▴ Zolmitriptan is indicated for the acute treatment of migraine with and without aura.▴ The drug is a serotonin 5-HT1B/1Dreceptor agonist that has little or no affinity for other serotonin receptors or receptors of other neurotransmitters.▴ Preclinical studies indicate that zolmitriptan has a novel dual mechanism of action, having effects at both central (trigeminal nucleus caudalis) and peripheral (trigeminovascular system) targets.▴ Studies in volunteers demonstrate that zolmitriptan has relatively good oral bioavailability.▴ Zolmitriptan is effective in alleviating migraine headache and also nonheadache symptoms such as photophobia, phonophobia and nausea.▴ The tolerability of zolmitriptan is good, with the most common adverse experiences being paraesthesia, asthenia, nausea, somnolence and dizziness. Heaviness, tightness or pressure in the chest have been reported, but have not been associated with ECG abnormalities.