Astepro is unique among antihistamines presently available in the USA because it is administered by nasal spray. After intranasal administration, its systemic bioavailability is approximately 40%. Astepro has an onset of action within the first hour of administration and reaches peak activity at 1–3 hours after administration. Duration of activity is about 12 hours. Intranasal administration results in maximal plasma concentrations in 2–3 hours. Astepro has an active metabolite, desmethylAstepro, which probably extends the duration of action of the drug. The half-life of the parent compound is 22 hours and that of the active metabolite 54 hours. Ten days after oral administration of 4 mg radiolabeled Astepro, approximately 24% of the radioactivity was recovered in the urine and 75% in the feces.
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