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trifluoperazine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2740 | 117-89-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A phenothiazine with actions similar to CHLORPROMAZINE. It is used as an antipsychotic and an antiemetic.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 20 | mg | O |
| 8 | mg | P |
| 20 | mg | R |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 50 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| BA (Bioavailability) | 95 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 4.153 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.334 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 13.677 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 30.903 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 1.110 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 2.940 | % | High | 1 |
| herg | hERG pIC50 | 5.979 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 14.791 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 44.259 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 0.850 | % | High | 1 |
| kinase-safety-class | ACVR2B,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,JAK2,JAK3,MAP3K7,MAPK10,MAPK7,MET,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TGFBR1,TTK | 36 | |||
| kinase-selectivity-class | AXL,PDK4 | 2 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.297 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 95.499 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 1.100 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 5.176 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 1 | |||
| pppb | Pig plasma protein binding (% unbound) | 3.020 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 201.372 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 4.240 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 1 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 41.687 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| April 16, 1959 | FDA |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Drug abuse | 99.76 | 54.14 | 32 | 567 | 82315 | 90545533 |
| Persecutory delusion | 64.20 | 54.14 | 12 | 587 | 3196 | 90624652 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Antipsychotic drug level below therapeutic | 638.96 | 232.23 | 115 | 2120 | 3089 | 42616011 |
| Disinhibition | 616.54 | 232.23 | 115 | 2120 | 3780 | 42615320 |
| Therapeutic product effect variable | 616.05 | 232.23 | 111 | 2124 | 2998 | 42616102 |
| Obsessive-compulsive disorder | 576.99 | 232.23 | 119 | 2116 | 6624 | 42612476 |
| Euphoric mood | 564.50 | 232.23 | 116 | 2119 | 6337 | 42612763 |
| Increased appetite | 521.68 | 232.23 | 115 | 2120 | 8791 | 42610309 |
| Akathisia | 503.36 | 232.23 | 115 | 2120 | 10336 | 42608764 |
| Suicide attempt | 362.08 | 232.23 | 122 | 2113 | 45978 | 42573122 |
| Leukaemia | 306.98 | 232.23 | 69 | 2166 | 5703 | 42613397 |
| Therapeutic product effect incomplete | 272.28 | 232.23 | 111 | 2124 | 70828 | 42548272 |
| Weight increased | 242.73 | 232.23 | 116 | 2119 | 107867 | 42511233 |
| Leukopenia | 236.53 | 232.23 | 102 | 2133 | 74644 | 42544456 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Antipsychotic drug level below therapeutic | 275.92 | 74.00 | 43 | 1627 | 1692 | 110585937 |
| Therapeutic product effect variable | 256.63 | 74.00 | 43 | 1627 | 2675 | 110584954 |
| Disinhibition | 250.52 | 74.00 | 43 | 1627 | 3091 | 110584538 |
| Euphoric mood | 241.30 | 74.00 | 49 | 1621 | 8778 | 110578851 |
| Obsessive-compulsive disorder | 220.58 | 74.00 | 44 | 1626 | 7197 | 110580432 |
| Akathisia | 208.98 | 74.00 | 49 | 1621 | 17064 | 110570565 |
| Increased appetite | 183.43 | 74.00 | 43 | 1627 | 14934 | 110572695 |
| Dyslipidaemia | 180.70 | 74.00 | 43 | 1627 | 15922 | 110571707 |
| Suicide attempt | 161.53 | 74.00 | 60 | 1610 | 103334 | 110484295 |
| Schizoaffective disorder | 157.40 | 74.00 | 29 | 1641 | 3107 | 110584522 |
| Irritability | 138.13 | 74.00 | 44 | 1626 | 47765 | 110539864 |
| Leukaemia | 110.16 | 74.00 | 25 | 1645 | 7493 | 110580136 |
| Leukopenia | 98.76 | 74.00 | 47 | 1623 | 148744 | 110438885 |
| Prescribed overdose | 98.15 | 74.00 | 40 | 1630 | 87541 | 110500088 |
| Obesity | 97.85 | 74.00 | 43 | 1627 | 113308 | 110474321 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N05AB06 | NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Phenothiazines with piperazine structure |
| FDA CS | M0016525 | Phenothiazines |
