Fluticasone

Fluticasone generics contain the active ingredient fluticasone propionate and are identical in active ingredient to the original product Flutide. They are used as maintenance therapy for the long-term treatment of bronchial asthma.

Fluticasone is one of the most potent inhaled corticosteroids and is used at lower doses than budesonide or beclomethasone. It has low oral bioavailability and therefore few systemic side effects.

Available, e.g., as Fluticason Cipla® or as the combination product salmeterol/fluticasone propionate.

Fluticasone propionate has a strong anti-inflammatory effect:

Mechanism of action: 1. Binds with high affinity to glucocorticoid receptors 2. The complex migrates into the cell nucleus 3. Activates anti-inflammatory genes 4. Inhibits pro-inflammatory cytokines

Pharmacological advantages:

• Highest receptor affinity among ICS
• Oral bioavailability < 1% (almost exclusively local effect)
• High lipophilicity – good retention in lung tissue
• Strong and long-lasting anti-inflammatory effect

Equivalent doses: 100 µg fluticasone ≈ 200 µg budesonide ≈ 200 µg beclomethasone

Fluticasone generics are suitable for:

• Bronchial asthma of all severity levels
• Adults and children (depending on the formulation)
• As maintenance therapy (controller)

Advantages of generics:

• Same active ingredient as Flutide

Not suitable:

• For the acute treatment of shortness of breath
• For patients on ritonavir therapy, unless the benefit outweighs the risk (CYP3A4 interaction!)

Fluticason Cipla / generics:

• 50 µg, 125 µg, 250 µg per puff

Salmeterol/fluticasone propionate (combination):

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

Dosage for asthma (adults):

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

Note the equivalent doses: Fluticasone is twice as potent as budesonide!

Metered-dose inhaler: 1. Remove the protective cap, shake 2. Breathe out deeply 3. Close your lips around the mouthpiece 4. Breathe in slowly while releasing a puff 5. Hold your breath for 10 seconds 6. Rinse your mouth and spit out

Dry powder inhaler (if available):

• Breath-actuated – inhale forcefully
• Rinse your mouth after inhalation

Important:

• Use regularly, 2x daily
• Rinse your mouth after each inhalation
• Do not stop abruptly

Do not use in case of:

• Hypersensitivity to fluticasone

Use with caution in case of:

• Concomitant therapy with ritonavir or cobicistat (risk of Cushing's syndrome, use only if the benefit outweighs the risk)
• Active pulmonary tuberculosis
• Fungal infections of the airways
• Severe hepatic impairment

Pregnancy: Can be used for asthma.

Breastfeeding: Use is possible. Low systemic exposure.

Very common (>10%):

• Oral thrush

Common (1-10%):

• Hoarseness
• Throat irritation

Uncommon:

• Headache
• Taste disturbances

Rare (at high doses):

• Adrenal suppression
• Osteoporosis
• Cataract, glaucoma
• Slowed growth in children

Important: Particular caution with CYP3A4 inhibitors – they can drastically increase systemic fluticasone levels!

Critical interaction:

• Ritonavir, cobicistat – Avoid the combination unless the benefit outweighs the risk. Greatly increased systemic fluticasone levels, Cushing's syndrome possible
• Ketoconazole, itraconazole – increased levels

During HIV therapy with ritonavir, cobicistat or other CYP3A4 inhibitors: Avoid the combination unless the benefit outweighs the risk. Your doctor will decide whether another medicine is suitable.

No relevant interaction with:

• Bronchodilators
• Antihistamines