amisulpride 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
sulpiride derivatives and analogues 179 71675-85-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • barhemsys
  • amisulpride
  • aminosultopride
  • deniban
  • solian
A benzamide derivative that is used as an antipsychotic agent for the treatment of schizophrenia. It is also used as an antidepressive agent.
  • Molecular weight: 369.48
  • Formula: C17H27N3O4S
  • CLOGP: 1.97
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 2
  • TPSA: 101.73
  • ALOGS: -3.10
  • ROTB: 7
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.40 g O
7.50 mg P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 4 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 50 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 46.40 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 48 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
fu (Fraction unbound in plasma) 0.52 % Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,ITK,PDK1,PDK2,PRKDC 13
kinase-selectivity-class AXL,GRK2,PDK1,SIK2,TEK 5
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 3.258 Moderate 0.69
pfas-class PFAS structural alert (1 = True, 0 = False) 0
rat-kpuu-brain Rat brain Kpuu 0.013 % Moderate 0.69

Approvals:

DateAgencyCompanyOrphan
Feb. 26, 2020 FDA ACACIA PHARMA LTD
Jan. 1, 1986 YEAR INTRODUCED

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 487.43 27.81 145 10344 16158 90601800
Hyperprolactinaemia 318.34 27.81 82 10407 5351 90612607
Schizophrenia 244.39 27.81 84 10405 14830 90603128
Akathisia 223.07 27.81 73 10416 11086 90606872
Mental impairment 186.94 27.81 71 10418 16649 90601309
Drug abuse 169.07 27.81 110 10379 82237 90535721
Blood prolactin increased 165.75 27.81 45 10444 3592 90614366
Myocarditis 162.94 27.81 61 10428 13745 90604213
Sopor 153.90 27.81 69 10420 24575 90593383
Electrocardiogram QT prolonged 151.70 27.81 98 10391 72358 90545600
Parkinsonism 140.37 27.81 55 10434 14010 90603948
Drug interaction 130.31 27.81 160 10329 276293 90341665
Refusal of examination 126.41 27.81 22 10467 202 90617756
Antipsychotic drug level increased 123.28 27.81 36 10453 3743 90614215
Eosinophil count decreased 119.97 27.81 34 10455 3178 90614780
Neuroleptic malignant syndrome 109.58 27.81 47 10442 15049 90602909
Galactorrhoea 107.40 27.81 34 10455 4638 90613320
Delusion 106.79 27.81 45 10444 13795 90604163
Psychotic disorder 106.74 27.81 58 10431 31172 90586786
Salivary hypersecretion 95.83 27.81 37 10452 9055 90608903
Neutropenia 94.49 27.81 123 10366 224781 90393177
Hallucination, auditory 94.23 27.81 43 10446 15932 90602026
Differential white blood cell count abnormal 88.82 27.81 21 10468 957 90617001
Sedation 88.28 27.81 60 10429 48111 90569847
Dystonia 85.97 27.81 41 10448 16778 90601180
Somnolence 85.72 27.81 113 10376 208971 90408987
Antipsychotic drug level decreased 82.92 27.81 17 10472 396 90617562
Metabolic syndrome 79.77 27.81 22 10467 1860 90616098
Suicidal ideation 79.67 27.81 67 10422 73788 90544170
Hallucination 77.75 27.81 63 10426 65896 90552062
Aggression 76.08 27.81 44 10445 26624 90591334
Mental disorder 73.26 27.81 46 10443 32272 90585686
Leukopenia 70.93 27.81 72 10417 100638 90517320
Treatment noncompliance 70.87 27.81 54 10435 51673 90566285
Pain 70.20 27.81 15 10474 996326 89621632
Agitation 66.51 27.81 58 10431 67040 90550918
Tardive dyskinesia 66.29 27.81 30 10459 10900 90607058
Endocarditis enterococcal 59.94 27.81 12 10477 247 90617711
Neutrophil count increased 58 27.81 33 10456 19357 90598601
Antipsychotic drug level above therapeutic 57.84 27.81 16 10473 1368 90616590
Mitral valve replacement 57.07 27.81 13 10476 502 90617456
Intentional self-injury 54.83 27.81 37 10452 29297 90588661
Mydriasis 54.41 27.81 29 10460 14983 90602975
Psychotic symptom 54.27 27.81 17 10472 2239 90615719
Arthralgia 54.20 27.81 12 10477 778510 89839448
CSF measles antibody positive 53.88 27.81 9 10480 63 90617895
Suicide attempt 53.25 27.81 54 10435 75345 90542613
Rubella antibody positive 53.04 27.81 9 10480 70 90617888
Respiratory syncytial virus test positive 52.48 27.81 14 10475 1044 90616914
Tobacco interaction 52.07 27.81 9 10480 79 90617879
Troponin increased 51.95 27.81 27 10462 13254 90604704
Inappropriate antidiuretic hormone secretion 49.90 27.81 30 10459 19475 90598483
