Corticosteroid Aerosols in the Treatment of Asthma

Abstract

Since the 1950s, corticosteroid aerosols have proved useful in the treatment of asthma. Although their precise mechanism of action is not known, these topical agents have beneficial antiinflammatory and decongestive effects on the bronchial tree in both the allergic and nonallergic forms of this disease. Four of the newer aerosolized steroids--beclomethasone dipropionate, triamcinolone acetonide, flunisolide and budesonide--have been evaluated in clinical trials. The last drug is still investigational. Their side effects are minimal, the major ones being oral candidiasis and dysphonia. They are most effective when used prophylactically and should not be administered during acute asthmatic attacks, as insufficient amounts of drug are inhaled when the airways are obstructed. Patients must be instructed in the correct techniques of administering steroid aerosols to ensure optimal therapy.

A Short-Term Investigation of Dysphonia in Asthmatic Patients Using Inhaled Budesonide

“…1 The most common local adverse effects of inhaled corticosteroid therapy have been reported to be candidiasis and dyphonia. 2 Candidiasis rarely causes major clinical problems, and can usually be treated effectively without discontinuing inhaled corticosteroid.…”

Corticosteroid Therapy in the Management of Asthma

“…These agents have been shown to be highly effective with minimal systemic side effects, and thus have become a major therapeutic modality in the treatment of asthma and allergic rhinitis. 10 Currently, three different preparations of corticosteroid aerosols are available in the United States (Table 3).…”

“…A BDP dose of 400 µg is said to be comparable in efficacy against asthma to 5 to 10 mg of oral prednisone. 10 The usual adult dose of BDP is 400 µg/day, but 1000 µg/day may be required in some patients. Mild adrenal suppression may be seen at doses greater than 1600 µg/day.…”

“…TAA has been shown to be effective therapy for mild-to-moderate asthma in both short-term and long-term studies. 10,17,18…”

Binding affinities of rimexolone (ORG 6216), flunisolide and their putative metabolites for the glucocorticoid receptor of human synovial tissue

“…Rimexolone (ORG 6216), presently in clinical trials for intraarticular use, and flunisolide, used as aerosol in the treatment of asthma, have been shown to express high local activity with only low systemic side effects [1][2][3][4][5]. Relative binding affinities of glucocorticoid agonists for the human glucocorticoid receptor correlate well with their pharmacological activity at the site of action [6].…”