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

Stem definition	Drug id	CAS RN
	1212	69-23-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: fluphenazine fluorfenazine fluorophenazine fluorphenazine ftorphenazine phthorphenazine fluphenazine hydrochloride fluphenazine dihydrochloride fluphenazine HCl flufenazin	A phenothiazine used in the treatment of PSYCHOSES. Its properties and uses are generally similar to those of CHLORPROMAZINE. Molecular weight: 437.53 Formula: C22H26F3N3OS CLOGP: 4.32 LIPINSKI: 0 HAC: 4 HDO: 1 TPSA: 29.95 ALOGS: -4.36 ROTB: 7 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

fluphenazine
fluorfenazine
fluorophenazine
fluorphenazine
ftorphenazine
phthorphenazine
fluphenazine hydrochloride
fluphenazine dihydrochloride
fluphenazine HCl
flufenazin

A phenothiazine used in the treatment of PSYCHOSES. Its properties and uses are generally similar to those of CHLORPROMAZINE.

Molecular weight: 437.53
Formula: C22H26F3N3OS
CLOGP: 4.32
LIPINSKI: 0
HAC: 4
HDO: 1
TPSA: 29.95
ALOGS: -4.36
ROTB: 7

Status: OFP

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

Drug dosage:

Dose	Unit	Route
10	mg	O
1	mg	P

ADMET properties:

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Property	Value	Reference
CL (Clearance)	9.70 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	2.90 L/kg	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	2.70 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	12.30 hours	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.65 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
EoM (Fraction excreted unchanged in urine)	0.10 %	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.04 %	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.03 mg/mL	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Sept. 9, 1959	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
Salivary hypersecretion	54.94	40.08	14	842	7652	63480514
Neuroleptic malignant syndrome	53.17	40.08	15	841	12041	63476125
Accommodation disorder	50.85	40.08	8	848	373	63487793
Blood prolactin increased	49.08	40.08	11	845	3492	63484674
Suicide attempt	41.70	40.08	19	837	60899	63427267

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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
Neuroleptic malignant syndrome	120.50	43.31	37	1018	17897	34937979
Priapism	103.23	43.31	25	1030	4969	34950907
Compartment syndrome	61.76	43.31	15	1040	3003	34952873
Salivary hypersecretion	58.62	43.31	18	1037	8626	34947250
Torsade de pointes	57.45	43.31	17	1038	7192	34948684
Sedation	53.34	43.31	21	1034	20985	34934891

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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
Neuroleptic malignant syndrome	173.56	39.49	51	1803	27508	79715026
Salivary hypersecretion	119.52	39.49	33	1821	14191	79728343
Priapism	112.15	39.49	25	1829	4480	79738054
Torsade de pointes	88.38	39.49	28	1826	19284	79723250
Sedation	74.36	39.49	32	1822	51863	79690671
Compartment syndrome	57.84	39.49	15	1839	5067	79737467
Extrapyramidal disorder	49.73	39.49	19	1835	22660	79719874
Parkinsonism	47.83	39.49	17	1837	16567	79725967
Accommodation disorder	42.87	39.49	8	1846	590	79741944
Embolism venous	41.00	39.49	11	1843	4228	79738306

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N05AB02	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:149553	anticoronaviral drug
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
Schizophrenia	indication	58214004	DOID:5419
Psychotic disorder	indication	69322001
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

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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	2.72	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	9.27	WOMBAT-PK	CHEMBL
Mu-type opioid receptor	GPCR	P35372	OPRM_HUMAN		Ki	5.08	DRUG MATRIX
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	7.65	WOMBAT-PK
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	6.50	WOMBAT-PK
Sigma non-opioid intracellular receptor 1	Membrane receptor	Q99720	SGMR1_HUMAN		Ki	8.07	DRUG MATRIX
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		Ki	5.33	DRUG MATRIX
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	6.10	DRUG MATRIX
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	5.71	DRUG MATRIX
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	6.84	WOMBAT-PK
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	8.04	WOMBAT-PK

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External reference:

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ID	Source
001473	NDDF
001476	NDDF
146-56-5	SECONDARY_CAS_RN
203207	RXNORM
204	IUPHAR_LIGAND_ID
3372	PUBCHEM_CID
372730004	SNOMEDCT_US
4017723	VANDF
4019762	VUID
4019762	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Fluphenazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0121-0653	SOLUTION, CONCENTRATE	5 mg	ORAL	ANDA	16 sections
Fluphenazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0121-0654	ELIXIR	0.50 mg	ORAL	ANDA	16 sections
Fluphenazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0121-0654	ELIXIR	0.50 mg	ORAL	ANDA	16 sections
Fluphenazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0121-0654	ELIXIR	0.50 mg	ORAL	ANDA	16 sections
Fluphenazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0527-1788	TABLET, FILM COATED	1 mg	ORAL	ANDA	14 sections
Fluphenazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0527-1788	TABLET, FILM COATED	1 mg	ORAL	ANDA	14 sections
Fluphenazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0527-1789	TABLET, FILM COATED	2.50 mg	ORAL	ANDA	14 sections
Fluphenazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0527-1789	TABLET, FILM COATED	2.50 mg	ORAL	ANDA	14 sections
Fluphenazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0527-1790	TABLET, FILM COATED	5 mg	ORAL	ANDA	14 sections
Fluphenazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0527-1790	TABLET, FILM COATED	5 mg	ORAL	ANDA	14 sections

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