Coma 49.44 27.81 51 10438 72581 90545377
Blood bilirubin decreased 48.96 27.81 13 10476 952 90617006
Catatonia 47.74 27.81 20 10469 6036 90611922
Loss of consciousness 47.22 27.81 69 10420 140169 90477789
Blood brain barrier defect 47.16 27.81 9 10480 143 90617815
Tremor 46.78 27.81 72 10417 153101 90464857
Pruritus 45.19 27.81 5 10484 541520 90076438
Aortic valve replacement 44.44 27.81 12 10477 937 90617021
Cogwheel rigidity 42.99 27.81 14 10475 2088 90615870
Organic brain syndrome 42.69 27.81 9 10480 241 90617717
Confusional state 42.49 27.81 119 10370 386086 90231872
Troponin T increased 42.28 27.81 13 10476 1610 90616348
Hypotension 41.58 27.81 106 10383 325291 90292667
Overdose 41.13 27.81 69 10420 157640 90460318
Thyroxine free decreased 41.02 27.81 11 10478 837 90617121
Grandiosity 40.79 27.81 9 10480 300 90617658
Transferrin saturation decreased 40.23 27.81 11 10478 900 90617058
White blood cell count increased 40.07 27.81 44 10445 67197 90550761
Euphoric mood 39.77 27.81 17 10472 5392 90612566
Aspartate aminotransferase decreased 39.30 27.81 11 10478 982 90616976
Thunderclap headache 39.23 27.81 9 10480 359 90617599
Cognitive disorder 38.92 27.81 44 10445 69363 90548595
Joint swelling 38.74 27.81 6 10483 503294 90114664
Hypersensitivity 38.43 27.81 4 10485 454673 90163285
Pain in extremity 37.98 27.81 4 10485 450525 90167433
Rash 37.45 27.81 23 10466 796077 89821881
Sinus tachycardia 37.36 27.81 29 10460 28484 90589474
Drug ineffective 37.23 27.81 280 10209 1384018 89233940
CSF protein increased 37.09 27.81 10 10479 776 90617182
Toxicity to various agents 37.00 27.81 94 10395 287752 90330206
Wrong patient received product 36.10 27.81 14 10475 3463 90614495
Mean cell haemoglobin decreased 35.70 27.81 16 10473 5679 90612279
Amenorrhoea 35.19 27.81 20 10469 11702 90606256
Cerebral artery stenosis 34.99 27.81 9 10480 582 90617376
Binge eating 34.78 27.81 9 10480 596 90617362
Bladder trabeculation 34.58 27.81 6 10483 54 90617904
Ventricular dyskinesia 34.57 27.81 7 10482 153 90617805
Muscle rigidity 34.02 27.81 21 10468 14288 90603670
Negative thoughts 33.80 27.81 10 10479 1087 90616871
Accommodation disorder 32.99 27.81 8 10481 406 90617552
Red cell distribution width increased 31.81 27.81 19 10470 12188 90605770
Neutrophil count decreased 31.33 27.81 40 10449 71492 90546466
Systemic lupus erythematosus 31.05 27.81 3 10486 361893 90256065
Vertigo 30.52 27.81 39 10450 69772 90548186
Pleocytosis 30.23 27.81 9 10480 999 90616959
Respiratory depression 29.95 27.81 20 10469 15555 90602403
Intentional overdose 29.89 27.81 45 10444 93789 90524169
Morose 29.81 27.81 5 10484 36 90617922
Mean cell haemoglobin concentration decreased 29.56 27.81 13 10476 4415 90613543
Drug level increased 29.53 27.81 25 10464 27737 90590221
Waxy flexibility 29.46 27.81 6 10483 135 90617823
Mean cell volume decreased 29.34 27.81 13 10476 4493 90613465
Eating disorder 29.28 27.81 25 10464 28048 90589910
Mania 29.26 27.81 19 10470 14105 90603853
Serum ferritin decreased 28.84 27.81 11 10478 2603 90615355
Sitting disability 28.80 27.81 7 10482 359 90617599
Miosis 27.98 27.81 16 10473 9468 90608490

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
Antipsychotic drug level below therapeutic 552.01 26.26 144 15297 3060 42602834
Akathisia 451.11 26.26 162 15279 10289 42595605
Disinhibition 428.43 26.26 123 15318 3772 42602122
Therapeutic product effect variable 409.28 26.26 113 15328 2996 42602898
Obsessive-compulsive disorder 393.62 26.26 131 15310 6612 42599282
Euphoric mood 371.23 26.26 124 15317 6329 42599565
Increased appetite 343.17 26.26 127 15314 8779 42597115
Extrapyramidal disorder 296.17 26.26 136 15305 16276 42589618
Schizophrenia 290.97 26.26 118 15323 10432 42595462
Suicide attempt 287.23 26.26 189 15252 45911 42559983
Neuroleptic malignant syndrome 261.44 26.26 136 15305 21336 42584558
Antipsychotic drug level increased 242.10 26.26 83 15358 4583 42601311
Weight increased 214.18 26.26 228 15213 107755 42498139
Salivary hypersecretion 195.22 26.26 90 15351 10853 42595041
Leukopenia 194.53 26.26 183 15258 74563 42531331
White blood cell count increased 192.87 26.26 147 15294 44940 42560954
Neutrophil count increased 189.64 26.26 107 15334 19697 42586197
Electrocardiogram QT prolonged 182.72 26.26 146 15295 47799 42558095
Hyperprolactinaemia 180.71 26.26 55 15386 2068 42603826
