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

Stem definitionDrug idCAS RN
sulpiride derivatives 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: ONP
    • 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

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 218.25 26.13 76 6912 11694 50586442
Sopor 153.31 26.13 68 6920 19811 50578325
Schizophrenia 149.64 26.13 51 6937 7346 50590790
Hyperprolactinaemia 134.34 26.13 39 6949 3326 50594810
Blood prolactin increased 119.66 26.13 35 6953 3064 50595072
Drug abuse 114.83 26.13 82 6906 59764 50538372
Electrocardiogram QT prolonged 97 26.13 70 6918 51816 50546320
Neuroleptic malignant syndrome 95.28 26.13 41 6947 11089 50587047
Akathisia 93.10 26.13 37 6951 8192 50589944
Metabolic syndrome 83.23 26.13 22 6966 1325 50596811
Antipsychotic drug level increased 81.17 26.13 26 6962 3083 50595053
Differential white blood cell count abnormal 76.23 26.13 18 6970 681 50597455
Hallucination, auditory 74.09 26.13 34 6954 10694 50587442
Mental impairment 73.38 26.13 35 6953 12009 50586127
Galactorrhoea 72.66 26.13 25 6963 3698 50594438
Psychotic disorder 69.17 26.13 41 6947 21771 50576365
Myocarditis 67.11 26.13 29 6959 7918 50590218
Confusional state 66.20 26.13 103 6885 185825 50412311
Parkinsonism 64.12 26.13 29 6959 8818 50589318
Pain 61.49 26.13 5 6983 578898 50019238
Sedation 58.77 26.13 42 6946 30568 50567568
Aggression 57.48 26.13 36 6952 21080 50577056
Delusion 53.29 26.13 27 6961 10542 50587594
Mydriasis 53.15 26.13 27 6961 10600 50587536
Dystonia 53.03 26.13 28 6960 11898 50586238
Mental disorder 51.24 26.13 34 6954 21957 50576179
Tremor 49.98 26.13 70 6918 114833 50483303
Neutropenia 48.51 26.13 79 6909 147886 50450250
Neutrophil count increased 48.47 26.13 28 6960 14167 50583969
Hallucination 47.08 26.13 44 6944 46613 50551523
Drug interaction 46.75 26.13 92 6896 199529 50398607
CSF measles antibody positive 46.36 26.13 8 6980 57 50598079
Salivary hypersecretion 45.85 26.13 21 6967 6570 50591566
Rubella antibody positive 45.54 26.13 8 6980 64 50598072
Tardive dyskinesia 43.86 26.13 21 6967 7258 50590878
Treatment noncompliance 43.75 26.13 35 6953 30115 50568021
Blood brain barrier defect 43.49 26.13 8 6980 85 50598051
Overdose 42.23 26.13 60 6928 99667 50498469
Suicide attempt 41.42 26.13 43 6945 51689 50546447
Thunderclap headache 38.97 26.13 8 6980 156 50597980
Organic brain syndrome 37.67 26.13 8 6980 185 50597951
White blood cell count increased 37.26 26.13 37 6951 42203 50555933
Binge eating 36.97 26.13 9 6979 388 50597748
Antipsychotic drug level decreased 36.84 26.13 8 6980 206 50597930
Catatonia 36.08 26.13 15 6973 3721 50594415
Intentional self-injury 36.04 26.13 28 6960 23084 50575052
CSF protein increased 35.29 26.13 9 6979 470 50597666
Ventricular dyskinesia 34.68 26.13 7 6981 125 50598011
Arthralgia 34.61 26.13 9 6979 438693 50159443
Grandiosity 34.51 26.13 8 6980 279 50597857
Negative thoughts 34.39 26.13 10 6978 856 50597280
Cognitive disorder 34.11 26.13 36 6952 44087 50554049
Leukopenia 33.68 26.13 44 6944 67484 50530652
Bladder trabeculation 33.52 26.13 6 6982 54 50598082
Blood folate decreased 33.38 26.13 9 6979 584 50597552
