haloperidol 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:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.04 mg/mL	Benet LZ, Broccatelli F, Oprea TI
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
BA (Bioavailability)	60 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	17 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	7.80 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.08 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	35 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
April 12, 1967	FDA	ORTHO MCNEIL

FDA Adverse Event Reporting System (Female)

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
Extrapyramidal disorder	1780.19	58.23	329	3783	2018	2351955
Neuroleptic malignant syndrome	1463.67	58.23	274	3838	1806	2352167
Intentional self-injury	1090.84	58.23	241	3871	3886	2350087
Weight increased	997.38	58.23	318	3794	22019	2331954
Akathisia	520.33	58.23	112	4000	1562	2352411
Somnolence	509.35	58.23	196	3916	23289	2330684
Intentional overdose	501.70	58.23	161	3951	11160	2342813
Dystonia	495.55	58.23	113	3999	2081	2351892
Suicide attempt	477.63	58.23	155	3957	11127	2342846
Catatonia	477.46	58.23	93	4019	757	2353216
Drug interaction	441.36	58.23	188	3924	28975	2324998
Toxicity to various agents	426.81	58.23	190	3922	32564	2321409
Sopor	409.14	58.23	109	4003	3886	2350087
Agitation	408.04	58.23	137	3975	10914	2343059
Muscle rigidity	406.32	58.23	93	4019	1738	2352235
Parkinsonism	391.25	58.23	87	4025	1418	2352555
Electrocardiogram QT prolonged	374.06	58.23	118	3994	7696	2346277
Tremor	348.18	58.23	144	3968	20517	2333456
Confusional state	328.65	58.23	145	3967	24199	2329774
Salivary hypersecretion	313.85	58.23	70	4042	1155	2352818
Overdose	309.28	58.23	131	3981	19776	2334197
Coma	305.44	58.23	105	4007	8951	2345022
Psychotic disorder	302.08	58.23	89	4023	4590	2349383
Sedation	293.78	58.23	81	4031	3281	2350692
Delirium	279.62	58.23	86	4026	5137	2348836
Tardive dyskinesia	250.08	58.23	62	4050	1642	2352331
Dyskinesia	248.47	58.23	77	4035	4712	2349261
Schizophrenia	237.93	58.23	57	4055	1302	2352671
Delusion	228.60	58.23	60	4052	2005	2351968
Aggression	227.58	58.23	72	4040	4714	2349259
Tachycardia	225.09	58.23	99	4013	16310	2337663
Torsade de pointes	223.60	58.23	60	4052	2186	2351787
Hyperprolactinaemia	216.70	58.23	47	4065	675	2353298
Dysphagia	207.64	58.23	87	4025	12718	2341255
Fall	205.29	58.23	132	3980	46967	2307006
Hypothermia	202.62	58.23	55	4057	2093	2351880
Depressed level of consciousness	202.32	58.23	74	4038	7530	2346443
Blood creatine phosphokinase increased	198.34	58.23	66	4046	5070	2348903
Hallucination, auditory	192.23	58.23	53	4059	2139	2351834
Dysarthria	185.11	58.23	66	4046	6236	2347737
Suicidal ideation	181.94	58.23	76	4036	11011	2342962
Hypertonia	181.66	58.23	45	4067	1185	2352788
Condition aggravated	180.98	58.23	106	4006	31873	2322100
Psychomotor hyperactivity	180.27	58.23	49	4063	1873	2352100
Drug ineffective	178.97	58.23	166	3946	101458	2252515
Treatment noncompliance	177.96	58.23	62	4050	5472	2348501
Toxic epidermal necrolysis	177.62	58.23	54	4058	3090	2350883
Restlessness	177.61	58.23	59	4053	4504	2349469
Hallucination	168.59	58.23	66	4046	8082	2345891
Exposure during pregnancy	167.91	58.23	93	4019	25126	2328847
Cognitive disorder	160.45	58.23	57	4055	5324	2348649
Drug abuse	153.32	58.23	69	4043	11957	2342016