Leukaemia 178.00 26.26 70 15371 5702 42600192
Hallucination, auditory 177.59 26.26 93 15348 14771 42591123
Mental impairment 176.10 26.26 87 15354 12230 42593664
Delusion 175.50 26.26 92 15349 14642 42591252
Schizoaffective disorder 150.59 26.26 47 15394 1923 42603971
Therapeutic product effect incomplete 147.97 26.26 154 15287 70785 42535109
Blood prolactin increased 147.52 26.26 48 15393 2250 42603644
Obesity 147.02 26.26 85 15356 16374 42589520
Myocarditis 138.52 26.26 86 15355 18852 42587042
Psychotic disorder 135.45 26.26 100 15341 29108 42576786
Dyslipidaemia 133.06 26.26 66 15375 9352 42596542
Treatment noncompliance 123.16 26.26 105 15336 37567 42568327
Prescribed overdose 110.78 26.26 65 15376 12862 42593032
Sedation 99.71 26.26 85 15356 30390 42575504
Antipsychotic drug level above therapeutic 99.68 26.26 31 15410 1253 42604641
Antipsychotic drug level decreased 93.44 26.26 29 15412 1164 42604730
Toxicity to various agents 89.14 26.26 231 15210 228905 42376989
Eosinophil count decreased 88.36 26.26 37 15404 3539 42602355
Dystonia 88.27 26.26 56 15385 12734 42593160
Aggression 86.88 26.26 93 15348 44070 42561824
Blood creatine phosphokinase increased 78.31 26.26 92 15349 48246 42557648
Diarrhoea 77.84 26.26 35 15406 460814 42145080
Neutropenia 75.40 26.26 199 15242 199232 42406662
Persecutory delusion 75.28 26.26 33 15408 3531 42602363
Nausea 73.75 26.26 26 15415 396773 42209121
Drug interaction 73.67 26.26 238 15203 266761 42339133
Agitation 70.63 26.26 101 15340 64213 42541681
Drug ineffective 70.59 26.26 428 15013 629769 41976125
Tachycardia 70.33 26.26 129 15312 100958 42504936
Psychotic symptom 70.22 26.26 28 15413 2362 42603532
Suicidal ideation 68.78 26.26 86 15355 48075 42557819
Neutrophil count decreased 68.78 26.26 99 15342 63316 42542578
White blood cell count decreased 67.09 26.26 133 15308 110263 42495631
Irritability 63.88 26.26 64 15377 28064 42577830
Paranoia 62.69 26.26 47 15394 13979 42591915
Thinking abnormal 61.32 26.26 36 15405 7125 42598769
Overdose 60.59 26.26 124 15317 105140 42500754
Arthralgia 58.83 26.26 4 15437 205234 42400660
Neglect of personal appearance 55.91 26.26 15 15426 355 42605539
Pleurothotonus 53.05 26.26 19 15422 1192 42604702
Drug abuse 51.74 26.26 116 15325 104655 42501239
Spasmodic dysphonia 50.83 26.26 15 15426 506 42605388
Intentional self-injury 48.88 26.26 42 15399 15160 42590734
Tardive dyskinesia 46.98 26.26 30 15411 6894 42599000
Dyspnoea 46.86 26.26 55 15386 442566 42163328
Pneumonia 44.10 26.26 53 15388 422096 42183798
Pain 43.79 26.26 17 15424 244831 42361063
Pruritus 43.34 26.26 8 15433 188763 42417131
Breast engorgement 42.68 26.26 7 15434 9 42605885
Rash 42.19 26.26 24 15417 276930 42328964
Parkinsonism 41.79 26.26 33 15408 10590 42595304
Disease progression 40.56 26.26 3 15438 143653 42462241
Social anxiety disorder 40.28 26.26 13 15428 593 42605301
Psychomotor retardation 40.01 26.26 23 15418 4376 42601518
Restlessness 39.79 26.26 51 15390 29198 42576696
Drug level increased 39.34 26.26 48 15393 26152 42579742
Galactorrhoea 38.39 26.26 12 15429 493 42605401
Hallucination, visual 37.37 26.26 42 15399 20978 42584916
Hallucination, tactile 36.59 26.26 12 15429 576 42605318
Differential white blood cell count abnormal 36.35 26.26 16 15425 1728 42604166
Red blood cell sedimentation rate decreased 36.19 26.26 10 15431 265 42605629
Muscle rigidity 36.11 26.26 32 15409 12027 42593867
Lymphocyte count decreased 35.50 26.26 47 15394 27762 42578132
Sopor 33.63 26.26 32 15409 13170 42592724
Left ventricular dysfunction 33.41 26.26 30 15411 11471 42594423
Pain in extremity 33.26 26.26 7 15434 150597 42455297
Type 2 diabetes mellitus 32.99 26.26 37 15404 18434 42587460
Somnolence 32.82 26.26 119 15322 140986 42464908
Slow speech 32.77 26.26 15 15426 1775 42604119
Hyperlactacidaemia 31.72 26.26 20 15421 4496 42601398
Fatigue 31.17 26.26 70 15371 435571 42170323
Catatonia 30.34 26.26 22 15419 6217 42599677
Faecaloma 30.24 26.26 22 15419 6248 42599646
Blepharospasm 29.97 26.26 13 15428 1355 42604539
Delusion of reference 29.75 26.26 7 15434 95 42605799
Diffuse large B-cell lymphoma stage II 29.74 26.26 6 15435 37 42605857
Gallbladder injury 29.71 26.26 8 15433 192 42605702
Hypoventilation 29.65 26.26 18 15423 3784 42602110
Acute kidney injury 28.80 26.26 56 15385 367281 42238613
