In recent years, with the introduction of new molecules into the arsenal of psychiatric therapy, the historical significance of classical psychotropic drugs to modern society has been lost. Keep in mind that its modern history is very short, born in the 1950s with the introduction of lithium, chlorpromazine, and imipramine, known as the "revolution of psychopharmacology." The purpose of this work it to review how psychoactive substances have been discovered, developed, and applied over the millennia. The text presents the drugs that are used in medicine, their origins, the principles of biological theories of mental disorders, and contribution of basic research.