Zolmitriptan is used to treat the symptoms of migraine headaches .
Zolmitriptan is in a class of medications called selective serotonin receptor agonists. It works by narrowing blood vessels around the brain, stopping pain signals from being sent to the brain.
Zolmitriptan does not prevent migraine attacks or reduce the number of headaches .
In clinical studies with Zolmitriptan conventional tablets the onset of efficacy is apparent from one hour.
Zolmitriptan is rapidly and well absorbed (at least 64%) after oral administration to man.
The mean absolute bioavailability of the parent compound is approximately 40%.
There is an active metabolite (the N-desmethyl metabolite) which is also a 5HT 1B/1D receptor agonist and is 2 to 6 times as potent, in animal models, as Zolmitriptan.
In healthy volunteers, 75% of Cmax is achieved within 1 hour, and after this the concentration of Zolmitriptan in plasma is maintained at approximately this level until 4-5 hours after dosing.
Zolmitriptan absorption is unaffected by the presence of food. There was no evidence of accumulation on multiple dosing of Zolmitriptan.
Zolmitriptan is eliminated largely by hepatic biotransformation followed by urinary excretion of the metabolites.
Over 60% of a single oral dose is excreted in the urine and about 30% in faeces mainly as unchanged parent compound.