thiothixene Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
2639 3313-26-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • thiothixene
  • tiotixene
  • cis-Thiothixene
  • thiothixene hydrochloride
  • thiothixene HCl
A thioxanthine used as an antipsychotic agent. Its effects are similar to the phenothiazine antipsychotics.
  • Molecular weight: 443.62
  • Formula: C23H29N3O2S2
  • CLOGP: 3.23
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 0
  • TPSA: 43.86
  • ALOGS: -4.50
  • ROTB: 4

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
30 mg O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
July 24, 1967 FDA PFIZER

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05AF04 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Thioxanthene derivatives
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:149553 anti-coronaviral agents
FDA EPC N0000180182 Typical Antipsychotic

Drug Use (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

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.72 Basic
pKa2 4.65 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 9.35 PDSP CHEMBL
5-hydroxytryptamine receptor 6 GPCR Ki 6.68 PDSP
5-hydroxytryptamine receptor 5A GPCR Ki 6.44 PDSP
5-hydroxytryptamine receptor 3A Ion channel Ki 5.73 PDSP
D(3) dopamine receptor GPCR Ki 9.41 PDSP
Alpha-1B adrenergic receptor GPCR Ki 7.46 PDSP
5-hydroxytryptamine receptor 7 GPCR Ki 7.82 PDSP
Sodium-dependent serotonin transporter Transporter Ki 5.41 PDSP
5-hydroxytryptamine receptor 2C GPCR Ki 5.87 PDSP
5-hydroxytryptamine receptor 1B GPCR Ki 6.82 PDSP
5-hydroxytryptamine receptor 1D GPCR Ki 6.18 PDSP
Histamine H2 receptor GPCR Ki 6.39 PDSP
D(1B) dopamine receptor GPCR Ki 6.58 PDSP
D(4) dopamine receptor GPCR Ki 6.69 PDSP
D(1A) dopamine receptor GPCR Ki 7.29 PDSP
Muscarinic acetylcholine receptor M3 GPCR Ki 5.40 PDSP
Alpha-2C adrenergic receptor GPCR Ki 7.28 PDSP
Alpha-2B adrenergic receptor GPCR Ki 7.30 PDSP
Muscarinic acetylcholine receptor M1 GPCR Ki 5.59 PDSP
Alpha-2A adrenergic receptor GPCR Ki 7.10 PDSP
Muscarinic acetylcholine receptor M5 GPCR Ki 5.32 PDSP
5-hydroxytryptamine receptor 1A GPCR Ki 6.39 PDSP
Muscarinic acetylcholine receptor M4 GPCR Ki 5.81 PDSP
Muscarinic acetylcholine receptor M2 GPCR Ki 5.68 PDSP
Histamine H1 receptor GPCR ANTAGONIST Ki 8.40 IUPHAR
Alpha-1A adrenergic receptor GPCR Ki 7.94 PDSP
5-hydroxytryptamine receptor 2A GPCR ANTAGONIST Ki 7.30 IUPHAR

External reference:

IDSource
4019947 VUID
N0000148032 NUI
D00374 KEGG_DRUG
22189-31-7 SECONDARY_CAS_RN
4018509 VANDF
4019947 VANDF
C0039955 UMLSCUI
CHEBI:9571 CHEBI
DB01623 DRUGBANK_ID
CHEMBL1201 ChEMBL_ID
CHEMBL1200902 ChEMBL_ID
CHEMBL3989824 ChEMBL_ID
D013888 MESH_DESCRIPTOR_UI
941651 PUBCHEM_CID
2114 INN_ID
7318FJ13YJ UNII
212 IUPHAR_LIGAND_ID
10510 RXNORM
2137 MMSL
5574 MMSL
5575 MMSL
d00391 MMSL
001529 NDDF
001530 NDDF
25538002 SNOMEDCT_US
372804006 SNOMEDCT_US
62529008 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Thiothixene HUMAN PRESCRIPTION DRUG LABEL 1 0378-1001 CAPSULE 1 mg ORAL ANDA 17 sections
Thiothixene HUMAN PRESCRIPTION DRUG LABEL 1 0378-2002 CAPSULE 2 mg ORAL ANDA 17 sections
Thiothixene HUMAN PRESCRIPTION DRUG LABEL 1 0378-3005 CAPSULE 5 mg ORAL ANDA 17 sections
Thiothixene HUMAN PRESCRIPTION DRUG LABEL 1 0378-5010 CAPSULE 10 mg ORAL ANDA 17 sections
Thiothixene HUMAN PRESCRIPTION DRUG LABEL 1 21695-161 CAPSULE 5 mg ORAL ANDA 18 sections
Thiothixene HUMAN PRESCRIPTION DRUG LABEL 1 51079-587 CAPSULE 2 mg ORAL ANDA 17 sections
Thiothixene HUMAN PRESCRIPTION DRUG LABEL 1 51079-588 CAPSULE 5 mg ORAL ANDA 17 sections
Thiothixene HUMAN PRESCRIPTION DRUG LABEL 1 51079-589 CAPSULE 10 mg ORAL ANDA 17 sections
Thiothixene HUMAN PRESCRIPTION DRUG LABEL 1 51407-275 CAPSULE 1 mg ORAL ANDA 16 sections
Thiothixene HUMAN PRESCRIPTION DRUG LABEL 1 51407-276 CAPSULE 2 mg ORAL ANDA 16 sections
Thiothixene HUMAN PRESCRIPTION DRUG LABEL 1 51407-277 CAPSULE 5 mg ORAL ANDA 16 sections
Thiothixene HUMAN PRESCRIPTION DRUG LABEL 1 51407-278 CAPSULE 10 mg ORAL ANDA 16 sections
Thiothixene HUMAN PRESCRIPTION DRUG LABEL 1 53808-0817 CAPSULE 10 mg ORAL ANDA 16 sections
Thiothixene HUMAN PRESCRIPTION DRUG LABEL 1 53808-1129 CAPSULE 2 mg ORAL ANDA 16 sections
Thiothixene HUMAN PRESCRIPTION DRUG LABEL 1 68151-2486 CAPSULE 5 mg ORAL ANDA 16 sections
Thiothixene HUMAN PRESCRIPTION DRUG LABEL 1 70518-1703 CAPSULE 5 mg ORAL ANDA 17 sections
Thiothixene HUMAN PRESCRIPTION DRUG LABEL 1 70518-2340 CAPSULE 10 mg ORAL ANDA 16 sections
Thiothixene HUMAN PRESCRIPTION DRUG LABEL 1 70518-2544 CAPSULE 2 mg ORAL ANDA 16 sections
Thiothixene HUMAN PRESCRIPTION DRUG LABEL 1 70518-2594 CAPSULE 5 mg ORAL ANDA 16 sections
Thiothixene Human Prescription Drug Label 1 70954-014 CAPSULE 1 mg ORAL ANDA 16 sections
Thiothixene Human Prescription Drug Label 1 70954-015 CAPSULE 2 mg ORAL ANDA 16 sections
Thiothixene Human Prescription Drug Label 1 70954-016 CAPSULE 5 mg ORAL ANDA 16 sections
Thiothixene Human Prescription Drug Label 1 70954-017 CAPSULE 10 mg ORAL ANDA 16 sections