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

Stem definitionDrug idCAS RN
623 113-59-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • chlorprothixene
  • chlorprothixen
  • chlorprotixen
  • chlorprotixene
  • chlothixen
  • chorprothixene
  • chlorprothixene hydrochloride
  • chlorprothixene HCl
  • taractan
A thioxanthine with effects similar to the phenothiazine antipsychotics.
  • Molecular weight: 315.86
  • Formula: C18H18ClNS
  • CLOGP: 5.48
  • LIPINSKI: 1
  • HAC: 1
  • HDO: 0
  • TPSA: 3.24
  • ALOGS: -5.94
  • ROTB: 3
  • Status: OFM
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.30 g O
50 mg P

ADMET properties:

PropertyValueReference
BA (Bioavailability) 41 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 13.70 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 11.50 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 25.80 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
June 19, 1967 FDA ROCHE

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
Neuroleptic malignant syndrome 79.77 41.13 24 1453 11106 50592541
Intentional self-injury 73.53 41.13 27 1450 23085 50580562
Drug interaction 70.61 41.13 53 1424 199568 50404079
Extrapyramidal disorder 70.01 41.13 22 1455 11748 50591899
Serotonin syndrome 61.02 41.13 24 1453 24689 50578958
Intentional overdose 47.80 41.13 27 1450 62477 50541170
Rhabdomyolysis 47.42 41.13 23 1454 39004 50564643
Depressed level of consciousness 43.97 41.13 24 1453 51929 50551718

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
Neuroleptic malignant syndrome 63.79 38.32 22 822 16126 29557557
Toxicity to various agents 40.92 38.32 36 808 173625 29400058
Tardive dyskinesia 40.81 38.32 12 832 5246 29568437

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
Neuroleptic malignant syndrome 137.08 34.43 46 2237 24950 64471499
Extrapyramidal disorder 76.46 34.43 28 2255 19524 64476925
Drug interaction 69.40 34.43 74 2209 362009 64134440
Serotonin syndrome 60.65 34.43 29 2254 39253 64457196
Toxicity to various agents 58.75 34.43 68 2215 363445 64133004
Muscle rigidity 57.29 34.43 22 2261 17451 64478998
Restlessness 57.28 34.43 28 2255 39757 64456692
Intentional overdose 42.91 34.43 31 2252 89913 64406536
Rhabdomyolysis 42.36 34.43 31 2252 91695 64404754
Myoglobin blood increased 36.45 34.43 10 2273 2737 64493712
Intentional self-injury 34.62 34.43 18 2265 29026 64467423

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05AF03 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Thioxanthene derivatives
CHEBI has role CHEBI:35717 hypnotics
CHEBI has role CHEBI:48561 dopaminergic antagonists
CHEBI has role CHEBI:48873 acetylcholine receptor antagonist
CHEBI has role CHEBI:50919 antiemetico
CHEBI has role CHEBI:65190 typical antipsychotic drugs
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
CHEBI has role CHEBI:176497 geroprotectors

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Schizophrenia indication 58214004 DOID:5419
Neuroleptic malignant syndrome contraindication 15244003 DOID:14464
Senile dementia contraindication 15662003
Agranulocytosis contraindication 17182001 DOID:12987
Shock contraindication 27942005
Parkinsonism contraindication 32798002
Disorder of cardiovascular system contraindication 49601007 DOID:1287
Epilepsy contraindication 84757009 DOID:1826
Leukopenia contraindication 84828003 DOID:615
Stupor contraindication 89458003
Tardive dyskinesia contraindication 102449007
Disease of blood AND/OR blood-forming organ contraindication 191124002 DOID:74
Alcohol withdrawal syndrome contraindication 191480000
Benign prostatic hyperplasia contraindication 266569009
Retention of urine contraindication 267064002
Neutropenic disorder contraindication 303011007 DOID:1227
Coma contraindication 371632003
Angle-closure glaucoma contraindication 392291006 DOID:13550
Breastfeeding (mother) contraindication 413712001
Carcinoma of female breast contraindication 447782002
Drug Induced CNS Depression contraindication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.66 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
D(2) dopamine receptor GPCR ANTAGONIST Ki 8.53 CHEMBL CHEMBL
5-hydroxytryptamine receptor 2A GPCR Ki 9.37 PDSP
5-hydroxytryptamine receptor 6 GPCR Ki 8.52 CHEMBL
D(3) dopamine receptor GPCR ANTAGONIST Ki 8.34 CHEMBL
D(1B) dopamine receptor GPCR Ki 8.05 CHEMBL
Histamine H1 receptor GPCR Ki 8.43 CHEMBL
Muscarinic acetylcholine receptor M1 GPCR Ki 7.96 PDSP
Muscarinic acetylcholine receptor M2 GPCR Ki 7.55 PDSP
Muscarinic acetylcholine receptor M3 GPCR Ki 7.66 PDSP
Muscarinic acetylcholine receptor M4 GPCR Ki 7.75 PDSP
Muscarinic acetylcholine receptor M5 GPCR Ki 7.60 PDSP
D(4) dopamine receptor GPCR Ki 9.19 PDSP
Solute carrier family 22 member 1 Transporter IC50 4.11 CHEMBL
D(1A) dopamine receptor GPCR Ki 7.74 CHEMBL
5-hydroxytryptamine receptor 7 GPCR Ki 8.25 CHEMBL
Histamine H1 receptor GPCR IC50 8.97 CHEMBL
Pleiotropic ABC efflux transporter of multiple drugs Transporter IC50 5.29 CHEMBL

External reference:

IDSource
4017788 VUID
N0000146149 NUI
D00790 KEGG_DRUG
2406 RXNORM
4017788 VANDF
C0008290 UMLSCUI
CHEBI:3651 CHEBI
CHEMBL908 ChEMBL_ID
DB01239 DRUGBANK_ID
D002749 MESH_DESCRIPTOR_UI
667467 PUBCHEM_CID
11976 IUPHAR_LIGAND_ID
886 INN_ID
6469-93-8 SECONDARY_CAS_RN
9S7OD60EWP UNII
001516 NDDF
005139 NDDF
387317000 SNOMEDCT_US
57002000 SNOMEDCT_US
88585004 SNOMEDCT_US
CHEMBL1256658 ChEMBL_ID

Pharmaceutical products:

None