Meclizine
Meclizine. First-generation H1 antagonist + mild anticholinergic — selectively reduces vestibular nausea / motion sickness. OTC for motion… Oral half-life 7.4 h.
First-generation H1 antagonist + mild anticholinergic — selectively reduces vestibular nausea / motion sickness. OTC for motion sickness; off-label for vertigo + Meniere disease.
PK: the half-life of 7.4 h is verbatim but needs its population stated, which it did not have: the study is in CHILDREN AGED 5 TO 10 WITH ACHONDROPLASIA, dosed AFTER MEALS, at steady state after fourteen days, and 7.4 h is the 12.5 mg cohort alone. The same programme fasted single-dose value is 8.5 h. A FIXED ABSORPTION RATE IS INDEFENSIBLE because food nearly DOUBLES the time to peak, from 1.7 h fasted to 3.7 h fed, and the stored rate of 1 was not even a collision with either — a bare default. F 0.5 IS NOT MEASURABLE IN HUMANS: there is no intravenous meclizine formulation and no human intravenous study exists, the only such comparison being in rats and dogs. V 140 L appears in no human abstract. Metabolism is dominated by CYP2D6 with large between-subject variability, and absorption rate is formulation-dependent while exposure is not.
Pharmacokinetics
- Oral — t½ 7.4 h
Sources: PMID:37428729, PMID:32282831