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triflupromazine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2742 | 146-54-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A phenothiazine used as an antipsychotic agent and as an antiemetic.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.10 | g | O |
| 0.10 | g | P |
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 3.569 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.109 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 16.368 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 76.560 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 1.730 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 5.190 | % | High | 1 |
| herg | hERG pIC50 | 6.002 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 26.122 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 31.046 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 1.850 | % | High | 1 |
| kinase-safety-class | ACVR2B,AKT1,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K7,MAPK10,MAPK12,MAPK7,MAPKAPK2,MET,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TTK | 40 | |||
| kinase-selectivity-class | PDK4 | 1 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.664 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 161.065 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 1.980 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 2.518 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 1 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 1 | Moderate | 0.70 | |
| pppb | Pig plasma protein binding (% unbound) | 6.010 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 213.304 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 9.580 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 2 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 225.424 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 16, 1957 | 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 | N05AA05 | NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Phenothiazines with aliphatic side-chain |
| MeSH PA | D000932 | Antiemetics |
| MeSH PA | D002492 | Central Nervous System Depressants |
| MeSH PA | D005765 | Gastrointestinal Agents |
| MeSH PA | D011619 | Psychotropic Drugs |
| MeSH PA | D014150 | Antipsychotic Agents |
| MeSH PA | D015259 | Dopamine Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018492 | Dopamine Antagonists |
| CHEBI has role | CHEBI:48561 | dopaminergic antagonist |
| CHEBI has role | CHEBI:50919 | antiemetic |
| CHEBI has role | CHEBI:65190 | first generation antipsychotic |
| CHEBI has role | CHEBI:149553 | anticoronaviral agent |
Related Drugs by ATC class:
N05AA Phenothiazines with aliphatic side-chain 6 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Nausea and vomiting | indication | 16932000 | |
| Psychotic disorder | indication | 69322001 | |
| Vomiting | indication | 422400008 | |
| Nausea | indication | 422587007 | |
| Alcoholism | contraindication | 7200002 | |
| Organophosphate poisoning | contraindication | 8260003 | |
| Weight gain finding | contraindication | 8943002 | |
| Neuroleptic malignant syndrome | contraindication | 15244003 | DOID:14464 |
| Senile dementia | contraindication | 15662003 | |
| Chronic disease of respiratory system | contraindication | 17097001 | |
| Myocardial infarction | contraindication | 22298006 | DOID:5844 |
| Glaucoma | contraindication | 23986001 | DOID:1686 |
| Orthostatic hypotension | contraindication | 28651003 | |
| Torsades de pointes | contraindication | 31722008 | |
| Parkinsonism | contraindication | 32798002 | |
| Conduction disorder of the heart | contraindication | 44808001 | |
| Chronic heart failure | contraindication | 48447003 | |
| Bradycardia | contraindication | 48867003 | |
| Extrapyramidal disease | contraindication | 76349003 | |
| Hyperglycemia | contraindication | 80394007 | DOID:4195 |
| Epilepsy | contraindication | 84757009 | DOID:1826 |
| Leukopenia | contraindication | 84828003 | DOID:615 |
| Stupor | contraindication | 89458003 | |
| Tardive dyskinesia | contraindication | 102449007 | |
| Prolonged QT interval | contraindication | 111975006 | |
| Acute disease of cardiovascular system | contraindication | 128487001 | |
| Angina pectoris | contraindication | 194828000 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Metabolic syndrome X | contraindication | 237602007 | DOID:14221 |
| Hyperprolactinemia | contraindication | 237662005 | DOID:12700 |
| Benign prostatic hyperplasia | contraindication | 266569009 | |
| Retention of urine | contraindication | 267064002 | |
| Anemia | contraindication | 271737000 | DOID:2355 |
| Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
| Neutropenic disorder | contraindication | 303011007 | DOID:1227 |
| Coma | contraindication | 371632003 | |
| At risk for aspiration | contraindication | 371736008 | |
| Visual impairment | contraindication | 397540003 | |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Myocardial ischemia | contraindication | 414795007 | DOID:3393 |
| Obesity | contraindication | 414916001 | DOID:9970 |
| Congenital long QT syndrome | contraindication | 442917000 | |
| Carcinoma of female breast | contraindication | 447782002 |
🐶 Veterinary Drug Use
| Species | Use | Relation |
|---|---|---|
| Dogs | Anxiety | Indication |
| Dogs | Control psychomotor overactivity | Indication |
| Dogs | Pain and pruritus | Indication |
| Cats | Anxiety | Indication |
| Cats | Control psychomotor overactivity | Indication |
| Cats | Pain and pruritus | Indication |
| Horses | Anxiety | Indication |
| Horses | Control psychomotor overactivity | Indication |
| Horses | Pain and pruritus | Indication |
🐶 Veterinary products
| Product | Applicant | Ingredients |
|---|---|---|
| Vetame Injectable, Vetame Tablets | Zoetis Inc. | 1 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.04 | Basic |
| pKa2 | 2.72 | 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 | Ki | 8.55 | PDSP | CHEMBL | |||
| Multidrug resistance protein 1 | Transporter | Ki | 4.80 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | Ki | 8.40 | PDSP | |||||
| Histone deacetylase 6 | Enzyme | IC50 | 5.43 | CHEMBL | |||||
| Trypanothione reductase | Enzyme | Ki | 4.52 | CHEMBL | |||||
| Cholinesterase | Enzyme | IC50 | 5.13 | CHEMBL | |||||
| Pleiotropic ABC efflux transporter of multiple drugs | Transporter | IC50 | 5.31 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019958 | VUID |
| N0000148043 | NUI |
| D00390 | KEGG_DRUG |
| 4017744 | VANDF |
| 4019958 | VANDF |
| C0040989 | UMLSCUI |
| CHEBI:9711 | CHEBI |
| CHEMBL570 | ChEMBL_ID |
| DB00508 | DRUGBANK_ID |
| CHEMBL1201102 | ChEMBL_ID |
| D014273 | MESH_DESCRIPTOR_UI |
| 5568 | PUBCHEM_CID |
| 4330 | IUPHAR_LIGAND_ID |
| 725 | INN_ID |
| 1098-60-8 | SECONDARY_CAS_RN |
| RO16TQF95Y | UNII |
| 10805 | RXNORM |
| 5626 | MMSL |
| d03152 | MMSL |
| 001472 | NDDF |
| 004589 | NDDF |
| 30329006 | SNOMEDCT_US |
| 398816002 | SNOMEDCT_US |
| 6992002 | SNOMEDCT_US |
| RO16TQF95Y | INXIGHT DRUGS |
Pharmaceutical products:
None