| 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 |
| FDA EPC | N0000175746 | Phenothiazine |
| CHEBI has role | CHEBI:35476 | antipsychotic agent |
| CHEBI has role | CHEBI:37930 | phenothiazine antipsychotic drug |
| CHEBI has role | CHEBI:48561 | dopaminergic antagonist |
| CHEBI has role | CHEBI:50919 | antiemetic |
| CHEBI has role | CHEBI:75835 | anti-anaemic agent |
| CHEBI has role | CHEBI:77402 | EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor |
| CHEBI has role | CHEBI:86385 | EC 5.3.3.5 (cholestenol Δ-isomerase) inhibitor |
| CHEBI has role | CHEBI:130181 | calmodulin antagonist |
Related Drugs by ATC class:
N05AB Phenothiazines with piperazine structure 9 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Anxiety | indication | 48694002 | |
| Schizophrenia | indication | 58214004 | DOID:5419 |
| Neuroleptic malignant syndrome | contraindication | 15244003 | DOID:14464 |
| Senile dementia | contraindication | 15662003 | |
| Cirrhosis of liver | contraindication | 19943007 | DOID:5082 |
| Glaucoma | contraindication | 23986001 | DOID:1686 |
| Orthostatic hypotension | contraindication | 28651003 | |
| Retinal disorder | contraindication | 29555009 | DOID:5679 |
| Alcoholic liver damage | contraindication | 41309000 | |
| Low blood pressure | contraindication | 45007003 | |
| Chronic hepatitis | contraindication | 76783007 | DOID:2237 |
| Epilepsy | contraindication | 84757009 | DOID:1826 |
| Tardive dyskinesia | contraindication | 102449007 | |
| Diminished sweating | contraindication | 111980002 | |
| Angina pectoris | contraindication | 194828000 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| 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 |
| Visual impairment | contraindication | 397540003 | |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Carcinoma of female breast | contraindication | 447782002 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.74 | Basic |
| pKa2 | 4.74 | Basic |
| pKa3 | 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 | 8.84 | PDSP | CHEMBL | |||
| Alpha-2A adrenergic receptor | GPCR | Ki | 6.19 | PDSP | |||||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 7.82 | CHEMBL | |||||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | Ki | 5.29 | DRUG MATRIX | |||||
| 3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase | Enzyme | Ki | 8.10 | CHEMBL | |||||
| Multidrug resistance protein 1 | Transporter | Ki | 5.19 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 6.02 | PDSP | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | ANTAGONIST | Ki | 7.90 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 2C | GPCR | ANTAGONIST | Ki | 6.40 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 6 | GPCR | Ki | 6.85 | PDSP | |||||
| 5-hydroxytryptamine receptor 7 | GPCR | Ki | 6.54 | PDSP | |||||
| Alpha-1A adrenergic receptor | GPCR | Ki | 7.62 | PDSP | |||||
| Alpha-2B adrenergic receptor | GPCR | Ki | 6.79 | PDSP | |||||
| D(3) dopamine receptor | GPCR | ANTAGONIST | Ki | 9.25 | PDSP | ||||
| Histamine H1 receptor | GPCR | ANTAGONIST | Ki | 7.20 | IUPHAR | ||||
| Muscarinic acetylcholine receptor M3 | GPCR | Ki | 6 | PDSP | |||||
| Alpha-2C adrenergic receptor | GPCR | Ki | 6.41 | PDSP | |||||
| D(4) dopamine receptor | GPCR | ANTAGONIST | Ki | 7.38 | PDSP | ||||
| Calmodulin | Cytosolic other | Kd | 6 | CHEMBL | |||||
| DNA-dependent protein kinase catalytic subunit | Kinase | IC50 | 4 | CHEMBL | |||||
| Emopamil-binding protein-like | Enzyme | Ki | 8.41 | CHEMBL | |||||
| Sodium channel alpha subunits; brain (Types I, II, III) | Ion channel | IC50 | 5.30 | CHEMBL | |||||
| Trypanothione reductase | Enzyme | Ki | 4.64 | CHEMBL | |||||
| D(2) dopamine receptor | GPCR | Kd | 9.27 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 6.39 | CHEMBL | |||||
| NS3 | Enzyme | IC50 | 6.15 | CHEMBL | |||||
| Beta-glucuronidase | Enzyme | IC50 | 5.11 | CHEMBL | |||||
| Lysozyme C-1 | Enzyme | IC50 | 5.05 | CHEMBL | |||||
| C-8 sterol isomerase | Enzyme | Ki | 6.30 | CHEMBL | |||||
| Pleiotropic ABC efflux transporter of multiple drugs | Transporter | IC50 | 5.85 | CHEMBL | |||||
| Adrenergic receptor alpha-1 | GPCR | Ki | 7.53 | CHEMBL | |||||
| Serotonin 2 (5-HT2) receptor | GPCR | Kd | 8.98 | CHEMBL | |||||
| Calmodulin | Cytosolic other | Kd | 5.47 | CHEMBL | |||||
| Genome polyprotein | Polyprotein | IC50 | 6.16 | CHEMBL | |||||
| Sarcoplasmic/endoplasmic reticulum calcium ATPase 1 | Enzyme | IC50 | 4.35 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019957 | VUID |