Pulmonary embolism	152.20	58.23	78	4034	18005	2335968
Rhabdomyolysis	151.82	58.23	58	4054	6646	2347327
Hypotension	151.22	58.23	95	4017	32341	2321632
Off label use	148.50	58.23	130	3982	73468	2280505
Cardiac arrest	148.06	58.23	72	4040	14858	2339115
Drug hypersensitivity	144.42	58.23	106	4006	46537	2307436
Abnormal behaviour	140.29	58.23	50	4062	4710	2349263
Sluggishness	140.06	58.23	35	4077	955	2353018
Cogwheel rigidity	138.59	58.23	27	4085	218	2353755
Hyponatraemia	134.32	58.23	65	4047	13260	2340713
Urinary retention	133.09	58.23	45	4067	3622	2350351
Altered state of consciousness	130.82	58.23	45	4067	3815	2350158
Mutism	127.75	58.23	26	4086	268	2353705
Bradykinesia	119.25	58.23	28	4084	583	2353390
Pyrexia	118.54	58.23	100	4012	53608	2300365
Pleurothotonus	118.40	58.23	24	4088	242	2353731
Oculogyric crisis	116.95	58.23	25	4087	333	2353640
Completed suicide	114.25	58.23	68	4044	20966	2333007
Bradycardia	113.74	58.23	53	4059	9928	2344045
Blood prolactin increased	108.46	58.23	29	4083	1038	2352935
General physical health deterioration	107.46	58.23	57	4055	14082	2339891
Galactorrhoea	107.37	58.23	30	4082	1269	2352704
Pneumonia aspiration	101.57	58.23	37	4075	3705	2350268
Paranoia	101.29	58.23	32	4080	2075	2351898
Gestational diabetes	100.93	58.23	29	4083	1358	2352615
Miosis	99.94	58.23	28	4084	1196	2352777
Psychomotor retardation	99.64	58.23	24	4088	559	2353414
Hyperthermia	99.31	58.23	29	4083	1439	2352534
Disorientation	98.80	58.23	42	4070	6330	2347643
Bradyphrenia	93.66	58.23	26	4086	1073	2352900
Anxiety	93.55	58.23	68	4044	29291	2324682
Dehydration	93.08	58.23	61	4051	22234	2331739
Gait disturbance	92.46	58.23	61	4051	22484	2331489
Vomiting	92.22	58.23	99	4013	71503	2282470
Ileus paralytic	92.22	58.23	24	4088	772	2353201
Leukocytosis	92.03	58.23	34	4078	3542	2350431
Intentional product misuse	88.71	58.23	44	4068	9445	2344528
Loss of consciousness	84.85	58.23	54	4058	18713	2335260
Drooling	84.49	58.23	22	4090	709	2353264
Accidental exposure to product by child	83.41	58.23	21	4091	590	2353383
Seizure	83.26	58.23	59	4053	24407	2329566
Electrolyte imbalance	81.84	58.23	27	4085	2010	2351963
Hyperhidrosis	81.44	58.23	49	4063	15373	2338600
Respiratory disorder	81.20	58.23	32	4080	3972	2350001
Accidental exposure to product	81.20	58.23	40	4072	8457	2345516
Mental status changes	77.36	58.23	34	4078	5548	2348425
Negativism	76.88	58.23	15	4097	122	2353851
Unresponsive to stimuli	75.10	58.23	32	4080	4844	2349129
Medication error	74.31	58.23	34	4078	6097	2347876
Acute kidney injury	73.74	58.23	58	4054	28064	2325909
Maternal exposure during pregnancy	72.77	58.23	45	4067	14818	2339155
Torticollis	72.47	58.23	17	4095	352	2353621
Serotonin syndrome	70.76	58.23	28	4084	3512	2350461
Cholestasis	69.40	58.23	28	4084	3693	2350280
Dementia	67.17	58.23	25	4087	2656	2351317
Hepatocellular injury	67.08	58.23	28	4084	4027	2349946
Inappropriate antidiuretic hormone secretion	67.02	58.23	24	4088	2285	2351688
Cardio-respiratory arrest	66.98	58.23	36	4076	9110	2344863
Stupor	66.54	58.23	18	4094	673	2353300
Hyperreflexia	66.27	58.23	19	4093	882	2353091
Mania	65.73	58.23	24	4088	2416	2351557
Product use in unapproved indication	65.43	58.23	38	4074	11162	2342811
Musculoskeletal stiffness	64.86	58.23	39	4073	12208	2341765
Neutropenia	64.26	58.23	48	4064	21500	2332473
Constipation	64.10	58.23	48	4064	21581	2332392
Speech disorder	63.44	58.23	31	4081	6433	2347540
