Migraine is a common, often disabling, neurovascular disease that has been shown 
to be associated with abnormal serotonergic activity. Drugs that modulate 
serotonin receptors are commonly used in the acute treatment of a migraine 
attack. Zolmitriptan, a 5-hydroxytryptophan(1B/1D) receptor agonist, is once 
such drug that is used in acute migraine therapy. Zolmitriptan is FDA approved 
for the treatment of acute migraine attacks and there is recent literature 
demonstrating its efficacy in the acute treatment of cluster attacks. It is 
rapidly absorbed and is detectable in the plasma within 2 - 5 min for the nasal 
spray formulation and within 15 min for the oral formulations. Zolmitriptan 
reaches peak plasma levels in 2 - 4 h and significant plasma levels are 
maintained for up to 6 h and lower levels for over 15 h. As zolmitriptan's 
metabolism is predominantly hepatic, patients with severe hepatic impairment 
should not receive zolmitriptan. However, only 25% of zolmitriptan is bound to 
plasma proteins and thus it is unlikely for drug interactions involving the 
displacement of highly protein-bound drugs. Zolmitriptan is generally very well 
tolerated and less than half of patients in clinical trials have reported 
adverse events, most of which are mild and transient, although rare serious 
cardiovascular events have been reported with all triptans. When patients are 
appropriately selected, zolmitriptan is both a safe and effective acute care 
migraine treatment. In this review the biological role of serotonin and its 
receptors is covered, followed by an in-depth review of the pharmacodynamics, 
pharmacokinetics and efficacy of zolmitriptan. Finally, the clinical application 
of zolmitriptan's use in patients is dicussed.