Zolmitriptan is a new oral acute treatment for migraine. It is a selective and 
potent agonist at the serotonin (5-HT)(1B/1D) receptor and was developed to 
improve on the oral bioavailability, tissue selectivity and CNS penetration of 
earlier compounds. Animal studies confirmed that these objectives had been 
attained. In man, zolmitriptan is rapidly absorbed after oral administration, 
with at least 75% of the eventual C(max) reached within 1 h. Oral 
bioavailability is approximately 40%. The elimination half-life of zolmitriptan 
is approximately 2.5 h and the primary route of elimination is metabolism, with 
one of the metabolites being pharmacologically active. A consistent 2-h headache 
response rate of 60-70% was observed at doses of 2.5 mg and above. Long-term 
treatment response is high (> 80%) and consistent. In addition, there is 
evidence from electrophysiology in migraineurs that zolmitriptan has a central 
action not shared by sumatriptan. Zolmitriptan is well-tolerated. The nature and 
incidence of the most frequently reported adverse events are similar to those of 
other 5-HT(1B/1D) agonists. Long-term zolmitriptan usage was associated with an 
improvement in quality of life. Zolmitriptan is a suitable first-line drug for 
acute treatment for migraine.