Leukopenia	63.31	58.23	36	4076	10160	2343813
Lethargy	62.91	58.23	34	4078	8696	2345277
Multiple organ dysfunction syndrome	61.39	58.23	32	4080	7609	2346364
Respiratory failure	61.29	58.23	39	4073	13489	2340484
Disturbance in attention	61.05	58.23	29	4083	5656	2348317
Psychomotor skills impaired	60.07	58.23	15	4097	407	2353566
Eosinophilic myocarditis	59.73	58.23	12	4100	115	2353858
Generalised tonic-clonic seizure	59.52	58.23	28	4084	5344	2348629
Drug level increased	59.06	58.23	23	4089	2764	2351209

FDA Adverse Event Reporting System (Male)

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
Extrapyramidal disorder	2110.77	48.01	425	4541	1952	1739863
Neuroleptic malignant syndrome	2101.01	48.01	444	4522	2704	1739111
Weight increased	1158.32	48.01	358	4608	10999	1730816
Dystonia	958.02	48.01	216	4750	1798	1740017
Agitation	705.70	48.01	245	4721	10781	1731034
Intentional self-injury	684.59	48.01	174	4792	2499	1739316
Toxicity to various agents	629.56	48.01	296	4670	28845	1712970
Somnolence	568.16	48.01	234	4732	16505	1725310
Muscle rigidity	546.08	48.01	135	4831	1713	1740102
Akathisia	505.33	48.01	119	4847	1209	1740606
Tachycardia	498.55	48.01	197	4769	12431	1729384
Blood creatine phosphokinase increased	452.95	48.01	167	4799	8689	1733126
Dyskinesia	444.68	48.01	134	4832	3685	1738130
Drug interaction	430.18	48.01	226	4740	27732	1714083
Electrocardiogram QT prolonged	427.33	48.01	142	4824	5403	1736412
Tremor	425.93	48.01	178	4788	12953	1728862
Completed suicide	411.04	48.01	185	4781	16127	1725688
Tardive dyskinesia	400.51	48.01	96	4870	1056	1740759
Delirium	400.47	48.01	140	4826	6222	1735593
Suicide attempt	395.02	48.01	144	4822	7237	1734578
Intentional overdose	389.62	48.01	144	4822	7526	1734289
Parkinsonism	389.05	48.01	97	4869	1272	1740543
Aggression	381.71	48.01	144	4822	7971	1733844
Drug ineffective	381.15	48.01	282	4684	63519	1678296
Sedation	347.00	48.01	108	4858	3309	1738506
Catatonia	345.36	48.01	81	4885	804	1741011
Psychotic disorder	344.08	48.01	118	4848	4938	1736877
Sopor	338.68	48.01	94	4872	1907	1739908
Dysphagia	313.10	48.01	133	4833	10035	1731780
Rhabdomyolysis	305.23	48.01	134	4832	10956	1730859
Confusional state	278.87	48.01	155	4811	21123	1720692
Coma	257.06	48.01	105	4861	7157	1734658
Altered state of consciousness	254.91	48.01	86	4880	3411	1738404
Restlessness	233.37	48.01	85	4881	4236	1737579
Cognitive disorder	233.20	48.01	85	4881	4245	1737570
Salivary hypersecretion	225.80	48.01	64	4902	1401	1740414
Torsade de pointes	222.99	48.01	62	4904	1262	1740553
Hypertonia	216.04	48.01	61	4905	1316	1740499
Dysarthria	213.59	48.01	84	4882	5175	1736640
Schizophrenia	200.51	48.01	63	4903	1983	1739832
Hypothermia	197.37	48.01	60	4906	1688	1740127
Condition aggravated	190.23	48.01	121	4845	21029	1720786
Hallucination, auditory	190.15	48.01	61	4905	2056	1739759
Overdose	184.50	48.01	109	4857	16592	1725223
Pyrexia	173.70	48.01	157	4809	46243	1695572
Treatment noncompliance	169.65	48.01	71	4895	5130	1736685
Hyperhidrosis	168.73	48.01	93	4873	12395	1729420
Cardiac arrest	168.18	48.01	101	4865	15829	1725986
Delusion	166.95	48.01	56	4910	2175	1739640
Hyperthermia	157.08	48.01	50	4916	1641	1740174
Hallucination	156.70	48.01	77	4889	8093	1733722
Drug abuse	155.44	48.01	91	4875	13598	1728217
Oropharyngeal spasm	152.83	48.01	26	4940	30	1741785
Fall	151.44	48.01	116	4850	27098	1714717
