Migraine is a disease of neurovascular origin that affects the quality of life of more than one billion people and ranks sixth among the most common diseases in the world. Migraine is characterized by a moderate or severe recurrent and throbbing headache, accompanied by nausea, vomiting, and photo-phonophobia. It usually starts in adolescence and is twice as common in women as in men. It is classified as with or without aura and has chronic or acute treatment types according to the frequency of occurrence. In acute treatment, analgesics that relieve pain in the fastest way are preferred, while there are different options in chronic treatment. While non-specific methods were used in the treatment of migraine until the 1950s, triptans, ditans, and CGRP-receptor-dependent therapies (monoclonal antibodies and gepants) started to be used in the clinic more recently. In this Review, we focus on the synthesis, side effects, and pharmacological and pharmacokinetic properties of FDA-approved drugs used in acute and preventive-specific treatment of migraine.