Fluticasone propionate mechanism of action
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Anti-Inflammatory Mechanism of Fluticasone Propionate
Fluticasone propionate is a potent corticosteroid that works mainly by reducing inflammation in the airways and nasal passages. It achieves this by inhibiting the production and release of various proinflammatory mediators, including chemokines (such as IL-8, MIP-1α, and RANTES) and cytokines (like IL-1β, IL-6, and GM-CSF), which are typically elevated during allergic reactions and inflammation. This reduction in inflammatory mediators leads to a decrease in symptoms associated with allergic rhinitis and other inflammatory airway diseases .
Modulation of Immune Cell Function and Gene Expression
Fluticasone propionate directly suppresses several aspects of immune cell function, particularly neutrophil activity. It reduces neutrophil chemotaxis (movement toward inflammation sites) and inhibits their ability to degrade connective tissue, which helps limit tissue damage during inflammation. However, it does not significantly affect the generation of superoxide anion by neutrophils . Additionally, fluticasone propionate decreases the expression of certain transcription factors (IRF4 and BATF) involved in the differentiation of Th9 cells, a T cell subset implicated in allergic responses, further contributing to its anti-inflammatory effects .
Glucocorticoid Receptor Activation and Nuclear Translocation
The primary mechanism of fluticasone propionate involves binding to glucocorticoid receptors in the cytosol. Once bound, the receptor-drug complex translocates to the cell nucleus, where it influences gene expression. This process leads to the suppression of genes that promote inflammation and the activation of genes that help resolve inflammation. When used in combination with long-acting β2-agonists (LABAs), fluticasone propionate can also increase the production of β2-receptors, enhancing bronchodilation and further reducing airway inflammation .
Effects on Epithelial Barrier and Vascular Response
Fluticasone propionate helps restore and maintain the integrity of the respiratory epithelial barrier, which can be disrupted during infections or allergic reactions. For example, it has been shown to prevent the increase in epithelial permeability caused by SARS-CoV-2 infection and reduce the expression of ACE2, the receptor used by the virus to enter cells . In allergic rhinitis, long-term use of fluticasone propionate reduces nasal airflow resistance, secretion volume, and eosinophil counts, indicating both anti-inflammatory and vascular effects .
Clinical Efficacy and Safety
Clinical studies confirm that fluticasone propionate is effective in controlling symptoms of seasonal and perennial allergic rhinitis, with a safety profile similar to placebo and minimal systemic side effects due to its low oral bioavailability .
Conclusion
Fluticasone propionate acts through multiple mechanisms to reduce inflammation and allergic responses in the airways. It suppresses the production of proinflammatory mediators, modulates immune cell function and gene expression, stabilizes the epithelial barrier, and exerts beneficial vascular effects. These actions make it a highly effective and well-tolerated treatment for allergic rhinitis, asthma, and related conditions 1234567.
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