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molindone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 1830 | 7416-34-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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)
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 50 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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 |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| 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:
| Source | Code | Description |
|---|---|---|
| ATC | N05AE02 | NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Indole derivatives |
| MeSH PA | D002492 | Central Nervous System Depressants |
| MeSH PA | D011619 | Psychotropic Drugs |
| MeSH PA | D014150 | Antipsychotic Agents |
| FDA EPC | N0000180182 | Typical Antipsychotic |
| CHEBI has role | CHEBI:35476 | antipsychotic agent |
Related Drugs by ATC class:
N05AE Indole derivatives 4 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 level | Dissociation constant | Type (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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| D(2) dopamine receptor | GPCR | ANTAGONIST | IC50 | 6.16 | WOMBAT-PK | CHEMBL | |||
| 5-hydroxytryptamine receptor 2A | GPCR | ANTAGONIST | Ki | 6.50 | IUPHAR | IUPHAR | |||
| 5-hydroxytryptamine receptor 6 | GPCR | Ki | 6.00 | PDSP | |||||
| Alpha-2A adrenergic receptor | GPCR | Ki | 5.96 | PDSP | |||||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 6.91 | WOMBAT-PK | |||||
| 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 | |||||
| 5-hydroxytryptamine receptor 2C | GPCR | Ki | 5 | PDSP | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 5.42 | 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:
| ID | Source |
|---|---|
| 4019843 | VUID |
| N0000147930 | NUI |
| D00796 | KEGG_DRUG |
| 4018544 | VANDF |
| 4019843 | VANDF |
| C0026388 | UMLSCUI |
| CHEBI:6965 | CHEBI |
| CHEMBL460 | ChEMBL_ID |
| DB01618 | DRUGBANK_ID |
| CHEMBL1200419 | ChEMBL_ID |
| D008972 | MESH_DESCRIPTOR_UI |
| 23897 | PUBCHEM_CID |
| 207 | IUPHAR_LIGAND_ID |
| 2376 | INN_ID |
| 15622-65-8 | SECONDARY_CAS_RN |
| 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 |
| RT3Y3QMF8N | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 |