Drug intelligence / Profile preview

fluspirilene

Development stage
Unknown
Lead developer
Janssen Pharmaceutica
Modality
Small Molecules
Administration
Intramuscular
01

Overview

Fluspirilene is a long-acting antipsychotic medication primarily used in the treatment of chronic schizophrenia. It belongs to the diphenylbutylpiperidine class of typical antipsychotics and is administered as a depot injection, typically given once weekly. ## Mechanism of Action Fluspirilene works primarily by blocking dopamine D2 receptors in the brain, which is the main mechanism for its antipsychotic effects. It also has activity at dopamine D3 receptors and demonstrates calcium channel-blocking properties, particularly N-type calcium channels. This calcium channel blockade contributes to inhibiting glutamate release, which may enhance its antipsychotic action[1][5]. ## Clinical Use The medication is administered intramuscularly as a depot injection, allowing for gradual release of the active drug over time. The typical initial dosage is 2 mg weekly, which can be increased based on patient response. Maintenance dosages generally range from 1-10 mg weekly[7]. Fluspirilene has been marketed under brand names such as Redeptin, Imap, and R6218[2]. While it was previously available in the UK, production there ceased in 1993, though it remains in use in several countries including Argentina, Belgium, Canada, Germany, Holland, Ireland, and Israel[3]. ## Side Effects Like other antipsychotics, fluspirilene can cause extrapyramidal symptoms including parkinsonian symptoms, dystonia, akathisia, and tardive dyskinesia. Other potential adverse effects include neuroleptic malignant syndrome, cardiovascular effects, endocrine disturbances, and antimuscarinic symptoms[7]. ## Research Applications Beyond its use in schizophrenia, fluspirilene has been investigated for potential applications in cancer treatment. Studies have shown it may have inhibitory effects on glioma cell proliferation and invasion, suggesting potential use in glioblastoma treatment. It has also been studied as a cyclin-dependent kinase 2 inhibitor for potential treatment of hepatocellular carcinoma[5].

Brand names
RedeptinImap
Other names
FluspirilenoFluspirilenum
02

Targets

MDM2 (Mouse double minute 2 homolog)DRD3 (Dopamine receptor D3)DRD2 (Dopamine D2 Receptor)CDK2 (Cyclin-dependent kinase 2)CACNA1B (Voltage-dependent N-type calcium channel subunit alpha-1B)

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