The use of drugs in sports goes back centuries, about all the way back to the very invention of the concept of sports.
 In ancient times, when the fittest of a nation were selected as athletes or combatants, they were fed diets and given treatments considered beneficial. For instance, Scandinavian mythology says
Berserkers could drink a mixture called "butotens", to greatly increase their physical power at the risk of insanity. One theory is that the mixture was prepared from the
Amanita muscaria mushroom, though this has been disputed. The German missionary and doctor
Albert Schweitzer wrote of
Gabon in the early 19th century: "The people of the country can, having eaten certain leaves or roots, toil vigorously all day without feeling hungry, thirsty or tired and all the time showing a happiness and gaiety."
ancient Olympics in Greece have been alleged to have been contaminated with forms of doping. In
ancient Rome, where
chariot racing had become a huge part of their culture, athletes drank
herbal infusions to strengthen them before chariot races.
More recently, a participant in an endurance
walking race in
Britain, Abraham Wood, said in 1807 that he had used
laudanum (which contains
opiates) to keep him awake for 24 hours while competing against Robert Barclay Allardyce.
 By April 1877, walking races had stretched to 500 miles and the following year, also at the Agricultural Hall in
Islington, London, to 520 miles. The Illustrated London News chided:
- It may be an advantage to know that a man can travel 520 miles in 138 hours, and manage to live through a week with an infinitesimal amount of rest, though we fail to perceive that anyone could possibly be placed in a position where his ability in this respect would be of any use to him [and] what is to be gained by a constant repetition of the fact.
The event proved popular, however, with 20,000 spectators attending each day.
 Encouraged, the promoters developed the idea and soon held similar races for cyclists.
- "...and much more likely to endure their miseries publicly; a tired walker, after all, merely sits down – a tired cyclist falls off and possibly brings others crashing down as well. That's much more fun".
The fascination with six-day bicycle races spread across the Atlantic and the same appeal brought in the crowds in America as well. And the more spectators paid at the gate, the higher the prizes could be and the greater was the incentive of riders to stay awake—or be kept awake—to ride the greatest distance. Their exhaustion was countered by
soigneurs (the French word for "carers"), helpers akin to seconds in
boxing. Among the treatments they supplied was
nitroglycerine, a drug used to stimulate the heart after cardiac attacks and which was credited with improving riders' breathing.
 Riders suffered hallucinations from the exhaustion and perhaps the drugs. The American champion
Major Taylor refused to continue the New York race, saying: "I cannot go on with safety, for there is a man chasing me around the ring with a knife in his hand."
Public reaction turned against such trials, whether individual races or in teams of two. One report said:
- An athletic contest in which the participants 'go queer' in their heads, and strain their powers until their faces become hideous with the tortures that rack them, is not sport, it is brutality. It appears from the reports of this singular performance that some of the bicycle riders have actually become temporarily insane during the contest... Days and weeks of recuperation will be needed to put the racers in condition, and it is likely that some of them will never recover from the strain.
The father of
anabolic steroids in the United States was
John Ziegler (1917–1983), a physician for the U.S. weightlifting team in the mid-20th century. In 1954, on his tour to Vienna with his team for the world championship, Ziegler learned from his Russian colleague that the Soviet weightlifting team's success was due to their use of
testosterone as a performance-enhancing drug. Deciding that U.S. athletes needed chemical assistance to remain competitive, Ziegler worked with the CIBA Pharmaceutical Company to develop an oral anabolic steroid. This resulted in the creation of
methandrostenolone, which appeared on the market in 1960. During the Olympics that year, the Danish cyclist
Knud Enemark Jensen collapsed and died while competing in the 100-kilometer (62-mile) race. An autopsy later revealed the presence of
amphetamines and a drug called
nicotinyl tartrate in his system.
The American specialist in doping, Max M. Novich, wrote: "Trainers of the old school who supplied treatments which had cocaine as their base declared with assurance that a rider tired by a six-day race would get his second breath after absorbing these mixtures."
 John Hoberman, a professor at the University of Texas in Austin, Texas, said six-day races were "de facto experiments investigating the physiology of stress as well as the substances that might alleviate exhaustion."