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

Stem definition	Drug id	CAS RN
sulpiride derivatives and analogues	179	71675-85-9

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
0.40	g	O
7.50	mg	P

ADMET properties:

Property	Value	Reference
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

Approvals:

Date	Agency	Company	Orphan
Feb. 26, 2020	FDA	ACACIA PHARMA LTD
Jan. 1, 1986	YEAR INTRODUCED

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	314.09	26.25	102	8339	13182	63467399
Schizophrenia	221.39	26.25	73	8368	9879	63470702
Hyperprolactinaemia	160.97	26.25	46	8395	3854	63476727
Blood prolactin increased	156.71	26.25	44	8397	3459	63477122
Sopor	151.79	26.25	69	8372	22095	63458486
Drug abuse	146.39	26.25	101	8340	72417	63408164
Mental impairment	142.92	26.25	58	8383	14093	63466488
Akathisia	137.18	26.25	50	8391	9096	63471485
Refusal of examination	112.21	26.25	20	8421	183	63480398
Neuroleptic malignant syndrome	100.15	26.25	43	8398	12013	63468568
Electrocardiogram QT prolonged	97.35	26.25	73	8368	59457	63421124
Myocarditis	92.98	26.25	39	8402	10286	63470295
Eosinophil count decreased	91.12	26.25	26	8415	2164	63478417
Differential white blood cell count abnormal	85.21	26.25	20	8421	766	63479815
Psychotic disorder	82.35	26.25	48	8393	25664	63454917
Delusion	80.94	26.25	37	8404	11980	63468601
Metabolic syndrome	80.46	26.25	22	8419	1566	63479015
Antipsychotic drug level increased	79.58	26.25	26	8415	3409	63477172
Antipsychotic drug level decreased	77.37	26.25	16	8425	337	63480244
Neutropenia	76.89	26.25	105	8336	174900	63305681
Parkinsonism	76.20	26.25	34	8407	10405	63470176
Dystonia	76.01	26.25	37	8404	13782	63466799
Sedation	75.75	26.25	53	8388	38756	63441825
Galactorrhoea	74.73	26.25	26	8415	4129	63476452
Drug interaction	71.35	26.25	117	8324	229014	63251567
Hallucination, auditory	69.52	26.25	34	8407	12790	63467791
Leukopenia	65.35	26.25	65	8376	77225	63403356
Aggression	65.19	26.25	40	8401	23458	63457123
Confusional state	63.43	26.25	113	8328	236267	63244314
Mental disorder	61.59	26.25	40	8401	25879	63454702
Pain	59.58	26.25	13	8428	740615	62739966
Suicidal ideation	57.44	26.25	55	8386	62366	63418215
Salivary hypersecretion	56.05	26.25	25	8416	7641	63472940
Intentional self-injury	54.64	26.25	37	8404	25650	63454931
Mydriasis	53.96	26.25	28	8413	11928	63468653
Antipsychotic drug level above therapeutic	50.76	26.25	14	8427	1029	63479552
Blood bilirubin decreased	49.51	26.25	13	8428	792	63479789
Neutrophil count increased	48.06	26.25	29	8412	16498	63464083
Hallucination	47.99	26.25	47	8394	54770	63425811
Arthralgia	47.84	26.25	9	8432	569701	62910880
CSF measles antibody positive	46.66	26.25	8	8433	57	63480524
Tremor	45.86	26.25	71	8370	132168	63348413
Rubella antibody positive	45.84	26.25	8	8433	64	63480517
Treatment noncompliance	44.38	26.25	38	8403	37287	63443294
Troponin increased	43.66	26.25	23	8418	10098	63470483
Blood brain barrier defect	43.30	26.25	8	8433	91	63480490
Thyroxine free decreased	41.63	26.25	11	8430	687	63479894
Overdose	41.60	26.25	63	8378	115015	63365566
Tardive dyskinesia	41.52	26.25	21	8420	8481	63472100
Transferrin saturation decreased	40.53	26.25	11	8430	761	63479820
Aspartate aminotransferase decreased	40.31	26.25	11	8430	777	63479804
Grandiosity	39.82	26.25	9	8432	291	63480290
Suicide attempt	38.64	26.25	44	8397	60874	63419707
Rash	37.37	26.25	14	8427	560857	62919724
Catatonia	37.27	26.25	16	8425	4461	63476120
Organic brain syndrome	37.26	26.25	8	8433	203	63480378
Thunderclap headache	36.54	26.25	8	8433	223	63480358
Euphoric mood	35.92	26.25	16	8425	4871	63475710
White blood cell count increased	35.87	26.25	38	8403	48523	63432058
Binge eating	35.57	26.25	9	8432	473	63480108
Ventricular dyskinesia	34.94	26.25	7	8434	125	63480456
CSF protein increased	34.88	26.25	9	8432	512	63480069
Cognitive disorder	34.87	26.25	40	8401	55775	63424806
Agitation	34.29	26.25	41	8400	59716	63420865
Pruritus	34.23	26.25	4	8437	361449	63119132
Cogwheel rigidity	34.17	26.25	12	8429	1958	63478623
Negative thoughts	34.09	26.25	10	8431	917	63479664
Bladder trabeculation	33.75	26.25	6	8435	54	63480527
Sinus tachycardia	33.62	26.25	27	8414	24241	63456340
Pain in extremity	33.11	26.25	3	8438	331483	63149098
Accommodation disorder	32.55	26.25	8	8433	373	63480208
Mean cell haemoglobin decreased	31.92	26.25	15	8426	5164	63475417
Blood folate decreased	31.70	26.25	9	8432	735	63479846
Cerebral artery stenosis	30.72	26.25	8	8433	472	63480109
Serum ferritin decreased	29.85	26.25	11	8430	2059	63478522
Toxicity to various agents	29.75	26.25	86	8355	247164	63233417
Loss of consciousness	29.73	26.25	55	8386	118066	63362515
Neutrophil count abnormal	29.68	26.25	12	8429	2880	63477701
Red cell distribution width increased	29.40	26.25	18	8423	10506	63470075
Mean cell volume decreased	29.16	26.25	13	8428	3965	63476616
Morose	29.11	26.25	5	8436	36	63480545
Coma	28.77	26.25	39	8402	64325	63416256
Blood phosphorus increased	28.71	26.25	12	8429	3133	63477448
Sitting disability	28.68	26.25	7	8434	317	63480264
Waxy flexibility	28.59	26.25	6	8435	136	63480445
Amenorrhoea	27.80	26.25	17	8424	9897	63470684
Serotonin syndrome	27.75	26.25	26	8415	28656	63451925
Somnolence	27.39	26.25	68	8373	178617	63301964
Cor pulmonale acute	27.13	26.25	7	8434	398	63480183
Mean cell haemoglobin concentration decreased	27.11	26.25	12	8429	3600	63476981
Cardiogenic shock	27.09	26.25	21	8420	17911	63462670
Troponin T increased	27.07	26.25	9	8432	1245	63479336
Hypochromic anaemia	26.83	26.25	10	8431	1932	63478649
Supraventricular tachycardia	26.69	26.25	19	8422	14252	63466329
Overweight	26.67	26.25	12	8429	3739	63476842

