The prevalence of asthma is higher among elite athletes than in the general population. This has resulted in the frequent use of anti-asthmatic medication such as beta2-agonists among asthmatic athletes. Beta2-agonists are on the prohibited list of WADA. The use of the beta2-agonist salbutamol is only permitted in therapeutic inhaled doses. Most studies have reported the lack of ergogenic effects of therapeutic doses of inhaled beta2-agonists measured in maximal oxygen uptake. No previous studies have examined any possible effects of high-dose inhaled salbutamol on oxygen uptake kinetics. We enrolled nine healthy well-trained men in a randomized, blinded, placebo-controlled crossover study. Subjects were randomized to inhalation of 40 puffs of 0.2 mg salbutamol or two placebo tablets and performed an incremental test to exhaustion and three submaximal tests at 75% of peak power to determine oxygen uptake kinetics. During the incremental test, there were no effects of inhaled salbutamol on VO2max in absolute or relative terms, and no effect on peak power and lactate threshold. During the submaximal test, we found no effects on the time constant, time delay, the mean response time or O2 deficit related to oxygen uptake kinetics. In conclusion, no ergogenic effect of a high dose of salbutamol on aerobic capacity was found.