Oedema peripheral 28.69 26.26 7 15434 136069 42469825
Alcohol abuse 28.61 26.26 18 15423 4031 42601863
Overweight 28.52 26.26 15 15426 2397 42603497
Abnormal behaviour 28.21 26.26 41 15400 26410 42579484
Conduction disorder 27.92 26.26 15 15426 2503 42603391
Lower respiratory tract infection 27.87 26.26 52 15389 41154 42564740
Disturbance in attention 27.19 26.26 43 15398 29823 42576071
Psychomotor hyperactivity 26.85 26.26 26 15415 10932 42594962
Sarcoma metastatic 26.49 26.26 6 15435 68 42605826
Asthenia 26.44 26.26 38 15403 280755 42325139
Erythema 26.30 26.26 4 15437 108789 42497105

FDA Adverse Event Reporting System (Geriatric)

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 711.20 22.32 252 21472 28615 110538960
Schizophrenia 423.96 22.32 160 21564 21666 110545909
Hyperprolactinaemia 416.35 22.32 118 21606 6457 110561118
Akathisia 404.65 22.32 145 21579 16968 110550607
Neuroleptic malignant syndrome 377.57 22.32 167 21557 33892 110533683
Antipsychotic drug level increased 304.51 22.32 94 21630 6921 110560654
Myocarditis 303.23 22.32 138 21586 29917 110537658
Electrocardiogram QT prolonged 284.91 22.32 207 21517 108753 110458822
Mental impairment 276.89 22.32 119 21605 22520 110545055
Antipsychotic drug level below therapeutic 266.26 22.32 63 21661 1672 110565903
Hallucination, auditory 249.97 22.32 116 21608 26281 110541294
Delusion 248.88 22.32 112 21612 23643 110543932
Blood prolactin increased 247.97 22.32 73 21651 4569 110563006
Salivary hypersecretion 247.91 22.32 102 21622 17319 110550256
Neutrophil count increased 222.86 22.32 117 21607 34535 110533040
Drug abuse 211.81 22.32 215 21509 177196 110390379
White blood cell count increased 204.49 22.32 162 21562 96680 110470895
Drug interaction 200.80 22.32 355 21369 499828 110067747
Psychotic disorder 185.92 22.32 119 21605 50818 110516757
Dystonia 179.92 22.32 92 21632 25713 110541862
Leukopenia 176.96 22.32 180 21544 148611 110418964
Eosinophil count decreased 176.88 22.32 60 21664 5958 110561617
Schizoaffective disorder 174.91 22.32 51 21673 3085 110564490
Suicide attempt 172.63 22.32 151 21573 103243 110464332
Euphoric mood 172.39 22.32 65 21659 8762 110558813
Parkinsonism 163.14 22.32 82 21642 22105 110545470
Sopor 162.91 22.32 97 21627 36449 110531126
Disinhibition 161.77 22.32 48 21676 3086 110564489
Neutropenia 160.73 22.32 274 21450 374346 110193229
Antipsychotic drug level decreased 154.20 22.32 39 21685 1373 110566202
Treatment noncompliance 149.55 22.32 120 21604 72870 110494705
Aggression 149.00 22.32 110 21614 59100 110508475
Therapeutic product effect variable 146.29 22.32 43 21681 2675 110564900
Sedation 145.83 22.32 116 21608 69567 110498008
Obsessive-compulsive disorder 140.23 22.32 53 21671 7188 110560387
Galactorrhoea 136.30 22.32 45 21679 4110 110563465
Pain 132.89 22.32 16 21708 954939 109612636
Psychotic symptom 127.33 22.32 42 21682 3825 110563750
Suicidal ideation 127.13 22.32 122 21602 93815 110473760
Antipsychotic drug level above therapeutic 119.99 22.32 36 21688 2404 110565171
Refusal of examination 118.68 22.32 23 21701 225 110567350
Somnolence 117.61 22.32 210 21514 297239 110270336
Agitation 109.99 22.32 123 21601 112928 110454647
Arthralgia 108.54 22.32 13 21711 779619 109787956
Tardive dyskinesia 105.17 22.32 52 21672 13527 110554048
Increased appetite 103.23 22.32 53 21671 14924 110552651
Drug ineffective 98.76 22.32 570 21154 1519970 109047605
Differential white blood cell count abnormal 96.55 22.32 30 21694 2254 110565321
Overdose 94.86 22.32 167 21557 233627 110333948
Persecutory delusion 93.45 22.32 38 21686 6253 110561322
Tachycardia 90.79 22.32 161 21563 226484 110341091
White blood cell count decreased 90.67 22.32 162 21562 229228 110338347
Intentional self-injury 88.48 22.32 67 21657 37362 110530213
Weight increased 87.91 22.32 229 21495 419415 110148160
Nausea 86.39 22.32 70 21654 1235620 109331955
Thinking abnormal 85.75 22.32 47 21677 15093 110552482
Diarrhoea 85.47 22.32 60 21664 1139445 109428130
Dyslipidaemia 83.42 22.32 47 21677 15918 110551657
Blood creatine phosphokinase increased 82.43 22.32 86 21638 72991 110494584
Metabolic syndrome 82.35 22.32 29 21695 3218 110564357
Irritability 78.08 22.32 69 21655 47740 110519835
Pruritus 77.74 22.32 11 21713 581549 109986026
Rash 71.65 22.32 36 21688 820928 109746647
