Urine and serum concentrations of inhaled and oral terbutaline.

We examined urine and serum concentrations after therapeutic use of single and repetitive doses of inhaled and supratherapeutic oral use of terbutaline. We compared the concentrations in 10 asthmatics and 10 healthy subjects in an open-label, cross-over study with 2 mg inhaled and 10 mg oral terbutaline on 2 study days. Further, 10 healthy subjects were administrated 1 mg inhaled terbutaline in 4 repetive doses with total 4 mg. Blood samples were collected at baseline and during 6 h after the first inhalations. Urine samples were collected at baseline and during 12 h after the first inhalations. Median (IQR) urine concentrations peaked in the period 0-4 h after inhalation with Cmax 472 (324) ng/mL in asthmatics and 661 (517) ng/mL in healthy subjects, and 4-8 h after oral use with Cmax 666 (877) ng/mL in asthmatic and 402 (663) ng/mL in healthy subjects. In conclusion we found no significant differences in urine and serum concentrations between asthmatic and healthy subjects. We compared urine and serum concentrations after therapeutic inhaled doses and supratherapeutic oral doses and observed significant statistical differences in both groups but found it impossible to distinguish between therapeutic and prohibited use based on doping tests with urine and blood samples.

High-dose inhaled salbutamol has no acute effects on aerobic capacity or oxygen uptake kinetics in healthy trained men.

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 VO(2max) 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 O(2) deficit related to oxygen uptake kinetics. In conclusion, no ergogenic effect of a high dose of salbutamol on aerobic capacity was found.

Urine concentrations of repetitive doses of inhaled salbutamol.

We examined blood and urine concentrations of repetitive doses of inhaled salbutamol in relation to the existing cut-off value used in routine doping control. We compared the concentrations in asthmatics with regular use of beta2-agonists prior to study and healthy controls with no previous use of beta2-agonists. We enrolled 10 asthmatics and 10 controls in an open-label study in which subjects inhaled repetitive doses of 400 microgram salbutamol every second hour (total 1600 microgram), which is the permitted daily dose by the World Anti-Doping Agency (WADA). Blood samples were collected at baseline, 30 min, 1, 2, 3, 4, and 6 h after the first inhalations. Urine samples were collected at baseline, 0-4 h, 4-8 h, and 8-12 h after the first inhalations. Median urine concentrations peaked in the period 4-8 h after the first inhalations in the asthmatics and between 8-12 h in controls and the median ranged from 268 to 611 ng×mL (-1). No samples exceeded the WADA threshold value of 1000 ng×mL (-1) when corrected for the urine specific gravity. When not corrected one sample exceeded the cut-off value with urine concentration of 1082 ng×mL (-1). In conclusion we found no differences in blood and urine concentrations between asthmatic and healthy subjects. We found high variability in urine concentrations between subjects in both groups. The variability between subjects was still present after the samples were corrected for urine specific gravity.

Strength of two- and one-leg extension in man.

Two- and one-leg extension strengths were compared in 155 female and male, untrained and trained (eight bicyclists, 38 weight-lifters) subjects and in a polio patient with almost no strength in one leg. On average two-leg strength was 82 +/- 1.3% (SE) of the sum of the strength of the right and left legs (leg-strength ratio) with no significant difference between the untrained and trained subjects. In the polio patient two-leg strength was lower than the strength of the strongest leg. A similar leg-strength ratio was found when measurements were made with a knee angle of 150 degrees (n = 128) and 90 degrees (n = 25). The ratio did not change when re-determined after 1 year (n = 9). Moderate changes in the subjects' position during measurements did not affect one-leg strength (n = 13). However, familiarization with the experimental apparatus increased the leg-strength ratio from 80 +/- 2.5% to 97 +/- 2.9% (P less than 0.01) (n = 18). In contrast, two-arm extension strength was similar to the sum of the strength of the right and left arms (n = 15). The results demonstrate that two-leg strength in general is lower than the sum of the strength of the right and left legs, and that this phenomenon is found even after intensive endurance or strength training. However, familiarization with the experimental apparatus can increase the relative two-leg strength which suggests that muscle strength in man may be limited by the central nervous systems' ability to activate maximally all synergistic muscles and/or to control antagonistic muscles.