Drug intelligence / Profile preview

azaperone

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

Overview

Azaperone is a pyridinylpiperazine and butyrophenone neuroleptic drug with sedative, tranquilizing, and antiemetic effects. It is primarily used as a veterinary tranquilizer, especially in pigs and occasionally in elephants. Its use in humans as an antipsychotic is rare. Azaperone acts mainly as a dopamine receptor antagonist (notably at the D3 dopamine receptor), but also exhibits antihistaminic, anticholinergic, and alpha-adrenergic blocking properties. The drug produces sedation by inhibiting central dopaminergic pathways and may cause hypotension due to its peripheral vasodilatory effects[1][2][5]. It is administered intramuscularly, metabolized hepatically, and has an elimination half-life of about 4 hours[2].

Brand names
StresnilSuicalm
Other names
Azaperon
02

Targets

HRH1 (Histamine H1 Receptor)ADRA1A (α1A)DRD3 (Dopamine receptor D3)mAChR (Muscarinic acetylcholine receptors)

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