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Review
, 154 (3), 606-22

Pharmacology of Stimulants Prohibited by the World Anti-Doping Agency (WADA)

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Review

Pharmacology of Stimulants Prohibited by the World Anti-Doping Agency (WADA)

J R Docherty. Br J Pharmacol.

Abstract

This review examines the pharmacology of stimulants prohibited by the World Anti-Doping Agency (WADA). Stimulants that increase alertness/reduce fatigue or activate the cardiovascular system can include drugs like ephedrine available in many over-the-counter medicines. Others such as amphetamines, cocaine and hallucinogenic drugs, available on prescription or illegally, can modify mood. A total of 62 stimulants (61 chemical entities) are listed in the WADA List, prohibited in competition. Athletes may have stimulants in their body for one of three main reasons: inadvertent consumption in a propriety medicine; deliberate consumption for misuse as a recreational drug and deliberate consumption to enhance performance. The majority of stimulants on the list act on the monoaminergic systems: adrenergic (sympathetic, transmitter noradrenaline), dopaminergic (transmitter dopamine) and serotonergic (transmitter serotonin, 5-HT). Sympathomimetic describes agents, which mimic sympathetic responses, and dopaminomimetic and serotoninomimetic can be used to describe actions on the dopamine and serotonin systems. However, many agents act to mimic more than one of these monoamines, so that a collective term of monoaminomimetic may be useful. Monoaminomimietic actions of stimulants can include blockade of re-uptake of neurotransmitter, indirect release of neurotransmitter, direct activation of monoaminergic receptors. Many of the stimulants are amphetamines or amphetamine derivatives, including agents with abuse potential as recreational drugs. A number of agents are metabolized to amphetamine or metamphetamine. In addition to the monoaminomimetic agents, a small number of agents with different modes of action are on the list. A number of commonly used stimulants are not considered as Prohibited Substances.

Figures

Figure 1
Figure 1
Sites of drug action at monoaminergic synapses. (1) Monoamine re-uptake inhibition, either non-selective inhibition or selective re-uptake inhibition of NA (selective NA re-uptake inhibitor), DA (SDRI) or 5-HT (serotonin)(serotonin re-uptake inhibitor). (2) Indirect monoaminomimetic actions, by action as substrate for monoamine re-uptake transporters (2a) or as a substrate for VMAT-2 (2b) to release (displace) monoamine (MA) neurotransmitter. (3) Inhibition of MAO. This is not a major site of action of stimulants (see text). (4) Stimulation (or block) of presynaptic inhibitory autoreceptors (that is, receptors for that neurotransmitter) or heteroceptors (that is, receptors for another transmitter) (A). Receptors can also be facilitatory. (5) Stimulation (or block) of postsynaptic receptors (B). These may be adrenergic, dopaminergic or serotonergic receptors. There may be more than one subtype of postsynaptic receptor so that the drug may behave differently from the monoamine neurotransmitter by selective actions at certain receptors. 5-HT, 5-hydroxytryptamine, serotonin; MAO, monoamine oxidase; VMAT, vesicular monoamine transporter.

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