perphenazine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2113 | 58-39-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An antipsychotic phenothiazine derivative with actions and uses similar to those of CHLORPROMAZINE.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 30 | mg | O |
| 7 | mg | P |
| 10 | mg | P |
| 16 | mg | R |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.99 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 40 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 18 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 27 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.07 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 9.40 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Feb. 27, 1957 | 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 |
|---|---|---|---|---|---|---|
| Ileus paralytic | 84.68 | 49.20 | 13 | 146 | 783 | 2357143 |
| Completed suicide | 74.04 | 49.20 | 20 | 139 | 21014 | 2336912 |
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 |
|---|
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N05AB03 | NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Phenothiazines with piperazine structure |
| FDA EPC | N0000175746 | Phenothiazine |
| FDA CS | M0016525 | Phenothiazines |
| 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 |
| CHEBI has role | CHEBI:48561 | dopaminergic antagonist |
| CHEBI has role | CHEBI:50919 | antiemetic |
| CHEBI has role | CHEBI:37930 | phenothiazine antipsychotic drug |
| MeSH PA | D014149 | Tranquilizing Agents |
Drug Use (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Nausea and vomiting | indication | 16932000 | |
| Schizophrenia | indication | 58214004 | DOID:5419 |
| Mixed anxiety and depressive disorder | indication | 231504006 | |
| Suicidal thoughts | contraindication | 6471006 | |
| Alcoholism | contraindication | 7200002 | |
| Organophosphate poisoning | contraindication | 8260003 | |
| Weight gain finding | contraindication | 8943002 | |
| Sinus tachycardia | contraindication | 11092001 | |
| 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 | |
| Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
| Conduction disorder of the heart | contraindication | 44808001 | |
| Chronic heart failure | contraindication | 48447003 | |
| Bradycardia | contraindication | 48867003 | |
| Paralytic ileus | contraindication | 55525008 | DOID:8442 |
| Extrapyramidal disease | contraindication | 76349003 | |
| Hyperglycemia | contraindication | 80394007 | DOID:4195 |
| Chronic idiopathic constipation | contraindication | 82934008 | |
| Open-angle glaucoma | contraindication | 84494001 | DOID:1067 |
| 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 | |
| Bipolar affective disorder, current episode manic | contraindication | 191618007 | |
| 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 | |
| Syncope | contraindication | 271594007 | |
| 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 | |
| Angle-closure glaucoma | contraindication | 392291006 | DOID:13550 |
| Visual impairment | contraindication | 397540003 | |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Myocardial ischemia | contraindication | 414795007 | DOID:3393 |
| Obesity | contraindication | 414916001 | DOID:9970 |
| Myocardial infarction in recovery phase | contraindication | 418044006 | |
| Congenital long QT syndrome | contraindication | 442917000 | |
| Carcinoma of female breast | contraindication | 447782002 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.21 | Basic |
| pKa2 | 4.21 | Basic |
| pKa3 | 2.21 | 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 | 9.32 | WOMBAT-PK | CHEMBL | |||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | Ki | 5.46 | DRUG MATRIX | |||||
| D(4) dopamine receptor | GPCR | Ki | 7.59 | WOMBAT-PK | |||||
| Alpha-2C adrenergic receptor | GPCR | Ki | 7.07 | WOMBAT-PK | |||||
| Aldehyde oxidase | Enzyme | IC50 | 7.48 | WOMBAT-PK | |||||
| Histamine H1 receptor | GPCR | Ki | 8.09 | WOMBAT-PK | |||||
| D(3) dopamine receptor | GPCR | Ki | 9.52 | WOMBAT-PK | |||||
| Alpha-2B adrenergic receptor | GPCR | Ki | 6.98 | WOMBAT-PK | |||||
| Alpha-1A adrenergic receptor | GPCR | Ki | 8 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 7 | GPCR | Ki | 7.64 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 6 | GPCR | Ki | 7.55 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 2C | GPCR | Ki | 6.88 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | Ki | 8.25 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 6.07 | WOMBAT-PK | |||||
| Alpha-2A adrenergic receptor | GPCR | Ki | 6.19 | WOMBAT-PK | |||||
| Muscarinic acetylcholine receptor M3 | GPCR | Ki | 5.73 | PDSP | |||||
