The Full Wiki

Meclizine: Wikis

  

Note: Many of our articles have direct quotes from sources you can cite, within the Wikipedia article! This article doesn't yet, but we're working on it! See more info or our list of citable articles.

Encyclopedia

From Wikipedia, the free encyclopedia

Meclizine
Systematic (IUPAC) name
1-[(4-chlorophenyl)(phenyl)methyl]-4-(3-methylbenzyl)piperazine
Identifiers
CAS number 569-65-3
ATC code A04AB04 R06AE05
PubChem 4034
DrugBank APRD00354
ChemSpider 3894
Chemical data
Formula C 25H27ClN2  
Mol. mass 390.948 g/mol
SMILES eMolecules & PubChem
Physical data
Boiling point 230 °C (446 °F)
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life 6 hours
Excretion  ?
Therapeutic considerations
Pregnancy cat. B(US)
Legal status OTC (US); OTC (Canada)
Routes Oral, Insufflation, Sublingual/Buccal.
 Yes check.svgY(what is this?)  (verify)

Meclizine (proposed INN is meclozine) is an antihistamine considered to be an antiemetic.[1] It is sold under the brand names of Bonine, Bonamine, Antivert, Postafen, 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. Note that in Canada, Antivert (no longer available) was a combination of meclizine and nicotinic acid.

Meclizine is a 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 anti-pruritic effects. 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. Related to this is the reported ability of meclizine to potentiate the anti-spasmodic, anti-diarrhoeal, and other effects of diphenoxylate, loperamide, and difenoxin. 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, with some methadone users potentiating their doses with meclizine or hydroxyzine (cyclizine has only just recently been introduced to the U.S. OTC market in 2009, sold under the brand name Marezine at higher prices than generic equivalents of meclizine and hydroxyzine).

Contents

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 infections 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

Due to its possible anticholinergic action, meclizine should be used carefully with patients who suffer from asthma, glaucoma, or an enlarged prostate gland.

References

External links








Got something to say? Make a comment.
Your name
Your email address
Message