Aphilan R - General Information
Aphilan R is an antihistamine of the piperazine derivative family. [Wikipedia]
Pharmacology of Aphilan R
Aphilan R is a piperazine-derivative antihistamine used as an antivertigo/antiemetic agent. Aphilan R 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.
Aphilan R for patients
Take with food, water, or milk to minimize gastric irritation. Swallow the extended-release dosage form whole (do not crush). If you miss a dose, take as soon as possible but do not take if it is almost time for your next dose. DO NOT double up on doses. Notify your doctor if skin tests using allergens is required as this medication may interfere with test results. Avoid use of alcohol or other CNS depressants while taking this medication. This medication can cause drowsiness or dizziness. Use caution while taking this medicine when driving or using equipment. Talk to your doctor if you are taking appetite suppressants. This medication can cause insomnia. Take the medication a few hours before bedtime if this occurs. This medication can cause dryness of mouth - use sugarless gum, candy, ice, or saliva substitute for relief. Check with your dentist if dry mouth continues for more than 2 weeks.
Aphilan R 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).
Aphilan R 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).
Additional information about Aphilan R
Aphilan R Indication: For prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness and vertigo (dizziness caused by other medical problems).
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.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Buclizine
Synonyms: Buclizina [Inn-Spanish]; Buclizine Dihydrochloride; Buclizine Hydrochloride; Buclizinum [Inn-Latin]; Histabutyzine Dihydrochloride; Vibazine Hydrochloride
Drug Category: Antiemetics; Anticholinergic Agents; Antihistamines
Drug Type: Small Molecule; Approved
Other Brand Names containing Buclizine: Aphilan R; Aphilan-R Base; Bucladin; Bucladin-S; Buclifen; Buclina; Buclodin; Histabuticine; Histabutizine; Histabutyzine; Histabutyzine Dihydrochloride; Histabutyzine Hydrochloride; Hitabutyzyne; Longifene; Posdel; Postafen; Softran; Vibazine;
Absorption: Rapidly absorbed following oral administration.
Toxicity (Overdose): Not Available
Protein Binding: Not Available
Half Life: Not Available
Dosage Forms of Aphilan R: Not Available
Chemical IUPAC Name: 1-[(4-tert-butylphenyl)methyl]-4-[(4-chlorophenyl)-phenylmethyl]piperazine
Chemical Formula: C28H33ClN2
Buclizine on Wikipedia: http://en.wikipedia.org/wiki/Buclizine
Organisms Affected: Humans and other mammals