The name ‘serotonin’ is derived from the vasoconstrictor substance released from a clot into the serum. Serotonin or 5 HT is considered to be an important neurotransmitter, a local gut hormone, causative agent of migraine headache as well as mediator of ‘carcinoid syndrome’ of carcinoid tumor and component of platelet aggregation. Migraine is characterized by recurrent moderate to severe, throbbing unilateral headache with or without preliminary autonomic symptoms or aura. Migraine may be classified into two types following as the classic type associated with aura and common type. This chapter covers the treatment of migraine, comparison of the pharmacological parameters of the triptans, adverse effects, and other drugs used in migraine.