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
Antipsychotic drug level below therapeutic	441.75	25.71	112	10974	2435	34943410
Akathisia	363.72	25.71	125	10961	7984	34937861
Disinhibition	341.42	25.71	96	10990	3130	34942715
Therapeutic product effect variable	324.39	25.71	87	10999	2369	34943476
Obsessive-compulsive disorder	318.11	25.71	103	10983	5461	34940384
Euphoric mood	292.53	25.71	97	10989	5544	34940301
Increased appetite	266.38	25.71	97	10989	7332	34938513
Schizophrenia	230.59	25.71	91	10995	8575	34937270
Suicide attempt	205.17	25.71	137	10949	38979	34906866
Neuroleptic malignant syndrome	192.78	25.71	100	10986	17834	34928011
Extrapyramidal disorder	189.66	25.71	89	10997	12791	34933054
Antipsychotic drug level increased	182.66	25.71	62	11024	3803	34942042
Electrocardiogram QT prolonged	167.07	25.71	123	10963	40829	34905016
Neutrophil count increased	165.54	25.71	89	10997	17057	34928788
Leukopenia	141.85	25.71	134	10952	62722	34883123
White blood cell count increased	135.82	25.71	109	10977	41042	34904803
Salivary hypersecretion	128.04	25.71	60	11026	8584	34937261
Weight increased	125.72	25.71	151	10935	92882	34852963
Blood prolactin increased	118.80	25.71	37	11049	1723	34944122
Obesity	116.36	25.71	64	11022	12814	34933031
Mental impairment	115.02	25.71	59	11027	10263	34935582
Leukaemia	114.27	25.71	46	11040	4557	34941288
Hyperprolactinaemia	113.83	25.71	35	11051	1561	34944284
Therapeutic product effect incomplete	112.54	25.71	107	10979	50434	34895411
Psychotic disorder	110.04	25.71	78	11008	24374	34921471
Hallucination, auditory	104.31	25.71	58	11028	11859	34933986
Delusion	103.82	25.71	59	11027	12576	34933269
Dyslipidaemia	98.77	25.71	48	11038	7440	34938405
Antipsychotic drug level decreased	97.34	25.71	28	11058	989	34944856
Antipsychotic drug level above therapeutic	96.31	25.71	29	11057	1204	34944641
Prescribed overdose	85.54	25.71	49	11037	10598	34935247
Blood creatine phosphokinase increased	83.20	25.71	86	11000	44771	34901074
Sedation	67.87	25.71	55	11031	20951	34924894
White blood cell count decreased	58.65	25.71	107	10979	95338	34850507
Drug ineffective	57.84	25.71	291	10795	456460	34489385
Schizoaffective disorder	57.66	25.71	20	11066	1307	34944538
Tachycardia	57.18	25.71	99	10987	84673	34861172
Aggression	57.07	25.71	66	11020	38898	34906947
Dystonia	56.78	25.71	38	11048	10807	34935038
Neutropenia	56.07	25.71	141	10945	156637	34789208
Pleurothotonus	55.62	25.71	19	11067	1186	34944659
Nausea	54.46	25.71	20	11066	339888	34605957
Toxicity to various agents	50.79	25.71	159	10927	200203	34745642
Diarrhoea	50.16	25.71	31	11055	389881	34555964
Neutrophil count decreased	47.29	25.71	69	11017	51035	34894810
Drug interaction	43.84	25.71	164	10922	225782	34720063
Breast engorgement	43.61	25.71	7	11079	9	34945836
Psychotic symptom	41.81	25.71	17	11069	1726	34944119
Lower respiratory tract infection	40.41	25.71	50	11036	31587	34914258
Myocarditis	40.38	25.71	34	11052	13648	34932197
Drug level increased	40.27	25.71	42	11044	22054	34923791
Arthralgia	39.63	25.71	4	11082	170037	34775808
Agitation	38.62	25.71	67	11019	57332	34888513
Persecutory delusion	38.47	25.71	18	11068	2562	34943283
Thinking abnormal	38.26	25.71	24	11062	6113	34939732
Suicidal ideation	36.59	25.71	54	11032	40334	34905511
Irritability	36.43	25.71	42	11044	24648	34921197
Left ventricular dysfunction	36.17	25.71	28	11058	9979	34935866
Paranoia	35.63	25.71	30	11056	12038	34933807
Sopor	35.48	25.71	30	11056	12106	34933739
Treatment noncompliance	35.23	25.71	44	11042	28056	34917789
Parkinsonism	34.37	25.71	25	11061	8113	34937732
Blepharospasm	33.96	25.71	13	11073	1125	34944720
Hypoventilation	33.69	25.71	18	11068	3396	34942449
Conduction disorder	32.33	25.71	15	11071	2095	34943750
Abnormal behaviour	31.14	25.71	39	11047	24930	34920915
Diffuse large B-cell lymphoma stage II	30.82	25.71	6	11080	35	34945810
Somnolence	30.71	25.71	91	10995	111025	34834820
Pain in extremity	29.40	25.71	3	11083	126510	34819335
Psychomotor hyperactivity	28.57	25.71	24	11062	9598	34936247
Disturbance in attention	28.41	25.71	38	11048	25907	34919938
Sarcoma metastatic	27.71	25.71	6	11080	63	34945782
Differential white blood cell count abnormal	27.54	25.71	12	11074	1447	34944398
Subacute endocarditis	27.45	25.71	6	11080	66	34945779
Platelet count increased	26.73	25.71	23	11063	9503	34936342
Pain	26.61	25.71	16	11070	204659	34741186
Suspiciousness	26.59	25.71	8	11078	331	34945514
Rebound psychosis	26.53	25.71	7	11079	178	34945667
Hypertension	26.35	25.71	99	10987	136344	34809501
Fatigue	25.88	25.71	49	11037	370604	34575241

