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

Stem definition	Drug id	CAS RN
antipsychotics, risperidone derivatives	4137	144598-75-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: RO76477 RO 76477 paliperidone invega xeplion	Molecular weight: 426.49 Formula: C23H27FN4O3 CLOGP: 1.87 LIPINSKI: 0 HAC: 7 HDO: 1 TPSA: 82.17 ALOGS: -3.16 ROTB: 4 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

RO76477
RO 76477
paliperidone
invega
xeplion

Molecular weight: 426.49
Formula: C23H27FN4O3
CLOGP: 1.87
LIPINSKI: 0
HAC: 7
HDO: 1
TPSA: 82.17
ALOGS: -3.16
ROTB: 4

Status: OFP

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

Drug dosage:

Dose	Unit	Route
6	mg	O
2.50	mg	P

ADMET properties:

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Property	Value	Reference
EoM (Fraction excreted unchanged in urine)	59 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	4	Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability)	28 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
t_half (Half-life)	24.60 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	1.18 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.24 %	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.03 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

Date	Agency	Company	Orphan
Dec. 19, 2006	FDA	JANSSEN PHARMS
June 25, 2007	EMA

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 prolactin abnormal	1166.69	25.43	234	12044	2845	63473899
Anosognosia	1075.04	25.43	220	12058	2976	63473768
Sexual dysfunction	1023.76	25.43	223	12055	4136	63472608
Galactorrhoea	1017.49	25.43	220	12058	3935	63472809
Disturbance in social behaviour	1003.57	25.43	216	12062	3777	63472967
Metabolic disorder	914.21	25.43	219	12059	6284	63470460
Dystonia	908.07	25.43	254	12024	13565	63463179
Personality change	838.06	25.43	207	12071	6766	63469978
Sedation	787.89	25.43	292	11986	38517	63438227
Dyskinesia	743.32	25.43	266	12012	31736	63445008

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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
Gynaecomastia	564.71	23.27	190	12429	9990	34934322
Dystonia	472.30	23.27	169	12450	10676	34933636
Psychotic disorder	348.68	23.27	172	12447	24280	34920032
Treatment noncompliance	309.10	23.27	166	12453	27934	34916378
Extrapyramidal disorder	304.94	23.27	129	12490	12751	34931561
Akathisia	295.93	23.27	111	12508	7998	34936314
Intentional self-injury	258.02	23.27	117	12502	13654	34930658
Weight increased	255.45	23.27	234	12385	92799	34851513
Anosognosia	248.93	23.27	60	12559	913	34943399
Sedation	241.91	23.27	128	12491	20878	34923434

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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
Blood prolactin abnormal	1146.80	23.13	246	18881	3355	79721906
Anosognosia	1141.57	23.13	247	18880	3517	79721744
Dystonia	1131.83	23.13	349	18778	21050	79704211
Sexual dysfunction	1052.57	23.13	265	18862	7498	79717763
Disturbance in social behaviour	1009.34	23.13	235	18892	4735	79720526
Metabolic disorder	899.29	23.13	242	18885	8928	79716333
Sedation	846.64	23.13	354	18773	51541	79673720
Personality change	805.81	23.13	227	18900	9943	79715318
Dyskinesia	752.29	23.13	312	18815	44461	79680800
Suicide attempt	731.77	23.13	369	18758	82563	79642698

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N05AX13	NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Other antipsychotics
CHEBI has role	CHEBI:35471	psychotropic drugs
CHEBI has role	CHEBI:37890	alpha-adrenergic receptor blockaders
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:49103	drug metabolites
CHEBI has role	CHEBI:63726	neuroprotective agents
CHEBI has role	CHEBI:65191	atypical antipsychotic agent
FDA EPC	N0000175430	Atypical Antipsychotic

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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
Schizoaffective disorder	indication	68890003	DOID:5418
Psychotic disorder	indication	69322001
Mixed bipolar I disorder	off-label use	16506000	DOID:3312
Bipolar disorder in remission	off-label use	85248005
Bipolar affective disorder, current episode manic	off-label use	191618007
Bipolar affective disorder, current episode depression	off-label use	191627008	DOID:3312
Infantile autism	off-label use	408857007
Depression Treatment Adjunct	off-label use
Priapism	contraindication	6273006	DOID:9286

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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	7.78	Basic
pKa2	2.73	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	8.47	PDSP	DRUG LABEL
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	ANTAGONIST	Ki	8.96	PDSP	DRUG LABEL
Beta-2 adrenergic receptor	GPCR	P07550	ADRB2_HUMAN		Ki	5.30	PDSP
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	7.39	PDSP
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	7.93	PDSP
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	5.89	CHEMBL
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	5.43	PDSP
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	6.22	PDSP
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	7.21	PDSP
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	7.32	PDSP

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External reference:

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ID	Source
011888	NDDF
115237	PUBCHEM_CID
23004	MMSL
4025875	VUID
4025875	VANDF
425483000	SNOMEDCT_US
426276000	SNOMEDCT_US
679314	RXNORM
7258	IUPHAR_LIGAND_ID
7977	INN_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Paliperidone	HUMAN PRESCRIPTION DRUG LABEL	1	0378-3978	TABLET, FILM COATED, EXTENDED RELEASE	1.50 mg	ORAL	ANDA	33 sections
Paliperidone	HUMAN PRESCRIPTION DRUG LABEL	1	0378-3978	TABLET, FILM COATED, EXTENDED RELEASE	1.50 mg	ORAL	ANDA	33 sections
Paliperidone	HUMAN PRESCRIPTION DRUG LABEL	1	0378-3978	TABLET, FILM COATED, EXTENDED RELEASE	1.50 mg	ORAL	ANDA	33 sections
Paliperidone	HUMAN PRESCRIPTION DRUG LABEL	1	0378-3979	TABLET, FILM COATED, EXTENDED RELEASE	3 mg	ORAL	ANDA	33 sections
Paliperidone	HUMAN PRESCRIPTION DRUG LABEL	1	0378-3979	TABLET, FILM COATED, EXTENDED RELEASE	3 mg	ORAL	ANDA	33 sections
Paliperidone	HUMAN PRESCRIPTION DRUG LABEL	1	0378-3979	TABLET, FILM COATED, EXTENDED RELEASE	3 mg	ORAL	ANDA	33 sections
Paliperidone	HUMAN PRESCRIPTION DRUG LABEL	1	0378-3980	TABLET, FILM COATED, EXTENDED RELEASE	6 mg	ORAL	ANDA	33 sections
Paliperidone	HUMAN PRESCRIPTION DRUG LABEL	1	0378-3980	TABLET, FILM COATED, EXTENDED RELEASE	6 mg	ORAL	ANDA	33 sections
Paliperidone	HUMAN PRESCRIPTION DRUG LABEL	1	0378-3980	TABLET, FILM COATED, EXTENDED RELEASE	6 mg	ORAL	ANDA	33 sections
Paliperidone	HUMAN PRESCRIPTION DRUG LABEL	1	0378-3981	TABLET, FILM COATED, EXTENDED RELEASE	9 mg	ORAL	ANDA	33 sections

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