Central nervous system stimulants

by George AJ
School of Pharmacy and Chemistry,
Liverpool John Moores University, UK.
Baillieres Best Pract Res Clin Endocrinol Metab 2000 Mar; 14(1):79-88


Three major types of CNS stimulant are currently abused in sport: amphetamine, cocaine and caffeine. Each drug type has its own characteristic mechanism of action on CNS neurones and their associated receptors and nerve terminals. Amphetamine is widely abused in sports requiring intense anaerobic exercise where it prolongs the tolerance to anaerobic metabolism. It is addictive, and chronic abuse causes marked behavioural change and sometimes psychosis. Major sports abusing amphetamine are cycling, American football, ice-hockey and baseball. Cocaine increases tolerance to intense exercise, yet most of its chronic effects on energy metabolism are negative. Its greatest effects seem to be as a central stimulant and the enhancement of short-term anaerobic exercise. It is highly addictive and can cause cerebral and cardiovascular fatalities. Caffeine enhances fatty acid metabolism leading to glucose conservation, which appears to benefit long-distance endurance events such as skiing. Caffeine is also addictive, and chronic abuse can lead to cardiac damage. Social abuse of each of the three drugs is often difficult to distinguish from their abuse in sport.