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Inhaled Corticosteroid

Fluticasone

A potent inhaled corticosteroid for preventing asthma, combined with long-acting bronchodilators in COPD, and sprayed nasally for rhinitis.

Drug card

How it works
Activating glucocorticoid receptors to switch off airway inflammation
Used for
  • Maintenance treatment to prevent asthma
  • COPD, combined with a long-acting bronchodilator
  • Allergic rhinitis and nasal polyps (nasal spray)
  • Eczema (cream)
Known for
  • Oral thrush (candidiasis)
  • Hoarse voice and throat irritation

Study it as a flashcard, and it comes back before you forget it.

Mechanism of action

How does fluticasone work?

A trifluorinated corticosteroid that binds the glucocorticoid receptor 18 times as strongly as dexamethasone and over three times as strongly as budesonide. The receptor induces lipocortin, which blocks phospholipase A2, and turns down NF-kB, so prostaglandins, leukotrienes and cytokines fall. CYP3A4 clears it, so ritonavir can raise levels enough to cause Cushing's syndrome.

Like other inhaled corticosteroids: Inhaled corticosteroids enter airway cells and bind the glucocorticoid receptor, which moves to the nucleus and changes gene expression: anti-inflammatory proteins rise and cytokines and other mediators fall, so fewer mast cells, eosinophils and lymphocytes inflame the airway. Benefit builds over days to weeks, not at once. Inhaled, they act strongly where they land with little whole-body effect.

Uses

What is fluticasone used for?

  • Maintenance treatment to prevent asthma
  • COPD, combined with a long-acting bronchodilator
  • Allergic rhinitis and nasal polyps (nasal spray)
  • Eczema (cream)

Side effects

Side effects of fluticasone

  • Oral thrush (candidiasis)Known for
  • Hoarse voice and throat irritationKnown for
  • Headache
  • Nausea and vomiting
  • Adrenal suppression at high dosesSerious
  • Cushing's syndrome, especially with ritonavirSerious
  • Slower growth in children
  • Lower bone mineral density
  • Glaucoma (raised eye pressure)Serious
  • Cataracts
  • Worse infections, severe chickenpox or measlesSerious
  • Paradoxical bronchospasmSerious

Known for marks what an exam expects you to know it for.

Watch for

Cautions and what sets it apart

  • Strong CYP3A4 inhibitors such as ritonavir and ketoconazole are not recommended with it.
  • It is not for acute attacks or status asthmaticus.
  • Severe milk-protein allergy rules out the dry-powder inhaler.
  • Long-term use calls for checks of bone density, children's growth and the eyes.

Good to know: It binds the glucocorticoid receptor most strongly of the three inhaled steroids here: nearly twice beclometasone's active form and over 3 times budesonide.

Remember it

A way to remember it

Steroid in the lungs, thrush on the tongue.

Some of each dose stays in the mouth and throat, so oral thrush and a hoarse voice are the classic local side effects; rinsing the mouth afterwards lowers the risk.

Written for biofideX

Its class

Inhaled corticosteroids

Sources

Checked against

Written for biofideX in plain words, after checking these references:

For learning pharmacology, not for treatment decisions: no doses are given, and a prescriber, pharmacist or the product's own label is the word on any one patient. Spotted a mistake? Tell us and we'll correct it.

Practice it

Lungs and allergy

Fluticasone is one of 16 drugs practiced together here: their classes, how they work, what they treat and what they're known for.

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