FDA Adverse Event Reporting System (Geriatric)

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	435.29	22.27	166	15947	22513	79705762
Schizophrenia	347.31	22.27	127	15986	15313	79712962
Neuroleptic malignant syndrome	285.60	22.27	130	15983	27429	79700846
Akathisia	254.11	22.27	97	16016	13162	79715113
Electrocardiogram QT prolonged	223.77	22.27	168	15945	90218	79638057
Hyperprolactinaemia	215.34	22.27	66	16047	4610	79723665
Blood prolactin increased	207.84	22.27	62	16051	3949	79724326
Mental impairment	207.34	22.27	93	16020	18943	79709332
Antipsychotic drug level increased	195.62	22.27	65	16048	5892	79722383
Antipsychotic drug level below therapeutic	183.79	22.27	44	16069	1194	79727081
Neutrophil count increased	180.12	22.27	97	16016	29299	79698976
Sopor	164.26	22.27	95	16018	32915	79695360
Delusion	161.47	22.27	80	16033	20343	79707932
White blood cell count increased	150.60	22.27	123	15990	74510	79653765
Antipsychotic drug level decreased	148.59	22.27	37	16076	1187	79727088
Psychotic disorder	144.43	22.27	95	16018	41307	79686968
Hallucination, auditory	142.97	22.27	74	16039	20619	79707656
Drug abuse	141.15	22.27	169	15944	162522	79565753
Salivary hypersecretion	140.71	22.27	65	16048	14159	79714116
Dystonia	129.36	22.27	70	16043	21329	79706946
Neutropenia	122.47	22.27	213	15900	287497	79440778
Myocarditis	120.09	22.27	67	16046	21666	79706609
Leukopenia	116.03	22.27	130	15983	116383	79611892
Antipsychotic drug level above therapeutic	115.82	22.27	34	16079	2046	79726229
Euphoric mood	111.25	22.27	46	16067	7680	79720595
Drug interaction	111.07	22.27	253	15860	414930	79313345
Refusal of examination	108.56	22.27	21	16092	197	79728078
Suicide attempt	108.39	22.27	107	16006	82825	79645450
Eosinophil count decreased	99.42	22.27	34	16079	3362	79724913
Sedation	99.36	22.27	83	16030	51812	79676463
Pain	98.63	22.27	13	16100	703789	79024486
Parkinsonism	96.76	22.27	53	16060	16531	79711744
Aggression	96.53	22.27	81	16032	50877	79677398
Disinhibition	91.92	22.27	30	16083	2568	79725707
Galactorrhoea	89.45	22.27	32	16081	3614	79724661
Differential white blood cell count abnormal	85.87	22.27	27	16086	2050	79726225
Metabolic syndrome	82.43	22.27	28	16085	2712	79725563
Obsessive-compulsive disorder	81.00	22.27	34	16079	5893	79722382
Blood creatine phosphokinase increased	80.32	22.27	82	16031	66008	79662267
Arthralgia	79.01	22.27	11	16102	571792	79156483
Therapeutic product effect variable	78.44	22.27	25	16088	1984	79726291
Suicidal ideation	72.24	22.27	83	16030	76257	79652018
White blood cell count decreased	69.29	22.27	131	15982	188157	79540118
Nausea	63.74	22.27	60	16053	957136	78771139
Treatment noncompliance	61.96	22.27	64	16049	52204	79676071
Schizoaffective disorder	60.87	22.27	21	16092	2131	79726144
Mental disorder	59.76	22.27	50	16063	31252	79697023
Somnolence	59.73	22.27	142	15971	238839	79489436
Tachycardia	59.68	22.27	119	15994	177649	79550626
Agitation	59.09	22.27	86	16027	99629	79628646
