paliperidone indications/contra

Stem definitionDrug idCAS RN
antipsychotics, risperidone derivatives 4137 144598-75-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • RO76477
  • RO 76477
  • paliperidone
  • invega
  • xeplion
  • Molecular weight: 426.49
  • Formula: C23H27FN4O3
  • CLOGP: 1.07
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 1
  • TPSA: 82.17
  • ALOGS: -3.16
  • ROTB: 4

Drug dosage:

DoseUnitRoute
6 mg O
2.50 mg P

Approvals:

DateAgencyCompanyOrphan
June 25, 2007 EMA
Dec. 19, 2006 FDA JANSSEN PHARMS

FDA Adverse Event Reporting System

scroll-->
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
Galactorrhoea 1171.37 36.71 212 5744 997 3378906
Blood prolactin increased 993.50 36.71 189 5767 1219 3378684
Extrapyramidal disorder 959.55 36.71 217 5739 3526 3376377
Psychotic disorder 874.32 36.71 238 5718 8496 3371407
Schizophrenia 624.22 36.71 144 5812 2550 3377353
Akathisia 593.88 36.71 138 5818 2525 3377378
Weight increased 517.96 36.71 211 5745 26529 3353374
Dystonia 511.75 36.71 131 5825 3636 3376267
Treatment noncompliance 486.37 36.71 152 5804 8793 3371110
Hospitalisation 475.87 36.71 185 5771 20540 3359363
Hyperprolactinaemia 442.93 36.71 88 5868 725 3379178
Neuroleptic malignant syndrome 438.64 36.71 120 5836 4321 3375582
Intentional self-injury 438.32 36.71 124 5832 5061 3374842
Drug ineffective 388.58 36.71 285 5671 115805 3264098
Suicide attempt 376.00 36.71 145 5811 15702 3364201
Intentional overdose 363.65 36.71 140 5816 15085 3364818
Aggression 338.64 36.71 123 5833 11262 3368641
Amenorrhoea 334.09 36.71 88 5868 2729 3377174
Sedation 320.16 36.71 101 5855 6000 3373903
Inappropriate schedule of drug administration 319.56 36.71 124 5832 13629 3366274
Off label use 304.64 36.71 184 5772 53793 3326110
Completed suicide 279.18 36.71 144 5812 30970 3348933
Tachycardia 262.35 36.71 126 5830 23245 3356658
Hallucination, auditory 253.74 36.71 75 5881 3566 3376337
Agitation 251.17 36.71 116 5840 19590 3360313
Tardive dyskinesia 239.15 36.71 66 5890 2445 3377458
Suicidal ideation 231.15 36.71 106 5850 17599 3362304
Delusion 229.55 36.71 69 5887 3476 3376427
Catatonia 226.19 36.71 56 5900 1344 3378559
Dyskinesia 217.51 36.71 79 5877 7206 3372697

Pharmacologic Action:

scroll-->
SourceCodeDescription
ATC N05AX13 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Other antipsychotics
FDA EPC N0000175430 Atypical Antipsychotic
CHEBI has role CHEBI:48561 dopaminergic antagonist
CHEBI has role CHEBI:48279 serotonergic antagonist
CHEBI has role CHEBI:37890 alpha-adrenergic antagonist
CHEBI has role CHEBI:37955 H1-receptor antagonist
CHEBI has role CHEBI:35471 psychotropic drug
CHEBI has role CHEBI:65191 second generation antipsychotic
CHEBI has role CHEBI:63726 neuroprotective agent

Drug Use (View source of the data)