Cardio-respiratory arrest	150.18	48.01	78	4888	9215	1732600
Oculogyric crisis	140.14	48.01	33	4933	332	1741483
Musculoskeletal stiffness	138.99	48.01	64	4902	5812	1736003
Incorrect route of product administration	135.86	48.01	54	4912	3411	1738404
Speech disorder	134.71	48.01	58	4908	4490	1737325
Disorientation	133.85	48.01	61	4905	5408	1736407
Pneumonia aspiration	132.87	48.01	60	4906	5206	1736609
Sluggishness	132.52	48.01	36	4930	668	1741147
Hypotension	132.15	48.01	111	4855	29543	1712272
Depressed level of consciousness	128.96	48.01	63	4903	6529	1735286
Gait disturbance	127.60	48.01	78	4888	12592	1729223
Seizure	124.39	48.01	92	4874	20349	1721466
Disturbance in attention	122.12	48.01	53	4913	4181	1737634
Intestinal pseudo-obstruction	120.72	48.01	26	4940	167	1741648
Abnormal behaviour	119.24	48.01	59	4907	6283	1735532
Urinary retention	115.93	48.01	55	4911	5340	1736475
Hyperprolactinaemia	114.44	48.01	26	4940	220	1741595
Psychomotor hyperactivity	112.44	48.01	40	4926	1853	1739962
Hyponatraemia	110.49	48.01	63	4903	8937	1732878
Stupor	107.93	48.01	30	4936	608	1741207
Cogwheel rigidity	106.93	48.01	24	4942	191	1741624
Bradyphrenia	106.74	48.01	30	4936	634	1741181
Drooling	106.10	48.01	31	4935	756	1741059
Accidental exposure to product	101.12	48.01	46	4920	4055	1737760
Mental status changes	100.96	48.01	52	4914	6023	1735792
Bradycardia	98.77	48.01	62	4904	10472	1731343
Drug hypersensitivity	96.23	48.01	70	4896	15065	1726750
Unresponsive to stimuli	95.80	48.01	46	4920	4583	1737232
Body temperature increased	95.52	48.01	39	4927	2638	1739177
Medication error	94.73	48.01	46	4920	4697	1737118
Pulmonary embolism	93.63	48.01	65	4901	12994	1728821
Accidental exposure to product by child	93.54	48.01	28	4938	744	1741071
Off label use	92.99	48.01	103	4863	38468	1703347
Insomnia	91.68	48.01	70	4896	16206	1725609
Intentional product misuse	91.61	48.01	52	4914	7306	1734509
Anxiety	90.15	48.01	68	4898	15459	1726356
General physical health deterioration	86.40	48.01	62	4904	13056	1728759
Tachypnoea	86.34	48.01	35	4931	2323	1739492
Mania	86.22	48.01	34	4932	2099	1739716
Loss of consciousness	86.03	48.01	65	4901	14810	1727005
Leukocytosis	85.11	48.01	39	4927	3494	1738321
Eye movement disorder	85.09	48.01	27	4939	875	1740940
Antipsychotic drug level below therapeutic	82.67	48.01	19	4947	170	1741645
Bradykinesia	81.51	48.01	23	4943	493	1741322
Refusal of treatment by patient	81.46	48.01	28	4938	1169	1740646
Visceral congestion	81.40	48.01	17	4949	92	1741723
Myoclonus	80.39	48.01	33	4933	2262	1739553
Accidental overdose	79.00	48.01	39	4927	4125	1737690
Obsessive-compulsive disorder	78.99	48.01	25	4941	803	1741012
Torticollis	78.66	48.01	20	4946	283	1741532
Protrusion tongue	77.67	48.01	16	4950	80	1741735
Neutropenia	76.33	48.01	66	4900	18194	1723621
Mutism	75.89	48.01	18	4948	187	1741628
Swollen tongue	73.98	48.01	33	4933	2775	1739040
Choking	73.49	48.01	25	4941	1011	1740804
Opisthotonus	73.48	48.01	17	4949	157	1741658
Intestinal obstruction	73.00	48.01	35	4931	3472	1738343
Hyperreflexia	72.97	48.01	22	4944	599	1741216
Product packaging issue	71.38	48.01	17	4949	180	1741635
White blood cell count increased	70.93	48.01	44	4922	7268	1734547
Psychomotor retardation	70.77	48.01	20	4946	431	1741384
Autonomic nervous system imbalance	67.29	48.01	19	4947	408	1741407
Increased appetite	67.19	48.01	23	4943	948	1740867