Diarrhoea	58.82	22.27	55	16058	880434	78847841
Intentional self-injury	58.23	22.27	50	16063	32369	79695906
Psychotic symptom	56.24	22.27	21	16092	2676	79725599
Thinking abnormal	55.33	22.27	34	16079	13127	79715148
Pleurothotonus	53.97	22.27	20	16093	2496	79725779
Increased appetite	53.07	22.27	32	16081	11946	79716329
Pain in extremity	52.75	22.27	6	16107	364532	79363743
Rash	52.04	22.27	26	16087	578332	79149943
Persecutory delusion	50.31	22.27	23	16090	4886	79723389
Back pain	49.51	22.27	3	16110	304177	79424098
Pruritus	49.13	22.27	10	16103	394638	79333637
Negative thoughts	48.87	22.27	16	16097	1383	79726892
Tardive dyskinesia	48.80	22.27	29	16084	10542	79717733
Weight increased	48.17	22.27	144	15969	277242	79451033
Mean cell volume decreased	47.03	22.27	22	16091	4925	79723350
Muscle rigidity	46.99	22.27	36	16077	19846	79708429
Waxy flexibility	46.91	22.27	11	16102	272	79728003
Overdose	46.58	22.27	110	16003	184096	79544179
Confusional state	46.00	22.27	155	15958	317842	79410433
Drug ineffective	45.80	22.27	373	15740	1080540	78647735
Neutrophil count decreased	45.75	22.27	74	16039	93885	79634390
Wrong patient received product	45.34	22.27	21	16092	4597	79723678
Dyslipidaemia	43.74	22.27	28	16085	11605	79716670
Troponin increased	43.62	22.27	34	16079	19221	79709054
Obesity	43.42	22.27	44	16069	35081	79693194
CSF measles antibody positive	43.31	22.27	8	16105	57	79728218
Psychomotor hyperactivity	43.13	22.27	32	16081	16817	79711458
Rubella antibody positive	42.83	22.27	8	16105	61	79728214
Mydriasis	41.82	22.27	32	16081	17611	79710664
Overweight	41.14	22.27	19	16094	4131	79724144
Irritability	41.05	22.27	46	16067	41098	79687177
Binge eating	40.50	22.27	11	16102	498	79727777
Blood bilirubin decreased	40.42	22.27	13	16100	1062	79727213
Hallucination	39.67	22.27	66	16047	85679	79642596
Mean cell haemoglobin decreased	39.39	22.27	21	16092	6203	79722072
Joint swelling	38.76	22.27	6	16107	288640	79439635
Sinus tachycardia	38.09	22.27	42	16071	36866	79691409
Catatonia	37.78	22.27	23	16090	8733	79719542
Peripheral swelling	37.61	22.27	5	16108	269612	79458663
Abnormal behaviour	36.82	22.27	41	16072	36380	79691895
Breast engorgement	36.75	22.27	7	16106	60	79728215
Abdominal discomfort	36.57	22.27	4	16109	250723	79477552
Blood brain barrier defect	36.53	22.27	8	16105	144	79728131
Hyperlactacidaemia	35.75	22.27	19	16094	5576	79722699
Dyspnoea	34.88	22.27	76	16037	856949	78871326
Nasopharyngitis	34.72	22.27	5	16108	253876	79474399
Rhabdomyolysis	34.53	22.27	69	16044	103062	79625213
Drug level increased	33.99	22.27	41	16072	39610	79688665
Priapism	33.68	22.27	17	16096	4488	79723787
Type 2 diabetes mellitus	33.43	22.27	49	16064	57073	79671202
Left ventricular dysfunction	33.03	22.27	29	16084	19332	79708943
Swelling	32.80	22.27	3	16110	216708	79511567
Headache	32.77	22.27	51	16062	653721	79074554
Oromandibular dystonia	32.57	22.27	11	16102	1047	79727228
Thyroxine free decreased	32.47	22.27	11	16102	1056	79727219
Prescribed overdose	32.19	22.27	39	16074	37844	79690431
