ciclesonide intranasal (Rx)

1-10%

Headache (3.1-6.6%)

Epistaxis (2.9-6%)

Nasopharyngitis (3.7%)

Nasal discomfort (3.2%)

Ear pain (2.2%)

<1%

Nasal congestion

Nasal ulcer

Dizziness

Localized infections of nose/mouth with Candida albicans

Contraindications

Hypersensitivity

Cautions

Epistaxis, Candida albicans infection, nasal septal perforation, and impaired wound healing reported; monitor patients periodically for signs of adverse effects on nasal mucosa

Avoid spraying directly onto nasal septum

Avoid use in patients with recent nasal ulcers, nasal surgery, or nasal trauma

Monitor for change in vision or with history of increased IOP, glaucoma, and/or cataracts

Potential worsening of existing tuberculosis; fungal, bacterial, viral, or parasitic infections, or ocular herpes simplex

Corticosteroids are known to cause immunosuppression; more serious or even fatal infections (eg, chickenpox or measles) may occur in susceptible patients

Hypercorticism and adrenal suppression with very high dosages or at the regular dosage in susceptible individuals; discontinue gradually if these changes occur

Potential reduction in growth velocity in children

Nasal/inhaled corticosteroids may increase risk for glaucoma and cataracts

Ocular toxicity

• Monitor patients for signs or symptoms of ocular toxicity, which may include blurred vision and reduced visual acuity
• Immune-mediated ocular toxicity may be associated with retinal detachment or permanent vision loss
• Administer corticosteroid eye drops to patients who develop uveitis, iritis, or episcleritis
• Permanently discontinue therapy for immune-mediated ocular disease that is unresponsive to local immunosuppressive therapy
• If uveitis occurs in combination with other immune-mediated adverse reactions, consider a Vogt Koyanagi-Harada-like syndrome, which has been observed in patients receiving drug and may require treatment with systemic steroids to reduce risk of permanent vision loss

Pregnancy Category: C

Lactation: Unknown whether distributed in breast milk; however, other corticosteroids are excreted in human milk; exercise caution

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Glucocorticoid

Ciclesonide is a prodrug that is enzymatically hydrolyzed to a pharmacologically active metabolite, C21-desisobutyryl-ciclesonide (des-ciclesonide or RM1) following intranasal application; desciclesonide has anti-inflammatory activity with 120 times the affinity for the glucocorticoid receptor than the parent compound

Absorption

Bioavailability: Negligible

Distribution

Protein Bound: >99%

Vd: 2.9 L/kg (parent compound); 12.1 L/kg (active metabolite)

Metabolism

Metabolites: Prodrug that is enzymatically hydrolyzed to a pharmacologically active metabolite, C21-desisobutyryl-ciclesonide (des-ciclesonide or RM1)

Metabolized by: Desciclesonide metabolized in liver by CYP3A4 and to a lesser extent by CYP2D6

Elimination

Excretion: Feces (66%); urine (~20%)