scroll-->
DiseaseRelationSNOMED_IDDOID
Schizophrenia indication 58214004
Schizoaffective disorder indication 68890003 DOID:5418
Psychotic disorder indication 69322001
Priapism contraindication 6273006 DOID:9286
Suicidal thoughts contraindication 6471006
Weight gain finding contraindication 8943002
Neuroleptic malignant syndrome contraindication 15244003 DOID:14464
Senile dementia contraindication 15662003
Agranulocytosis contraindication 17182001 DOID:12987
Lowered convulsive threshold contraindication 19260006
Myocardial infarction contraindication 22298006 DOID:5844
Stenosis of intestine contraindication 23065003
Short bowel syndrome contraindication 26629001 DOID:10605
Hypovolemia contraindication 28560003
Orthostatic hypotension contraindication 28651003
Torsades de pointes contraindication 31722008
Parkinsonism contraindication 32798002 DOID:13548
Crohn's disease contraindication 34000006
Dehydration contraindication 34095006
Hypokalemia contraindication 43339004
Conduction disorder of the heart contraindication 44808001
Low blood pressure contraindication 45007003
Chronic heart failure contraindication 48447003
Hyperlipidemia contraindication 55822004 DOID:1168
Cerebrovascular disease contraindication 62914000 DOID:6713
Substance abuse contraindication 66214007
Diabetes mellitus contraindication 73211009 DOID:9351
Extrapyramidal disease contraindication 76349003
Diffuse Lewy body disease contraindication 80098002 DOID:12217
Hyperglycemia contraindication 80394007 DOID:4195
Leukopenia contraindication 84828003 DOID:615
Tardive dyskinesia contraindication 102449007
Increased intestinal motility contraindication 102624003
Prolonged QT interval contraindication 111975006
Seizure disorder contraindication 128613002 DOID:1826
Hypomagnesemia contraindication 190855004
Angina pectoris contraindication 194828000
Impaired renal function disorder contraindication 197663003
Metabolic syndrome X contraindication 237602007 DOID:14221
Hyperprolactinemia contraindication 237662005 DOID:12700
Esophageal dysmotility contraindication 266434009 DOID:9192
Neutropenic disorder contraindication 303011007 DOID:1227
At risk for aspiration contraindication 371736008
Impaired cognition contraindication 386806002
Breastfeeding (mother) contraindication 413712001
Obesity contraindication 414916001 DOID:9970
Gastrointestinal hypomotility contraindication 421807004
Acquired torsion dystonia contraindication 433493000
Congenital long QT syndrome contraindication 442917000
Carcinoma of female breast contraindication 447782002
Intestinal Cystic Fibrosis contraindication
Esophageal Compression contraindication
Mixed bipolar I disorder off-label use 16506000 DOID:3312
Bipolar disorder in remission off-label use 85248005
Bipolar affective disorder, current episode manic off-label use 191618007
Bipolar affective disorder, current episode depression off-label use 191627008 DOID:3312
Infantile autism off-label use 408857007 DOID:12849
Depression Treatment Adjunct off-label use

Acid dissociation constants calculated using MoKa v3.0.0

scroll-->
Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.78 Basic
pKa2 2.73 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

scroll-->
TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
5-hydroxytryptamine receptor 2A GPCR ANTAGONIST Ki 8.96 PDSP DRUG LABEL
D(2) dopamine receptor GPCR ANTAGONIST Ki 8.47 PDSP DRUG LABEL
Histamine H1 receptor GPCR Ki 8.25 PDSP
5-hydroxytryptamine receptor 7 GPCR Ki 8.57 PDSP
Sodium-dependent serotonin transporter Transporter Ki 5.43 PDSP
Histamine H4 receptor GPCR Ki 5.06 PDSP
5-hydroxytryptamine receptor 6 GPCR Ki 5.62 PDSP
5-hydroxytryptamine receptor 5A GPCR Ki 6.56 PDSP
Prostaglandin E2 receptor EP3 subtype GPCR Ki 5 PDSP
5-hydroxytryptamine receptor 2B GPCR Ki 7.21 PDSP
5-hydroxytryptamine receptor 1E GPCR Ki 5.99 PDSP
5-hydroxytryptamine receptor 2C GPCR Ki 7.32 PDSP
5-hydroxytryptamine receptor 1B GPCR Ki 7.64 PDSP
5-hydroxytryptamine receptor 1D GPCR Ki 7.72 PDSP
Histamine H2 receptor GPCR Ki 6.92 PDSP
D(1B) dopamine receptor GPCR Ki 7.54 PDSP
D(4) dopamine receptor GPCR Ki 7.27 PDSP
D(1A) dopamine receptor GPCR Ki 7.39 PDSP
Alpha-2C adrenergic receptor GPCR Ki 8.20 PDSP
Alpha-2B adrenergic receptor GPCR Ki 7.64 PDSP
Alpha-2A adrenergic receptor GPCR Ki 7.93 PDSP
5-hydroxytryptamine receptor 1A GPCR Ki 6.22 PDSP
Alpha-1A adrenergic receptor GPCR Ki 8.55 WOMBAT-PK
Beta-2 adrenergic receptor GPCR Ki 5.30 PDSP
Beta-1 adrenergic receptor GPCR Ki 5.30 PDSP
D(3) dopamine receptor GPCR Ki 9.05 PDSP
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 5.89 CHEMBL
Alpha-1B adrenergic receptor GPCR Ki 9.15 PDSP