Loss of consciousness 33.20 26.13 55 6933 104298 50493838
Accommodation disorder 32.59 26.13 8 6980 357 50597779
Cerebral artery stenosis 31.79 26.13 8 6980 396 50597740
Coma 31.42 26.13 39 6949 56840 50541296
Rash 30.85 26.13 11 6977 437460 50160676
Agitation 30.13 26.13 37 6951 53347 50544789
Type 2 diabetes mellitus 30.10 26.13 30 6958 34345 50563791
Intentional overdose 30.04 26.13 40 6948 62464 50535672
Waxy flexibility 29.27 26.13 6 6982 116 50598020
Pleocytosis 29.20 26.13 8 6980 552 50597584
Antipsychotic drug level above therapeutic 29.11 26.13 9 6979 950 50597186
Morose 28.93 26.13 5 6983 36 50598100
Cor pulmonale acute 28.29 26.13 7 6981 323 50597813
Serotonin syndrome 28.23 26.13 25 6963 24688 50573448
Hypochromic anaemia 27.78 26.13 10 6978 1686 50596450
Vertigo 27.77 26.13 35 6953 51797 50546339
Pain in extremity 27.17 26.13 3 6985 272862 50325274
Amenorrhoea 27.02 26.13 16 6972 8468 50589668
Cardiogenic shock 26.75 26.13 20 6968 15579 50582557

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 332.26 27.60 85 9426 1889 29563127
Akathisia 262.94 27.60 94 9417 6648 29558368
Disinhibition 236.40 27.60 69 9442 2538 29562478
Therapeutic product effect variable 230.63 27.60 63 9448 1814 29563202
Schizophrenia 227.88 27.60 84 9427 6481 29558535
Obsessive-compulsive disorder 225.54 27.60 76 9435 4500 29560516
Euphoric mood 194.63 27.60 69 9442 4756 29560260
Increased appetite 182.84 27.60 70 9441 5994 29559022
Neuroleptic malignant syndrome 172.30 27.60 90 9421 16058 29548958
Neutrophil count increased 171.24 27.60 87 9424 14655 29550361
Electrocardiogram QT prolonged 153.91 27.60 112 9399 36025 29528991
Antipsychotic drug level increased 148.55 27.60 51 9460 3192 29561824
Suicide attempt 132.39 27.60 100 9411 34010 29531006
Extrapyramidal disorder 131.84 27.60 66 9445 10765 29554251
Blood prolactin increased 123.31 27.60 37 9474 1497 29563519
Salivary hypersecretion 120.18 27.60 55 9456 7354 29557662
Mental impairment 118.06 27.60 58 9453 9083 29555933
White blood cell count increased 117.63 27.60 97 9414 37419 29527597
Leukopenia 105.19 27.60 108 9403 55095 29509921
Obesity 99.55 27.60 53 9458 9810 29555206
Antipsychotic drug level decreased 96.73 27.60 27 9484 842 29564174
Psychotic disorder 95.57 27.60 67 9444 20287 29544729
Antipsychotic drug level above therapeutic 94.77 27.60 28 9483 1073 29563943
Weight increased 93.45 27.60 119 9392 76548 29488468
Delusion 93.17 27.60 53 9458 11163 29553853
Hallucination, auditory 89.69 27.60 49 9462 9544 29555472
Blood creatine phosphokinase increased 89.37 27.60 86 9425 40558 29524458
Therapeutic product effect incomplete 82.35 27.60 81 9430 39224 29525792
Dyslipidaemia 73.92 27.60 37 9474 6024 29558992
Prescribed overdose 64.06 27.60 38 9473 8645 29556371
Leukaemia 64.03 27.60 29 9482 3781 29561235
Tachycardia 60.72 27.60 94 9417 72316 29492700
Hyperprolactinaemia 58.25 27.60 20 9491 1250 29563766
Aggression 57.83 27.60 64 9447 35477 29529539
Dystonia 55.06 27.60 36 9475 9713 29555303
Sedation 52.40 27.60 44 9467 17361 29547655
Neutropenia 50.83 27.60 123 9388 131588 29433428
Neutrophil count decreased 47.36 27.60 64 9447 43503 29521513
