Brands, Medical Use, Clinical Data
Drug Category
- Antiemetics
- Antihistamine
- Anticholinergic
Dosage Forms
Brands / Synonyms
Aphilan R; Aphilan-R Base; Bucladin; Bucladin-S; Buclifen; Buclina; Buclizina [Inn-Spanish]; Buclizine Dihydrochloride; Buclizine Hydrochloride; Buclizine, Hydrochloride; Buclizinum [Inn-Latin]; Buclodin; Histabuticine; Histabutizine; Histabutyzine; Histabutyzine Dihydrochloride; Histabutyzine Hydrochloride; Hitabutyzyne; Longifene; Posdel; Postafen; Softran; Vibazine; Vibazine Hydrochloride
Indications
For prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness and vertigo (dizziness caused by other medical problems).
Pharmacology
Buclizine is a piperazine-derivative antihistamine used as an antivertigo/antiemetic agent. Buclizine is used in the prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness. Additionally, it has been used in the management of vertigo in diseases affecting the vestibular apparatus. Although the mechanism by which buclizine exerts its antiemetic and antivertigo effects has not been fully elucidated, its central anticholinergic properties are partially responsible. The drug depresses labyrinth excitability and vestibular stimulation, and it may affect the medullary chemoreceptor trigger zone. It also possesses anticholinergic, antihistaminic, central nervous system depressant, and local anesthetic effects.
Mechanism of Action
Vomiting (emesis) is essentially a protective mechanism for removing irritant or otherwise harmful substances from the upper GI tract. Emesis or vomiting is controlled by the vomiting centre in the medulla region of the brain, an important part of which is the chemotrigger zone (CTZ). The vomiting centre possesses neurons which are rich in muscarinic cholinergic and histamine containing synapses. These types of neurons are especially involved in transmission from the vestibular apparatus to the vomiting centre. Motion sickness principally involves overstimulation of these pathways due to various sensory stimuli. Hence the action of buclizine which acts to block the histamine receptors in the vomiting centre and thus reduce activity along these pathways. Furthermore since buclizine possesses anti-cholinergic properties as well, the muscarinic receptors are similarly blocked.
Absorption
Rapidly absorbed following oral administration.
Toxicity
Not Available
Biotrnasformation / Drug Metabolism
Hepatic.
Contraindications
Contraindicated in the following: blood disease, heart or blood vessel
disease (may cause more serious conditions to develop), enlarged prostate, urinary tract blockage or difficult
urination (antihistamines may cause urinary problems to become worse), epilepsy (antihistamines may increase the
chance of seizures), glaucoma (may cause a slight increase in inner eye pressure that may worsen the condition,
jaundice (antihistamines may make the condition worse), liver disease (antihistamines may build up in the body, which
may increase the chance of side effects such as muscle spasms), Reye's syndrome (antihistamines may increase the
chance of uncontrolled movements).
Drug Interactions
This drug may interact with alcohol or other CNS depressants (may potentiate the
CNS depressant effects of either these medications or antihistamines), anticholinergics or other medications with
anticholinergic activity (anticholinergic effects may be potentiated when these medications are used concurrently
with antihistamines), and monoamine oxidase (MAO) inhibitors (concurrent use with antihistamines may prolong and
intensify the anticholinergic and CNS depressant effects of antihistamines).
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