Mental disorder 71.50 22.32 60 21664 38731 110528844
Neutrophil count decreased 70.52 22.32 102 21622 120839 110446736
Hallucination, visual 70.41 22.32 60 21664 39545 110528030
Muscle rigidity 68.09 22.32 48 21676 23983 110543592
Troponin increased 67.53 22.32 52 21672 29714 110537861
Toxicity to various agents 66.98 22.32 227 21497 480328 110087247
Paranoia 66.45 22.32 46 21678 22328 110545247
Joint swelling 65.10 22.32 6 21718 442839 110124736
Drug level increased 64.57 22.32 62 21662 47657 110519918
Pain in extremity 63.27 22.32 10 21714 487108 110080467
Hyperlactacidaemia 59.07 22.32 30 21694 8256 110559319
Dyspnoea 58.89 22.32 79 21645 1106793 109460782
Spasmodic dysphonia 58.45 22.32 15 21709 560 110567015
Neglect of personal appearance 58.16 22.32 14 21710 400 110567175
Back pain 57.38 22.32 4 21720 370992 110196583
Hallucination 56.88 22.32 84 21640 101348 110466227
Swelling 56.65 22.32 3 21721 351038 110216537
Nasopharyngitis 56.24 22.32 6 21718 394355 110173220
Pleurothotonus 54.65 22.32 20 21704 2478 110565097
Respiratory depression 53.88 22.32 47 21677 31954 110535621
Drug hypersensitivity 53.27 22.32 12 21712 454078 110113497
Hypersensitivity 53.12 22.32 8 21716 403990 110163585
Catatonia 52.97 22.32 31 21693 11269 110556306
Rhabdomyolysis 52.69 22.32 89 21635 120312 110447263
Headache 51.05 22.32 59 21665 882318 109685257
Peripheral swelling 50.89 22.32 9 21715 404025 110163550
Endocarditis enterococcal 49.13 22.32 12 21712 365 110567210
CSF measles antibody positive 49.12 22.32 9 21715 63 110567512
Abdominal discomfort 49.12 22.32 9 21715 393849 110173726
Mydriasis 48.72 22.32 38 21686 22119 110545456
Rubella antibody positive 48.63 22.32 9 21715 67 110567508
Tobacco interaction 48.24 22.32 10 21714 141 110567434
Overweight 47.82 22.32 24 21700 6440 110561135
Mitral valve replacement 47.72 22.32 13 21711 613 110566962
Mean cell volume decreased 47.64 22.32 23 21701 5679 110561896
Coma 47.49 22.32 84 21640 117785 110449790
Troponin T increased 47.31 22.32 21 21703 4285 110563290
Leukaemia 47.21 22.32 25 21699 7493 110560082
Wrong patient received product 47.10 22.32 24 21700 6650 110560925
Negative thoughts 46.76 22.32 16 21708 1630 110565945
Waxy flexibility 46.58 22.32 11 21713 289 110567286
Mean cell haemoglobin decreased 45.46 22.32 24 21700 7150 110560425
Sinus tachycardia 44.25 22.32 49 21675 44444 110523131
Psychomotor retardation 43.60 22.32 24 21700 7768 110559807
Pneumonia 43.18 22.32 66 21658 876648 109690927
Psychomotor hyperactivity 42.91 22.32 34 21690 20243 110547332
Paraesthesia 42.69 22.32 3 21721 276518 110291057
Social anxiety disorder 42.14 22.32 13 21711 953 110566622
Alopecia 42.05 22.32 10 21714 364743 110202832
Stomatitis 41.52 22.32 3 21721 270239 110297336
Abnormal behaviour 40.57 22.32 44 21680 38995 110528580
Respiratory syncytial virus test positive 40.41 22.32 14 21710 1480 110566095
Febrile neutropenia 40.00 22.32 7 21717 316760 110250815
Oculogyric crisis 39.90 22.32 18 21706 3814 110563761
Gynaecomastia 39.20 22.32 24 21700 9466 110558109
Blood brain barrier defect 39.18 22.32 9 21715 209 110567366
Alcohol abuse 38.53 22.32 19 21705 4910 110562665
Binge eating 38.49 22.32 11 21713 619 110566956
Leukocytosis 38.29 22.32 50 21674 53778 110513797
Breast engorgement 37.38 22.32 7 21717 56 110567519
Hallucination, tactile 37.37 22.32 12 21712 1003 110566572
Blood bilirubin decreased 37.07 22.32 13 21711 1424 110566151
Cardiomyopathy 36.98 22.32 39 21685 33486 110534089
Fatigue 36.58 22.32 120 21604 1215838 109351737
Depressed mood 36.47 22.32 52 21672 60757 110506818
Wheezing 36.07 22.32 4 21720 255226 110312349
Mania 35.93 22.32 31 21693 20765 110546810
Erythema 35.60 22.32 7 21717 291440 110276135
Slow speech 35.28 22.32 16 21708 3432 110564143
Drug resistance 34.98 22.32 49 21675 56325 110511250
Intentional product use issue 34.75 22.32 4 21720 247902 110319673
Contusion 34.70 22.32 3 21721 233358 110334217
Faecaloma 33.71 22.32 26 21698 14882 110552693
Gastrointestinal disorder 33.67 22.32 4 21720 241948 110325627
Loss of consciousness 32.99 22.32 99 21625 196207 110371368
Left ventricular dysfunction 32.68 22.32 31 21693 23462 110544113
Priapism 32.65 22.32 18 21706 5843 110561732
Delusion of reference 32.64 22.32 8 21716 247 110567328
Intentional overdose 32.60 22.32 77 21647 132424 110435151
