Drug intelligence / Profile preview

chlorpromazine

Development stage
Approved
Lead developer
Sanofi
Modality
Small Molecules
Administration
Intramuscular, Intravenous, Oral, Rectal
01

Overview

Chlorpromazine is a prototypical first-generation (typical) phenothiazine antipsychotic drug developed in the early 1950s. It revolutionized psychiatric care and laid the foundation for modern psychopharmacology. Chlorpromazine primarily acts as an antagonist at post-synaptic dopamine D2 receptors in the mesolimbic pathway, thereby alleviating positive symptoms of schizophrenia and acute mania. It also exhibits broad-spectrum antagonism at various other receptors, including serotonin (5-HT2A, 5-HT2C), histamine H1, alpha-1 adrenergic, and muscarinic M1/M2 acetylcholine receptors. This multi-receptor profile contributes to its diverse clinical indications, which include the treatment of schizophrenia, bipolar mania, severe behavioral problems in children, intractable hiccups, acute intermittent porphyria, and severe nausea and vomiting. However, this broad activity is also associated with a range of side effects, such as sedation, orthostatic hypotension, anticholinergic effects, and extrapyramidal symptoms.

Brand names
AmpliactilChlorpromChlorpromanylContominFenactilHibernalKlorpromanLargactilMegaphenNovomazinaPlegomazinPromaparSanopronThorazineWintermin
Other names
2-chloropromazineaminazinaminazinechloropromazinechlorpromazine hydrochloridechlorpromazine monohydrochloridechlorpromazinium chlorideclorpromazinaCPZ
02

Targets

HTR2A (Serotonin receptor 5-HT2A)HTR2C (5-hydroxytryptamine 2C receptor)ADRA1A (α1A)ADRA1B (α1B)CaM (Calmodulin)DRD1 (Dopamine D1 Receptor)DRD2 (Dopamine D2 Receptor)DRD3 (Dopamine receptor D3)DRD4 (Dopamine D4 Receptor)HRH1 (Histamine H1 Receptor)M1 (Muscarinic acetylcholine receptor M1)CHRM2 (M2)

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