Meclizine and Meclozine: Difference between pages
(Difference between pages)
Content deleted Content added
mNo edit summary |
|||
| Line 1: | Line 1: | ||
#REDIRECT [[Meclizine]] |
|||
{{article issues |
|||
|cleanup=October 2009 |
|||
|refimprove=October 2009 |
|||
}} |
|||
{{drugbox |
|||
| verifiedrevid = 304592550 |
|||
| IUPAC_name = (''R/S'')-1-[(4-chlorophenyl)(phenyl)methyl]-4-(3-methylbenzyl)piperazine |
|||
| image = Meclizine.svg |
|||
| width = 200px |
|||
| CASNo_Ref = {{cascite}} |
|||
| CAS_number = 569-65-3 |
|||
| ChemSpiderID = 3894 |
|||
| ATC_prefix = A04 |
|||
| ATC_suffix = AB04 |
|||
| ATC_supplemental = {{ATC|R06|AE05}} |
|||
| PubChem = 4034 |
|||
| DrugBank = APRD00354 |
|||
| smiles = Cc1cccc(c1)CN2CCN(CC2)C(c3ccc(Cl)cc3)c4ccccc4 |
|||
| C=25 | H=27 | Cl=1 | N=2 |
|||
| molecular_weight = 390.948 g/mol |
|||
| boiling_point = 230 |
|||
| bioavailability = |
|||
| protein_bound = |
|||
| metabolism = |
|||
| elimination_half-life = 6 hours |
|||
| pregnancy_US= B |
|||
| legal_status = [[Over-the-counter drug|OTC]] ([[United States|US]]); [[Over-the-counter drug|OTC]] ([[Canada]]) |
|||
| routes_of_administration = Oral, Insufflation, Sublingual/Buccal. |
|||
}} |
|||
'''Meclizine''' (proposed [[International Nonproprietary Name|INN]], or '''meclizine''') is an [[antihistamine]] considered to be an [[antiemetic]].<ref name="pmid15272053">{{cite journal |author=Huang W, Zhang J, Wei P, Schrader WT, Moore DD |title=Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for human CAR |journal=Molecular endocrinology (Baltimore, Md.) |volume=18 |issue=10 |pages=2402–8 |year=2004 |month=October |pmid=15272053 |doi=10.1210/me.2004-0046 |url=http://mend.endojournals.org/cgi/pmidlookup?view=long&pmid=15272053}}</ref> It is sold under the brand names of '''Bonine''', '''Bonamine''', '''Antivert''', '''Postafen''', '''Sea Legs''', and '''Dramamine (Less Drowsy Formulation)''', and is most commonly used to inhibit [[nausea]] and [[vomiting]]. '''Emesafene''' is a combination of meclizine (1/3) and [[pyridoxine]] (2/3). An alternative to [[dimenhydrinate]] (Dramamine, Gravol, Gravamin, and Vertirosan), meclizine is considered to be equally effective, but with reduced side effects. In Canada, Antivert (no longer available) was a combination of meclizine and [[nicotinic acid]]. |
|||
Meclizine is the first-generation antihistamine of the [[piperazine]] class. It differs from the protoype of this class, [[cyclizine]], primarily in having an average half-life of 6 hours vs. 20 hours for cyclizine (though half-life should not be confused with frequency of duration). Meclizine is less [[anticholinergic]] than many other antihistamines and other agents used for their [[anti-emetic]] and [[antipruritic|anti-pruritic]] effects.{{Fact|date=March 2009}} Along with the aforementioned efficacy against nausea and itching, meclizine also shares the [[anxiolytic]], analgesic-sparing (potentiating), [[sedative]], and other effects of its chemical relatives cyclizine and [[hydroxyzine]] to varying extents.{{Fact|date=March 2009}} Related to this is the reported ability of meclozine to potentiate the anti-spasmodic, [[anti-diarrhoeal]], and other effects of [[diphenoxylate]], [[loperamide]], and [[difenoxin]].{{Fact|date=March 2009}} Meclizine is sometimes combined with opioids, especially ones of the open-chain class like [[methadone]], [[dextropropoxyphene]] and [[dipipanone]] (originally combined with meclizine's parent drug cyclizine, the brand name of this combination is Diconal). The trend of mixing piperazine antihistamines has caught on in the United States{{fact|date=January 2010}}, with some methadone users potentiating their doses with meclizine or [[hydroxyzine]] (cyclizine has only just recently been introduced to the U.S. [[Over-the-counter drug|OTC]] market in 2009, sold under the brand name Marezine at higher prices than generic equivalents of meclizine and hydroxyzine). |
|||
==Uses== |
|||
===Motion sickness=== |
|||
Meclizine is effective in inhibiting the symptoms of [[motion sickness]], such as nausea, vomiting, and dizziness. |
|||
===Vertigo=== |
|||
Meclizine may be effective in relieving [[vertigo]] experienced as a result of [[inner ear infection]]s or other conditions. |
|||
==Risks of use== |
|||
===Drowsiness=== |
|||
Drowsiness may result as a side effect of taking meclizine. While the effects are less than those of [[dimenhydrinate]], users are advised not to operate heavy machinery while under the influence. The consumption of alcohol while under the influence of meclizine may result in additional drowsiness. |
|||
===Anticholinergics=== |
|||
Because of its possible [[anticholinergic]] action, meclizine should be used carefully with patients who suffer from [[asthma]], [[glaucoma]], or an [[enlarged prostate]] gland. |
|||
==References== |
|||
{{reflist}} |
|||
==External links== |
|||
*[http://bioinf.charite.de/superdrug/fullinfo.php?cas=000569653 University of Berlin's Institute of Biochemistry] |
|||
*[http://www.numarkpharmacists.com/hn/Drug/Meclizine.htm Numark Pharmacies Information Page on Meclozine] |
|||
*[http://www.rxlist.com/cgi/generic/mecliz_wcp.htm Rxlist Medical Dictionary] |
|||
{{Antiemetics}} |
|||
{{Cholinergics}} |
|||
{{Histaminergics}} |
|||
{{Piperazines}} |
|||
[[Category:Antiemetics]] |
|||
[[Category:Piperazines]] |
|||
[[Category:Organochlorides]] |
|||
[[de:Meclozin]] |
|||
[[fr:Méclizine]] |
|||
[[hu:Meklizin]] |
|||
[[ja:メクリジン]] |
|||
[[nn:Meklozin]] |
|||
[[th:มีโคลซีน]] |
|||
Revision as of 00:53, 8 November 2010
Redirect to: