Meclizine
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Meclizine
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| Systematic (IUPAC) name | |
| 1-[(4-chlorophenyl)(phenyl)methyl]-4-(3-methylbenzyl)piperazine | |
| Identifiers | |
| CAS number | |
| ATC code | A04 R06 |
| PubChem | |
| DrugBank | |
| ChemSpider | |
| Chemical data | |
| Formula | C25H27ClN2 |
| Mol. mass | 390.948 g/mol |
| SMILES | & |
| 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 | |
| Routes | Oral |
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 a 12-hour duration of action.[citation needed] Meclizine is less anticholinergic than many other antihistamines and other agents used for their anti-emetic and anti-pruritic effects.[citation needed] 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.[citation needed] Related to this is the reported ability of meclizine to potentiate the anti-spasmodic, anti-diarrhoeal, and other effects of diphenoxylate, loperamide, and difenoxin. Yet another use for Meclizine is for the potentiation of opioids, especially ones of the open-chain class like Methadone, Dextropropoxyphene and Dipipanone (originally combined with Meclizine's parent drug Cyclizine, which proved to provide a very euphoric rush when injected. The brand name of this combo-drug was/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 (as Cyclazine isn't available in the U.S.).[citation needed]
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[edit] Uses
[edit] Motion sickness
Meclizine is effective in inhibiting the symptoms of motion sickness, such as nausea, vomiting, and dizziness.
[edit] Vertigo
Meclizine may be effective in relieving vertigo experienced as a result of inner ear infections or other conditions.
[edit] Risks of use
[edit] 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.
[edit] Anticholinergics
Due to its possible anticholinergic action, meclizine should be used carefully with patients who suffer from asthma, glaucoma, or an enlarged prostate gland.
[edit] References
- ^ Huang W, Zhang J, Wei P, Schrader WT, Moore DD (October 2004). "Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for human CAR". Molecular endocrinology (Baltimore, Md.) 18 (10): 2402–8. doi:. PMID 15272053. http://mend.endojournals.org/cgi/pmidlookup?view=long&pmid=15272053.
[edit] External links
- University of Berlin's Institute of Biochemistry
- Numark Pharmacies Information Page on Meclizine
- Rxlist Medical Dictionary
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