Fluticasone

Products

The active ingredient fluticasone has been approved in many countries since 1994 and is included in numerous drugs:

• Powder inhalers (Arnuity Ellipta, Seretide + salmeterol, Relvar Ellipta + vilanterol, Trelegy Ellipta + vilanterol + umeclidinium bromide).
• Metered dose inhalers (Axotide, Seretide + salmeterol, Flutiform + formoterol).
• Nasal sprays (Avamys, Nasofan, Dymista + azelastine).
• Nasal suspensions (flutinase).
• Creams and ointments (Cutivate)

Structure and properties

Fluticasone (C₂₂H₂₇F₃O₄S, M_r = 444.5 g/mol) is a synthetic and trifluorinated glucocorticoid. It is present in the drugs as a lipophilic ester, either as fluticasone propionate or as fluticasone fluorate (position 17). The fluticasone propionate shown is present as a white powder that is practically insoluble in water.

Effects

Fluticasone (ATC R03BA05) has antiallergic, anti-inflammatory, and immunosuppressive properties. The effects are due to binding to intracellular glucocorticoid receptors. Fluticasone has low water solubility, high first-pass metabolism, and therefore deep oral bioavailability. It has high potency and only low mineralcorticoid activity.

Indications

• Bronchial asthma
• Chronic obstructive pulmonary disease (COPD)
• Inflammatory skin diseases
• Nasal polyps
• Seasonal and perennial allergic rhinitis, e.g. hay fever.

Dosage

The application depends on the selected drug. In general, regular use usually leads to a better effect. After inhalation, it is important to rinse the mouth with water to prevent oral thrush and throat irritation from developing.

Contraindications

For complete precautions, refer to the drug label of the corresponding products.

Interactions

Fluticasone is metabolized by CYP3A4. When combined with potent CYP3A4 inhibitors, plasma levels of fluticasone may increase.

Adverse effects

The most common potential adverse effects associated with inhalation include headache and nasopharyngitis. The nasal sprays often cause nosebleeds, nasal ulceration, a usually transient increase in intraocular pressure, and headache. When applied to the skin, itching can often occur.