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Buclizine
drug data and news
Buclizine drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Buclizine | ||
| Brand Names/Synonyms | A 7668; AH 2526; Aphilan R; Aphilan-R Base; Bucladin; Bucladin-S; Buclifen; Buclina; Buclizina [Inn-Spanish]; Buclizine; Buclizine Dihydrochloride; Buclizine Hydrochloride; Buclizine, Hydrochloride; Buclizinum [Inn-Latin]; Buclodin; Histabuticine; Histabutizine; Histabutyzine; Histabutyzine Dihydrochloride; Histabutyzine Hydrochloride; Hitabutyzyne; Longifene; None; Posdel; Postafen; Softran; UCB 4445; UCB-4445; Vibazine; Vibazine Hydrochloride | ||
| Indication | For prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness and vertigo (dizziness caused by other medical problems). | ||
| Sponsored links | Description | Not Available | |
| 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. | ||
| Buclizine News (When available) |
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| Dosage Forms | TABLET (50 mg) | ||
| Drug_Category | Antiemetics; Antihistamine; Anticholinergic; ATC:R06AE01 | ||
| Absorption | Rapidly absorbed following oral administration. | ||
| Interactions |
Interactions for Buclizine: 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). | ||
| Toxicity | Not Available | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 1-[(4-chlorophenyl)-phenyl-methyl]-4-[(4-tert-butylphenyl)methyl]piperazine | ||
| Chemical Formula | C28H33ClN2 | ||
| Molecular Weight | 433.028 g/mol | ||
| Smiles String | CC(C)(C)C1=CC=C(C=C1)CN2CCN(CC2)C(C3=CC=CC=C3)C4=CC=C(C=C4)Cl | ||
| Melting Point | 218 oC (BP) | ||
| Water Solubility | Not Available | ||
| State | Liquid | ||
| LogP/Hphobicity | 7.749 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Hepatic. | ||
| Half Life | Not Available | ||
| Protein Binding [%] | Not Available | ||
| RxList Link | Not Available>RXlist | ||
| Sponsored links | |||
| Drug Reference | http://www.drugs.com/cons/Buclizine.html | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00723 | ||
| CAS Registry Number | 82-95-1 | ||
| KEGG Compound ID | C07777 | ||
| PubChem ID | SID:9979 | ||
| PharmGKB ID | PA448679 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | Not Available |
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