Eating disorder 32.45 22.32 35 21689 30823 110536752
Cough 32.30 22.32 26 21698 461615 110105960
Confusional state 32.25 22.32 179 21545 468501 110099074
Aortic valve replacement 31.84 22.32 12 21712 1614 110565961
Apathy 31.75 22.32 26 21698 16213 110551362
Inappropriate antidiuretic hormone secretion 31.47 22.32 36 21688 33815 110533760
Postmortem blood drug level increased 31.36 22.32 11 21713 1206 110566369
Oromandibular dystonia 31.34 22.32 11 21713 1208 110566367
Thyroxine free decreased 31.33 22.32 11 21713 1209 110566366
Electrocardiogram QT shortened 31.29 22.32 8 21716 294 110567281
Prescribed overdose 30.96 22.32 59 21665 87522 110480053
Asthma 30.59 22.32 6 21718 250285 110317290
Thunderclap headache 30.47 22.32 9 21715 569 110567006
Organic brain syndrome 30.33 22.32 9 21715 578 110566997
Transferrin saturation decreased 30.30 22.32 11 21713 1332 110566243
Lymphocyte count decreased 30.08 22.32 46 21678 57197 110510378
Conduction disorder 29.83 22.32 15 21709 4040 110563535
Left ventricular dilatation 29.69 22.32 11 21713 1411 110566164
Aspartate aminotransferase decreased 29.64 22.32 11 21713 1417 110566158
Psychomotor skills impaired 29.54 22.32 18 21706 7040 110560535
Disorientation 29.28 22.32 51 21673 70620 110496955
Obesity 29.12 22.32 67 21657 113284 110454291
Synovitis 28.79 22.32 9 21715 274083 110293492
Discomfort 28.79 22.32 4 21720 214703 110352872
Rebound psychosis 28.72 22.32 8 21716 410 110567165
Bladder trabeculation 28.60 22.32 6 21718 90 110567485
Withdrawal syndrome 28.55 22.32 33 21691 31347 110536228
Sarcoma metastatic 28.53 22.32 6 21718 91 110567484
Infection 28.48 22.32 18 21706 362182 110205393
Asthenia 28.34 22.32 58 21666 688941 109878634
Pyrexia 28.12 22.32 87 21637 898178 109669397
Suspiciousness 27.96 22.32 9 21715 758 110566817
Wound 27.86 22.32 6 21718 234431 110333144
Muscle spasms 27.71 22.32 10 21714 278147 110289428
Disease progression 27.51 22.32 7 21717 244027 110323548
Hypoventilation 27.30 22.32 18 21706 8063 110559512
Diffuse large B-cell lymphoma stage II 27.07 22.32 6 21718 118 110567457
Dyspepsia 26.96 22.32 3 21721 190962 110376613
Red blood cell sedimentation rate decreased 26.68 22.32 10 21714 1324 110566251
Cerebral artery stenosis 26.48 22.32 9 21715 898 110566677
Dry mouth 26.17 22.32 4 21720 199944 110367631
Grandiosity 26.14 22.32 8 21716 571 110567004
Red cell distribution width increased 25.97 22.32 24 21700 17578 110549997
Tremor 25.90 22.32 93 21631 202139 110365436
Social avoidant behaviour 25.88 22.32 15 21709 5354 110562221
Morose 25.79 22.32 5 21719 49 110567526
Maternal exposure during pregnancy 25.66 22.32 9 21715 254874 110312701
CSF protein increased 25.60 22.32 10 21714 1481 110566094
Hypoaesthesia 25.56 22.32 15 21709 314208 110253367
Arteriosclerosis coronary artery 25.56 22.32 28 21696 25090 110542485
Abdominal pain upper 25.25 22.32 19 21705 349092 110218483
Cogwheel rigidity 25.23 22.32 13 21711 3685 110563890
Intracranial pressure increased 25.20 22.32 19 21705 10516 110557059
Accommodation disorder 25.19 22.32 8 21716 645 110566930
Amenorrhoea 25.13 22.32 18 21706 9213 110558362
Mean cell haemoglobin concentration decreased 25.09 22.32 15 21709 5667 110561908
Cognitive disorder 25.03 22.32 54 21670 87457 110480118
Lung disorder 24.99 22.32 3 21721 180044 110387531
Serum ferritin decreased 24.70 22.32 12 21712 3002 110564573
Drug dependence 24.61 22.32 39 21685 49981 110517594
Injection site pain 24.61 22.32 3 21721 177919 110389656
Stupor 24.56 22.32 17 21707 8248 110559327
Injury 24.49 22.32 3 21721 177262 110390313
Platelet count increased 24.47 22.32 28 21696 26306 110541269
Loss of libido 24.26 22.32 12 21712 3121 110564454
Acute psychosis 24.22 22.32 14 21710 4973 110562602
Antisocial personality disorder 24.22 22.32 5 21719 69 110567506
Right ventricular dilatation 24.18 22.32 11 21713 2376 110565199
Asphyxia 24.17 22.32 21 21703 14194 110553381
Product dose omission issue 23.93 22.32 17 21707 321765 110245810
Dyskinesia 23.79 22.32 39 21685 51407 110516168
Hangover 23.68 22.32 11 21713 2491 110565084
Oedema peripheral 23.62 22.32 18 21706 328642 110238933
Serotonin syndrome 23.61 22.32 42 21682 59111 110508464
Agranulocytosis 23.56 22.32 43 21681 61717 110505858
Ventricular dyskinesia 23.56 22.32 7 21717 452 110567123
