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

Stem definition	Drug id	CAS RN
psychotropics, phenylpiperazine derivatives	242	129722-12-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: aripiprazole hydrate aripiprazole abilify arpizol pripiprazole OPC-14597	A piperazine and quinolone derivative that is used primarily as an antipsychotic agent. It is a partial agonist of SEROTONIN RECEPTOR, 5-HT1A and DOPAMINE D2 RECEPTORS, where it also functions as a post-synaptic antagonist, and an antagonist of SEROTONIN RECEPTOR, 5-HT2A. It is used for the treatment of SCHIZOPHRENIA and BIPOLAR DISORDER, and as an adjunct therapy for the treatment of depression. Molecular weight: 448.39 Formula: C23H27Cl2N3O2 CLOGP: 5.11 LIPINSKI: 1 HAC: 5 HDO: 1 TPSA: 44.81 ALOGS: -4.76 ROTB: 7 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

aripiprazole hydrate
aripiprazole
abilify
arpizol
pripiprazole
OPC-14597

A piperazine and quinolone derivative that is used primarily as an antipsychotic agent. It is a partial agonist of SEROTONIN RECEPTOR, 5-HT1A and DOPAMINE D2 RECEPTORS, where it also functions as a post-synaptic antagonist, and an antagonist of SEROTONIN RECEPTOR, 5-HT2A. It is used for the treatment of SCHIZOPHRENIA and BIPOLAR DISORDER, and as an adjunct therapy for the treatment of depression.

Molecular weight: 448.39
Formula: C23H27Cl2N3O2
CLOGP: 5.11
LIPINSKI: 1
HAC: 5
HDO: 1
TPSA: 44.81
ALOGS: -4.76
ROTB: 7

Status: OFP

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

Drug dosage:

Dose	Unit	Route
15	mg	O
13.30	mg	P
15	mg	P

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	87 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
t_half (Half-life)	75 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	4.90 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	0.83 mL/min/kg	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.56 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.01 %	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.00 mg/mL	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

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Date	Agency	Company
Jan. 23, 2006	PMDA	Otsuka Pharmaceutical Co., Ltd
June 4, 2004	EMA
Nov. 15, 2002	FDA	OTSUKA

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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
Akathisia	1643.70	11.81	588	93565	8558	63386311
Tardive dyskinesia	1639.63	11.81	576	93577	7926	63386943
Dystonia	1364.34	11.81	575	93578	13244	63381625
Suicide attempt	1130.86	11.81	842	93311	60076	63334793
Extrapyramidal disorder	1102.42	11.81	489	93664	12795	63382074
Dyskinesia	996.84	11.81	610	93543	31392	63363477
Sedation	982.77	11.81	649	93504	38160	63356709
Sexual dysfunction	955.20	11.81	325	93828	4034	63390835
Blood prolactin abnormal	927.17	11.81	292	93861	2787	63392082
Suicidal ideation	818.85	11.81	704	93449	61717	63333152

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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	1319.28	14.07	523	68355	7586	34880467
Neuroleptic malignant syndrome	1205.51	14.07	624	68254	17310	34870743
Psychotic disorder	1120.96	14.07	661	68217	23791	34864262
Tardive dyskinesia	915.71	14.07	366	68512	5424	34882629
Extrapyramidal disorder	905.34	14.07	462	68416	12418	34875635
Dystonia	817.79	14.07	408	68470	10437	34877616
Sedation	801.23	14.07	505	68373	20501	34867552
Weight increased	615.96	14.07	834	68044	92199	34795854
Delusion	608.76	14.07	353	68525	12282	34875771
Parkinsonism	604.14	14.07	303	68575	7835	34880218

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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	2162.96	11.83	817	131095	12442	79600034
Dystonia	1883.35	11.83	848	131064	20551	79591925
Tardive dyskinesia	1865.14	11.83	690	131222	9881	79602595
Extrapyramidal disorder	1789.46	11.83	833	131079	21846	79590630
Neuroleptic malignant syndrome	1673.09	11.83	846	131066	26713	79585763
Sedation	1504.98	11.83	984	130928	50911	79561565
Suicide attempt	1442.61	11.83	1153	130759	81779	79530697
Psychotic disorder	1402.16	11.83	866	131046	40536	79571940
Dyskinesia	1320.23	11.83	858	131054	43915	79568561
Parkinsonism	1209.18	11.83	577	131335	16007	79596469

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FDA Adverse Event Reporting System (Pediatric)

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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
Enterococcal sepsis	28.03	25.07	10	1019	10	88753
Right ventricular false tendon	28.03	25.07	10	1019	10	88753

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Pharmacologic Action:

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Source	Code	Description
ATC	N05AX12	NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Other antipsychotics
CHEBI has role	CHEBI:35941	serotonin agonists
CHEBI has role	CHEBI:37955	H1 receptor antagonists
CHEBI has role	CHEBI:49103	drug metabolites
CHEBI has role	CHEBI:65191	atypical antipsychotic agent
FDA EPC	N0000175430	Atypical Antipsychotic
MeSH PA	D000928	Antidepressive Agents
MeSH PA	D014150	Antipsychotic Agents
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D002492	Central Nervous System Depressants

