[The discovery of haloperidol]

Haloperidol was synthesized on the 11th of February 1958 by Bert Hermans at the Janssen Laboratories, Beerse, Belgium. Simple but ingenuous methods of animal pharmacology suggested to Paul Janssen and his collegues that this butyrophenone derivative, called R1625, then halop-peridol, would be of great interest: qualitatively, the pharmacological action of R1625 was similar to chlorpromazine, but R1625 was very more powerful since it produced effects with much smaller doses than chlorpromazine. Soon after the synthesis and animal studies, haloperidol was administered in humans by Divry, Bobon et Collard, psychiatrists at the Liege Hospital. The first clinical publication, on the 28th of October, 1958, described the effects of haloperidol in agitation states. The subsequent clinical studies, including those of the prestigious French school of Sainte-Anne hospital, confirmed that haloperidol belongs to the pharmacological family of neuroleptics, as it was defined by J. Delay and P. Deniker in 1955. These clinical studies demonstrated also that haloperidol was particularly active against delusions and hallucinations. Numbers of chronically inpatients were able to leave hospital and to live home thanks to this new drug, which remains one of the more prescribed neuroleptics 40 years after its discovery.