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Loratadine

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From Pharmacopedia

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Summary
Common uses
Allergic rhinitis0, Chronic idiopathic urticaria0
Pharmacy
Starting dose
10 mg PO once daily
Preparations
10 mg tablets; 5 mg ODT and chewables; 1 mg/mL oral syrup; combo Claritin-D (with pseudoephedrine, behind-counter)
US FDA Max
10 mg/d (adults)
Pharmacology
Routes
Oral
Onset
1-3 hours (slower onset than cetirizine; symptom relief somewhat less)
Duration
24 hours
Half-life
~8 hours (parent); ~28 hours (desloratadine, the active metabolite, marketed separately as Clarinex)[1]
Bioavailability
High (oral; food prolongs absorption modestly)[1]
Pregnancy
Generally considered safe; widely used. Loratadine and cetirizine are the most-recommended 2nd-gen H1s in pregnancy and lactation.[citation needed]
Legal status
OTC in US
Purported mechanism
Loratadine is a selective peripheral H1 receptor antagonist with very limited blood-brain barrier penetration, producing antihistaminic effect without significant sedation; it is metabolized by CYP3A4 and CYP2D6 to desloratadine, the longer-half-life active metabolite.0 Less reliably anticholinergic than first-generation H1s; minimal antiemetic effect. Desloratadine (Clarinex) is the active enantiomer-of-metabolite version marketed as a Rx alternative.

References

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  1. 1.0 1.1 FDA Prescribing Information, Claritin (loratadine), Bayer, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019835s050lbl.pdf