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

Stem definitionDrug idCAS RN
antipsychotics, haloperidol derivatives 1353 52-86-8

Description:

MoleculeDescription

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:

DoseUnitRoute
8 mg O
8 mg P
3.30 mg P

ADMET properties:

PropertyValueReference
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 ┬ÁM/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:

DateAgencyCompanyOrphan
April 12, 1967 FDA ORTHO MCNEIL

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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:

SourceCodeDescription
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)

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (acidic/basic)
pKa1 8.36 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
D(2) dopamine receptor GPCR INVERSE AGONIST Ki 9.15 WOMBAT-PK CHEMBL
Alpha-1B adrenergic receptor GPCR Ki 8.10 PDSP
5-hydroxytryptamine receptor 1B GPCR Ki 6.57 PDSP
Histamine H2 receptor GPCR Ki 6.00 PDSP
Muscarinic acetylcholine receptor M3 GPCR Ki 5 PDSP
Alpha-2C adrenergic receptor GPCR Ki 6.26 PDSP
Alpha-2B adrenergic receptor GPCR Ki 6.32 PDSP
Alpha-2A adrenergic receptor GPCR Ki 5.95 PDSP
Muscarinic acetylcholine receptor M5 GPCR Ki 6.18 PDSP
5-hydroxytryptamine receptor 1D GPCR ANTAGONIST Ki 6.60 IUPHAR
Potassium voltage-gated channel subfamily H member 1 Ion channel BLOCKER IC50 6.20 IUPHAR
Mu-type opioid receptor GPCR Ki 6.00 DRUG MATRIX
Sodium-dependent noradrenaline transporter Transporter Ki 5.74 DRUG MATRIX
Alpha-1D adrenergic receptor GPCR Ki 7.55 DRUG MATRIX
D(3) dopamine receptor GPCR INVERSE AGONIST Ki 8.52 WOMBAT-PK
5-hydroxytryptamine receptor 2A GPCR ANTAGONIST Ki 7 WOMBAT-PK
Sigma non-opioid intracellular receptor 1 Membrane receptor EC50 8.92 WOMBAT-PK
Calmodulin Cytosolic other IC50 6.30 WOMBAT-PK
D(1B) dopamine receptor GPCR Ki 7.52 WOMBAT-PK
Alpha-1A adrenergic receptor GPCR Ki 7.90 WOMBAT-PK
5-hydroxytryptamine receptor 7 GPCR Ki 6.45 WOMBAT-PK
5-hydroxytryptamine receptor 2B GPCR Ki 6.10 WOMBAT-PK
Multidrug resistance protein 1 Transporter Ki 6.70 WOMBAT-PK
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase Enzyme Ki 6.72 WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 7.50 WOMBAT-PK
D(1A) dopamine receptor GPCR Ki 7.82 WOMBAT-PK
5-hydroxytryptamine receptor 1A GPCR Ki 5.55 CHEMBL
Sodium channel alpha subunits; brain (Types I, II, III) Ion channel IC50 5.92 CHEMBL
Muscarinic acetylcholine receptor M1 GPCR Ki 5.80 CHEMBL
5-hydroxytryptamine receptor 6 GPCR Ki 5.22 CHEMBL
5-hydroxytryptamine receptor 2C GPCR Ki 5.33 CHEMBL
Histamine H1 receptor GPCR Ki 6.36 CHEMBL
Sodium-dependent serotonin transporter Transporter Ki 5.74 CHEMBL
5-hydroxytryptamine receptor 1E GPCR Ki 5.30 PDSP
5-hydroxytryptamine receptor 1F GPCR Ki 5.30 PDSP
Beta-2 adrenergic receptor GPCR Ki 5.30 PDSP
D(4) dopamine receptor GPCR INVERSE AGONIST Kd 9.42 SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 5A GPCR Ki 5.65 PDSP
Alpha-1B adrenergic receptor GPCR Ki 8.31 DRUG MATRIX
Membrane-associated progesterone receptor component 1 Membrane receptor Ki 7.44 DRUG MATRIX
Transporter Transporter Ki 5.26 CHEMBL
Dopamine receptor GPCR IC50 8.74 CHEMBL
5-hydroxytryptamine receptor 7 GPCR Ki 6.58 CHEMBL
Muscarinic acetylcholine receptor GPCR Ki 5.13 CHEMBL
D(2) dopamine receptor GPCR Ki 9.52 CHEMBL
D(3) dopamine receptor GPCR Ki 8.52 CHEMBL
Serotonin 2 (5-HT2) receptor GPCR Ki 8.38 CHEMBL
Dopamine receptor GPCR Ki 8.70 CHEMBL
Adrenergic receptor alpha-2 GPCR Ki 5.57 CHEMBL
Alpha-1A adrenergic receptor GPCR IC50 7.70 CHEMBL
AP-2 complex subunit sigma Unclassified Ki 7.62 CHEMBL
Muscarinic acetylcholine receptor M1 GPCR Ki 5.74 CHEMBL
Adenylate cyclase Enzyme IC50 5.64 CHEMBL
Muscarinic acetylcholine receptor M2 GPCR Ki 6.62 CHEMBL
D(3) dopamine receptor GPCR Ki 8.52 CHEMBL
Alpha-1A adrenergic receptor GPCR Kd 7.76 CHEMBL
Serotonin 1 (5-HT1) receptor GPCR IC50 4.70 CHEMBL
5-hydroxytryptamine receptor 1A GPCR Ki 6.40 CHEMBL
D(1A) dopamine receptor GPCR Ki 7.70 CHEMBL
Pol polyprotein Enzyme Ki 7 CHEMBL
Histamine H1 receptor GPCR Ki 6.42 CHEMBL
5-hydroxytryptamine receptor 2A GPCR Ki 7.52 CHEMBL
Opioid receptor GPCR Ki 5.92 CHEMBL
Sigma non-opioid intracellular receptor 1 Membrane receptor Ki 9.05 CHEMBL
D(2) dopamine receptor GPCR Ki 8.32 CHEMBL
Serotonin 2 (5-HT2) receptor GPCR Ki 7.58 CHEMBL
5-hydroxytryptamine receptor 2A GPCR IC50 7.52 CHEMBL
D(2) dopamine receptor GPCR Ki 9.70 CHEMBL
Protease Enzyme Ki 7 CHEMBL
D(1A) dopamine receptor GPCR Ki 7.03 CHEMBL
Sigma non-opioid intracellular receptor 1 Membrane other Ki 9.08 CHEMBL
C-8 sterol isomerase Enzyme Ki 9.30 CHEMBL
5-hydroxytryptamine receptor 2A GPCR Ki 7.35 CHEMBL
Histamine H1 receptor GPCR Ki 6.40 CHEMBL
5-hydroxytryptamine receptor 7 GPCR ANTAGONIST Ki 6.30 IUPHAR
G protein-activated inward rectifier potassium channel 2 Ion channel GATING INHIBITOR EC50 4.10 IUPHAR

External reference:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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