Fluticasone propionate for external use: pharmacological properties and clinical effectiveness

Abstract

Topical corticosteroids are first-line medications in the treatment of an overwhelming number of both acute and chronic inflammatory noninfectious skin diseases. These drugs can be characterized as the drugs of choice in dermatological practice, which is determined by anti-inflammatory, immunosuppressive and antiproliferative effects of corticosteroids. Nevertheless, the use of these drugs in some cases may be limited by the potential risk of adverse side effects, which, in turn, determines a rather widespread corticophobia among patients, as well as among some doctors. In this regard, the current efforts of pharmaceutical companies are focused on the development of topical corticosteroids with the least number of side effects without loss of clinical efficacy. The synthetic carbothioate corticosteroid fluticasone propionate (FP) is a medium strength (class III) synthetic fluorinated corticosteroid for topical treatment of skin conditions. Its molecule has a high degree of lipophilicity, which allows it to be actively absorbed into the skin. The drug has a high affinity to glucocorticoid receptors against the background of the absence of mineralcorticoid activity. In addition, FP is relatively quickly subjected to enzymatic hydrolysis to inactive metabolites. This determines the high clinical efficacy of this drug with minimal risk of both local and systemic adverse events. It is available as cream and ointment with the same efficacy, but with different concentrations (0.05 or 0.005%) of the active substance. This article reviews the pharmacology and safety profile as well as the use of topical FP in clinical practice.