amisulpride indications/contra

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

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • amisulpride
  • aminosultopride
  • deniban
  • solian
  • Molecular weight: 369.48
  • Formula: C17H27N3O4S
  • CLOGP: 1.80
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 2
  • TPSA: 101.73
  • ALOGS: -3.10
  • ROTB: 7

Drug dosage:

DoseUnitRoute
0.40 g O

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1986 YEAR INTRODUCED

FDA Adverse Event Reporting System

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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
Schizophrenia 264.02 47.85 51 870 2643 3382295
Neuroleptic malignant syndrome 261.57 47.85 55 866 4386 3380552
Electrocardiogram QT prolonged 252.71 47.85 63 858 10732 3374206
Blood creatine phosphokinase increased 165.75 47.85 47 874 12966 3371972
Blood prolactin increased 158.49 47.85 30 891 1378 3383560
Sedation 149.30 47.85 37 884 6064 3378874
Overdose 147.04 47.85 54 867 33924 3351014
Extrapyramidal disorder 145.36 47.85 33 888 3710 3381228
White blood cell count increased 144.15 47.85 42 879 12718 3372220
Psychotic disorder 136.12 47.85 37 884 8697 3376241
Drug interaction 126.83 47.85 53 868 46759 3338179
Tachycardia 115.31 47.85 41 880 23330 3361608
Intentional self-injury 114.56 47.85 29 892 5156 3379782
Antipsychotic drug level decreased 102.49 47.85 15 906 133 3384805
Depressed level of consciousness 100.19 47.85 31 890 11434 3373504
Toxicity to various agents 100.19 47.85 45 876 47009 3337929
Weight increased 99.01 47.85 38 883 26702 3358236
Drug abuse 97.35 47.85 34 887 18296 3366642
Hyperprolactinaemia 95.67 47.85 18 903 795 3384143
Agitation 94.95 47.85 34 887 19672 3365266
Neutropenia 94.22 47.85 39 882 33347 3351591
Hallucination, auditory 93.56 47.85 23 898 3618 3381320
Tardive dyskinesia 91.26 47.85 21 900 2490 3382448
Neutrophil count decreased 90.67 47.85 28 893 10245 3374693
Intentional overdose 87.61 47.85 30 891 15195 3369743
Neutrophil count increased 86.67 47.85 22 899 3938 3381000
Aggression 83.72 47.85 27 894 11358 3373580
Sopor 82.81 47.85 21 900 3743 3381195
Salivary hypersecretion 82.80 47.85 19 902 2223 3382715
Delusion 79.08 47.85 20 901 3525 3381413

Pharmacologic Action:

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SourceCodeDescription
ATC N05AL05 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Benzamides
CHEBI has role CHEBI:65191 second generation antipsychotic

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Chronic schizophrenia indication 83746006
Dysthymia off-label use 78667006 DOID:12139

Acid dissociation constants calculated using MoKa v3.0.0

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

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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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 8.49 WOMBAT-PK SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 2B GPCR Ki 7.89 PDSP
Alpha-2A adrenergic receptor GPCR Ki 5.95 PDSP
5-hydroxytryptamine receptor 1D GPCR Ki 5.87 PDSP
Alpha-2C adrenergic receptor GPCR Ki 5.81 PDSP
5-hydroxytryptamine receptor 1B GPCR Ki 5.76 PDSP
D(4) dopamine receptor GPCR Ki 5.63 PDSP
5-hydroxytryptamine receptor 6 GPCR Ki 5.38 PDSP
5-hydroxytryptamine receptor 2A GPCR Ki 5.08 PDSP
5-hydroxytryptamine receptor 7 GPCR Ki 7.94 PDSP
D(3) dopamine receptor GPCR ANTAGONIST Ki 7.40 IUPHAR

External reference:

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IDSource
963 IUPHAR_LIGAND_ID
C0103045 UMLSCUI
D07310 KEGG_DRUG
8110R61I4U UNII
4960 INN_ID
391761004 SNOMEDCT_US
005229 NDDF
46303 RXNORM
321636003 SNOMEDCT_US
CHEMBL243712 ChEMBL_ID
2159 PUBCHEM_CID
DB06288 DRUGBANK_ID
CHEBI:64045 CHEBI

Pharmaceutical products:

None