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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
Mixed bipolar I disorder	indication	16506000	DOID:3312
Schizophrenia	indication	58214004	DOID:5419
Bipolar disorder in remission	indication	85248005
Bipolar affective disorder, current episode manic	indication	191618007
Infantile autism	indication	408857007
Agitation associated with Bipolar Mania	indication
Depression Treatment Adjunct	indication
Agitation associated with Schizophrenia	indication
Suicidal thoughts	contraindication	6471006
Neuroleptic malignant syndrome	contraindication	15244003	DOID:14464

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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	7.84	Basic
pKa2	0.67	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
10MG	ABILIFY	OTSUKA	N021436	Nov. 15, 2002	RX	TABLET	ORAL	9387182	Dec. 25, 2023	ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
10MG	ABILIFY MYCITE KIT	OTSUKA	N207202	Nov. 13, 2017	RX	TABLET	ORAL	9387182	Dec. 25, 2023	ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
10MG	ABILIFY	OTSUKA	N021436	Nov. 15, 2002	RX	TABLET	ORAL	9125939	July 28, 2026	ACUTE TREATMENT OF MANIC AND MIXED EPISODES ASSOCIATED WITH BIPOLAR I DISORDER
10MG	ABILIFY MYCITE KIT	OTSUKA	N207202	Nov. 13, 2017	RX	TABLET	ORAL	9125939	July 28, 2026	ACUTE TREATMENT OF MANIC AND MIXED EPISODES ASSOCIATED WITH BIPOLAR I DISORDER
10MG	ABILIFY	OTSUKA	N021436	Nov. 15, 2002	RX	TABLET	ORAL	8759350	March 2, 2027	ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
10MG	ABILIFY MYCITE KIT	OTSUKA	N207202	Nov. 13, 2017	RX	TABLET	ORAL	8759350	March 2, 2027	ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
10MG	ABILIFY MYCITE KIT	OTSUKA	N207202	Nov. 13, 2017	RX	TABLET	ORAL	9444503	Nov. 19, 2027	METHOD OF USING A RECEIVER TO IDENTIFY A SIGNAL FROM A TABLET EMBEDDED WITH A SENSOR THAT COMMUNICATES INFORMATION THROUGH THE BODY OF A PATIENT
10MG	ABILIFY MYCITE KIT	OTSUKA	N207202	Nov. 13, 2017	RX	TABLET	ORAL	8674825	April 9, 2029	METHOD OF USING A RECEIVER TO RECEIVE A SIGNAL FROM A TABLET EMBEDDED WITH A SENSOR THAT COMMUNICATES INFORMATION THROUGH THE BODY OF A PATIENT
10MG	ABILIFY MYCITE KIT	OTSUKA	N207202	Nov. 13, 2017	RX	TABLET	ORAL	8956288	July 6, 2029	METHOD OF USING A TABLET EMBEDDED WITH A SENSOR THAT COMMUNICATES INFORMATION VIA A SIGNAL THROUGH THE BODY OF A PATIENT TO A RECEIVER
10MG	ABILIFY MYCITE KIT	OTSUKA	N207202	Nov. 13, 2017	RX	TABLET	ORAL	8945005	Aug. 19, 2029	METHOD OF USING A TABLET EMBEDDED WITH A SENSOR THAT COMMUNICATES INFORMATION VIA A SIGNAL THROUGH THE BODY OF A PATIENT TO A RECEIVER

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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	PARTIAL AGONIST	Ki	8.71	WOMBAT-PK	CHEMBL
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	ANTAGONIST	Ki	7.90	WOMBAT-PK	CHEMBL
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN	PARTIAL AGONIST	Ki	8.15	WOMBAT-PK	DRUG LABEL
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	7.13	PDSP
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		Ki	6.22	CHEMBL
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN		IC50	6.11	CHEMBL
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	6.83	WOMBAT-PK
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	5.68	PDSP
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	9.44	PDSP
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	7.36	WOMBAT-PK

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External reference:

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ID	Source
9SC	PDB_CHEM_ID
009852	NDDF
17034	MMSL
231328	MMSL
34	IUPHAR_LIGAND_ID
352393	RXNORM
4021367	VUID
4021367	VANDF
406784005	SNOMEDCT_US
406785006	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Aripiprazole	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8259	TABLET	5 mg	ORAL	ANDA	33 sections
Aripiprazole	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8375	TABLET	5 mg	ORAL	ANDA	32 sections
Aripiprazole	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8375	TABLET	5 mg	ORAL	ANDA	32 sections
Aripiprazole	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6509	TABLET	2 mg	ORAL	ANDA	31 sections
Aripiprazole	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6509	TABLET	2 mg	ORAL	ANDA	31 sections
Aripiprazole	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6510	TABLET	5 mg	ORAL	ANDA	31 sections
Aripiprazole	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6510	TABLET	5 mg	ORAL	ANDA	31 sections
Aripiprazole	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6511	TABLET	10 mg	ORAL	ANDA	31 sections
Aripiprazole	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6511	TABLET	10 mg	ORAL	ANDA	31 sections
Aripiprazole	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6512	TABLET	15 mg	ORAL	ANDA	31 sections

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