Drug intelligence / Profile preview

promazine

Development stage
Discontinued
Lead developer
Sanofi
Modality
Small Molecules
01

Overview

Promazine is a first-generation (typical) antipsychotic of the phenothiazine class. It is primarily used as a short-term adjunct for the treatment of moderate to severe psychomotor agitation and restlessness, particularly in elderly patients. Its antipsychotic effect is relatively weak compared to other agents in its class and it is not commonly used for general psychiatric indications. Promazine acts mainly by antagonizing dopamine receptors (types 1, 2, and 4), serotonin receptors (5-HT2A and 5-HT2C), muscarinic acetylcholine receptors (M1–M5), alpha(1)-adrenergic receptors, and histamine H1-receptors. The drug’s sedative effects are attributed to its antihistaminic and anticholinergic activity; it has lower risk of extrapyramidal side effects due to greater activity at serotonin than dopamine type-2 receptors[1][3][4]. Promazine was approved for medical use in the United States in the 1950s but is no longer commercially available there; it remains available elsewhere and also sees use as a tranquilizer in veterinary medicine[4].

Brand names
SparineTranquazine
Other names
promazine hydrochloride
02

Targets

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

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