Nausea 45.76 27.60 18 9493 289237 29275779
Lower respiratory tract infection 45.31 27.60 49 9462 26453 29538563
White blood cell count decreased 44.81 27.60 89 9422 83273 29481743
Drug ineffective 44.04 27.60 231 9280 362939 29202077
Breast engorgement 43.52 27.60 7 9504 9 29565007
Diarrhoea 43.16 27.60 27 9484 332671 29232345
Schizoaffective disorder 41.68 27.60 15 9496 1077 29563939
Thinking abnormal 41.48 27.60 24 9487 5212 29559804
Agitation 38.02 27.60 63 9448 51241 29513775
Psychotic symptom 37.91 27.60 15 9496 1399 29563617
Hypoventilation 36.58 27.60 18 9493 2823 29562193
Suicidal ideation 36.21 27.60 50 9461 34666 29530350
Paranoia 36.15 27.60 28 9483 9849 29555167
Pleurothotonus 34.95 27.60 13 9498 1025 29563991
Blepharospasm 34.74 27.60 13 9498 1042 29563974
Left ventricular dysfunction 34.25 27.60 26 9485 8876 29556140
Parkinsonism 34.23 27.60 24 9487 7254 29557762
Conduction disorder 34.09 27.60 15 9496 1825 29563191
Sopor 33.64 27.60 28 9483 10906 29554110
Disturbance in attention 32.13 27.60 37 9474 21387 29543629
Persecutory delusion 31.92 27.60 15 9496 2126 29562890
Abnormal behaviour 31.47 27.60 38 9473 23089 29541927
Arthralgia 31.32 27.60 4 9507 139613 29425403
Diffuse large B-cell lymphoma stage II 31.04 27.60 6 9505 33 29564983
Treatment noncompliance 30.05 27.60 38 9473 24189 29540827
Subacute endocarditis 29.67 27.60 6 9505 43 29564973
Platelet count increased 28.83 27.60 23 9488 8440 29556576
Toxicity to various agents 28.63 27.60 121 9390 173540 29391476
Drug interaction 28.37 27.60 132 9379 197253 29367763
Sarcoma metastatic 27.98 27.60 6 9505 59 29564957

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 318.84 21.23 129 13585 19423 64465595
Schizophrenia 299.42 21.23 106 13608 11062 64473956
Neuroleptic malignant syndrome 253.60 21.23 118 13596 24878 64460140
Electrocardiogram QT prolonged 206.16 21.23 155 13559 79293 64405725
Neutrophil count increased 181.02 21.23 94 13620 25080 64459938
Blood prolactin increased 177.78 21.23 54 13660 3474 64481544
Akathisia 177.50 21.23 73 13641 11437 64473581
Mental impairment 165.24 21.23 77 13637 16266 64468752
Antipsychotic drug level increased 161.98 21.23 55 13659 5060 64479958
Sopor 161.15 21.23 92 13622 29569 64455449
Hyperprolactinaemia 153.84 21.23 50 13664 4015 64481003
Antipsychotic drug level below therapeutic 139.30 21.23 34 13680 951 64484067
White blood cell count increased 130.85 21.23 110 13604 65904 64419114
Hallucination, auditory 126.78 21.23 65 13649 16874 64468144
Delusion 123.01 21.23 65 13649 17949 64467069
Salivary hypersecretion 119.12 21.23 56 13658 12057 64472961
Antipsychotic drug level decreased 115.45 21.23 29 13685 915 64484103
Psychotic disorder 113.75 21.23 78 13636 34500 64450518
Dystonia 103.74 21.23 59 13655 18806 64466212
Drug abuse 92.87 21.23 127 13587 132247 64352771
Antipsychotic drug level above therapeutic 91.68 21.23 28 13686 1833 64483185
Neutropenia 88.75 21.23 172 13542 239452 64245566
Galactorrhoea 87.93 21.23 31 13683 3188 64481830
Aggression 87.39 21.23 75 13639 46157 64438861
Parkinsonism 87.33 21.23 48 13666 14325 64470693
Pain 85.99 21.23 9 13705 553502 63931516
Metabolic syndrome 85.28 21.23 28 13686 2320 64482698
