The present work offers an analysis of the historical development of the discovery and use of
barbiturates in the field of psychiatry and neurology, a century after their clinical introduction. Beginning with the synthesis of malonylurea by von Baeyer in 1864, and up to the decline of
barbiturate therapy in the 1960s, it describes the discovery of the
sedative properties of
barbital, by von Mering and Fischer (1903), the subsequent synthesis of
phenobarbital by this same group (1911), and the gradual clinical incorporation of different
barbiturates (
butobarbital,
amobarbital,
secobarbital,
pentobarbital,
thiopental, etc). We describe the role played in
therapy by
barbiturates throughout their history: their traditional use as
sedative and hypnotic agents, their use with schizophrenic patients in so-called "sleep cures" (Klaesi, Cloetta), the discovery of the
antiepileptic properties of
phenobarbital (Hauptmann) and their use in the treatment of
epilepsy, and the introduction of
thiobarbiturates in
intravenous anesthesia (Lundy, Waters). We also analyze, from the historical perspective, the problems of safety (phenomena of dependence and death by overdose) which, accompanied by the introduction of a range of
psychoactive drugs in the 1950s, brought an end to
barbiturate use, except in specific applications, such as the induction of
anesthesia and the treatment of certain types of epileptic crisis.