Scroll

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

Stem definition	Drug id	CAS RN
antipsychotics, haloperidol derivatives	1353	52-86-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: haloperidol aloperidin haloperin sigaperidol haloperidol lactate	A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279) Molecular weight: 375.87 Formula: C21H23ClFNO2 CLOGP: 3.85 LIPINSKI: 0 HAC: 3 HDO: 1 TPSA: 40.54 ALOGS: -4.93 ROTB: 6 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

haloperidol
aloperidin
haloperin
sigaperidol
haloperidol lactate

A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279)

Molecular weight: 375.87
Formula: C21H23ClFNO2
CLOGP: 3.85
LIPINSKI: 0
HAC: 3
HDO: 1
TPSA: 40.54
ALOGS: -4.93
ROTB: 6

Status: OFP

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

Drug dosage:

Dose	Unit	Route
8	mg	O
8	mg	P
3.30	mg	P

ADMET properties:

Show entries

Search:

Property	Value	Reference
CL (Clearance)	7.80 mL/min/kg	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	60 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
t_half (Half-life)	35 hours	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
Vd (Volume of distribution)	17 L/kg	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	1 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.57 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
fu (Fraction unbound in plasma)	0.08 %	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.04 mg/mL	Benet LZ, Broccatelli F, Oprea TI

Showing 1 to 9 of 9 entries

Previous1Next

Approvals:

Date	Agency	Company	Orphan
April 12, 1967	FDA	ORTHO MCNEIL

FDA Adverse Event Reporting System (Female)

Show entries

Search:

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	1642.36	14.77	513	40811	11543	63436155
Extrapyramidal disorder	1399.16	14.77	465	40859	12819	63434879
Intentional self-injury	853.59	14.77	389	40935	25298	63422400
Drug interaction	483.01	14.77	666	40658	228465	63219233
Akathisia	477.83	14.77	191	41133	8955	63438743
Catatonia	456.21	14.77	153	41171	4324	63443374
Dystonia	417.39	14.77	196	41128	13623	63434075
Sopor	383.47	14.77	216	41108	21948	63425750
Muscle rigidity	362.45	14.77	168	41156	11332	63436366
Agitation	332.28	14.77	290	41034	59467	63388231

Showing 1 to 10 of 335 entries

Previous1 2 3 4 5…34Next

FDA Adverse Event Reporting System (Male)

Show entries

Search:

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	1961.40	13.90	808	52466	17126	34886531
Extrapyramidal disorder	1782.91	13.90	688	52586	12192	34891465
Dystonia	729.98	13.90	348	52926	10497	34893160
Akathisia	625.58	13.90	286	52988	7823	34895834
Intentional self-injury	614.94	13.90	335	52939	13436	34890221
Muscle rigidity	461.58	13.90	253	53021	10265	34893392
Sedation	417.50	13.90	306	52968	20700	34882957
Agitation	405.73	13.90	468	52806	56931	34846726
Catatonia	380.50	13.90	175	53099	4850	34898807
Psychotic disorder	367.82	13.90	302	52972	24150	34879507

Showing 1 to 10 of 369 entries

Previous1 2 3 4 5…37Next

FDA Adverse Event Reporting System (Geriatric)

Show entries

Search:

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	3429.85	13.64	1223	80007	26336	79636822
Extrapyramidal disorder	3006.26	13.64	1055	80175	21624	79641534
Intentional self-injury	1436.84	13.64	688	80542	31731	79631427
Dystonia	1024.15	13.64	479	80751	20920	79642238
Akathisia	842.70	13.64	362	80868	12897	79650261
Catatonia	810.15	13.64	313	80917	8443	79654715
Muscle rigidity	787.63	13.64	391	80839	19491	79643667
Agitation	707.01	13.64	675	80555	99040	79564118
Drug interaction	624.20	13.64	1332	79898	413851	79249307
Salivary hypersecretion	576.00	13.64	284	80946	13940	79649218

