Drug intelligence / Profile preview

propiomazine

Development stage
Unknown
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous, Intramuscular
01

Overview

Propiomazine is a phenothiazine derivative classified as an antihistamine and sedative. It is primarily used to treat insomnia and to provide sedation or relieve anxiety before or during surgery and other procedures. Propiomazine may also be used in combination with analgesics during labor. While structurally related to antipsychotics like clozapine and sometimes described as an atypical antipsychotic agent, it is not therapeutically used as a neuroleptic because it does not block dopamine receptors strongly enough for that purpose. Its main pharmacological action is antagonism of histamine H1 receptor (antihistaminic effect), which accounts for its sedative properties. Additionally, propiomazine acts as an antagonist at dopamine (D1, D2, D4), serotonin (5-HT2A and 5-HT2C), muscarinic acetylcholine (M1–M5), and alpha-1 adrenergic receptors[2][3][6][8]. The drug has oral bioavailability of about 33%, high protein binding (~81%), and an elimination half-life of approximately 9 hours[3][6].

Brand names
PropavanLargonIndormSerentinDorevaneDorevan
Other names
propionylpromethazine
02

Targets

HRH1 (Histamine H1 Receptor)

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