Caffeine and the central nervous system: mechanisms of action, biochemical, metabolic and psychostimulant effects.

Caffeine is a common substance in the diets of most athletes and it is now appearing in many new products, including energy drinks, sport gels, alcoholic beverages and diet aids. It can be a powerful ergogenic aid at levels that are considerably lower than the acceptable limit of the International Olympic Committee and could be beneficial in training and in competition. Caffeine does not improve maximal oxygen capacity directly, but could permit the athlete to train at a greater power output and/or to train longer. It has also ben shown to increase speed and/or power output in simulated race conditions. These effects have been found in activities that last as little as 60 seconds or as long as 2 hours. There is less information about the effects of caffeine on strength; however, recent work suggests no effect on maximal ability, but enhanced endurance or resistance to fatigue. There is no evidence that caffeine ingestion before exercise leads to dehydration, ion imbalance, or any other adverse effects. The ingestion of caffeine as coffee appears to be ineffective compared to doping with pure caffeine. Related compounds such as theophylline are also potent ergogenic aids. Caffeine may act synergistically with other drugs including ephedrine and anti-inflammatory agents. It appears that male and female athletes have similar caffeine pharmacokinetics, i.e., for a given dose of caffeine, the time course and absolute plasma concentrations of caffeine and its metabolites are the same. In addition, exercise or dehydration does not affect caffeine pharmacokinetics. The limited information available suggests that caffeine non-users and users respond similarly and that withdrawal from caffeine may not be important. The mechanism(s) by which caffeine elicits its ergogenic effects are unknown, but the popular theory that it enhances fat oxidation and spares muscle glycogen has very little support and is an incomplete explanation at best. Caffeine may work, in part, by creating a more favourable intracellular ionic environment in active muscle. This could facilitate force production by each motor unit.

Caffeine and exercise: metabolism, endurance and performance

Position Statement: The position of The Society regarding caffeine supplementation and sport performance is summarized by the following seven points: 1.) Caffeine is effective for enhancing sport performance in trained athletes when consumed in low-to-moderate dosages (~3-6 mg/kg) and overall does not result in further enhancement in performance when consumed in higher dosages (≥ 9 mg/kg). 2.) Caffeine exerts a greater ergogenic effect when consumed in an anhydrous state as compared to coffee. 3.) It has been shown that caffeine can enhance vigilance during bouts of extended exhaustive exercise, as well as periods of sustained sleep deprivation. 4.) Caffeine is ergogenic for sustained maximal endurance exercise, and has been shown to be highly effective for time-trial performance. 5.) Caffeine supplementation is beneficial for high-intensity exercise, including team sports such as soccer and rugby, both of which are categorized by intermittent activity within a period of prolonged duration. 6.) The literature is equivocal when considering the effects of caffeine supplementation on strength-power performance, and additional research in this area is warranted. 7.) The scientific literature does not support caffeine-induced diuresis during exercise, or any harmful change in fluid balance that would negatively affect performance.

/pdf/international-society-of-sports-nutrition-position-stand-1fibenkpb4.pdf

International society of sports nutrition position stand: caffeine and performance

Medicine & Science in sports & Exercise

This study examined the exercise responses of well-trained endurance athletes to various doses of caffeine to evaluate the impact of the drug on exercise metabolism and endurance capacity. Subjects (n = 8) withdrew from all dietary sources of caffeine for 48 h before each of four tests. One hour before exercise they ingested capsules of placebo or caffeine (3, 6, or 9 mg/kg), rested quietly, and then ran at 85% of maximal O2 consumption to voluntary exhaustion. Blood samples for methylxanthine, catecholamine, glucose, lactate, free fatty acid, and glycerol analyses were taken every 15 min. Plasma caffeine concentration increased with each dose (P < 0.05). Its major metabolite, paraxanthine, did not increase between the 6 and 9 mg/kg doses, suggesting that hepatic caffeine metabolism was saturated. Endurance was enhanced with both 3 and 6 mg/kg of caffeine (increases of 22 +/- 9 and 22 +/- 7%, respectively; both P < 0.05) over the placebo time of 49.4 +/- 4.2 min, whereas there was no significant effect with 9 mg/kg of caffeine. In contrast, plasma epinephrine was not increased with 3 mg/kg of caffeine but was greater with the higher doses (P < 0.05). Similarly only the highest dose of caffeine resulted in increases in glycerol and free fatty acids (P < 0.05). Thus the highest dose had the greatest effect on epinephrine and blood-borne metabolites yet had the least effect on performance. The lowest dose had little or no effect on epinephrine and metabolites but did have an ergogenic effect. These results are not compatible with the traditional theory that caffeine mediates its ergogenic effect via enhanced catecholamines.

