Abstract: Epilepsy is one of the most common neurological conditions, which is characterized by recurrent unprovoked seizures. Drug treatment is still the main method for the disease. Although remarkable progress has been made in the development of antiepileptic drugs in recent years, there is still a poor curative effect on patients with refractory epilepsy. This review will focus on the current status and pathogenesis of epilepsy, as well as the antiepileptic drugs (targeting sodium channels, calcium channels, potassium channels, and the balance of γ-aminobuyric acid/glutamate system, respectively) that have been developed based on classical epileptogenic mechanisms. Further the antiepileptic drugs acting on new targets (epigenetic interferers, synaptic vesicle glycoprotein 2A modulators, mammalian target of rapamycin signal pathway blockers, carbonic anhydrase inhibitors, cannabidiol and adenosine inhibitors) have also been discussed.