Chemical Properties
Off-White Powder
Uses
Used as an antiemetic
Brand name
Bucladin (Stuart).
Definition
ChEBI: Buclizine dihydrochloride is a hydrochloride salt that is obtained by reaction of buclizine with 2 equivalents of hydrogen chloride. It has a role as a central nervous system depressant, a local anaesthetic, a histamine antagonist, a cholinergic antagonist and an antiemetic. It contains a buclizine(2+).
Manufacturing Process
1 mol 4-chlorobenzhydril chloride was heated in toluene to reflux with 1 mol
ethyl ester of piperazine 1-carboxylic acid at about 150°C in a presence of an
excess of triethyl amine. On cooling the triethyl amine hydrochloride was
filtered off, a solvent was removed in vacuum and the residue [(4-chlorophenyl)-
phenyl-methyl]piperazine carboxylic acid ethyl ester was boiled
straight away with potassium hydroxide in ethanol for 48 hours. After
removing ethanol in vacuum to dryness, the residue was dissolved in benzene
and washed with water. The benzene solution was dried, benzene removed in
vacuum. The residue was distilled to give 4-chlorobezhydryl-piperazine. It had
given the desired 1-(p-tert-butylbenzyl)-4-(p-chloro-α-phenylbenzyl)-
piperazine, buclizine, by a reaction with 4-tert-butylbenzyl chloride in the
presence of any halogen hydrochloride acceptor (triethyl amine, sodium or
potassium carbonate and so on). The obtained product had BP: 230°-
240°C/0.001 mm Hg.
Therapeutic Function
Antihistaminic, Antiallergic, Antinauseant,
Tranquilizer, Appetite stimulant
General Description
Buclizine hydrochloride, l-(p-tertbutylbenzyl)-4-(p-chloro-α-phenylbenzyl)piperazinedihydrochloride (Bucladin-S), is a white to slightly yellowcrystalline powder that is insoluble in water. The highlylipid-soluble buclizine has CNS depressant, antiemetic, andantihistaminic properties. This drug has been discontinued inthe United States.
Biological Activity
Buclizine is a piperazine antihistamine and anticholinergic th at exerts its antiemetic and antimotion sickness effects.''Histamine H1 receptor antagonist