Metabolic, catecholamine, and exercise performance responses to various doses of caffeine

The influence of specific training on benefits from caffeine (Caf) ingestion was examined during a sprint test in a group of highly trained swimmers (T) and compared with the response of a group of untrained occasional swimmers (UT). Seven T and seven UT subjects swam freestyle two randomly assigned 2 × 100 m distances, at maximal speed and separated by 20 min of passive recovery, once after Caf (250 mg) and once after placebo (Pla) ingestion. Anaerobic capacity was assessed by the mean velocity (meters per second) during each 100 m and blood was sampled from the fingertip just before and 1, 3, 5, 7, and 9 min after each 100 m for resting and maximal blood lactate concentration ([1a−]b, max) determination. The [[1a−]b, max was significantly enhanced by Caf in both T and UT subjects (P<0.01). However, only T subjects exhibited significant improvement in their swimming velocity (P<0.01) after Caf or any significant impairment during the second 100 m. In light of these results, it appears that specific training is necessary to benefit from the metabolic adaptations induced by Caf during supramaximal exercise requiring a high anaerobic capacity.

Benefits of caffeine ingestion on sprint performance in trained and untrained swimmers

In order to determine the effects of caffeine ingestion on performance and metabolic responses during supramaximal exercise, six healthy volunteers performed the Wingate Anaerobic Test twice. Sixty min before each trial, while in a fasting state, they took capsules containing either caffeine (5 mg/kg) or a placebo, according to a single blind and randomized procedure. Caffeine administration did not significantly change either maximal anaerobic capacity (AC) or power (AP) and power decrease (PD). It did, however, induce significant (p less than 0.05) increases in both catecholamine and blood lactate levels as compared to values obtained after placebo administration. Moreover, maximal blood lactate occurred earlier (p less than 0.05), and lactate output seemed to be greater with caffeine (p less than 0.01). There was a strong correlation, both with and without caffeine, between epinephrine and lactate levels (r = 0.81) and between both AP and AC and lactate levels. These data suggest that caffeine, essentially via epinephrine, modifies glycolytic metabolism but fails to improve performance during the Wingate Anaerobic Test in nonspecifically trained subjects.

Effects of caffeine ingestion on performance and anaerobic metabolism during the Wingate Test.

Seven men were studied during maximal cycle ergometer exercise, to assess the effects of a single or continuous caffeine ingestion on performance and catecholamine secretion. A single blind and randomised procedure was followed with three trials at 100 +/- 5% VO2 max until exhaustion. The first trial was performed after a single administration of 250 mg of caffeine (a). The second and third trials were performed after a treatment of 5 days with 250 mg caffeine per day (continuous = c) and after placebo (p). a and c caffeine administration, 60 min prior to exercise, did not significantly change the time to exhaustion, but increased the plasma levels of both epinephrine (E) and norepinephrine (NE) at exhaustion (p less than 0.05). Single ingestion of caffeine accelerated the elimination of E and NE and increased the maximal blood lactic acid. These data suggest that both single and continuous administration of caffeine do not enhance performance during maximal cycle ergometer exercise, but do increase the exercise response of catecholamine. Only a single administration modifies the blood lactate accumulation.

Effect of acute or chronic administration of caffeine on performance and on catecholamines during maximal cycle ergometer exercise

This study was conducted to determine catecholamine response to maximal intensity exercise of a few seconds' duration. To do this, epinephrine (E) and norepinephrine (NE) levels were measured during Force-Velocity Test. Blood samples were taken at the end of each sprint. Compared to rest (E0 = 77.4 +/- 3.8 pg/ml), the E concentration significantly increased after the first sprint (E2 = 109.8 +/- 14.7 pg/ml) and after the last one (E8 = 126.9 +/- 19.4 pg/ml) which correspond to the exhaustion state of our subjects. NE concentration doubled after the first sprint (NE2 = 589.1 +/- 94.7 pg/ml) and remained at this level until the end of the test. E2 seems to have been a stress reaction to an unfamiliar test. E8 may represent the "exercise plus exhaustion" stimulus on the stimulation of the adrenal gland (AG). This would suggest that stimulus intensity plays a role even when duration is very brief, although the time factor seems to limit the response of AG. The evolution of NE suggest that the brief duration of the sprints may limit the adatation response of NE to energy demands.

M. Audran

Papers

Benefits of caffeine ingestion on sprint performance in trained and untrained swimmers

Effects of caffeine ingestion on performance and anaerobic metabolism during the Wingate Test.

Effect of acute or chronic administration of caffeine on performance and on catecholamines during maximal cycle ergometer exercise

Influence of brief high intensity exercise on plasma adrenaline and noradrenaline levels