A comparison of the pharmacokinetics and tolerability of the novel antimigraine compound zolmitriptan in adolescents and adults

This open-label, parallel-group study assessed pharmocokinetics and tolerab ility of zolmitriptan, a 5-HT1B/1D agonist for the acute treatment of migra ine, and its active metabolite, 183C91, in adolescents compared with adults . Twenty-one healthy adolescent and 18 healthy adult volunteers (with and w ithout history off migraine) received a single 5-mg dose of zolmitriptan. M ean ages were 14.5 years (range 12-17) for adolescents (13 girls, 8 boys) a nd 39.1 years (range 18-65) for adults (12 women, 6 men). The area under th e curve (AUC) and highest observed plasma concentration (C-max) of zolmitri ptan were similar in both age groups; the half life was 3.01 hours in adole scents versus 3.75 hours in adults. The AUC and Cmax of 183C91, however, we re 36% and 39% higher in adolescents, respectively; the half-life was simil ar in both age groups. Adverse events were similar in both groups in terms of nature, intensity, and frequency. Exposure to zolmitriptan was not signi ficantly different in adolescents compared with adults, but a shorter half- life in adolescents suggests faster elimination in this age group. Exposure to 183C91 was higher in adolescents, suggesting that formation of the meta bolite is at least one of the elimination routes of zolmitriptan that occur s at a faster rate in adolescents.