Meclizine (Antivert)
Antivert®, Bonine®, Dramamine® Non-Drowsy | Bonikraft™ | Dramamine® Less Drowsy | Meclicot™ | Medivert™ | Meni-D™
Classification:
Antihistamines
Gastrointestinal Agents
Neurological Agents
Description: Meclizine is a piperazine-derivative H1-receptor antagonist. Meclizine is structurally and pharmacologically similar to buclizine, cyclizine, and hydroxyzine. It is used as an antivertigo/antiemetic agent, specifically, 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. However, the efficacy of meclizine in these conditions has not been established. While prophylactic use of meclizine is most effective in the treatment of motion sickness, other factors such as patient age, and type, severity, and duration of motion influence its effectiveness. It has been suggested that meclizine causes fewer anticholinergic effects than scopolamine. Meclizine was approved by the FDA in 1953.
Antivert Tablets(Tab 50 mg)
Mechanism of Action: Meclizine is an antagonist at H1-receptors. It also possesses anticholinergic, central nervous system depressant, and local anesthetic effects. Although the mechanism by which meclizine 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.
Pharmacokinetics: In general, H1-blockers are well absorbed after oral administration. The onset of action of meclizine is about 1 hour, with effects lasting between 8 - 24 hours. Distribution of meclizine has not been fully characterized. Meclizine may be excreted into breast milk; however, it is not known whether it crosses the placenta. Metabolism in humans is unknown, although animal studies suggest hepatic metabolism. The plasma half-life in humans is about 6 hours. Meclizine is excreted in the urine as metabolites and in the feces as unchanged drug.
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[ Revised 3/15/2005 9:13:00 AM ]
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