Abstract: Methods for administering beta-adrenergic inverse agonists with improved pharmacokinetic profiles for the treatment of pulmonary airway diseases are disclosed. The beta adrenergic inverse agonists are formulated in a controlled-release formulation comprising: (1) a beta-adrenergic inverse agonist in a therapeutically effective quantity; and (2) at least one agent that controls release of the beta-adrenergic inverse agonist resulting in a pharmacokinetic profile that minimizes acute detrimental reduction in airway function with the first dose and with each successive dose. This pharmacokinetic profile typically results in slow release of the drug into the bloodstream resulting in a large average Tmax>4 hours. The controlled-release formulation may consist of multilayered matrix or erosional tablets, gastric-retention tablets, osmotic pump oral formulations, multiparticulate capsules or tablets or dermal patch.