Blood creatine phosphokinase increased 83.31 21.23 81 13633 58477 64426541
Suicide attempt 82.42 21.23 88 13626 70919 64414099
Myocarditis 79.71 21.23 48 13666 16995 64468023
Sedation 77.83 21.23 67 13647 41395 64443623
Differential white blood cell count abnormal 75.60 21.23 24 13690 1786 64483232
Drug interaction 74.35 21.23 206 13508 361877 64123141
Leukopenia 69.26 21.23 96 13618 101146 64383872
Euphoric mood 66.43 21.23 31 13683 6560 64478458
Arthralgia 59.68 21.23 11 13703 442249 64042769
Tachycardia 58.53 21.23 110 13604 149469 64335549
Treatment noncompliance 56.01 21.23 57 13657 43425 64441593
Disinhibition 55.21 21.23 20 13694 2223 64482795
Agitation 54.83 21.23 80 13634 88287 64396731
Obsessive-compulsive disorder 52.74 21.23 24 13690 4794 64480224
Mental disorder 52.20 21.23 44 13670 26401 64458617
White blood cell count decreased 51.99 21.23 108 13606 157729 64327289
Nausea 49.23 21.23 57 13657 785743 63699275
Negative thoughts 49.00 21.23 16 13698 1302 64483716
Tardive dyskinesia 48.56 21.23 28 13686 9150 64475868
Overdose 47.73 21.23 105 13609 159461 64325557
Confusional state 47.14 21.23 142 13572 261002 64224016
Waxy flexibility 47.08 21.23 11 13703 254 64484764
Suicidal ideation 46.83 21.23 64 13650 66478 64418540
Schizoaffective disorder 46.09 21.23 16 13698 1571 64483447
Diarrhoea 45.70 21.23 52 13662 722652 63762366
Thinking abnormal 45.06 21.23 29 13685 11527 64473491
Intentional self-injury 44.74 21.23 42 13672 29002 64456016
Pain in extremity 44.32 21.23 6 13708 303079 64181939
Somnolence 43.80 21.23 118 13596 203527 64281491
Persecutory delusion 43.28 21.23 20 13694 4138 64480880
CSF measles antibody positive 42.90 21.23 8 13706 57 64484961
Rubella antibody positive 42.43 21.23 8 13706 61 64484957
Therapeutic product effect variable 41.75 21.23 15 13699 1629 64483389
Back pain 41.66 21.23 3 13711 250168 64234850
Pruritus 41.62 21.23 8 13706 312392 64172626
Rash 41.48 21.23 23 13691 458526 64026492
Eosinophil count decreased 41.48 21.23 17 13697 2635 64482383
Psychotic symptom 41.44 21.23 16 13698 2122 64482896
Binge eating 41.29 21.23 11 13703 439 64484579
Neutrophil count decreased 40.96 21.23 65 13649 77131 64407887
Muscle rigidity 40.65 21.23 32 13682 17441 64467577
Obesity 40.14 21.23 34 13680 20528 64464490
Hallucination 39.60 21.23 62 13652 72726 64412292
Weight increased 39.41 21.23 117 13597 213231 64271787
Mydriasis 37.70 21.23 29 13685 15283 64469735
Breast engorgement 37.65 21.23 7 13707 49 64484969
Hyperlactacidaemia 37.43 21.23 19 13695 4825 64480193
Catatonia 37.02 21.23 22 13692 7598 64477420
Blood brain barrier defect 36.90 21.23 8 13706 130 64484888
Wrong patient received product 35.77 21.23 17 13697 3745 64481273
Intentional overdose 33.72 21.23 65 13649 89879 64395139
Oromandibular dystonia 33.61 21.23 11 13703 902 64484116
Conduction disorder 33.16 21.23 15 13699 2953 64482065
Thunderclap headache 32.97 21.23 8 13706 218 64484800
Psychomotor hyperactivity 32.62 21.23 26 13688 14425 64470593
Overweight 31.45 21.23 15 13699 3331 64481687
Increased appetite 31.26 21.23 22 13692 10124 64474894
Left ventricular dysfunction 30.99 21.23 27 13687 16927 64468091
