Flutide

Flutide is an inhaled corticosteroid (ICS) from GlaxoSmithKline that contains the active ingredient fluticasone propionate. It is used for the long-term treatment of bronchial asthma.

Fluticasone has a higher potency than budesonide or beclometasone and is therefore used at lower doses. It acts almost exclusively locally in the airways and, when used correctly, causes hardly any systemic side effects.

Flutide is available as a metered-dose inhaler and as a Diskus (dry powder inhaler).

Fluticasone has an anti-inflammatory effect in the airways:

Mechanism of action: 1. Fluticasone binds to glucocorticoid receptors in the cells 2. The complex migrates into the cell nucleus 3. Anti-inflammatory genes are activated 4. Pro-inflammatory genes are inhibited

Effects:

• Reduces inflammatory cells in the airways
• Decreases swelling of the mucous membranes
• Lowers bronchial hyperresponsiveness
• Prevents structural changes of the airways (remodeling)

Pharmacokinetics:

• High lipophilicity – good penetration into the lungs
• Low oral bioavailability (<1%)
• Almost complete first-pass metabolism
• Therefore few systemic effects

Flutide is suitable for:

• All degrees of asthma severity
• As maintenance therapy (controller)
• Children aged 2 years and older (Diskus from 4 years, Flutide mite 50 µg metered-dose inhaler from 2 years, in children aged 2 to 4 years with the Babyhaler inhalation aid)
• Patients who are not adequately controlled with low-dose ICS

Advantages:

• High potency – lower doses needed
• Few systemic effects
• Various dosage forms

Limitations:

• No acute effect on shortness of breath
• Full effect only after days to weeks

Flutide Diskus:

• 50 µg, 100 µg, 250 µg, 500 µg per single dose

Flutide metered-dose inhaler:

• 50 µg, 125 µg, 250 µg per puff

Dosage for asthma (adults):

• Mild: 100-250 µg 2x daily
• Moderate: 250-500 µg 2x daily
• Severe: 500-1000 µg 2x daily

For children: Lower doses depending on age and severity.

Equivalent doses: Fluticasone is about twice as potent as budesonide or beclometasone.

Flutide Diskus: 1. Open the Diskus (thumb on the thumb grip, push outward) 2. Push the lever back until it clicks (dose ready) 3. Breathe out deeply (not into the Diskus) 4. Close your lips firmly around the mouthpiece 5. Breathe in steadily and deeply 6. Hold your breath for 10 seconds 7. Close the Diskus, rinse your mouth

Metered-dose inhaler:

• Recommended with a spacer for better drug deposition
• Coordination between spraying and breathing in
• Rinse your mouth after inhalation

Important:

• Use regularly, even without symptoms
• Rinse your mouth after each inhalation (to prevent oral thrush)
• Do not stop abruptly

Do not use in case of:

• Hypersensitivity to fluticasone
• Acute asthma attack (no immediate effect)

Use with caution in case of:

• Active pulmonary tuberculosis
• Fungal infections of the airways
• Severe hepatic impairment (delayed breakdown)
• Use of CYP3A4 inhibitors (e.g., ritonavir)

Pregnancy: Can be used if there is an appropriate indication. Asthma control is more important than theoretical risks.

Breastfeeding: Use is possible. Small amounts pass into breast milk.

Very common (≥10%):

• Oral thrush (oral candidiasis)

Common (1-10%):

• Hoarseness
• Throat irritation
• Cough

Uncommon:

• Headache
• Taste disturbances
• Skin rash

Rare (with high doses/long-term therapy):

• Adrenal suppression
• Slowed growth in children
• Reduced bone density
• Cataract, glaucoma
• Behavioral changes (children)

Prevention:

• Rinse your mouth after inhalation
• Use the lowest possible effective dose
• Regular check-ups in children

Interactions:

• Ritonavir and other strong CYP3A4 inhibitors – greatly increased fluticasone exposure, Cushing's syndrome possible!
• Ketoconazole, itraconazole – increased fluticasone levels
• Cobicistat – similar interaction to ritonavir

Important: During HIV therapy with ritonavir or cobicistat: avoid fluticasone-containing inhalers if possible; use beclometasone as an alternative.