Drug withdrawal syndrome neonatal	66.57	48.01	21	4945	667	1741148
Spasmodic dysphonia	66.55	48.01	12	4954	24	1741791
Trismus	66.39	48.01	20	4946	543	1741272
Paranoia	65.13	48.01	28	4938	2153	1739662
Serotonin syndrome	64.71	48.01	30	4936	2758	1739057
Inappropriate antidiuretic hormone secretion	64.17	48.01	26	4940	1722	1740093
Respiratory arrest	63.99	48.01	38	4928	5801	1736014
Acute kidney injury	63.73	48.01	81	4885	34863	1706952
Agranulocytosis	63.42	48.01	32	4934	3544	1738271
Product use in unapproved indication	63.07	48.01	45	4921	9377	1732438
Respiratory distress	62.96	48.01	36	4930	5121	1736694
Sinus tachycardia	61.12	48.01	28	4938	2504	1739311
Sudden death	60.14	48.01	29	4937	2911	1738904
Hypertension	59.36	48.01	59	4907	19389	1722426
Waxy flexibility	55.59	48.01	11	4955	43	1741772
Arrhythmia	55.31	48.01	35	4931	5981	1735834
Hypokinesia	55.01	48.01	21	4945	1186	1740629
Psychotic symptom	54.35	48.01	14	4952	209	1741606
Oral discharge	53.63	48.01	10	4956	26	1741789
Foetal exposure during pregnancy	53.53	48.01	35	4931	6324	1735491
Hypoglycaemia	53.49	48.01	39	4927	8399	1733416
Aspartate aminotransferase increased	53.45	48.01	43	4923	10713	1731102
Suicidal ideation	53.16	48.01	39	4927	8479	1733336
Urinary incontinence	52.99	48.01	26	4940	2710	1739105
Disinhibition	52.82	48.01	15	4951	329	1741486
Nervous system disorder	52.61	48.01	25	4941	2429	1739386
Product dispensing error	51.76	48.01	22	4944	1644	1740171
Generalised tonic-clonic seizure	51.41	48.01	29	4937	4017	1737798
Mental impairment	51.36	48.01	23	4943	1950	1739865
Foetal alcohol syndrome	51.35	48.01	9	4957	14	1741801
Leukopenia	51.07	48.01	38	4928	8442	1733373
Therapeutic product effect variable	51.00	48.01	12	4954	120	1741695
Vomiting	50.55	48.01	76	4890	38239	1703576
Ataxia	50.53	48.01	24	4942	2329	1739486
Constipation	50.42	48.01	48	4918	14952	1726863
Irritability	50.39	48.01	32	4934	5500	1736315
Heart rate increased	50.37	48.01	34	4932	6476	1735339
Posturing	50.21	48.01	12	4954	129	1741686
Persecutory delusion	49.11	48.01	15	4951	427	1741388
Tic	48.83	48.01	17	4949	737	1741078
Drug withdrawal syndrome	48.40	48.01	29	4937	4496	1737319
Ileus paralytic	48.33	48.01	18	4948	949	1740866
Hallucination, visual	48.32	48.01	24	4942	2568	1739247
Muscle contracture	48.15	48.01	13	4953	235	1741580
Withdrawal syndrome	48.10	48.01	23	4943	2265	1739550

Pharmacologic Action:

Source	Code	Description
ATC	N05AD01	NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Butyrophenone derivatives
FDA EPC	N0000180182	Typical Antipsychotic
MeSH PA	D018726	Anti-Dyskinesia Agents
MeSH PA	D000932	Antiemetics
MeSH PA	D014150	Antipsychotic Agents
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D002492	Central Nervous System Depressants
MeSH PA	D015259	Dopamine Agents
MeSH PA	D018492	Dopamine Antagonists
MeSH PA	D005765	Gastrointestinal Agents
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018373	Peripheral Nervous System Agents
MeSH PA	D011619	Psychotropic Drugs
CHEBI has role	CHEBI:48561	dopaminergic antagonist
CHEBI has role	CHEBI:66956	antidyskinesia agent
CHEBI has role	CHEBI:50919	antiemetic
CHEBI has role	CHEBI:65190	first generation antipsychotic
CHEBI has role	CHEBI:48279	serotonergic antagonist
MeSH PA	D014149	Tranquilizing Agents

Drug Use (View source of the data)

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
