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Meclizine

From Pharmacopedia
(Redirected from Antivert)
Meclizine
Antivert (Rx), Bonine (OTC), Dramamine Less Drowsy (OTC)

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Summary
Common uses
Motion sickness prevention (OTC and FDA)0, Vertigo (FDA)0, Symptomatic Meniere disease (off-label)0
Pharmacy
Starting dose
Motion sickness: 25-50 mg PO 1 hour before travel, repeat every 24 hours as needed. Vertigo: 25-100 mg/day divided
Preparations
Tablets 12.5, 25 mg; chewable tablets 25 mg
US FDA Max
100 mg/day (vertigo)
Pharmacology
Routes
Oral
Onset
~1 hour
Duration
12-24 hours (long for an antihistamine)
Half-life
~6 hours[1]
Bioavailability
~25% (oral)[1]
Pregnancy
Older agent with substantial use experience; observational signals reassuring for first-trimester exposure.[citation needed]
Legal status
OTC as Bonine and Dramamine Less Drowsy; Rx-only as Antivert
Purported mechanism
First-generation H1 receptor antagonist with central nervous system penetration. Additional moderate anticholinergic activity contributes to the antiemetic and antivertigo effects, acting at central vestibular pathways and the chemoreceptor trigger zone of the area postrema. Less sedating than diphenhydramine on a milligram basis, but more sedating than the second-generation non-sedating antihistamines.0 Anticholinergic burden (dry mouth, blurred vision, urinary retention, cognitive effects) is the principal adverse-event concern and the basis for Beers-list cautions in elderly patients[1].

References

  1. 1.0 1.1 1.2 FDA Prescribing Information, Antivert (meclizine hydrochloride), Pfizer/various, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/010721s059lbl.pdf