Emotional distress 23.50 22.32 36 21688 44811 110522764
Disturbance in attention 23.45 22.32 43 21681 61952 110505623
Gallbladder injury 23.40 22.32 9 21715 1279 110566296
Social problem 23.39 22.32 10 21714 1864 110565711
Pericarditis 23.36 22.32 7 21717 219107 110348468
Neutrophilia 23.33 22.32 18 21706 10311 110557264
Hyperleukocytosis 23.20 22.32 12 21712 3427 110564148
Musculoskeletal pain 23.19 22.32 4 21720 183019 110384556
Pneumonia aspiration 23.09 22.32 50 21674 81183 110486392
Pulmonary valve incompetence 22.94 22.32 11 21713 2675 110564900
Drug screen false positive 22.87 22.32 9 21715 1360 110566215
Pancreas infection 22.84 22.32 7 21717 502 110567073
Restlessness 22.52 22.32 40 21684 56219 110511356
Akinesia 22.48 22.32 12 21712 3655 110563920
Cyclothymic disorder 22.45 22.32 6 21718 263 110567312

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05AL05 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Benzamides
MeSH PA D000928 Antidepressive Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D011619 Psychotropic Drugs
MeSH PA D014150 Antipsychotic Agents
MeSH PA D015259 Dopamine Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018492 Dopamine Antagonists
MeSH PA D018687 Antidepressive Agents, Second-Generation
FDA MoA N0000175799 Dopamine D2 Antagonists
FDA EPC N0000175800 Dopamine-2 Receptor Antagonist
CHEBI has role CHEBI:35469 antidepressant
CHEBI has role CHEBI:35474 anxiolytic drug
CHEBI has role CHEBI:35703 xenobiotic
CHEBI has role CHEBI:50779 appetite enhancer
CHEBI has role CHEBI:50919 antiemetic
CHEBI has role CHEBI:65191 second generation antipsychotic
CHEBI has role CHEBI:78298 environmental contaminant

Related Drugs by ATC class:

N05AL Benzamides 6 drugs
levosulpirideremoxipridesulpiridesultopridetiaprideveralipride

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

DiseaseRelationSNOMED_IDDOID
Postoperative nausea and vomiting indication 1488000
Chronic schizophrenia indication 83746006
Dysthymia off-label use 78667006 DOID:12139




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.78 acidic
pKa2 9.09 Basic
pKa3 0.54 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
10MG/4ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Sept. 1, 2020 RX SOLUTION INTRAVENOUS 12194022 March 10, 2031 PREVENTION AND TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING
10MG/4ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Sept. 1, 2020 RX SOLUTION INTRAVENOUS 12194022 March 10, 2031 PREVENTION OF POST-OPERATIVE NAUSEA AND VOMITING
10MG/4ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Sept. 1, 2020 RX SOLUTION INTRAVENOUS 9545426 March 10, 2031 PREVENTION OF POST-OPERATIVE NAUSEA AND VOMITING
10MG/4ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Sept. 1, 2020 RX SOLUTION INTRAVENOUS 9545426 March 10, 2031 TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING
10MG/4ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Sept. 1, 2020 RX SOLUTION INTRAVENOUS 9889118 March 10, 2031 PREVENTION OF POST-OPERATIVE NAUSEA AND VOMITING
10MG/4ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Sept. 1, 2020 RX SOLUTION INTRAVENOUS 9889118 March 10, 2031 TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING
5MG/2ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Feb. 26, 2020 RX SOLUTION INTRAVENOUS 12194022 March 10, 2031 PREVENTION AND TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING
5MG/2ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Feb. 26, 2020 RX SOLUTION INTRAVENOUS 12194022 March 10, 2031 PREVENTION OF POST-OPERATIVE NAUSEA AND VOMITING
5MG/2ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Feb. 26, 2020 RX SOLUTION INTRAVENOUS 9545426 March 10, 2031 PREVENTION OF POST-OPERATIVE NAUSEA AND VOMITING
5MG/2ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Feb. 26, 2020 RX SOLUTION INTRAVENOUS 9545426 March 10, 2031 TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING
5MG/2ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Feb. 26, 2020 RX SOLUTION INTRAVENOUS 9889118 March 10, 2031 PREVENTION OF POST-OPERATIVE NAUSEA AND VOMITING
5MG/2ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Feb. 26, 2020 RX SOLUTION INTRAVENOUS 9889118 March 10, 2031 TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING
