药代动力学与实验治疗学杂志

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Understanding the Pharmacokinetic Profile of Fluticasone: Implications for Therapeutic Efficacy and Safety

Zung Zang

Fluticasone is a widely used corticosteroid medication with potent anti-inflammatory properties, primarily used in the treatment of respiratory conditions such as asthma and chronic obstructive pulmonary disease (COPD). As with any medication, a thorough understanding of its pharmacokinetic profile is crucial to ensure optimal therapeutic efficacy and minimize the risk of adverse effects. This review aims to provide a comprehensive overview of the pharmacokinetics of fluticasone, including its absorption, distribution, metabolism, and elimination. Fluticasone exhibits high oral bioavailability, with minimal first-pass metabolism, when administered orally. However, it is predominantly administered via inhalation, which allows for targeted drug delivery to the lungs while minimizing systemic exposure. Upon inhalation, fluticasone is rapidly absorbed from the respiratory tract and undergoes extensive first-pass metabolism in the liver, primarily mediated by cytochrome P450 enzymes. The resulting metabolites are largely inactive and undergo further metabolism before elimination. The distribution of fluticasone is primarily limited to the tissues within the respiratory tract, where it exerts its anti-inflammatory effects. Minimal systemic distribution occurs due to its extensive hepatic metabolism and high protein binding. Fluticasone is primarily eliminated through hepatic metabolism, with the majority of the drug and its metabolites excreted in the feces.