For the acute treatment of adult migraine with or without auras.
Zolmitriptan binds with high affinity to human 5-HT<sub>1B</sub> and 5-HT<sub>1D</sub> receptors leading to cranial blood vessel constriction. Current theories proposed to explain the etiology of migraine headache suggest that symptoms are due to local cranial vasodilatation and/or to the release of sensory neuropeptides (vasoactive intestinal peptide, substance P and calcitonin gene-related peptide) through nerve endings in the trigeminal system. The therapeutic activity of zolmitriptan for the treatment of migraine headache can most likely be attributed to the agonist effects at the 5HT1B/1D receptors on intracranial blood vessels (including the arterio-venous anastomoses) and sensory nerves of the trigeminal system which result in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release.
Mean absolute oral bioavailability is approximately 40%. Food has no affect on the rate and extent of absorption.
The mean elimination half-life of zolmitriptan and of the active N-desmethyl metabolite is 3 hours.
* 8.4±3.3 L/kg
* 25.9 mL/min/kg