| N0000148042 | NUI |
| D00799 | KEGG_DRUG |
| 440-17-5 | SECONDARY_CAS_RN |
| 4018843 | VANDF |
| 4019957 | VANDF |
| C0040979 | UMLSCUI |
| CHEBI:45951 | CHEBI |
| CHEMBL422 | ChEMBL_ID |
| CHEMBL1257040 | ChEMBL_ID |
| D014268 | MESH_DESCRIPTOR_UI |
| DB00831 | DRUGBANK_ID |
| 5566 | PUBCHEM_CID |
| 214 | IUPHAR_LIGAND_ID |
| 718 | INN_ID |
| 214IZI85K3 | UNII |
| 10800 | RXNORM |
| 2926 | MMSL |
| 5625 | MMSL |
| d00890 | MMSL |
| 001481 | NDDF |
| 004590 | NDDF |
| 373524005 | SNOMEDCT_US |
| 50754002 | SNOMEDCT_US |
| 71699007 | SNOMEDCT_US |
| TFP | PDB_CHEM_ID |
| 214IZI85K3 | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Trifluoperazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-2401 | TABLET, FILM COATED | 1 mg | ORAL | ANDA | 16 sections |
| Trifluoperazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-2402 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 16 sections |
| Trifluoperazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-2405 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 16 sections |
| Trifluoperazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-2410 | TABLET, FILM COATED | 10 mg | ORAL | ANDA | 16 sections |
| Trifluoperazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-8028 | TABLET, FILM COATED | 1 mg | ORAL | ANDA | 15 sections |
| Trifluoperazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-8032 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 15 sections |
| Trifluoperazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-8034 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 15 sections |
| Trifluoperazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-8036 | TABLET, FILM COATED | 10 mg | ORAL | ANDA | 15 sections |
| TRIFLUOPERAZINE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16590-305 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 11 sections |
| Trifluoperazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 48433-140 | TABLET, FILM COATED | 1 mg | ORAL | ANDA | 16 sections |
| Trifluoperazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 48433-141 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 16 sections |
| Trifluoperazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 48433-142 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 16 sections |
| Trifluoperazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 48433-143 | TABLET, FILM COATED | 10 mg | ORAL | ANDA | 16 sections |
| Trifluoperazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51079-572 | TABLET, FILM COATED | 1 mg | ORAL | ANDA | 16 sections |
| Trifluoperazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51079-573 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 16 sections |
| Trifluoperazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51079-574 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 16 sections |
| Trifluoperazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51079-575 | TABLET, FILM COATED | 10 mg | ORAL | ANDA | 16 sections |
| Trifluoperazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 53808-0629 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 15 sections |
| Trifluoperazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 53808-0819 | TABLET, FILM COATED | 10 mg | ORAL | ANDA | 15 sections |
| Trifluoperazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70518-2095 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 16 sections |
| Trifluoperazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70518-2106 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 16 sections |
| Trifluoperazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70518-4554 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 14 sections |
| Trifluoperazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70518-4686 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 14 sections |
| Trifluoperazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72162-2204 | TABLET, FILM COATED | 1 mg | ORAL | ANDA | 14 sections |
| Trifluoperazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72162-2205 | TABLET, FILM COATED | 10 mg | ORAL | ANDA | 14 sections |
| Trifluoperazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72162-2206 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 14 sections |
| Trifluoperazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72162-2207 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 14 sections |