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Levocetirizine

From Pharmacopedia
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Levocetirizine
Xyzal, Xyzal Allergy 24HR (OTC)

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Summary
Common uses
Allergic rhinitis (seasonal and perennial)0, Chronic idiopathic urticaria0
Pharmacy
Starting dose
5 mg PO once daily in the evening
Preparations
5 mg tablets; 2.5 mg/5 mL oral solution; OTC
US FDA Max
5 mg/d (adults)
Pharmacology
Routes
Oral
Onset
30-60 minutes
Duration
24 hours
Half-life
~8 hours (longer in elderly and renal impairment)[1]
Bioavailability
~85-90% (oral; not significantly affected by food)[1]
Pregnancy
Generally considered safe; widely used. Cetirizine and loratadine remain the more-studied alternatives.[citation needed]
Legal status
OTC in US
Purported mechanism
Levocetirizine is the active R-enantiomer of racemic cetirizine; it binds H1 receptors with ~2× the affinity of the racemate at half the dose, with minimal CNS penetration and minimal anticholinergic burden.0 Mostly renally cleared unchanged; dose-reduce in renal impairment. Like cetirizine, retains slightly more sedation than fexofenadine in some users[1].

References

  1. 1.0 1.1 1.2 FDA Prescribing Information, Xyzal (levocetirizine dihydrochloride), Sanofi, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022064s016lbl.pdf