External reference:

scroll-->
IDSource
4025875 VUID
N0000176080 NUI
C0753678 UMLSCUI
7258 IUPHAR_LIGAND_ID
D05339 KEGG_DRUG
117004004 SNOMEDCT_US
679314 RXNORM
23004 MMSL
d06297 MMSL
4025875 VANDF
425483000 SNOMEDCT_US
426276000 SNOMEDCT_US
N0000176080 NDFRT
011888 NDDF
838F01T721 UNII
7977 INN_ID
CHEMBL1621 ChEMBL_ID
DB01267 DRUGBANK_ID
115237 PUBCHEM_CID
CHEBI:82978 CHEBI

Pharmaceutical products:

scroll-->
ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0378-3978 TABLET, FILM COATED, EXTENDED RELEASE 1.50 mg ORAL ANDA 19 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0378-3979 TABLET, FILM COATED, EXTENDED RELEASE 3 mg ORAL ANDA 19 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0378-3980 TABLET, FILM COATED, EXTENDED RELEASE 6 mg ORAL ANDA 19 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0378-3981 TABLET, FILM COATED, EXTENDED RELEASE 9 mg ORAL ANDA 19 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0591-3692 TABLET, FILM COATED, EXTENDED RELEASE 1.50 mg ORAL ANDA 19 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0591-3693 TABLET, FILM COATED, EXTENDED RELEASE 3 mg ORAL ANDA 19 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0591-3694 TABLET, FILM COATED, EXTENDED RELEASE 6 mg ORAL ANDA 19 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 0591-3695 TABLET, FILM COATED, EXTENDED RELEASE 9 mg ORAL ANDA 19 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 10147-0951 TABLET, EXTENDED RELEASE 1.50 mg ORAL NDA 20 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 10147-0952 TABLET, EXTENDED RELEASE 3 mg ORAL NDA 20 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 10147-0953 TABLET, EXTENDED RELEASE 6 mg ORAL NDA 20 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 10147-0954 TABLET, EXTENDED RELEASE 9 mg ORAL NDA 20 sections
INVEGA HUMAN PRESCRIPTION DRUG LABEL 1 21695-455 TABLET, EXTENDED RELEASE 6 mg ORAL NDA 20 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 42292-026 TABLET, FILM COATED, EXTENDED RELEASE 3 mg ORAL ANDA 19 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 42292-027 TABLET, FILM COATED, EXTENDED RELEASE 6 mg ORAL ANDA 19 sections
INVEGA HUMAN PRESCRIPTION DRUG LABEL 1 50458-550 TABLET, EXTENDED RELEASE 3 mg ORAL NDA 20 sections
INVEGA HUMAN PRESCRIPTION DRUG LABEL 1 50458-551 TABLET, EXTENDED RELEASE 6 mg ORAL NDA 20 sections
INVEGA HUMAN PRESCRIPTION DRUG LABEL 1 50458-552 TABLET, EXTENDED RELEASE 9 mg ORAL NDA 20 sections
INVEGA HUMAN PRESCRIPTION DRUG LABEL 1 50458-554 TABLET, EXTENDED RELEASE 1.50 mg ORAL NDA 20 sections
INVEGA HUMAN PRESCRIPTION DRUG LABEL 1 64725-0550 TABLET, EXTENDED RELEASE 3 mg ORAL NDA 18 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 68151-5041 TABLET, FILM COATED, EXTENDED RELEASE 6 mg ORAL ANDA 18 sections
INVEGA HUMAN PRESCRIPTION DRUG LABEL 1 69189-0551 TABLET, EXTENDED RELEASE 6 mg ORAL NDA 18 sections
INVEGA HUMAN PRESCRIPTION DRUG LABEL 1 69189-0554 TABLET, EXTENDED RELEASE 1.50 mg ORAL NDA 20 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 69189-0951 TABLET, EXTENDED RELEASE 1.50 mg ORAL NDA 19 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 69189-0952 TABLET, EXTENDED RELEASE 3 mg ORAL NDA 19 sections
Paliperidone HUMAN PRESCRIPTION DRUG LABEL 1 70518-0850 TABLET, EXTENDED RELEASE 9 mg ORAL NDA 20 sections