Conduction disorder	32.03	22.27	15	16098	3364	79724911
Aspartate aminotransferase decreased	31.98	22.27	11	16102	1106	79727169
Hypersensitivity	31.88	22.27	7	16106	262232	79466043
Transferrin saturation decreased	31.70	22.27	11	16102	1135	79727140
Toxicity to various agents	31.50	22.27	168	15945	421372	79306903
Intentional overdose	30.91	22.27	67	16046	105893	79622382
Bladder trabeculation	30.85	22.27	6	16107	58	79728217
Oculogyric crisis	30.78	22.27	14	16099	2938	79725337
Drug hypersensitivity	30.74	22.27	11	16102	298905	79429370
Sarcoma metastatic	29.44	22.27	6	16107	75	79728200
Rebound psychosis	29.38	22.27	8	16105	366	79727909
Product use in unapproved indication	29.34	22.27	114	15999	250245	79478030
Suspiciousness	29.22	22.27	9	16104	638	79727637
Acute psychosis	29.01	22.27	15	16098	4165	79724110
Thunderclap headache	28.74	22.27	8	16105	397	79727878
Hypoventilation	28.69	22.27	18	16095	7206	79721069
Cognitive disorder	28.63	22.27	51	16062	69875	79658400
Hallucination, visual	28.31	22.27	34	16079	32695	79695580
Electrocardiogram QT shortened	28.24	22.27	7	16106	220	79728055
Diffuse large B-cell lymphoma stage II	27.83	22.27	6	16107	100	79728175
Organic brain syndrome	27.33	22.27	8	16105	476	79727799
Disorientation	27.28	22.27	47	16066	62729	79665546
Paranoia	27.09	22.27	26	16087	19406	79708869
Serum ferritin decreased	27.09	22.27	12	16101	2368	79725907
Arteriosclerosis coronary artery	27.06	22.27	25	16088	17791	79710484
Morose	26.45	22.27	5	16108	41	79728234
Febrile neutropenia	26.44	22.27	7	16106	230992	79497283
Pulmonary valve incompetence	26.18	22.27	11	16102	1909	79726366
Right ventricular dilatation	26.15	22.27	11	16102	1915	79726360
Hyperleukocytosis	26.03	22.27	12	16101	2598	79725677
Psychomotor skills impaired	25.84	22.27	15	16098	5222	79723053
Grandiosity	25.81	22.27	8	16105	579	79727696
Platelet count increased	25.76	22.27	27	16086	22379	79705896
Accommodation disorder	25.67	22.27	8	16105	590	79727685
Tremor	25.52	22.27	84	16029	169999	79558276
Troponin T increased	25.48	22.27	13	16100	3509	79724766
Erythema	25.12	22.27	7	16106	223283	79504992
Pneumonia	24.84	22.27	61	16052	660185	79068090
Left ventricular dilatation	24.53	22.27	9	16104	1092	79727183
Fatigue	24.42	22.27	101	16012	929626	78798649
Cough	24.28	22.27	23	16090	366766	79361509
Dyskinesia	24.19	22.27	37	16076	44736	79683539
Ventricular dyskinesia	24.18	22.27	7	16106	401	79727874
Antisocial personality disorder	24.08	22.27	5	16108	69	79728206
Cerebral artery stenosis	23.73	22.27	8	16105	757	79727518
CSF protein increased	23.49	22.27	9	16104	1231	79727044
Postmortem blood drug level increased	23.29	22.27	8	16105	801	79727474
Blood folate decreased	23.15	22.27	9	16104	1280	79726995
Tobacco interaction	23.10	22.27	5	16108	85	79728190
Congestive cardiomyopathy	22.86	22.27	19	16094	11761	79716514
Asthenia	22.78	22.27	43	16070	511646	79216629
Red cell distribution width increased	22.40	22.27	21	16092	15221	79713054