Chemotherapy-induced nausea and vomiting	off-label use	236084000
Neuroleptic malignant syndrome	contraindication	15244003	DOID:14464
Senile dementia	contraindication	15662003
Agranulocytosis	contraindication	17182001	DOID:12987
Thyrotoxic crisis	contraindication	29028009	DOID:12837
Torsades de pointes	contraindication	31722008
Parkinsonism	contraindication	32798002
Hypothyroidism	contraindication	40930008	DOID:1459
Hypokalemia	contraindication	43339004
Low blood pressure	contraindication	45007003
Extrapyramidal disease	contraindication	76349003
Leukopenia	contraindication	84828003	DOID:615
Tardive dyskinesia	contraindication	102449007
Prolonged QT interval	contraindication	111975006
Seizure disorder	contraindication	128613002
Hypomagnesemia	contraindication	190855004
Angina pectoris	contraindication	194828000
Disease of liver	contraindication	235856003	DOID:409
Retention of urine	contraindication	267064002
Neutropenic disorder	contraindication	303011007	DOID:1227
Coma	contraindication	371632003
Breastfeeding (mother)	contraindication	413712001
Central nervous system depression	contraindication	418072004
Acquired torsion dystonia	contraindication	433493000
Congenital long QT syndrome	contraindication	442917000
Carcinoma of female breast	contraindication	447782002
Smokes tobacco daily	contraindication	449868002
Drug Induced CNS Depression	contraindication

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:

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
Alpha-1B adrenergic receptor	GPCR	P35368	ADA1B_HUMAN		Ki	8.10	PDSP
5-hydroxytryptamine receptor 1B	GPCR	P28222	5HT1B_HUMAN		Ki	6.57	PDSP
Histamine H2 receptor	GPCR	P25021	HRH2_HUMAN		Ki	6.00	PDSP
Muscarinic acetylcholine receptor M3	GPCR	P20309	ACM3_HUMAN		Ki	5	PDSP
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN		Ki	6.26	PDSP
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	6.32	PDSP
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	5.95	PDSP
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN		Ki	6.18	PDSP
5-hydroxytryptamine receptor 1D	GPCR	P28221	5HT1D_HUMAN	ANTAGONIST	Ki	6.60	IUPHAR
Potassium voltage-gated channel subfamily H member 1	Ion channel	O95259	KCNH1_HUMAN	BLOCKER	IC50	6.20	IUPHAR
Mu-type opioid receptor	GPCR	P35372	OPRM_HUMAN		Ki	6.00	DRUG MATRIX
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	5.74	DRUG MATRIX
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN		Ki	7.55	DRUG MATRIX
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN	INVERSE AGONIST	Ki	8.52	WOMBAT-PK
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	ANTAGONIST	Ki	7	WOMBAT-PK
Sigma non-opioid intracellular receptor 1	Membrane receptor	Q99720	SGMR1_HUMAN		EC50	8.92	WOMBAT-PK
Calmodulin	Cytosolic other	P0DP23 P0DP24 P0DP25	CALM1_HUMAN CALM2_HUMAN CALM3_HUMAN		IC50	6.30	WOMBAT-PK
D(1B) dopamine receptor	GPCR	P21918	DRD5_HUMAN		Ki	7.52	WOMBAT-PK
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		Ki	7.90	WOMBAT-PK
5-hydroxytryptamine receptor 7	GPCR	P34969	5HT7R_HUMAN		Ki	6.45	WOMBAT-PK
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	6.10	WOMBAT-PK
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN		Ki	6.70	WOMBAT-PK
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase	Enzyme	Q15125	EBP_HUMAN		Ki	6.72	WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	7.50	WOMBAT-PK
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	7.82	WOMBAT-PK
