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Zolmitriptan Intranasal: A Review of the Pharmacokinetics
Migraine is a common disabling neurological disorder, associated with headache, nausea, and on
occasions vomiting. Zolmitriptan is a widely available serotonin receptor agonist with a long track
record in clinical studies and in the treatment of acute migraine. A nasal formulation has been
developed that has clear evidence for local absorption, resulting in plasma drug concentrations within
2 minutes of dosing, central nervous system penetrations 3 minutes later, and a significant efficacy
benefit versus placebo 10 to 15 minutes after dosing. Intranasal zolmitriptan offers advantages to
migraineurs, particularly those seeking a more rapid onset of effect without wishing to self-inject,
or those with gastrointestinal upset. The comparison of pharmacokinetic and clinical data available
from different formulations of zolmitriptan contributes both to the understanding of its mode of action
and the characteristics required of an acute migraine treatment if it is to meet patient needs.
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