Alvesco

Alvesco is an inhaled corticosteroid (ICS) that contains the active ingredient ciclesonide. It is a prodrug that is only converted into the active substance in the lungs – as a result, fewer local side effects such as oral thrush occur.

Ciclesonide has high lipophilicity and a long duration of action, so Alvesco only needs to be inhaled once a day. It is particularly well tolerated.

Alvesco is available as a metered-dose inhaler in various strengths.

Ciclesonide is a prodrug with site-specific activation:

Activation: 1. Ciclesonide itself is barely active 2. In the lungs, it is converted by esterases into the active desisobutyryl-ciclesonide (des-CIC) 3. Des-CIC has a 100-fold higher affinity for the glucocorticoid receptor

Advantages of the prodrug concept:

• Hardly any activation in the mouth → less oral thrush
• Very high lung deposition
• Low systemic availability
• Once-daily dosing possible

Anti-inflammatory effect:

• Reduces inflammatory cells and mediators
• Decreases mucosal swelling
• Lowers bronchial hyperresponsiveness

Alvesco is suitable for:

• Bronchial asthma in adults and adolescents aged 12 years and older
• Patients with local side effects from other ICS
• When once-daily dosing is desired

Advantages:

• Only once a day
• Less oral thrush and hoarseness
• Good tolerability
• High lipophilicity

Limitations:

• Not approved for children under 12 years of age
• Not for acute treatment

Alvesco metered-dose inhaler:

• 80 µg per puff
• 160 µg per puff

Dosage for asthma:

• Recommended dose: 160 µg once daily, sufficient for most patients
• In severe asthma and while reducing or stopping oral corticosteroids: up to 640 µg per day (320 µg twice daily)
• Once asthma is controlled: lowest effective dose, 80 µg once daily may be sufficient for some patients

Timing: When used once daily, preferably in the evening.

Metered-dose inhaler: 1. Remove the protective cap 2. Shaking is not necessary, as the aerosol is a solution 3. Breathe out deeply 4. Close your lips around the mouthpiece 5. Breathe in slowly and deeply while releasing the spray 6. Hold your breath for 10 seconds 7. Breathe out slowly

With a spacer:

• Spray into the spacer
• Breathe in and out normally 5-6 times
• Improves deposition of the active ingredient

Important:

• Use regularly, even when you have no symptoms
• Rinse your mouth after inhalation (even though the risk is lower)
• When switching from another ICS: take equivalent doses into account

Do not use in:

• Hypersensitivity to ciclesonide
• Children under 12 years of age

Use with caution in:

• Pulmonary tuberculosis
• Respiratory tract infections
• Severe hepatic impairment (prodrug activation could be altered)

Pregnancy: Limited data. Only if clearly indicated.

Breastfeeding: It is unknown whether it passes into breast milk.

Uncommon (0.1-1%):

• Headache
• Dysphonia (hoarseness) – but less frequent than with other ICS
• Oral thrush – less frequent than with other ICS
• Cough
• Nausea
• Paradoxical bronchospasm

Rare (0.01-0.1%):

• Allergic reactions

Systemic effects: Possible with high doses and long-term therapy, but lower than with other ICS.

Interactions:

• Strong CYP3A4 inhibitors (e.g. ketoconazole, itraconazole, ritonavir, nelfinavir) can increase the levels of the active form of ciclesonide. Concomitant use should be avoided unless the benefit outweighs the increased risk of systemic corticosteroid side effects.