Interaction of Rizatriptan with Rat Liver Monoamine Oxidases

Introduction Migraine is a common neurological disorder characterized by paroxysmal headache, usually unilateral, and frequently accompanied by generalized sensorial hyperaesthesia and gastrointestinal disturbances such as nausea 1. Migraine is thought to be caused by neurogenic vascular and inflamatory mechanisms and it has been suggested that serotonin (5-hydroxytryptamine; 5-HT), a neurotransmitter which has a complex role in basic processes such as sleep, memory, mood, hormone regulation, vascular and gastrointestinal smooth muscle contraction, may be involved in the genesis of migraine attacks 2,3. Recently, successful treatment of migraine has been achieved by administration of selective 5HT1B/1D agonists (triptans) such as sumatriptan, zolmitriptan, naratriptan, rizatriptan, almotriptan, and eletriptan 4,5. Rizatriptan (MK-0462) (Figure 1) is an orally active, highly selective 5-HT1B/1D agonist that constricts intracranial, extracerebral blood vessels and inhibits the neuropeptides from perivascular nerves, thus causes vasoconstriction on dilated Hacettepe University, Journal of Faculty of Pharmacy Volume 24 / Number 1 / January 2004 / pp. 25-35