Loxapine

NERVOUS SYSTEM

Key facts

Loxapine is an ofp drug catalogued in DrugCentral. It was first approved by the FDA in 1975. DrugCentral lists 37 molecular targets, including HTR2A, DRD4 and Htr2a. Recorded indications include Bipolar disorder and Schizophrenia.

• Approval status: ofp (first approved 1975 by the FDA).
• Molecular targets: HTR2A, DRD4, Htr2a and HRH1 (37 listed in DrugCentral).
• Indications: Bipolar disorder and Schizophrenia.
• ATC code: N05AH01 (Diazepines, oxazepines, thiazepines and oxepines).
• Molecular formula: C18H18ClN3O; molecular weight 327.81 g/mol.

Indications & contraindications

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

Indications (2)

• Bipolar disorder
• Schizophrenia

Contraindications (14)

• Alcoholism
• Benign prostatic hyperplasia
• Carcinoma of female breast
• Coma
• Disorder of cardiovascular system
• Drug Induced CNS Depression
• Glaucoma
• Hyperprolactinemia
• Neuroleptic malignant syndrome
• Pigmentary Retinopathy
• Retention of urine
• Seizure disorder
• Senile dementia
• Tardive dyskinesia

Mechanism & targets

Molecular targets (37)

Target	Gene	Action	Activity
5-hydroxytryptamine receptor 2A	HTR2A	antagonist	Ki 8.62
D(4) dopamine receptor	DRD4	antagonist	Ki 8.31
5-hydroxytryptamine receptor 2A	Htr2a	unknown	IC50 8.22
Histamine H1 receptor	HRH1	antagonist	Ki 8.20
5-hydroxytryptamine receptor 2C	HTR2C	antagonist	Ki 8.00
5-hydroxytryptamine receptor 6	HTR6	unknown	Ki 7.82
5-hydroxytryptamine receptor 6	Htr6	antagonist	Ki 7.80
Adrenergic receptor alpha-1	Adra1b|Adra1d|Adra1a	unknown	IC50 7.74
D(2) dopamine receptor	DRD2	antagonist	Ki 7.68
D(2) dopamine receptor	Drd2	unknown	Ki 7.68
D(3) dopamine receptor	DRD3	antagonist	IC50 7.66
Alpha-1A adrenergic receptor	ADRA1A	unknown	Ki 7.51
5-hydroxytryptamine receptor 7	Htr7	unknown	Ki 7.37
Alpha-1B adrenergic receptor	ADRA1B	unknown	Ki 7.28
D(1A) dopamine receptor	DRD1	unknown	Ki 7.27
D(1B) dopamine receptor	DRD5	unknown	Ki 7.12
Alpha-2C adrenergic receptor	ADRA2C	unknown	Ki 7.10
Alpha-2B adrenergic receptor	ADRA2B	unknown	Ki 6.97
Muscarinic acetylcholine receptor M3	CHRM3	unknown	Ki 6.91
Muscarinic acetylcholine receptor M5	CHRM5	unknown	Ki 6.83

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1975-02-25	FDA	—	—

ATC classification

ATC code	Therapeutic hierarchy
N05AH01	NERVOUS SYSTEM › PSYCHOLEPTICS › ANTIPSYCHOTICS › Diazepines, oxazepines, thiazepines and oxepines

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
Coma	1290.3
Poisoning deliberate	972.6
Neuroleptic malignant syndrome	647.6
Antipsychotic drug level below therapeutic	647.4
Disinhibition	599.5
Therapeutic product effect variable	578.1
Akathisia	533.9
Obsessive-compulsive disorder	526.9
Somnolence	492.9
Euphoric mood	490.0
Extrapyramidal disorder	489.1
Miosis	415.0

Chemical structure

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

• Molecular formula: C₁₈H₁₈ClN₃O
• Molecular weight: 327.81 g/mol
• CAS number: 1977-10-2
• InChIKey: XJGVXQDUIWGIRW-UHFFFAOYSA-N
• PubChem CID: 3964

CN1CCN(CC1)C1=NC2=C(OC3=CC=C(Cl)C=C13)C=CC=C2

Frequently asked questions

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

What is Loxapine used for?

DrugCentral lists the following indications for Loxapine: Bipolar disorder and Schizophrenia.

How does Loxapine work?

Its molecular targets in DrugCentral include HTR2A (antagonist), DRD4 (antagonist), Htr2a and HRH1 (antagonist).

When was Loxapine first approved?

Loxapine was first approved by the FDA in 1975.

What is the chemical formula of Loxapine?

Loxapine has the molecular formula C18H18ClN3O and a molecular weight of 327.81 g/mol.

Sources

• DrugCentral drug card 1613 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1201060 — compound record and bioactivity
• PubChem CID 3964 — chemical identifiers
• DrugBank DB00408 — drug record
• FDA UNII LER583670J — substance identity
• DailyMed: FDA labels for Loxapine — current prescribing information (label search)
• UniProt P28223 (HTR2A) — target protein
• UniProt P21917 (DRD4) — target protein
• UniProt P35367 (HRH1) — target protein
• UniProt P28335 (HTR2C) — target protein
• UniProt P50406 (HTR6) — target protein
• UniProt P14416 (DRD2) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

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