Edward J O'Connell1. 1. Department of Pediatrics, Allergy/Immunology, Mayo Clinic, Rochester, Minnesota 55905, USA. oconnell.edward@mayo.edu
Abstract
BACKGROUND: The aim of inhaled corticosteroid (ICS) therapy for asthma is to attain high therapeutic activity in the airways while keeping the risk of systemic adverse effects relatively low. However, the physicochemical and pharmacokinetic properties of various ICSs affect this ratio, thereby influencing their ability to fulfill the requirements of an ideal agent. OBJECTIVE: This article reviews the physical and pharmacokinetic properties of budesonide, outlining how they, safety data, and use of different inhalation devices enable budesonide to meet many of the clinical requirements of an ideal ICS for the treatment of asthma. RESULTS: ICS efficacy is influenced by lipophilicity, lung deposition, and retention in airway tissue, whereas the rate of elimination determines systemic activity. Budesonide is retained in the airways to a greater extent than other ICSs because of an esterification process that increases its lipophilicity. The prolonged retention of budesonide in the airways may contribute to its efficacy when administered QD. In addition to a pressurized metered-dose inhaler, budesonide is available as a dry-powder inhaler and in nebulized form, which can be used by asthma patients aged > or =6 months. CONCLUSIONS: When combined with delivery devices suitable for a spectrum of patient groups, the physical and pharmacokinetic properties of budesonide lend it many of the characteristics of an ideal ICS, including favorable efficacy and tolerability profiles.
BACKGROUND: The aim of inhaled corticosteroid (ICS) therapy for asthma is to attain high therapeutic activity in the airways while keeping the risk of systemic adverse effects relatively low. However, the physicochemical and pharmacokinetic properties of various ICSs affect this ratio, thereby influencing their ability to fulfill the requirements of an ideal agent. OBJECTIVE: This article reviews the physical and pharmacokinetic properties of budesonide, outlining how they, safety data, and use of different inhalation devices enable budesonide to meet many of the clinical requirements of an ideal ICS for the treatment of asthma. RESULTS:ICS efficacy is influenced by lipophilicity, lung deposition, and retention in airway tissue, whereas the rate of elimination determines systemic activity. Budesonide is retained in the airways to a greater extent than other ICSs because of an esterification process that increases its lipophilicity. The prolonged retention of budesonide in the airways may contribute to its efficacy when administered QD. In addition to a pressurized metered-dose inhaler, budesonide is available as a dry-powder inhaler and in nebulized form, which can be used by asthmapatients aged > or =6 months. CONCLUSIONS: When combined with delivery devices suitable for a spectrum of patient groups, the physical and pharmacokinetic properties of budesonide lend it many of the characteristics of an ideal ICS, including favorable efficacy and tolerability profiles.
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