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
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|

Disease	Relation	SNOMED_ID	DOID
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 level	Dissociation constant	Type (acidic/basic)
pKa1	13.78	acidic
pKa2	9.09	Basic
pKa3	0.54	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
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	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
10MG/4ML (2.5MG/ML)	BARHEMSYS	ACACIA	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	ACACIA	N209510	Sept. 1, 2020	RX	SOLUTION	INTRAVENOUS	9084765	Feb. 26, 2034	PREVENTION OF POST-OPERATIVE NAUSEA AND VOMITING
10MG/4ML (2.5MG/ML)	BARHEMSYS	ACACIA	N209510	Sept. 1, 2020	RX	SOLUTION	INTRAVENOUS	9084765	Feb. 26, 2034	TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING
5MG/2ML (2.5MG/ML)	BARHEMSYS	ACACIA	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	ACACIA	N209510	Feb. 26, 2020	RX	SOLUTION	INTRAVENOUS	9084765	Feb. 26, 2034	PREVENTION OF POST-OPERATIVE NAUSEA AND VOMITING
5MG/2ML (2.5MG/ML)	BARHEMSYS	ACACIA	N209510	Feb. 26, 2020	RX	SOLUTION	INTRAVENOUS	9084765	Feb. 26, 2034	TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING
10MG/4ML (2.5MG/ML)	BARHEMSYS	ACACIA	N209510	Sept. 1, 2020	RX	SOLUTION	INTRAVENOUS	11357753	Feb. 9, 2038	TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING
5MG/2ML (2.5MG/ML)	BARHEMSYS	ACACIA	N209510	Feb. 26, 2020	RX	SOLUTION	INTRAVENOUS	11357753	Feb. 9, 2038	TREATMENT OF POST-OPERATIVE NAUSEA AND VOMITING