10MG/4ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Sept. 1, 2020 RX SOLUTION INTRAVENOUS 9084765 Feb. 26, 2034 PREVENTION AND TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING
10MG/4ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Sept. 1, 2020 RX SOLUTION INTRAVENOUS 9084765 Feb. 26, 2034 PREVENTION OF POST-OPERATIVE NAUSEA AND VOMITING
10MG/4ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Sept. 1, 2020 RX SOLUTION INTRAVENOUS 9084765 Feb. 26, 2034 TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING
5MG/2ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Feb. 26, 2020 RX SOLUTION INTRAVENOUS 9084765 Feb. 26, 2034 PREVENTION AND TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING
5MG/2ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Feb. 26, 2020 RX SOLUTION INTRAVENOUS 9084765 Feb. 26, 2034 PREVENTION OF POST-OPERATIVE NAUSEA AND VOMITING
5MG/2ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Feb. 26, 2020 RX SOLUTION INTRAVENOUS 9084765 Feb. 26, 2034 TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING
10MG/4ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Sept. 1, 2020 RX SOLUTION INTRAVENOUS 11357753 Feb. 9, 2038 TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING
10MG/4ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Sept. 1, 2020 RX SOLUTION INTRAVENOUS 12005042 Feb. 9, 2038 PREVENTION AND TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING
10MG/4ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Sept. 1, 2020 RX SOLUTION INTRAVENOUS 12005042 Feb. 9, 2038 PREVENTION OF POST-OPERATIVE NAUSEA AND VOMITING
10MG/4ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Sept. 1, 2020 RX SOLUTION INTRAVENOUS 12005042 Feb. 9, 2038 TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING
10MG/4ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Sept. 1, 2020 RX SOLUTION INTRAVENOUS 12329740 Feb. 9, 2038 PREVENTION AND TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING
10MG/4ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Sept. 1, 2020 RX SOLUTION INTRAVENOUS 12329740 Feb. 9, 2038 TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING
5MG/2ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Feb. 26, 2020 RX SOLUTION INTRAVENOUS 11357753 Feb. 9, 2038 TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING
5MG/2ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Feb. 26, 2020 RX SOLUTION INTRAVENOUS 12005042 Feb. 9, 2038 PREVENTION AND TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING
5MG/2ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Feb. 26, 2020 RX SOLUTION INTRAVENOUS 12005042 Feb. 9, 2038 PREVENTION OF POST-OPERATIVE NAUSEA AND VOMITING
5MG/2ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Feb. 26, 2020 RX SOLUTION INTRAVENOUS 12005042 Feb. 9, 2038 TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING
5MG/2ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Feb. 26, 2020 RX SOLUTION INTRAVENOUS 12329740 Feb. 9, 2038 PREVENTION AND TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING
5MG/2ML (2.5MG/ML) BARHEMSYS LXO IRELAND N209510 Feb. 26, 2020 RX SOLUTION INTRAVENOUS 12329740 Feb. 9, 2038 TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
D(2) dopamine receptor GPCR ANTAGONIST Ki 8.55 WOMBAT-PK SCIENTIFIC LITERATURE
D(3) dopamine receptor GPCR ANTAGONIST Ki 8.50 WOMBAT-PK SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 2B GPCR Ki 7.89 PDSP
5-hydroxytryptamine receptor 6 GPCR Ki 5.38 PDSP
5-hydroxytryptamine receptor 7 GPCR Ki 7.94 PDSP
5-hydroxytryptamine receptor 1B GPCR Ki 5.76 PDSP
Alpha-2A adrenergic receptor GPCR Ki 5.95 PDSP
Alpha-2C adrenergic receptor GPCR Ki 5.81 PDSP
D(4) dopamine receptor GPCR Ki 5.63 PDSP
5-hydroxytryptamine receptor 1D GPCR Ki 5.87 PDSP
5-hydroxytryptamine receptor 2A GPCR Ki 5.08 PDSP
D(3) dopamine receptor GPCR ANTAGONIST Ki 7.40 IUPHAR

External reference:

IDSource
D07310 KEGG_DRUG
2284233 RXNORM
C0103045 UMLSCUI
CHEBI:64045 CHEBI
CHEMBL243712 ChEMBL_ID
DB06288 DRUGBANK_ID
D000077582 MESH_DESCRIPTOR_UI
2159 PUBCHEM_CID
963 IUPHAR_LIGAND_ID
4960 INN_ID
8110R61I4U UNII
17788 MMSL
331491 MMSL
d04990 MMSL
4039609 VANDF
005229 NDDF
321636003 SNOMEDCT_US
391761004 SNOMEDCT_US
8110R61I4U INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Barhemsys HUMAN PRESCRIPTION DRUG LABEL 1 71390-125 INJECTION, SOLUTION 2.50 mg INTRAVENOUS NDA 29 sections