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	5.55	CHEMBL
Sodium channel alpha subunits; brain (Types I, II, III)	Ion channel	P35498 Q99250 Q9NY46	SCN1A_HUMAN SCN2A_HUMAN SCN3A_HUMAN		IC50	5.92	CHEMBL
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		Ki	5.80	CHEMBL
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN		Ki	5.22	CHEMBL
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	5.33	CHEMBL
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN		Ki	6.36	CHEMBL
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	5.74	CHEMBL
5-hydroxytryptamine receptor 1E	GPCR	P28566	5HT1E_HUMAN		Ki	5.30	PDSP
5-hydroxytryptamine receptor 1F	GPCR	P30939	5HT1F_HUMAN		Ki	5.30	PDSP
Beta-2 adrenergic receptor	GPCR	P07550	ADRB2_HUMAN		Ki	5.30	PDSP
D(4) dopamine receptor	GPCR	P21917	DRD4_HUMAN	INVERSE AGONIST	Kd	9.42	SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 5A	GPCR	P47898	5HT5A_HUMAN		Ki	5.65	PDSP
Alpha-1B adrenergic receptor	GPCR		ADA1B_RAT		Ki	8.31	DRUG MATRIX
Membrane-associated progesterone receptor component 1	Membrane receptor		PGRC1_RAT		Ki	7.44	DRUG MATRIX
Transporter	Transporter		Q63380_RAT		Ki	5.26	CHEMBL
Dopamine receptor	GPCR		DRD1_BOVIN DRD2_BOVIN		IC50	8.74	CHEMBL
5-hydroxytryptamine receptor 7	GPCR		5HT7R_RAT		Ki	6.58	CHEMBL
Muscarinic acetylcholine receptor	GPCR		ACM1_RAT ACM2_RAT ACM3_RAT ACM4_RAT ACM5_RAT		Ki	5.13	CHEMBL
D(2) dopamine receptor	GPCR		DRD2_BOVIN		Ki	9.52	CHEMBL
D(3) dopamine receptor	GPCR		DRD3_RAT		Ki	8.52	CHEMBL
Serotonin 2 (5-HT2) receptor	GPCR		5HT2A_RAT 5HT2B_RAT 5HT2C_RAT		Ki	8.38	CHEMBL
Dopamine receptor	GPCR		DRD1_RAT DRD2_RAT DRD3_RAT DRD4_RAT DRD5_RAT		Ki	8.70	CHEMBL
Adrenergic receptor alpha-2	GPCR		ADA2A_RAT ADA2B_RAT ADA2C_RAT		Ki	5.57	CHEMBL
Alpha-1A adrenergic receptor	GPCR		ADA1A_BOVIN		IC50	7.70	CHEMBL
AP-2 complex subunit sigma	Unclassified		AP2S1_RAT		Ki	7.62	CHEMBL
Muscarinic acetylcholine receptor M1	GPCR		ACM1_RAT		Ki	5.74	CHEMBL
Adenylate cyclase	Enzyme		ADCY2_RAT ADCY3_RAT ADCY4_RAT ADCY5_RAT ADCY6_RAT ADCY8_RAT D4A3N4_RAT Q8CFM9_RAT		IC50	5.64	CHEMBL
Muscarinic acetylcholine receptor M2	GPCR		ACM2_RAT		Ki	6.62	CHEMBL
D(3) dopamine receptor	GPCR		DRD3_CHLAE		Ki	8.52	CHEMBL
Alpha-1A adrenergic receptor	GPCR		ADA1A_RAT		Kd	7.76	CHEMBL
Serotonin 1 (5-HT1) receptor	GPCR		5HT1A_RAT 5HT1B_RAT 5HT1D_RAT 5HT1F_RAT		IC50	4.70	CHEMBL
5-hydroxytryptamine receptor 1A	GPCR		5HT1A_RAT		Ki	6.40	CHEMBL
D(1A) dopamine receptor	GPCR		DRD1_RAT		Ki	7.70	CHEMBL
Pol polyprotein	Enzyme		Q72874_9HIV1		Ki	7	CHEMBL
Histamine H1 receptor	GPCR		HRH1_RAT		Ki	6.42	CHEMBL
5-hydroxytryptamine receptor 2A	GPCR		5HT2A_PIG		Ki	7.52	CHEMBL
Opioid receptor	GPCR		OPRD_RAT OPRK_RAT OPRM_RAT SGMR1_RAT		Ki	5.92	CHEMBL
Sigma non-opioid intracellular receptor 1	Membrane receptor		SGMR1_RAT		Ki	9.05	CHEMBL
D(2) dopamine receptor	GPCR		DRD2_CHLAE		Ki	8.32	CHEMBL
Serotonin 2 (5-HT2) receptor	GPCR		5HT2A_MOUSE 5HT2B_MOUSE 5HT2C_MOUSE		Ki	7.58	CHEMBL
5-hydroxytryptamine receptor 2A	GPCR		5HT2A_BOVIN		IC50	7.52	CHEMBL
D(2) dopamine receptor	GPCR		DRD2_RAT		Ki	9.70	CHEMBL
Protease	Enzyme		Q4U254_9ENTO		Ki	7	CHEMBL
D(1A) dopamine receptor	GPCR		DRD1_PIG		Ki	7.03	CHEMBL
Sigma non-opioid intracellular receptor 1	Membrane other		SGMR1_CAVPO		Ki	9.08	CHEMBL
C-8 sterol isomerase	Enzyme		ERG2_YEAST		Ki	9.30	CHEMBL
5-hydroxytryptamine receptor 2A	GPCR		5HT2A_RAT		Ki	7.35	CHEMBL