Showing 1 to 10 of 534 entries

Previous1 2 3 4 5…54Next

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Show entries

Search:

Source	Code	Description
ATC	N05AD01	NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Butyrophenone derivatives
CHEBI has role	CHEBI:48279	serotonin antagonists
CHEBI has role	CHEBI:48561	dopaminergic antagonists
CHEBI has role	CHEBI:50919	antiemetico
CHEBI has role	CHEBI:65190	typical antipsychotic drugs
CHEBI has role	CHEBI:66956	antidyskinetic agent
FDA EPC	N0000180182	Typical Antipsychotic
MeSH PA	D018726	Anti-Dyskinesia Agents
MeSH PA	D000932	Antiemetics
MeSH PA	D014150	Antipsychotic Agents

Showing 1 to 10 of 19 entries

Previous1 2Next

Drug Use | Suggest Off label Use Form| |View source of the data|

Show entries

Search:

Disease	Relation	SNOMED_ID	DOID
Gilles de la Tourette's syndrome	indication	5158005	DOID:11119
Schizophrenia	indication	58214004	DOID:5419
Psychotic disorder	indication	69322001
Chronic schizophrenia	indication	83746006
Delirium	off-label use	2776000
Nausea and vomiting	off-label use	16932000
Pain	off-label use	22253000
Anxiety disorder	off-label use	197480006	DOID:2030
Headache disorder	off-label use	230461009
Gastroparesis	off-label use	235675006

Showing 1 to 10 of 38 entries

Previous1 2 3 4Next

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.36	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Show entries

Search:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN	INVERSE AGONIST	Ki	9.15	WOMBAT-PK	CHEMBL
5-hydroxytryptamine receptor 5A	GPCR	P47898	5HT5A_HUMAN		Ki	5.65	PDSP
5-hydroxytryptamine receptor 1F	GPCR	P30939	5HT1F_HUMAN		Ki	5.30	PDSP
5-hydroxytryptamine receptor 1E	GPCR	P28566	5HT1E_HUMAN		Ki	5.30	PDSP
Beta-2 adrenergic receptor	GPCR	P07550	ADRB2_HUMAN		Ki	5.30	PDSP
Mu-type opioid receptor	GPCR	P35372	OPRM_HUMAN		Ki	6.00	DRUG MATRIX
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	7.82	WOMBAT-PK
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	5.95	PDSP
Sigma non-opioid intracellular receptor 1	Membrane receptor	Q99720	SGMR1_HUMAN		EC50	8.92	WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	7.50	WOMBAT-PK

Showing 1 to 10 of 82 entries

Previous1 2 3 4 5…9Next

External reference:

Show entries

Search:

ID	Source
001518	NDDF
001521	NDDF
10756001	SNOMEDCT_US
217483	RXNORM
2958	MMSL
3559	PUBCHEM_CID
386837002	SNOMEDCT_US
4018123	VUID
4018123	VANDF
4018125	VANDF

Showing 1 to 10 of 29 entries

Previous1 2 3Next

Pharmaceutical products:

Show entries

Search:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0121-0581	SOLUTION	2 mg	ORAL	ANDA	17 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0121-0581	SOLUTION	2 mg	ORAL	ANDA	17 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0121-0581	SOLUTION	2 mg	ORAL	ANDA	17 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9319	INJECTION	5 mg	INTRAMUSCULAR	ANDA	16 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9319	INJECTION	5 mg	INTRAMUSCULAR	ANDA	16 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9501	INJECTION	5 mg	INTRAMUSCULAR	ANDA	16 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9502	INJECTION	5 mg	INTRAMUSCULAR	ANDA	16 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0214	TABLET	2 mg	ORAL	ANDA	17 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0214	TABLET	2 mg	ORAL	ANDA	17 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0214	TABLET	2 mg	ORAL	ANDA	17 sections

Showing 1 to 10 of 30 entries

Previous1 2 3Next