Ciclesonide

Ciclesonide is an inhaled corticosteroid prodrug given once daily for asthma. It is activated in the lung by esterases to desisobutyryl-ciclesonide, which gives low oropharyngeal and systemic exposure.

Classification. Inhaled corticosteroid, glucocorticoid.

Mechanism. The active metabolite binds the glucocorticoid receptor with high affinity, suppressing airway inflammation. Fatty-acid conjugation in the lung prolongs retention.

Pharmacokinetics. Oral bioavailability of the active metabolite is under 1%. Highly protein bound. Metabolised by CYP3A4. Elimination is mainly faecal.

First-line, persistent asthma, adults and adolescents from 12 years. 160 micrograms once daily, preferably in the evening. If control is poor, up to 320 micrograms twice daily under specialist direction. Maximum 640 micrograms daily.

Alternative. Another ICS with a LABA for moderate or severe disease.

Younger children. Not advised under the licensed age; use another ICS.

Emergency. Not used.

Titration. Step down to 80 micrograms or 160 micrograms once daily when control holds for 3 months. No loading dose.

Contraindications. Hypersensitivity. Caution in active or quiescent tuberculosis.

Serious adverse effects. Adrenal suppression at high doses, growth effects in children, cataract, glaucoma, paradoxical bronchospasm.

Common adverse effects. Oral candidiasis (less frequent than with other ICS), hoarseness, headache.

Interactions. Strong CYP3A4 inhibitors such as ketoconazole raise the active metabolite exposure several-fold; ritonavir and cobicistat should be avoided.

Common prescribing errors. Using the product for acute relief. Starting it where refills are unreliable, which risks a gap in controller therapy.

Special groups.

• Pregnancy: limited data; use another ICS with more data. Breastfeeding: no data.

• Older adults: no adjustment.

• Kidney impairment: no adjustment. Liver impairment: exposure increases in severe cirrhosis; use with caution.

• East Africa: availability is limited; budesonide or beclometasone are more often stocked.

Formulations. Solution inhaler 80 and 160 micrograms/actuation.

Technique. Shake gently, use with a spacer, hold the breath for 10 seconds. A mouth rinse is still advised.

Baseline. Spirometry or peak flow, control score.

Monitoring. Control, reliever use, exacerbations, spirometry, height in adolescents.

Stop and reduce rules. Step down when control holds. Therapeutic drug monitoring is not used.

Referral and escalation. Refer if control fails on 640 micrograms daily or with repeated oral corticosteroid courses.