PURPOSE: Data on blood and urinary concentrations of salbutamol after inhalation and oral administration in healthy subjects are scarce. Accordingly, we examined the pharmacokinetics of inhaled and oral salbutamol in asthmatic subjects. METHODS: We enrolled 10 men aged 18-45 yr in an open-label study in which 0.8 mg of inhaled or 8 mg of systemic salbutamol was administered in a crossover design. All subjects had doctor-diagnosed asthma, used beta2 agonist when needed, and abstained from any medicine, beta2 agonist inclusive, for 14 d before visit. Urine was collected from all subjects (0-4, 4-8, and 8-12 h), and blood samples were taken at 0, 0.5, 1, 2, 3, 4, and 6 h after salbutamol administration. RESULTS: Maximum urine concentration was reached during the first 4 h after administration of both inhaled and oral salbutamol. We found differences in median urinary concentrations (Cmax) of 260.9 and 2422.2 ng x mL(-1), respectively (P