Fluticasone

Fluticasone
ATC Code D07AC17, R01AD08, R03BA05
Formula C22H27F3O4S
Molar Mass (g·mol−1) 444,51
Physical State solid
CAS Number 90566-53-3
PUB Number 5311101
Drugbank ID DB13867
Solubility sparingly soluble in water

Basics

Fluticasone is a synthetic glucocorticoid. It is available in 2 forms. Fluticasone furoate and fluticasone propionate. They are used in inhalers, nasal sprays and topical preparations for various inflammatory conditions. These include fluticasone is available by prescription only.

Pharmacology

Pharmacodynamics

Fluticasone acts because of its structural similarity to endogenous glucocorticoids. Unbound, it can penetrate the membrane of the cell and then bind with high affinity to intracellular glucocorticoid receptors.

The anti-inflammatory (anti-inflammatory) effect is achieved by interfering with the so-called arachidonic acid metabolism. Fluticasone causes fewer prostaglandins and leukotrienes to be produced at the end of this metabolism. These are significantly involved in the inflammatory process of the human body.

Fluticasone has an anti-allergic effect by preventing the release of histamine and simultaneously reducing the number and activity of certain B and T lymphocytes.

Pharmacokinetics

Plasma protein binding is approximately 99%. Metabolism occurs in the liver and is mainly catalyzed by the enzyme CYP3A4. Excretion is mainly via faeces (>90%).

Toxicity

Side effects

The most common side effect is yeast infections in the mouth (oral thrush). Furthermore, hoarseness, headache and fatigue may occur. To reduce the undesirable effects in the oral cavity, the mouth should be rinsed thoroughly with water after use.

In very rare cases, systemic and possibly serious side effects may occur. These include bone loss, edema, allergic reactions and impaired adrenocortical function.

Toxicological Data

LD50 (rat, oral): > 2000 mg-kg-1

Sources

  • Drugbank
  • PubChem
  • Aktories, Förstermann, Hofmann, Starke: Allgemeine und spezielle Pharmakologie und Toxikologie, Elsvier, 2017
Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter ist Autor zu pharmazeutischen Themen in der Medizin-Redaktion von Medikamio. Er befindet sich im letzten Semester seines Pharmaziestudiums an der Universität Wien und liebt das wissenschaftliche Arbeiten im Bereich der Naturwissenschaften.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer ist seit 2020 freie Autorin bei Medikamio und studierte Pharmazie an der Universität Wien. Sie arbeitet als Apothekerin in Wien und ihre Leidenschaft sind pflanzliche Arzneimittel und deren Wirkung.

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