risperidone indications/contra

Stem definitionDrug idCAS RN
antipsychotics, risperidone derivatives 2389 106266-06-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • risperidone
  • ripedon
  • rispadal
  • risperdal
  • risperidal
  • R 64,766
A selective blocker of DOPAMINE D2 RECEPTORS and SEROTONIN 5-HT2 RECEPTORS that acts as an atypical antipsychotic agent. It has been shown to improve both positive and negative symptoms in the treatment of SCHIZOPHRENIA.
  • Molecular weight: 410.49
  • Formula: C23H27FN4O2
  • CLOGP: 2.71
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 0
  • TPSA: 61.94
  • ALOGS: -3.38
  • ROTB: 4

Drug dosage:

DoseUnitRoute
5 mg O
2.70 mg P

Approvals:

DateAgencyCompanyOrphan
Dec. 29, 1993 FDA JANSSEN PHARMS

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
Neuroleptic malignant syndrome 3237.68 33.27 746 18022 3695 3363396
Extrapyramidal disorder 3161.17 33.27 709 18059 3034 3364057
Somnolence 2160.85 33.27 856 17912 31348 3335743
Intentional overdose 2155.21 33.27 704 18064 14521 3352570
Suicide attempt 2111.43 33.27 700 18068 15147 3351944
Drug interaction 1927.96 33.27 880 17888 45932 3321159
Intentional self-injury 1795.66 33.27 480 18288 4705 3362386
Weight increased 1708.59 33.27 687 18081 26053 3341038
Hyperprolactinaemia 1662.93 33.27 321 18447 492 3366599
Psychotic disorder 1637.37 33.27 501 18267 8233 3358858
Blood prolactin increased 1583.41 33.27 338 18430 1070 3366021
Treatment noncompliance 1470.01 33.27 464 18304 8481 3358610
Sedation 1293.32 33.27 385 18383 5716 3361375
Aggression 1274.29 33.27 442 18326 10943 3356148
Tardive dyskinesia 1266.98 33.27 314 18454 2197 3364894
Dystonia 1224.52 33.27 332 18436 3435 3363656
Completed suicide 1224.04 33.27 568 18200 30546 3336545
Parkinsonism 1197.88 33.27 297 18471 2081 3365010
Agitation 1149.46 33.27 475 18293 19231 3347860
Tachycardia 1142.91 33.27 497 18271 22874 3344217
Galactorrhoea 1072.76 33.27 239 18529 970 3366121
Akathisia 1061.92 33.27 276 18492 2387 3364704
Overdose 1050.41 33.27 526 18242 33452 3333639
Catatonia 1032.52 33.27 238 18530 1162 3365929
Dyskinesia 1024.54 33.27 336 18432 6949 3360142
Drug ineffective 963.65 33.27 780 17988 115310 3251781
Muscle rigidity 941.93 33.27 258 18510 2776 3364315
Off label use 893.62 33.27 554 18214 53423 3313668
Tremor 887.79 33.27 442 18326 27702 3339389
Schizophrenia 859.08 33.27 234 18534 2460 3364631

Pharmacologic Action:

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SourceCodeDescription
ATC N05AX08 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Other antipsychotics
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 D018490 Serotonin Agents
MeSH PA D012702 Serotonin Antagonists
MeSH PA D014149 Tranquilizing Agents
CHEBI has role CHEBI:48561 dopaminergic antagonist
CHEBI has role CHEBI:35471 psychotropic drug
CHEBI has role CHEBI:65191 second generation antipsychotic
CHEBI has role CHEBI:48279 serotonergic antagonist
CHEBI has role CHEBI:37890 alpha-adrenergic antagonist
CHEBI has role CHEBI:37955 H1-receptor antagonist
FDA EPC N0000175430 Atypical Antipsychotic

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Mixed bipolar I disorder indication 16506000 DOID:3312
Schizophrenia indication 58214004
Bipolar disorder in remission indication 85248005
Bipolar affective disorder, current episode manic indication 191618007
Infantile autism indication 408857007 DOID:12849
Priapism contraindication 6273006 DOID:9286
Suicidal thoughts contraindication 6471006
Asthenia contraindication 13791008
Neuroleptic malignant syndrome contraindication 15244003 DOID:14464
Senile dementia contraindication 15662003
Agranulocytosis contraindication 17182001 DOID:12987
Myocardial infarction contraindication 22298006 DOID:5844
Hypovolemia contraindication 28560003
Orthostatic hypotension contraindication 28651003
Parkinsonism contraindication 32798002 DOID:13548
Dehydration contraindication 34095006
Dysphagia contraindication 40739000
Conduction disorder of the heart contraindication 44808001
Low blood pressure contraindication 45007003
Chronic heart failure contraindication 48447003
Disorder of cardiovascular system contraindication 49601007 DOID:1287
Hyperlipidemia contraindication 55822004 DOID:1168
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Cerebrovascular disease contraindication 62914000 DOID:6713
Substance abuse contraindication 66214007
Diabetes mellitus contraindication 73211009 DOID:9351
Diffuse Lewy body disease contraindication 80098002 DOID:12217
Hyperglycemia contraindication 80394007 DOID:4195
Leukopenia contraindication 84828003 DOID:615
Tardive dyskinesia contraindication 102449007
Seizure disorder contraindication 128613002 DOID:1826
Cerebrovascular accident contraindication 230690007 DOID:6713
Disease of liver contraindication 235856003 DOID:409
Metabolic syndrome X contraindication 237602007 DOID:14221
Hyperprolactinemia contraindication 237662005 DOID:12700
Retention of urine contraindication 267064002
Neutropenic disorder contraindication 303011007 DOID:1227
At risk for aspiration contraindication 371736008
Fever contraindication 386661006
Hypothermia contraindication 386689009
Impaired cognition contraindication 386806002
Breastfeeding (mother) contraindication 413712001
Myocardial ischemia contraindication 414795007 DOID:3393
Obesity contraindication 414916001 DOID:9970
Carcinoma of female breast contraindication 447782002
Smokes tobacco daily contraindication 449868002
Predisposed to Torsades de Pointes Cardiac Arrhythmias contraindication
Bipolar affective disorder, current episode depression off-label use 191627008 DOID:3312
Toxoplasmosis associated with acquired immunodeficiency syndrome off-label use 421666009
Depression Treatment Adjunct off-label use