| Pleiotropic ABC efflux transporter of multiple drugs | Transporter | IC50 | 5.85 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 6 | GPCR | ANTAGONIST | Ki | 7.80 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 7 | GPCR | ANTAGONIST | Ki | 7.60 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| 4017939 | VUID |
| N0000146289 | NUI |
| C0031184 | UMLSCUI |
| D00503 | KEGG_DRUG |
| 41147003 | SNOMEDCT_US |
| 4017939 | VANDF |
| 2271 | MMSL |
| 8076 | RXNORM |
| 387229007 | SNOMEDCT_US |
| 5261 | MMSL |
| d00855 | MMSL |
| 001477 | NDDF |
| CHEMBL567 | ChEMBL_ID |
| DB00850 | DRUGBANK_ID |
| FTA7XXY4EZ | UNII |
| 637 | INN_ID |
| CHEBI:8028 | CHEBI |
| D010546 | MESH_DESCRIPTOR_UI |
| 4748 | PUBCHEM_CID |
| 209 | IUPHAR_LIGAND_ID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Perphenazine and Amitriptyline Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0378-0042 | TABLET, FILM COATED | 4 mg | ORAL | ANDA | 13 sections |
| Perphenazine and Amitriptyline Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0378-0073 | TABLET, FILM COATED | 4 mg | ORAL | ANDA | 13 sections |
| Perphenazine and Amitriptyline Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0378-0330 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 13 sections |
| Perphenazine and Amitriptyline Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0378-0442 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 13 sections |
| Perphenazine and Amitriptyline Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0378-0574 | TABLET, FILM COATED | 4 mg | ORAL | ANDA | 13 sections |
| Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-5350 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 12 sections |
| Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-5351 | TABLET, FILM COATED | 4 mg | ORAL | ANDA | 12 sections |
| Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-5352 | TABLET, FILM COATED | 8 mg | ORAL | ANDA | 12 sections |
| Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-5353 | TABLET, FILM COATED | 16 mg | ORAL | ANDA | 12 sections |
| Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-4101 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 13 sections |
| Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-4102 | TABLET, FILM COATED | 4 mg | ORAL | ANDA | 13 sections |
| Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-4103 | TABLET, FILM COATED | 8 mg | ORAL | ANDA | 13 sections |
| Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-4104 | TABLET, FILM COATED | 16 mg | ORAL | ANDA | 13 sections |
| Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0603-5060 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 14 sections |
| Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0603-5061 | TABLET, FILM COATED | 4 mg | ORAL | ANDA | 14 sections |
| Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0603-5062 | TABLET, FILM COATED | 8 mg | ORAL | ANDA | 14 sections |
| Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0603-5063 | TABLET, FILM COATED | 16 mg | ORAL | ANDA | 14 sections |
| Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0615-3584 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 12 sections |
| Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0615-3585 | TABLET, FILM COATED | 4 mg | ORAL | ANDA | 12 sections |
| Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0615-4511 | TABLET, FILM COATED | 8 mg | ORAL | ANDA | 12 sections |
| Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-1046 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 13 sections |
| Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-1047 | TABLET, FILM COATED | 4 mg | ORAL | ANDA | 13 sections |
| Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-1048 | TABLET, FILM COATED | 8 mg | ORAL | ANDA | 13 sections |
| Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-1049 | TABLET, FILM COATED | 16 mg | ORAL | ANDA | 13 sections |
| Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-8046 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 13 sections |
| Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-8047 | TABLET, FILM COATED | 4 mg | ORAL | ANDA | 13 sections |
| Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-8048 | TABLET, FILM COATED | 8 mg | ORAL | ANDA | 13 sections |
| Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-8049 | TABLET, FILM COATED | 16 mg | ORAL | ANDA | 13 sections |
| Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0904-6599 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 14 sections |
| Perphenazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0904-6600 | TABLET, FILM COATED | 4 mg | ORAL | ANDA | 14 sections |