Ciclex

Approved Indications:

• Asthma (Maintenance Treatment):
• Indicated for the maintenance treatment of asthma as prophylactic therapy in adults and adolescents aged 12 years and older.
• May be used in children ≥4 years for mild to moderate persistent asthma.
• Allergic Rhinitis (Seasonal and Perennial):
• Intranasal ciclesonide is indicated for symptomatic relief of nasal congestion, rhinorrhea, sneezing, and nasal itching associated with seasonal or perennial allergic rhinitis in adults and children aged ≥6 years.

Off-label / Clinically Accepted Uses:

• Nasal Polyps (Adjunctive):
• Used intranasally to reduce inflammation and polyp size.
• Non-allergic Rhinitis:
• In selected patients with non-allergic rhinitis for anti-inflammatory benefits.
• Eosinophilic Esophagitis (EoE):
• Used as a swallowed aerosol (off-label) in some pediatric and adult protocols.

Available Forms:

• Metered-dose inhaler (MDI): 80 mcg/actuation or 160 mcg/actuation
• Nasal spray: 50 mcg/actuation

For Asthma (Inhaled Route):

Adults and Adolescents ≥12 years:

• Initial dose: 80–160 mcg once daily via oral inhalation
• Maximum dose: 320 mcg/day
• Administer once daily in the evening

Pediatric Patients (4–11 years):

• Usual dose: 80 mcg once daily in the evening
• Higher doses not recommended due to limited data

For Allergic Rhinitis (Nasal Route):

Adults and Children ≥6 years:

• 2 sprays per nostril once daily (200 mcg total daily dose)

Special Populations:

• Renal impairment: No dosage adjustment required
• Hepatic impairment: Use with caution in severe hepatic dysfunction
• Elderly: No dose adjustment needed

Administration Tips:

• For inhalation: Rinse mouth after use to prevent oropharyngeal candidiasis
• For nasal spray: Prime before first use and if not used for ≥4 days; shake gently before each use

Ciclesonide is a prodrug corticosteroid that is converted to its active metabolite des-ciclesonide by esterases in the lungs or nasal mucosa. Des-ciclesonide exhibits strong anti-inflammatory activity by binding to glucocorticoid receptors, leading to the inhibition of multiple inflammatory cytokines, chemokines, and mediators. This reduces airway hyperresponsiveness, eosinophilic inflammation, and mucosal edema. The drug also suppresses activation and infiltration of immune cells such as mast cells and eosinophils, thereby relieving asthma and rhinitis symptoms.

• Absorption: Low systemic bioavailability (<1%) due to extensive first-pass metabolism
• Peak Plasma Time: ~1–2 hours after inhalation
• Distribution: Highly protein-bound (~99% to albumin)
• Metabolism: Hepatic activation by esterases to des-ciclesonide; further metabolism via CYP3A4
• Elimination: Primarily fecal; minor renal excretion
• Half-life:
• Ciclesonide: ~0.5 hours
• Des-ciclesonide: ~6–7 hours
• Bioavailability: Inhaled route – low systemic availability; nasal route – minimal systemic absorption

• Pregnancy:
• No FDA pregnancy category under the updated system.
• Animal studies show no teratogenicity at therapeutic doses. Use if benefits outweigh risks.
• Prolonged use of corticosteroids in pregnancy may affect fetal growth.
• Lactation:
• Unknown whether ciclesonide or its metabolites are excreted in human milk.
• Low systemic absorption suggests minimal risk. Caution is advised, especially with long-term use.
• Recommendation: Monitor infant growth if used during lactation; use lowest effective dose.

• Primary Class: Corticosteroid (Inhaled/Nasal)
• Subclass: Inhaled Glucocorticoid / Intranasal Anti-inflammatory Agent

• Hypersensitivity to ciclesonide or formulation components
• Acute bronchospasm (not for emergency relief)
• Untreated localized or systemic infections (e.g., tuberculosis)
• Status asthmaticus (requires systemic therapy)

• Not for Acute Asthma Attacks: Does not relieve bronchospasm; must be used with a fast-acting bronchodilator if needed
• Oral Candidiasis: Rinse mouth after inhalation to reduce risk
• Suppression of Hypothalamic-Pituitary-Adrenal (HPA) Axis: Rare at recommended doses but possible with prolonged or high-dose use
• Growth Suppression in Children: Monitor height regularly during long-term use
• Immunosuppression: Caution in patients with active infections or recent exposure to measles/varicella
• Glaucoma & Cataracts: Monitor with long-term use
• Paradoxical Bronchospasm: Discontinue if it occurs

Common Side Effects:

Inhalation (Asthma):

• Headache
• Cough
• Hoarseness
• Oropharyngeal candidiasis
• Nasal congestion

Nasal Spray (Rhinitis):

• Epistaxis (nosebleed)
• Nasal burning or irritation
• Pharyngitis
• Headache

Serious or Rare Side Effects:

• Adrenal suppression
• Growth retardation in children
• Glaucoma or posterior subcapsular cataract
• Paradoxical bronchospasm
• Anaphylaxis or angioedema (rare)

Onset: Most side effects occur within days to weeks; risk increases with higher doses or prolonged use

• CYP3A4 Inhibitors (e.g., ketoconazole, ritonavir, itraconazole):
• May increase systemic exposure to des-ciclesonide; caution with strong inhibitors
• Other Inhaled Steroids: Risk of additive systemic corticosteroid effects
• Live Vaccines: Avoid during long-term or high-dose corticosteroid use

Drug-Food Interactions:

• No significant food interactions reported

Drug-Alcohol Interactions:

• No direct interactions; however, excessive alcohol may exacerbate immunosuppression

• GINA 2024 Asthma Guidelines: Ciclesonide remains a valid option for stepwise asthma management in children and adults; valued for once-daily dosing and low systemic absorption
• ARIA 2023 Rhinitis Guidelines: Intranasal ciclesonide approved for long-term control of allergic rhinitis with lower risk of systemic corticosteroid exposure
• Safety Review (2023): No new significant safety concerns; continued recommendation to monitor pediatric growth and ocular health with chronic use

• Inhaler:
• Store at 20°C to 25°C (68°F to 77°F)
• Protect from direct sunlight and heat
• Do not freeze or expose to temperatures above 49°C (120°F)
• Do not puncture or incinerate pressurized canister
• Nasal Spray:
• Store at 20°C to 25°C (68°F to 77°F)
• Protect from light and moisture
• Shake gently before each use
• Discard after 120 actuations, even if spray seems to remain