Fluticasone

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.

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%).

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