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.78 Basic
pKa2 3.45 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 8.49 WOMBAT-PK CHEMBL
5-hydroxytryptamine receptor 2A GPCR ANTAGONIST Ki 9.36 WOMBAT-PK CHEMBL
D(3) dopamine receptor GPCR ANTAGONIST Ki 8.07 WOMBAT-PK
Histamine H2 receptor GPCR Ki 6.92 PDSP
D(1B) dopamine receptor GPCR Ki 7.02 PDSP
Muscarinic acetylcholine receptor M3 GPCR Ki 5 PDSP
Muscarinic acetylcholine receptor M4 GPCR Ki 5.54 PDSP
Muscarinic acetylcholine receptor M2 GPCR Ki 5.43 PDSP
Alpha-1D adrenergic receptor GPCR ANTAGONIST Ki 7.40 IUPHAR
5-hydroxytryptamine receptor 1F GPCR ANTAGONIST Ki 5.90 IUPHAR
5-hydroxytryptamine receptor 1E GPCR ANTAGONIST Ki 5.90 IUPHAR
Cytochrome P450 2D6 Enzyme IC50 5.28 DRUG MATRIX
5-hydroxytryptamine receptor 2C GPCR ANTAGONIST Ki 7.70 WOMBAT-PK
5-hydroxytryptamine receptor 5A GPCR Ki 6.69 WOMBAT-PK
Alpha-1B adrenergic receptor GPCR Ki 8.48 WOMBAT-PK
Alpha-2C adrenergic receptor GPCR Ki 8.49 WOMBAT-PK
5-hydroxytryptamine receptor 1D GPCR ANTAGONIST Ki 7.60 WOMBAT-PK
5-hydroxytryptamine receptor 1B GPCR ANTAGONIST Ki 7.49 WOMBAT-PK
Histamine H1 receptor GPCR Ki 7.48 WOMBAT-PK
Alpha-2B adrenergic receptor GPCR Ki 7.77 WOMBAT-PK
Alpha-1A adrenergic receptor GPCR Ki 8.55 WOMBAT-PK
5-hydroxytryptamine receptor 7 GPCR Ki 8.47 WOMBAT-PK
5-hydroxytryptamine receptor 2B GPCR Ki 7.42 WOMBAT-PK
5-hydroxytryptamine receptor 1A GPCR Ki 6.44 WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 6.79 WOMBAT-PK
Alpha-2A adrenergic receptor GPCR Ki 8 WOMBAT-PK
Beta-2 adrenergic receptor GPCR Ki 5.30 PDSP
Beta-1 adrenergic receptor GPCR Ki 5.30 PDSP
Solute carrier family 22 member 2 Transporter IC50 4.96 CHEMBL
Muscarinic acetylcholine receptor M1 GPCR Ki 5.55 CHEMBL
D(1A) dopamine receptor GPCR Ki 7.68 CHEMBL
Sodium-dependent serotonin transporter Transporter Ki 5.85 CHEMBL
Sigma non-opioid intracellular receptor 1 Membrane receptor Ki 5.37 CHEMBL
Multidrug and toxin extrusion protein 1 Transporter IC50 5.80 CHEMBL
5-hydroxytryptamine receptor 6 GPCR Ki 6.65 CHEMBL
Glycine receptor subunit alpha-1 Ion channel EC50 6.49 CHEMBL
D(4) dopamine receptor GPCR ANTAGONIST Ki 8 WOMBAT-PK
Alpha-1B adrenergic receptor GPCR Ki 8.97 DRUG MATRIX
Transporter Transporter Ki 4.55 CHEMBL
Histamine H1 receptor GPCR Ki 7.66 CHEMBL
5-hydroxytryptamine receptor 7 GPCR Ki 8.85 CHEMBL
D(2) dopamine receptor GPCR IC50 7.64 CHEMBL
D(3) dopamine receptor GPCR Ki 8.01 CHEMBL
Serotonin 2 (5-HT2) receptor GPCR Ki 9.85 CHEMBL
D(1A) dopamine receptor GPCR Ki 7.66 CHEMBL
Alpha-2A adrenergic receptor GPCR Ki 7.60 CHEMBL
Histamine H1 receptor GPCR IC50 7.10 CHEMBL
5-hydroxytryptamine receptor 2C GPCR Ki 7.84 CHEMBL
5-hydroxytryptamine receptor 1A GPCR IC50 6.37 CHEMBL
5-hydroxytryptamine receptor 2A GPCR Ki 9.82 CHEMBL
Beta-1 adrenergic receptor GPCR Ki 4.66 CHEMBL
Alpha-1A adrenergic receptor GPCR Ki 7.89 CHEMBL
Serotonin 1 (5-HT1) receptor GPCR Ki 6.47 CHEMBL
5-hydroxytryptamine receptor 1A GPCR Ki 6.89 CHEMBL
Serotonin 2 (5-HT2) receptor GPCR IC50 8.82 CHEMBL
D(2) dopamine receptor GPCR Ki 8.74 CHEMBL
5-hydroxytryptamine receptor 6 GPCR ANTAGONIST Ki 6.40 IUPHAR