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN	ANTAGONIST	Ki	8.55	WOMBAT-PK	SCIENTIFIC LITERATURE
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN	ANTAGONIST	Ki	8.50	WOMBAT-PK	SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	5.08	PDSP
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	7.89	PDSP
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN		Ki	5.38	PDSP
5-hydroxytryptamine receptor 7	GPCR	P34969	5HT7R_HUMAN		Ki	7.94	PDSP
5-hydroxytryptamine receptor 1D	GPCR	P28221	5HT1D_HUMAN		Ki	5.87	PDSP
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN		Ki	5.81	PDSP
D(4) dopamine receptor	GPCR	P21917	DRD4_HUMAN		Ki	5.63	PDSP
5-hydroxytryptamine receptor 1B	GPCR	P28222	5HT1B_HUMAN		Ki	5.76	PDSP
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	5.95	PDSP
D(3) dopamine receptor	GPCR		DRD3_RAT	ANTAGONIST	Ki	7.40	IUPHAR

External reference:

ID	Source
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
321636003	SNOMEDCT_US
391761004	SNOMEDCT_US
4039609	VANDF
005229	NDDF

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Barhemsys	HUMAN PRESCRIPTION DRUG LABEL	1	71390-125	INJECTION, SOLUTION	2.50 mg	INTRAVENOUS	NDA	30 sections
Barhemsys	HUMAN PRESCRIPTION DRUG LABEL	1	71390-125	INJECTION, SOLUTION	2.50 mg	INTRAVENOUS	NDA	30 sections