Après avoir été breveté par Parke-Davis pour usage humain et animal en 1966, il est devenu disponible sur ordonnance en 1969 sous forme de chlorhydrate de kétamine, sous le nom de Ketalar. La Food and Drug Administration des États-Unis l’a approuvé pour la consommation humaine en 1970. En raison de ses propriétés sympathomimétiques favorables et de sa large marge de sécurité, il a été administré comme anesthésique de terrain aux soldats pendant la guerre du Vietnam.

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