Airway selectivity: an update of pharmacokinetic factors affecting local and systemic disposition of inhaled steroids.
Topical corticosteroids remain the most efficacious single treatment for asthma and rhinitis, despite the emergence of newer drugs in recent years. The antiinflammatory properties of these products, combined with the targeting of formulations and optimization of the intrinsic pharmacokinetic features of the newer corticosteroid molecules has resulted in substantially improved airway selectivity. This review sets out to summarize the pharmacokinetic properties of inhaled corticosteroids that are important for the achievement of high levels of airway selectivity, with additional focus on the use of prodrugs/softdrugs relative to those of conventional corticosteroid molecules, mechanisms (such as esterification) by which retention at the target site is achieved while minimizing systemic exposure, and the role of plasma protein binding.
Edsbäcker
Staffan
S
Clinical Pharmacology and Development DMPK, AstraZeneca R&D, Lund, Sweden. Staffan.Edsbacker@astrazeneca.com
Johansson
Carl-Johan
CJ
D000280:Administration, Inhalation; D000305:Adrenal Cortex Hormones / Q000008:administration & dosage / Q000493:pharmacokinetics; D006801:Humans; D007700:Kinetics; D012137:Respiratory System / Q000378:metabolism*; D013256:Steroids / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*
D000305:Adrenal Cortex Hormones; D013256:Steroids