Zolmitriptan is a selective 5-HTIB / ID receptor agonist. Excited by intracranial vascular (including arteriovenous anastomoses) and 5-HTIB trigeminal sympathetic nervous system on / ID receptors, causing cerebral vasoconstriction and inhibit the release of pro-inflammatory neuropeptides. For adult aura or migraine with aura treatment.
Zolmitriptan is rapidly absorbed after oral administration. 1 hour up to the peak plasma concentration of 75%, followed by plasma concentration for 4 to 6 hours. The average absolute bioavailability of the parent compound is about 40%. One active metabolite (N- desmethyl metabolite), also a 5HT1D agonist. Animal test results showed that the efficacy of 2 to 6 times Zolmitriptan. Healthy adults after a single dose of zolmitriptan in the range of 2.5 ~ 50mg dose, zolmitriptan and area under the curve and peak plasma concentration of the active metabolite are dose proportional. Zolmitriptan absorption is not affected by food.
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