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

Stem definitionDrug idCAS RN
1830 7416-34-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • molindone
  • (+/-)-Molindone
  • molindone hydrochloride
  • moban
  • molindone HCl
  • molindone monohydrochloride
An indole derivative effective in schizophrenia and other psychoses and possibly useful in the treatment of the aggressive type of undersocialized conduct disorder. Molindone has much lower affinity for D2 receptors than most antipsychotic agents and has a relatively low affinity for D1 receptors. It has only low to moderate affinity for cholinergic and alpha-adrenergic receptors. Some electrophysiologic data from animals indicate that molindone has certain characteristics that resemble those of CLOZAPINE. (From AMA Drug Evaluations Annual, 1994, p283)
  • Molecular weight: 276.38
  • Formula: C16H24N2O2
  • CLOGP: 2.37
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 1
  • TPSA: 45.33
  • ALOGS: -2.77
  • ROTB: 3
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
50 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 2 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 11.63 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
Jan. 18, 1974 FDA

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05AE02 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Indole derivatives
MeSH PA D014150 Antipsychotic Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D011619 Psychotropic Drugs
MeSH PA D014149 Tranquilizing Agents
FDA EPC N0000180182 Typical Antipsychotic

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
Parkinsonism contraindication 32798002
Leukopenia contraindication 84828003 DOID:615
Tardive dyskinesia contraindication 102449007
Gastrointestinal obstruction contraindication 126765001
Neoplasm of brain contraindication 126952004 DOID:1319
Seizure disorder contraindication 128613002
Disease of liver contraindication 235856003 DOID:409
Hyperprolactinemia contraindication 237662005 DOID:12700
Neutropenic disorder contraindication 303011007 DOID:1227
Coma contraindication 371632003
Central nervous system depression contraindication 418072004
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 11.65 acidic
pKa2 7.09 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
5-hydroxytryptamine receptor 2A GPCR ANTAGONIST Ki 6.50 IUPHAR IUPHAR
D(2) dopamine receptor GPCR ANTAGONIST IC50 6.16 WOMBAT-PK CHEMBL
Sigma non-opioid intracellular receptor 1 Membrane receptor Ki 6.91 WOMBAT-PK
5-hydroxytryptamine receptor 1A GPCR Ki 5.42 PDSP
5-hydroxytryptamine receptor 2C GPCR Ki 5 PDSP
5-hydroxytryptamine receptor 6 GPCR Ki 6.00 PDSP
5-hydroxytryptamine receptor 7 GPCR Ki 6.58 CHEMBL
Alpha-1A adrenergic receptor GPCR Ki 5.58 PDSP
Alpha-2B adrenergic receptor GPCR Ki 6.25 PDSP
D(3) dopamine receptor GPCR Ki 7.42 PDSP
Histamine H1 receptor GPCR ANTAGONIST Ki 5.70 IUPHAR
Muscarinic acetylcholine receptor M3 GPCR Ki 5 PDSP
Alpha-2C adrenergic receptor GPCR Ki 6.76 PDSP
D(4) dopamine receptor GPCR Ki 5.62 PDSP
Alpha-2A adrenergic receptor GPCR Ki 5.96 PDSP
D(2) dopamine receptor GPCR Ki 7.48 CHEMBL
5-hydroxytryptamine receptor 2A GPCR Ki 5.85 CHEMBL
D(1A) dopamine receptor GPCR Ki 5.80 CHEMBL

External reference:

IDSource
4019843 VUID
N0000147930 NUI
D00796 KEGG_DRUG
15622-65-8 SECONDARY_CAS_RN
4018544 VANDF
4019843 VANDF
C0026388 UMLSCUI
CHEBI:6965 CHEBI
CHEMBL460 ChEMBL_ID
DB01618 DRUGBANK_ID
D008972 MESH_DESCRIPTOR_UI
23897 PUBCHEM_CID
207 IUPHAR_LIGAND_ID
2376 INN_ID
RT3Y3QMF8N UNII
227557 RXNORM
1830 MMSL
237227 MMSL
5127 MMSL
d00896 MMSL
001528 NDDF
004616 NDDF
372799001 SNOMEDCT_US
55124001 SNOMEDCT_US
61408004 SNOMEDCT_US
CHEMBL1200419 ChEMBL_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Molindone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42806-336 TABLET 5 mg ORAL ANDA 20 sections
Molindone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42806-337 TABLET 10 mg ORAL ANDA 20 sections
Molindone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42806-338 TABLET 25 mg ORAL ANDA 20 sections