Perphenazine

Phenothiazine — NERVOUS SYSTEM

Key facts

Perphenazine is an ofp drug in the Phenothiazine class catalogued in DrugCentral. It was first approved by the FDA in 1957. DrugCentral lists 20 molecular targets, including DRD3, DRD2 and HTR2A. Recorded indications include Mixed anxiety and depressive disorder, Nausea and vomiting and Schizophrenia.

• Approval status: ofp (first approved 1957 by the FDA).
• Drug class: Phenothiazine.
• Molecular targets: DRD3, DRD2, HTR2A and HRH1 (20 listed in DrugCentral).
• Indications: Mixed anxiety and depressive disorder, Nausea and vomiting and Schizophrenia.
• ATC code: N05AB03 (Phenothiazines with piperazine structure).
• Molecular formula: C21H26ClN3OS; molecular weight 403.98 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (3)

• Mixed anxiety and depressive disorder
• Nausea and vomiting
• Schizophrenia

Contraindications (49)

• Acute disease of cardiovascular system
• Alcoholism
• Anemia
• Angina pectoris
• Angle-closure glaucoma
• At risk for aspiration
• Benign prostatic hyperplasia
• Bipolar affective disorder, current episode manic
• Bradycardia
• Breastfeeding (mother)
• Carcinoma of female breast
• Chronic disease of respiratory system
• Chronic heart failure
• Chronic idiopathic constipation
• Coma
• Conduction disorder of the heart
• Congenital long QT syndrome
• Disease of liver
• Epilepsy
• Extrapyramidal disease
• Glaucoma
• Hyperglycemia
• Hyperprolactinemia
• Hyperthyroidism
• Leukopenia
• Metabolic syndrome X
• Myocardial infarction
• Myocardial infarction in recovery phase
• Myocardial ischemia
• Neuroleptic malignant syndrome
• + 19 more

Mechanism & targets

• Established pharmacologic class: Phenothiazine

Molecular targets (20)

Target	Gene	Action	Activity
D(3) dopamine receptor	DRD3	unknown	Ki 9.52
D(2) dopamine receptor	DRD2	antagonist	Ki 9.32
5-hydroxytryptamine receptor 2A	HTR2A	unknown	Ki 8.25
Histamine H1 receptor	HRH1	unknown	Ki 8.09
Alpha-1A adrenergic receptor	ADRA1A	unknown	Ki 8.00
5-hydroxytryptamine receptor 6	Htr6	antagonist	Ki 7.80
5-hydroxytryptamine receptor 7	HTR7	unknown	Ki 7.64
5-hydroxytryptamine receptor 7	Htr7	antagonist	Ki 7.60
D(4) dopamine receptor	DRD4	unknown	Ki 7.59
5-hydroxytryptamine receptor 6	HTR6	unknown	Ki 7.55
Aldehyde oxidase	AOX1	unknown	IC50 7.48
Alpha-2C adrenergic receptor	ADRA2C	unknown	Ki 7.07
Alpha-2B adrenergic receptor	ADRA2B	unknown	Ki 6.98
5-hydroxytryptamine receptor 2C	HTR2C	unknown	Ki 6.88
Retinal dehydrogenase 1	ALDH1A1	unknown	IC50 6.28
Alpha-2A adrenergic receptor	ADRA2A	unknown	Ki 6.19
5-hydroxytryptamine receptor 1A	HTR1A	unknown	Ki 6.07
Pleiotropic ABC efflux transporter of multiple drugs	PDR5	unknown	IC50 5.85
Muscarinic acetylcholine receptor M3	CHRM3	unknown	Ki 5.73
Potassium voltage-gated channel subfamily H member 2	KCNH2	unknown	Ki 5.46

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1957-02-27	FDA	—	—

ATC classification

ATC code	Therapeutic hierarchy
N05AB03	NERVOUS SYSTEM › PSYCHOLEPTICS › ANTIPSYCHOTICS › Phenothiazines with piperazine structure

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• FDA label: CYP2D6 · Informative PGx
• HCSC label
• PMDA label: CYP2D6 · Actionable PGx

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Antipsychotic drug level below therapeutic	702.5
Disinhibition	656.8
Akathisia	646.7
Therapeutic product effect variable	643.9
Obsessive-compulsive disorder	605.1
Euphoric mood	559.3
Increased appetite	476.0
Suicide attempt	324.9
Toxicity to various agents	295.2
Tardive dyskinesia	272.1
Leukaemia	259.8
Dyslipidaemia	227.6

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Perphenazine is on its molecule page.

• Molecular formula: C₂₁H₂₆ClN₃OS
• Molecular weight: 403.98 g/mol
• CAS number: —
• InChIKey: RGCVKNLCSQQDEP-UHFFFAOYSA-N
• PubChem CID: 4748

OCCN1CCN(CCCN2C3=CC=CC=C3SC3=CC=C(Cl)C=C23)CC1

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Perphenazine used for?

DrugCentral lists the following indications for Perphenazine: Mixed anxiety and depressive disorder, Nausea and vomiting and Schizophrenia.

How does Perphenazine work?

Its molecular targets in DrugCentral include DRD3, DRD2 (antagonist), HTR2A and HRH1.

When was Perphenazine first approved?

Perphenazine was first approved by the FDA in 1957.

What drug class does Perphenazine belong to?

Perphenazine is in the Phenothiazine class.

What is the chemical formula of Perphenazine?

Perphenazine has the molecular formula C21H26ClN3OS and a molecular weight of 403.98 g/mol.

Sources

• DrugCentral drug card 2113 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL567 — compound record and bioactivity
• PubChem CID 4748 — chemical identifiers
• DrugBank DB00850 — drug record
• FDA UNII FTA7XXY4EZ — substance identity
• DailyMed: FDA labels for Perphenazine — current prescribing information (label search)
• UniProt P35462 (DRD3) — target protein
• UniProt P14416 (DRD2) — target protein
• UniProt P28223 (HTR2A) — target protein
• UniProt P35367 (HRH1) — target protein
• UniProt P35348 (ADRA1A) — target protein
• UniProt P34969 (HTR7) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

How this page is built: methodology · editorial policy & corrections.