Histamine H1 receptor	GPCR		HRH1_CAVPO		Ki	6.40	CHEMBL
5-hydroxytryptamine receptor 7	GPCR		5HT7R_MOUSE	ANTAGONIST	Ki	6.30	IUPHAR
G protein-activated inward rectifier potassium channel 2	Ion channel		KCNJ6_MOUSE	GATING INHIBITOR	EC50	4.10	IUPHAR

External reference:

ID	Source
D006220	MESH_DESCRIPTOR_UI
4018123	VUID
N0000146461	NUI
C0018546	UMLSCUI
D00136	KEGG_DRUG
6387S86PK3	UNII
53515-91-6	SECONDARY_CAS_RN
10756001	SNOMEDCT_US
583	MMSL
5093	RXNORM
386837002	SNOMEDCT_US
4816	MMSL
d00027	MMSL
4018123	VANDF
001518	NDDF
CHEMBL54	ChEMBL_ID
DB00502	DRUGBANK_ID
918	INN_ID
CHEBI:5613	CHEBI
CHEMBL2096643	ChEMBL_ID
CHEMBL4297147	ChEMBL_ID
3559	PUBCHEM_CID
86	IUPHAR_LIGAND_ID

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0093-9604	SOLUTION, CONCENTRATE	2 mg	ORAL	ANDA	12 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0121-0581	SOLUTION	2 mg	ORAL	ANDA	13 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9319	INJECTION	5 mg	INTRAMUSCULAR	ANDA	12 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9501	INJECTION	5 mg	INTRAMUSCULAR	ANDA	12 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9502	INJECTION	5 mg	INTRAMUSCULAR	ANDA	12 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0214	TABLET	2 mg	ORAL	ANDA	12 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0257	TABLET	1 mg	ORAL	ANDA	12 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0327	TABLET	5 mg	ORAL	ANDA	12 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0334	TABLET	10 mg	ORAL	ANDA	12 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0335	TABLET	20 mg	ORAL	ANDA	12 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0351	TABLET	0.50 mg	ORAL	ANDA	12 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0615-2594	TABLET	0.50 mg	ORAL	ANDA	12 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0615-2595	TABLET	1 mg	ORAL	ANDA	12 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0615-2596	TABLET	2 mg	ORAL	ANDA	12 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0615-2597	TABLET	5 mg	ORAL	ANDA	12 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0615-2598	TABLET	10 mg	ORAL	ANDA	13 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0781-1391	TABLET	0.50 mg	ORAL	ANDA	13 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0781-1392	TABLET	1 mg	ORAL	ANDA	13 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0781-1393	TABLET	2 mg	ORAL	ANDA	13 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0781-1396	TABLET	5 mg	ORAL	ANDA	13 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0781-1397	TABLET	10 mg	ORAL	ANDA	13 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0781-1398	TABLET	20 mg	ORAL	ANDA	13 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0832-1510	TABLET	0.50 mg	ORAL	ANDA	13 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0832-1520	TABLET	1 mg	ORAL	ANDA	13 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0832-1530	TABLET	2 mg	ORAL	ANDA	13 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0832-1540	TABLET	5 mg	ORAL	ANDA	13 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0832-1550	TABLET	10 mg	ORAL	ANDA	13 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0832-1560	TABLET	20 mg	ORAL	ANDA	13 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0904-5923	TABLET	1 mg	ORAL	ANDA	13 sections
Haloperidol	HUMAN PRESCRIPTION DRUG LABEL	1	0904-5924	TABLET	2 mg	ORAL	ANDA	13 sections