Ciclesonide (3 brand names, 3 dosage forms, 2 routes)
Available dosage forms: AEROSOL, METERED, SPRAY, SPRAY, METERED.
Routes of administration: INHALATION, NASAL.
Brand Names
- ALVESCO
- OMNARIS
- ZETONNA
Indications and Usage
ALVESCO is indicated for the maintenance treatment of asthma as prophylactic therapy in adult and pediatric patients 12 years of age and older. Limitations of Use: ALVESCO is not indicated for the relief of acute bronchospasm. ALVESCO is not indicated for children under 12 years of age.
Contraindications
ALVESCO is contraindicated in: the primary treatment of status asthmaticus or other acute episodes of asthma where intensive measures are required. patients with known hypersensitivity to ciclesonide or any of the ingredients of ALVESCO. Rare cases of hypersensitivity reactions with manifestations such as angioedema, with swelling of the lips, tongue and pharynx, have been reported.
Adverse Reactions
The following clinically significant adverse reactions are described elsewhere in the labeling: Oropharyngeal Candidiasis [see Warnings and Precautions ( 5.1)] Immunosuppression and Risk of Infections [see Warnings and Precautions ( 5.3)] Hypercorticism and Adrenal Suppression [see Warnings and Precautions ( 5.5)] Reduction in Bone Mineral Density [see Warnings and Precautions ( 5.6)] Growth Effects [see Warnings and Precautions ( 5.7)] Glaucoma and Cataracts [see Warnings and Precautions ( 5.8)]
Drug Interactions
In clinical studies, concurrent administration of ciclesonide and other drugs commonly used in the treatment of asthma (albuterol, formoterol) had no effect on pharmacokinetics of des-ciclesonide [see Clinical Pharmacology ( 12.3)] . In vitrostudies and clinical pharmacology studies suggested that des-ciclesonide has no potential for metabolic drug interactions or protein binding-based drug interactions [see Clinical Pharmacology ( 12.3)] . In a drug interaction study, co-administration of orally inhaled ciclesonide and oral ketoconazole, a potent inhibitor of cytochrome P450 3A4, increased the exposure (AUC) of des-ciclesonide by approximately 3.6-fold at steady state, while levels of ciclesonide remained unchanged.
Mechanism of Action
Ciclesonide is a prodrug that is enzymatically hydrolyzed to a pharmacologically active metabolite, C21-desisobutyryl-ciclesonide (des-ciclesonide or RM1) following oral inhalation. Des-ciclesonide has anti-inflammatory activity with affinity for glucocorticoid receptors that is 120 times greater than the parent compound and 12 times greater than dexamethasone. The clinical significance of these findings is unknown. The precise mechanisms of corticosteroid action in asthma are unknown. Inflammation is recognized as an important component in the pathogenesis of asthma. Corticosteroids have been shown to have a wide range of inhibitory activities against multiple cell types (e.g., mast cells, eosinophils, basophils, lymphocytes, macrophages, and neutrophils) and mediators (e.g., histamine, eicosanoids, leukotrienes, and cytokines) involved in the asthmatic response. These anti-inflammatory actions of corticosteroids may contribute to their efficacy in asthma. Though effective for the treatment of asthma, corticosteroids do not affect asthma symptoms immediately. Individual patients will experience a variable time to onset and degree of symptom relief. Maximum benefit may not be achieved for four weeks or longer after starting treatment. When corticosteroids are discontinued, asthma stability may persist for several days or longer.
Overdosage
Chronic overdosage may result in signs/symptoms of hypercorticism [see Warnings and Precautions ( 5.5)] .