Preclinical studies have shown that
zolmitriptan is a selective
serotonin 5-HT(1B/1D) receptor agonist (
triptan). Randomised, placebo-controlled, double-blind trials in patients with
migraine have shown that
zolmitriptan has good efficacy measured using 2 h response and
pain-free rates.
Migraine-associated symptoms, including
nausea,
photophobia and
phonophobia, are also improved with
zolmitriptan. Oral
zolmitriptan (2.5 and 5 mg) has an onset of action within 45 min and efficacy is sustained in most patients who respond at 2 h. The orally-disintegrating
zolmitriptan tablet has the advantage that it may be taken immediately, without the need for additional fluids, any time a
migraine headache occurs. Patients may benefit in terms of improved efficacy from the convenience of the disintegrating
tablet, since there is evidence that taking
triptan therapy as early as possible in an attack is advantageous. For similar reasons, as well as improved efficacy, a
nasal spray formulation is in development.
Zolmitriptan is effective in the treatment of
migraine associated with menses and
migraine with aura. There is no tachyphylaxis following repeated doses for multiple attacks of
migraine over a prolonged period of time. Compared to placebo, the incidence of persistent
migraine headache is reduced by
zolmitriptan and recurrent
migraine headache occurs less frequently.
Zolmitriptan has also shown efficacy in the treatment of persistent and/or recurrent
migraine headache. Comparative clinical studies have shown overall that
zolmitriptan has similar or superior efficacy to
sumatriptan in the treatment of
migraine. Specifically,
zolmitriptan 2.5 mg was significantly more effective than
sumatriptan 25 or 50 mg according to a number of end points, including
headache response at 2 h. Oral
zolmitriptan is also effective in the acute treatment of
cluster headache.
Zolmitriptan is generally well tolerated, with most adverse events being mild-to-moderate, transient and resolving without intervention or the need for treatment withdrawal. The consistent efficacy in treating all types of
migraine and the choice of available formulations make
zolmitriptan acceptable to patients and a suitable first-line
therapy for the treatment of
migraine.