This chapter reports on the current and prospective anticonvulsant agents: their chemical structures, chemical names, pharmacokinetic parameters, and proposed mechanism(s) of action. Theoretical principles on structure‐activity development are presented as well as a brief explanation of animal testing to predict anticonvulsant activity. A hypothetical anticonvulsant model is presented that, within limits, is useful in elucidating the spatial/structural requirements for anticonvulsant activity against generalized epilepsy.