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INFOMATION:
Meclizine (INN,[1] or meclozine) is an antihistamine considered to be an antiemetic. It is sold under the brand names Bonine, Bonamine, Antivert, Postafen, Sea Legs, and Dramamine (Less Drowsy Formulation). Emesafene is a combination of meclizine (1/3) and pyridoxine (2/3). In Canada, Antivert Tab (which is no longer available) was a combination of meclizine and nicotinic acid.[2]
Classification
Meclizine is a first-generation antihistamine of the piperazine class. It is structurally and pharmacologically similar to buclizine, cyclizine, and hydroxyzine, but has a shorter half-life of six hours compared to cyclizine and hydroxyzine with about 20 hours (though half-life should not be confused with duration). It is used as an antivertigo/antiemetic agent, specifically in the prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness. 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).
Mechanism of action
Meclizine is an antagonist at H1 receptors. It possesses anticholinergic, central nervous system depressant, and local anesthetic effects. Its antiemetic and antivertigo effects are not fully understood, but its central anticholinergic properties are partially responsible. The drug depresses labyrinth excitability and vestibular stimulation, and it may affect the medullary chemoreceptor trigger zone.
Uses
Meclizine is approved by the U.S. Food and Drug Administration (FDA) to treat symptoms of motion sickness and for management of vertigo that stems from diseases affecting the vestibular system. Meclizine's safety and efficacy in children younger than 12 years old has not been established, therefore use in this population is not recommended. Also, meclizine should be taken with caution in the elderly (older than 65 years) because of increased risk of confusion and amnesia.
Motion sickness
Meclizine is effective in inhibiting the symptoms of motion sickness, such as nausea, vomiting, and dizziness. The recommended dose is 25–50 mg orally, taken one hour before travel. The dose may be repeated every 6 hours as needed.
The drug is also safe for treating nausea in pregnancy and is a first-line therapy for this use. Doxylamine is similarly safe.
Vertigo
Meclizine may be effective in relieving vertigo experienced as a result of inner ear infections or other conditions. The recommended dose is 25–100 mg per day orally, in divided doses.
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