Hypoventilation 30.91 21.23 18 13696 5988 64479030
Bladder trabeculation 30.55 21.23 6 13708 58 64484960
Rebound psychosis 30.54 21.23 7 13707 148 64484870
Prescribed overdose 30.54 21.23 29 13685 20302 64464716
Headache 30.35 21.23 41 13673 529426 63955592
Pleurothotonus 30.13 21.23 13 13701 2289 64482729
Disorientation 29.59 21.23 47 13667 55781 64429237
Sarcoma metastatic 29.52 21.23 6 13708 70 64484948
Psychomotor skills impaired 29.47 21.23 15 13699 3830 64481188
Abnormal behaviour 29.38 21.23 36 13678 33586 64451432
Platelet count increased 28.72 21.23 27 13687 18669 64466349
Right ventricular dilatation 28.67 21.23 11 13703 1434 64483584
Drug ineffective 28.62 21.23 288 13426 839959 63645059
Peripheral swelling 28.60 21.23 5 13709 209148 64275870
Hypersensitivity 28.44 21.23 4 13710 196448 64288570
Rhabdomyolysis 28.12 21.23 61 13653 91665 64393353
Diffuse large B-cell lymphoma stage II 27.94 21.23 6 13708 93 64484925
Refusal of examination 27.82 21.23 6 13708 95 64484923
Mean cell volume decreased 27.81 21.23 14 13700 3492 64481526
Joint swelling 27.66 21.23 6 13708 215376 64269642
Type 2 diabetes mellitus 27.44 21.23 35 13679 33985 64451033
Organic brain syndrome 27.37 21.23 8 13706 450 64484568
Tremor 27.06 21.23 81 13633 148149 64336869
Dyspnoea 26.87 21.23 72 13642 718602 63766416
Asthenia 26.76 21.23 31 13683 428013 64057005
Morose 26.65 21.23 5 13709 37 64484981
Fatigue 26.52 21.23 77 13637 748653 63736365
Accommodation disorder 26.43 21.23 8 13706 508 64484510
Nasopharyngitis 26.14 21.23 5 13709 196068 64288950
Cognitive disorder 25.99 21.23 44 13670 55043 64429975
Paranoia 25.86 21.23 24 13690 16328 64468690
Sinus tachycardia 25.78 21.23 33 13681 32155 64452863
Abdominal discomfort 25.73 21.23 4 13710 182318 64302700
Blepharospasm 25.38 21.23 13 13701 3362 64481656
Suspiciousness 25.36 21.23 8 13706 583 64484435
Irritability 25.32 21.23 35 13679 36711 64448307
Disturbance in attention 25.18 21.23 37 13677 41037 64443981
Arteriosclerosis coronary artery 24.96 21.23 23 13691 15506 64469512
Cerebral artery stenosis 24.50 21.23 8 13706 651 64484367
Tobacco interaction 24.39 21.23 5 13709 61 64484957
Blood folate decreased 24.36 21.23 9 13705 1058 64483960
Acute psychosis 24.09 21.23 13 13701 3739 64481279
CSF protein increased 24.05 21.23 9 13705 1096 64483922
Pulmonary valve incompetence 24.00 21.23 10 13704 1616 64483402
Dyslipidaemia 23.84 21.23 18 13696 9224 64475794
Ventricular dyskinesia 23.82 21.23 7 13707 401 64484617
Swelling 23.81 21.23 3 13711 160215 64324803
Postmortem blood drug level increased 23.37 21.23 8 13706 753 64484265
Leukocytosis 23.14 21.23 34 13680 37706 64447312
Faecaloma 23.02 21.23 18 13696 9710 64475308
Mean cell haemoglobin decreased 22.94 21.23 13 13701 4109 64480909
Drug hypersensitivity 22.84 21.23 11 13703 237804 64247214
Oculogyric crisis 22.71 21.23 11 13703 2527 64482491
Depressed level of consciousness 22.54 21.23 52 13662 81384 64403634
Hangover 22.49 21.23 10 13704 1891 64483127
Hyperleukocytosis 21.82 21.23 10 13704 2030 64482988
Grandiosity 21.58 21.23 7 13707 558 64484460
Loss of consciousness 21.57 21.23 75 13639 148290 64336728
