Drug intelligence / Profile preview

buclizine

Development stage
Unknown
Lead developer
Stuart Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

Buclizine is a first-generation piperazine-derived antihistamine with anticholinergic and moderate sedative properties. It acts primarily as an H1-histamine receptor antagonist, interfering with the action of histamine at the H1 receptor to reduce allergic symptoms and inflammation. Buclizine also exhibits central anticholinergic effects, which contribute to its antiemetic (prevention of nausea and vomiting) and antivertigo actions by depressing labyrinth excitability, vestibular stimulation, and possibly affecting the medullary chemoreceptor trigger zone. It is mainly used for the prevention and treatment of motion sickness, vertigo associated with vestibular disorders, migraine (in combination with analgesics), and occasionally in other conditions such as allergic reactions. Although it has been promoted as an appetite stimulant in children, this indication lacks robust clinical evidence[1][2][4][5][6][7].

Brand names
Bucladin-SHistabuticineHistabutizineHistabutyzine
Other names
buclizine hydrochloride
02

Targets

mAChR (Muscarinic acetylcholine receptors)HRH1 (Histamine H1 Receptor)

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