Cetirizine
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Cetirizine
Zyrtec, Zyrtec-D
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Pharmacy
Starting dose
10 mg PO once daily (5 mg in older adults or if sedation occurs)
Preparations
5 mg, 10 mg tablets; 5 mg, 10 mg chewables; 1 mg/mL oral syrup; OTC
US FDA Max
10 mg/d (adults)
Pharmacology
Routes
Oral
Onset
30-60 minutes
Duration
24 hours
Half-life
8-10 hours (longer in elderly and renal impairment)[1]
Bioavailability
High (oral); not significantly affected by food[1]
Pregnancy
Generally considered safe; widely used. Levocetirizine (the R-enantiomer) is an alternative with similar safety.[citation needed]
Legal status
OTC in US
Purported mechanism
Cetirizine is a selective peripheral H1 receptor antagonist; as a carboxylated zwitterion at physiologic pH it crosses the blood-brain barrier far less than first-generation antihistamines, producing materially less sedation while retaining peripheral antihistaminic activity.0 Minimal CYP metabolism; mostly renally cleared unchanged. Cetirizine is the active racemate; levocetirizine is the active R-enantiomer marketed separately[1].
References
edit- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Zyrtec (cetirizine HCl), Johnson & Johnson Consumer, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019835s062lbl.pdf