Microcytic anaemia 21.52 21.23 13 13701 4625 64480393
Drug level increased 21.25 21.23 31 13683 34165 64450853

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05AL05 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Benzamides
MeSH PA D000928 Antidepressive Agents
MeSH PA D018687 Antidepressive Agents, Second-Generation
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 D018377 Neurotransmitter Agents
MeSH PA D011619 Psychotropic Drugs
MeSH PA D014149 Tranquilizing Agents
FDA MoA N0000175799 Dopamine D2 Antagonists
FDA EPC N0000175800 Dopamine-2 Receptor Antagonist
CHEBI has role CHEBI:35703 Xenobiotic
CHEBI has role CHEBI:65191 atypical antipsychotic agent
CHEBI has role CHEBI:78298 environmental contaminants

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 ACACIA N209510 Sept. 1, 2020 RX SOLUTION INTRAVENOUS 9084765 March 10, 2031 PREVENTION OF POST-OPERATIVE NAUSEA AND VOMITING
10MG/4ML (2.5MG/ML) BARHEMSYS ACACIA N209510 Sept. 1, 2020 RX SOLUTION INTRAVENOUS 9084765 March 10, 2031 TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING
10MG/4ML (2.5MG/ML) BARHEMSYS ACACIA N209510 Sept. 1, 2020 RX SOLUTION INTRAVENOUS 9545426 March 10, 2031 PREVENTION OF POST-OPERATIVE NAUSEA AND VOMITING
10MG/4ML (2.5MG/ML) BARHEMSYS ACACIA N209510 Sept. 1, 2020 RX SOLUTION INTRAVENOUS 9545426 March 10, 2031 TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING
10MG/4ML (2.5MG/ML) BARHEMSYS ACACIA N209510 Sept. 1, 2020 RX SOLUTION INTRAVENOUS 9889118 March 10, 2031 PREVENTION OF POST-OPERATIVE NAUSEA AND VOMITING
10MG/4ML (2.5MG/ML) BARHEMSYS ACACIA N209510 Sept. 1, 2020 RX SOLUTION INTRAVENOUS 9889118 March 10, 2031 TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING
5MG/2ML (2.5MG/ML) BARHEMSYS ACACIA N209510 Feb. 26, 2020 RX SOLUTION INTRAVENOUS 9084765 March 10, 2031 PREVENTION OF POST-OPERATIVE NAUSEA AND VOMITING
5MG/2ML (2.5MG/ML) BARHEMSYS ACACIA N209510 Feb. 26, 2020 RX SOLUTION INTRAVENOUS 9084765 March 10, 2031 TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING
5MG/2ML (2.5MG/ML) BARHEMSYS ACACIA N209510 Feb. 26, 2020 RX SOLUTION INTRAVENOUS 9545426 March 10, 2031 PREVENTION OF POST-OPERATIVE NAUSEA AND VOMITING
5MG/2ML (2.5MG/ML) BARHEMSYS ACACIA N209510 Feb. 26, 2020 RX SOLUTION INTRAVENOUS 9545426 March 10, 2031 TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING
5MG/2ML (2.5MG/ML) BARHEMSYS ACACIA N209510 Feb. 26, 2020 RX SOLUTION INTRAVENOUS 9889118 March 10, 2031 PREVENTION OF POST-OPERATIVE NAUSEA AND VOMITING
5MG/2ML (2.5MG/ML) BARHEMSYS ACACIA N209510 Feb. 26, 2020 RX SOLUTION INTRAVENOUS 9889118 March 10, 2031 TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
10MG/4ML (2.5MG/ML) BARHEMSYS ACACIA N209510 Sept. 1, 2020 RX SOLUTION INTRAVENOUS Feb. 26, 2025 NEW CHEMICAL ENTITY
5MG/2ML (2.5MG/ML) BARHEMSYS ACACIA N209510 Feb. 26, 2020 RX SOLUTION INTRAVENOUS Feb. 26, 2025 NEW CHEMICAL ENTITY

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
005229 NDDF
4039609 VANDF
321636003 SNOMEDCT_US
391761004 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Barhemsys HUMAN PRESCRIPTION DRUG LABEL 1 71390-125 INJECTION, SOLUTION 2.50 mg INTRAVENOUS NDA 30 sections