ciclesonide inhaled (Rx)

>10%

Headache (11%)

Nasopharyngitis (11%)

1-10%

Epistaxis (4.9%)

Ear pain (2.2%)

Facial edema (3%)

Urticaria (3%)

Oral candidiasis (3%)

Back pain (3%)

Extremety pain (3%)

Conjunctivitis (3%)

Upper respiratory infection (9%)

Gastroenteritis (3%)

Sinusitis (3%)

Contraindications

Documented hypersensitivity

Treatment of acute asthma or status asthmaticus

Cautions

Caution in active serious infections

Secondary infections may occur as a result of prolonged use of corticosteroids

Avoid exposure to chickenpox or measles

Not for acute asthma treatment

When switching from oral corticosteroids

Bronchospasm may occur following inhalation (treat with fast acting bronchodilator)

High doses may cause suppression of hypothalamic-pituitary-adrenal axis, which can result in adrenal crisis

Long-term use may result in: reduced BMD; glaucoma or cataracts; increased IOP

Development of Kaposi's sarcoma associated with prolonged use of corticosteroids

Psychiatric disturbances reported with corticosteroid use

Pregnancy Category: C

Lactation: Not known if excreted in breast milk, use 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 prodrug, converted to active ingredient des-ciclesonide; has immunosuppressive properties, anti-inflammatory activity, and anti-inflammatory effects.

Distribution

Bioavailability: 63% (active metabolite)

Absorption: 52%

Protein Bound: 99% (IV)

Vd: 2.9 L/kg (ciclesonide); 12.1 L/kg (des-ciclesonide) following IV administration

Metabolism

Metabolized to active des-ciclesonide by esterases, then further metabolized by liver CYP3A4 and to a lesser extent, CYP2D6

Eliminiation

Following IV administration

• Half-life: 0.71 hr (ciclesonide); 6-7 hr (des-ciclesonide)
• Clearance: 152 L/L/hr (ciclesonide); 228 L/L/hr (des-ciclesonide)
• Excretion: Feces (66%); urine (20%)