External reference:

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IDSource
96 IUPHAR_LIGAND_ID
4020840 VUID
N0000148350 NUI
C0073393 UMLSCUI
D00426 KEGG_DRUG
CHEMBL85 ChEMBL_ID
DB00734 DRUGBANK_ID
4020840 VANDF
N0000005949 NDFRT
N0000148350 NDFRT
004392 NDDF
35636 RXNORM
146973 MMSL
d03180 MMSL
108386000 SNOMEDCT_US
386840002 SNOMEDCT_US
5429 MMSL
5073 PUBCHEM_CID
L6UH7ZF8HC UNII
6085 INN_ID
D018967 MESH_DESCRIPTOR_UI
CHEBI:8871 CHEBI
8NU PDB_CHEM_ID

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 0054-0063 SOLUTION 1 mg ORAL ANDA 20 sections
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 0378-3502 TABLET, FILM COATED 0.25 mg ORAL ANDA 19 sections
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 0378-3505 TABLET, FILM COATED 0.50 mg ORAL ANDA 19 sections
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 0378-3511 TABLET, FILM COATED 1 mg ORAL ANDA 19 sections
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 0378-3512 TABLET, FILM COATED 2 mg ORAL ANDA 19 sections
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 0378-3513 TABLET, FILM COATED 3 mg ORAL ANDA 19 sections
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 0378-3514 TABLET, FILM COATED 4 mg ORAL ANDA 19 sections
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 0603-9424 SOLUTION 1 mg ORAL ANDA 20 sections
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 0615-7505 TABLET, FILM COATED 0.25 mg ORAL ANDA 18 sections
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 0615-7506 TABLET, FILM COATED 0.50 mg ORAL ANDA 18 sections
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 0615-7507 TABLET, FILM COATED 1 mg ORAL ANDA 18 sections
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 0781-5310 TABLET, ORALLY DISINTEGRATING 0.50 mg ORAL ANDA 19 sections
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 0781-5311 TABLET, ORALLY DISINTEGRATING 1 mg ORAL ANDA 19 sections
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 0781-5312 TABLET, ORALLY DISINTEGRATING 2 mg ORAL ANDA 19 sections
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 0781-5313 TABLET, ORALLY DISINTEGRATING 3 mg ORAL ANDA 19 sections
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 0781-5314 TABLET, ORALLY DISINTEGRATING 4 mg ORAL ANDA 19 sections
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 0904-6357 TABLET 0.25 mg ORAL ANDA 20 sections
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 0904-6358 TABLET 0.50 mg ORAL ANDA 20 sections
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 0904-6359 TABLET 1 mg ORAL ANDA 20 sections
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 0904-6360 TABLET 2 mg ORAL ANDA 20 sections
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 0904-6361 TABLET 3 mg ORAL ANDA 20 sections
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 0904-6362 TABLET 4 mg ORAL ANDA 20 sections
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 13107-119 TABLET, FILM COATED 0.25 mg ORAL ANDA 20 sections
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 13107-120 TABLET, FILM COATED 0.50 mg ORAL ANDA 20 sections
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 13107-121 TABLET, FILM COATED 1 mg ORAL ANDA 20 sections
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 13107-122 TABLET, FILM COATED 2 mg ORAL ANDA 20 sections
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 13107-123 TABLET, FILM COATED 3 mg ORAL ANDA 20 sections
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 13107-124 TABLET, FILM COATED 4 mg ORAL ANDA 20 sections
Risperidone HUMAN PRESCRIPTION DRUG LABEL 1 13668-040 TABLET 4 mg ORAL ANDA 20 sections
RISPERIDONE HUMAN PRESCRIPTION DRUG LABEL 1 16590-641 TABLET 2 mg ORAL ANDA 19 sections