Paliperidone

Atypical Antipsychotic — NERVOUS SYSTEM

Key facts

Paliperidone is an ofp drug in the Atypical Antipsychotic class catalogued in DrugCentral. It was first approved by the FDA in 2006. DrugCentral lists 28 molecular targets, including ADRA1B, DRD3 and HTR2A. Recorded indications include Psychotic disorder, Schizoaffective disorder and Schizophrenia.

• Approval status: ofp (first approved 2006 by the FDA).
• Drug class: Atypical Antipsychotic.
• Molecular targets: ADRA1B, DRD3, HTR2A and HTR7 (28 listed in DrugCentral).
• Indications: Psychotic disorder, Schizoaffective disorder and Schizophrenia.
• ATC code: N05AX13 (Other antipsychotics).
• Molecular formula: C23H27FN4O3; molecular weight 426.49 g/mol.

Indications & contraindications

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

Indications (3)

• Psychotic disorder
• Schizoaffective disorder
• Schizophrenia

Off-label uses (6)

• Bipolar affective disorder, current episode depression
• Bipolar affective disorder, current episode manic
• Bipolar disorder in remission
• Depression Treatment Adjunct
• Infantile autism
• Mixed bipolar I disorder

Contraindications (49)

• Acquired torsion dystonia
• Agranulocytosis
• Angina pectoris
• At risk for aspiration
• Breastfeeding (mother)
• Carcinoma of female breast
• Cerebrovascular disease
• Chronic heart failure
• Conduction disorder of the heart
• Congenital long QT syndrome
• Crohn's disease
• Dehydration
• Diabetes mellitus
• Diffuse Lewy body disease
• Esophageal Compression
• Esophageal dysmotility
• Extrapyramidal disease
• Gastrointestinal hypomotility
• Hyperglycemia
• Hyperlipidemia
• Hyperprolactinemia
• Hypokalemia
• Hypomagnesemia
• Hypovolemia
• Impaired cognition
• Impaired renal function disorder
• Increased intestinal motility
• Intestinal Cystic Fibrosis
• Leukopenia
• Low blood pressure
• + 19 more

Mechanism & targets

• Established pharmacologic class: Atypical Antipsychotic

Molecular targets (28)

Target	Gene	Action	Activity
Alpha-1B adrenergic receptor	ADRA1B	unknown	Ki 9.15
D(3) dopamine receptor	DRD3	unknown	Ki 9.05
5-hydroxytryptamine receptor 2A	HTR2A	antagonist	Ki 8.96
5-hydroxytryptamine receptor 7	HTR7	unknown	Ki 8.57
Alpha-1A adrenergic receptor	ADRA1A	unknown	Ki 8.55
D(2) dopamine receptor	DRD2	antagonist	Ki 8.47
Histamine H1 receptor	HRH1	unknown	Ki 8.25
Alpha-2C adrenergic receptor	ADRA2C	unknown	Ki 8.20
Alpha-2A adrenergic receptor	ADRA2A	unknown	Ki 7.92
5-hydroxytryptamine receptor 1D	HTR1D	unknown	Ki 7.72
5-hydroxytryptamine receptor 1B	HTR1B	unknown	Ki 7.64
Alpha-2B adrenergic receptor	ADRA2B	unknown	Ki 7.63
D(1B) dopamine receptor	DRD5	unknown	Ki 7.54
D(1A) dopamine receptor	DRD1	unknown	Ki 7.39
5-hydroxytryptamine receptor 2C	HTR2C	unknown	Ki 7.32
D(4) dopamine receptor	DRD4	unknown	Ki 7.26
5-hydroxytryptamine receptor 2B	HTR2B	unknown	Ki 7.21
Histamine H2 receptor	HRH2	unknown	Ki 6.92
5-hydroxytryptamine receptor 5A	HTR5A	unknown	Ki 6.56
5-hydroxytryptamine receptor 1A	HTR1A	unknown	Ki 6.22

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2007-06-25	EMA	—	—
2006-12-19	FDA	—	JANSSEN PHARMS

ATC classification

ATC code	Therapeutic hierarchy
N05AX13	NERVOUS SYSTEM › PSYCHOLEPTICS › ANTIPSYCHOTICS › Other antipsychotics

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: CYP2D6 · No Clinical PGx
• FDA label: CYP2D6 · No Clinical PGx
• HCSC label: CYP2D6 · No Clinical PGx
• Swissmedic label: CYP2D6 · Informative 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
Dystonia	1812.4
Blood prolactin abnormal	1440.6
Anosognosia	1334.3
Sexual dysfunction	1225.8
Disturbance in social behaviour	1211.0
Sedation	1205.9
Galactorrhoea	1182.4
Dyskinesia	1152.1
Metabolic disorder	1026.3
Extrapyramidal disorder	1009.7
Blood prolactin increased	1006.6
Suicide attempt	926.1

Chemical structure

• Molecular formula: C₂₃H₂₇FN₄O₃
• Molecular weight: 426.49 g/mol
• CAS number: 144598-75-4
• InChIKey: PMXMIIMHBWHSKN-UHFFFAOYSA-N
• PubChem CID: 115237

CC1=C(CCN2CCC(CC2)C2=NOC3=C2C=CC(F)=C3)C(=O)N2CCCC(O)C2=N1

Frequently asked questions

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

What is Paliperidone used for?

DrugCentral lists the following indications for Paliperidone: Psychotic disorder, Schizoaffective disorder and Schizophrenia.

How does Paliperidone work?

Its molecular targets in DrugCentral include ADRA1B, DRD3, HTR2A (antagonist) and HTR7.

When was Paliperidone first approved?

Paliperidone was first approved by the FDA in 2006.

What drug class does Paliperidone belong to?

Paliperidone is in the Atypical Antipsychotic class.

What is the chemical formula of Paliperidone?

Paliperidone has the molecular formula C23H27FN4O3 and a molecular weight of 426.49 g/mol.

Sources

• DrugCentral drug card 4137 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1621 — compound record and bioactivity
• PubChem CID 115237 — chemical identifiers
• DrugBank DB01267 — drug record
• FDA UNII 838F01T721 — substance identity
• DailyMed: FDA labels for Paliperidone — current prescribing information (label search)
• UniProt P35368 (ADRA1B) — target protein
• UniProt P35462 (DRD3) — target protein
• UniProt P28223 (HTR2A) — target protein
• UniProt P34969 (HTR7) — target protein
• UniProt P35348 (ADRA1A) — target protein
• UniProt P14416 (DRD2) — 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.