
thilatazin
tranquisan
perphanzine

An antipsychotic phenothiazine derivative with actions and uses similar to those of CHLORPROMAZINE.

Molecular weight: 403.97
Formula: C21H26ClN3OS
CLOGP: 4.01
LIPINSKI: 0
HAC: 4
HDO: 1
TPSA: 29.95
ALOGS: -4.23
ROTB: 6

Status: OFP

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

Drug dosage:

Dose	Unit	Route
30	mg	O
7	mg	P
10	mg	P
16	mg	R

ADMET properties:

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Property	Value	Reference
t_half (Half-life)	9.40 hours	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	40 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
CL (Clearance)	27 mL/min/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ
Vd (Volume of distribution)	18 L/kg	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.99 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
fu (Fraction unbound in plasma)	0.07 %	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
Feb. 27, 1957	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
Blood magnesium increased	79.69	27.36	20	2870	3018	63483114
Pleural fibrosis	77.04	27.36	20	2870	3452	63482680
Presbyacusis	75.84	27.36	19	2871	2846	63483286
Pleural thickening	75.72	27.36	19	2871	2864	63483268
Tardive dyskinesia	71.43	27.36	23	2867	8479	63477653
Deafness neurosensory	65.91	27.36	19	2871	4836	63481296
Sopor	62.88	27.36	27	2863	22137	63463995
Drug abuse	60.83	27.36	39	2851	72479	63413653
Neuroleptic malignant syndrome	59.83	27.36	22	2868	12034	63474098
Epigastric discomfort	59.65	27.36	19	2871	6761	63479371

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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
Akathisia	464.17	46.23	111	2648	7998	34946174
Antipsychotic drug level below therapeutic	461.05	46.23	90	2669	2457	34951715
Therapeutic product effect variable	445.85	46.23	87	2672	2369	34951803
Disinhibition	439.83	46.23	90	2669	3136	34951036
Obsessive-compulsive disorder	434.16	46.23	98	2661	5466	34948706
Euphoric mood	400.43	46.23	92	2667	5549	34948623
Increased appetite	365.08	46.23	90	2669	7339	34946833
Suicide attempt	238.63	46.23	96	2663	39020	34915152
Therapeutic product effect incomplete	189.54	46.23	88	2671	50453	34903719
Leukaemia	177.44	46.23	46	2713	4557	34949615

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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
Akathisia	163.14	27.36	50	4271	13209	79726858
Antipsychotic drug level below therapeutic	123.16	27.36	25	4296	1213	79738854
Therapeutic product effect variable	116.56	27.36	26	4295	1983	79738084
Neuroleptic malignant syndrome	106.56	27.36	44	4277	27515	79712552
Disinhibition	104.70	27.36	25	4296	2573	79737494
Obsessive-compulsive disorder	93.06	27.36	27	4294	5900	79734167
Euphoric mood	86.00	27.36	27	4294	7699	79732368
Toxicity to various agents	75.73	27.36	103	4218	421437	79318630
Dyslipidaemia	75.16	27.36	27	4294	11606	79728461
Presbyacusis	73.93	27.36	19	4302	2641	79737426

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N05AB03	NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Phenothiazines with piperazine structure
CHEBI has role	CHEBI:37930	phenothiazine antipsychotic drugs
CHEBI has role	CHEBI:48561	dopaminergic antagonists
CHEBI has role	CHEBI:50919	antiemetico
FDA CS	M0016525	Phenothiazines
FDA EPC	N0000175746	Phenothiazine
MeSH PA	D014150	Antipsychotic Agents
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D002492	Central Nervous System Depressants
MeSH PA	D015259	Dopamine 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
Nausea and vomiting	indication	16932000
Schizophrenia	indication	58214004	DOID:5419
Mixed anxiety and depressive disorder	indication	231504006
Suicidal thoughts	contraindication	6471006
Alcoholism	contraindication	7200002
Organophosphate poisoning	contraindication	8260003
Weight gain finding	contraindication	8943002
Sinus tachycardia	contraindication	11092001
Neuroleptic malignant syndrome	contraindication	15244003	DOID:14464
Senile dementia	contraindication	15662003

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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	8.21	Basic
pKa2	4.21	Basic
pKa3	2.21	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	9.32	WOMBAT-PK	CHEMBL
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	6.07	WOMBAT-PK
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	8.25	WOMBAT-PK
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	6.19	WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		Ki	5.46	DRUG MATRIX
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN		Ki	7.55	WOMBAT-PK
5-hydroxytryptamine receptor 7	GPCR	P34969	5HT7R_HUMAN		Ki	7.64	WOMBAT-PK
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		Ki	8	WOMBAT-PK
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	6.98	WOMBAT-PK
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	9.52	WOMBAT-PK

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External reference:

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ID	Source
001477	NDDF
209	IUPHAR_LIGAND_ID
2271	MMSL
387229007	SNOMEDCT_US
4017939	VUID
4017939	VANDF
41147003	SNOMEDCT_US
4748	PUBCHEM_CID
5261	MMSL
637	INN_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Perphenazine	HUMAN PRESCRIPTION DRUG LABEL	1	0378-5350	TABLET, FILM COATED	2 mg	ORAL	ANDA	18 sections
Perphenazine	HUMAN PRESCRIPTION DRUG LABEL	1	0378-5351	TABLET, FILM COATED	4 mg	ORAL	ANDA	18 sections
Perphenazine	HUMAN PRESCRIPTION DRUG LABEL	1	0378-5352	TABLET, FILM COATED	8 mg	ORAL	ANDA	18 sections
Perphenazine	HUMAN PRESCRIPTION DRUG LABEL	1	0378-5353	TABLET, FILM COATED	16 mg	ORAL	ANDA	18 sections
Perphenazine	HUMAN PRESCRIPTION DRUG LABEL	1	0591-4101	TABLET, FILM COATED	2 mg	ORAL	ANDA	20 sections
Perphenazine	HUMAN PRESCRIPTION DRUG LABEL	1	0591-4102	TABLET, FILM COATED	4 mg	ORAL	ANDA	20 sections
Perphenazine	HUMAN PRESCRIPTION DRUG LABEL	1	0591-4103	TABLET, FILM COATED	8 mg	ORAL	ANDA	20 sections
Perphenazine	HUMAN PRESCRIPTION DRUG LABEL	1	0591-4104	TABLET, FILM COATED	16 mg	ORAL	ANDA	20 sections
Perphenazine	HUMAN PRESCRIPTION DRUG LABEL	1	0603-5060	TABLET, FILM COATED	2 mg	ORAL	ANDA	19 sections
Perphenazine	HUMAN PRESCRIPTION DRUG LABEL	1	0603-5060	TABLET, FILM COATED	2 mg	ORAL	ANDA	19 sections

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