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Current theories on the aetiology of migraine headache suggest that the symptoms are due to local cranial vasodilatation and/or to the release of vasoactive and pro-inflammatory peptides from sensory nerve endings in an activated trigeminal systemThe therapeutic activity of rizatriptan in migraine can most likely be attributed to agonist effects at 5-HT 1B/1D receptors on the extracerebralintracranial blood vesselswhich become dilated during a migraine attackand on nerve terminals in the trigeminal systemActivation of these receptors results in cranial vessel constrictioninhibition of neuropeptide release and reduced transmission in trigeminal pain pathways.

In a study evaluating subjects undergoing cardiac catheterizationan 18increase in mean pulmonary artery pressure was seen following dosing with another 5-HT 1 agonist.

The area under the curveAUCof rizatriptan is approximately 30higher in females than in malesThe presence of a migraine headache did not appear to affect the absorption or pharmacokinetics of rizatriptanFood has no significant effect on the bioavailability of rizatriptan but delays the time to reach peak concentration by an hourThe T max is delayed by approximately 1 hour when the tablets are administered in the fed stateIn clinical trialsrizatriptan was administered without regard to food.

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