Zetonna (ciclesonide)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Ciclesonide is a synthetic, nonhalogenated corticosteroid that has glucocorticoid activity.
Ciclesonide is a synthetic, nonhalogenated corticosteroid. Ciclesonide is a prodrug that is hydrolyzed by esterases in the nasal mucosa to its major active metabolite C21-desisobutyryl-ciclesonide (des-ciclesonide). Des-ciclesonide exhibits anti-inflammatory activity, with affinity for glucocorticoid receptors that is 120 times that of the parent compound.
The exact mechanism(s) of action of ciclesonide in allergic rhinitis remains unknown. However, corticosteroids have been shown to have a wide range of effects on multiple cell types (e.g., mast cells, eosinophils, neutrophils, macrophages, lymphocytes) and mediators (e.g., histamine, eicosanoids, leukotrienes, cytokines) involved in allergic inflammation. In adults and children 12 years of age and older receiving intranasal ciclesonide, reductions in nasal symptoms occurred within 24-48 hours following initiation of therapy and persisted throughout the 24-hour dosing interval.
Ciclesonide may alter adrenal function in pediatric patients. In several studies, decreases in 24-hour urinary free cortisol concentrations and/or mean morning plasma cortisol concentrations were numerically larger in children 2-11 years of age receiving intranasal ciclesonide (25, 100, or 200 mcg daily) compared with those receiving placebo. Effects of ciclesonide nasal spray on adrenal function in adults and adolescents have not been established.
Following intranasal administration at recommended dosages (200 mcg daily), only negligible concentrations (less than 1%) of ciclesonide and des-ciclesonide were detected in adults; however, des-ciclesonide was detected in 50% of children 6-11 years of age receiving recommended intranasal dosages of the drug. Ciclesonide and des-ciclesonide are extensively (at least 99%) bound to plasma proteins (mainly albumin and alpha1-acid glycoprotein); des-ciclesonide is not appreciably bound to human transcortin. Des-ciclesonide, the major active metabolite of ciclesonide, is metabolized by the cytochrome P-450 (CYP) microsomal enzyme system, principally by the isoenzyme 3A4 (CYP3A4) and, to a lesser extent, by CYP2D6.
Other potentially active metabolites of ciclesonide have not been fully characterized. Following IV or oral administration of ciclesonide, the terminal elimination half-life of des-ciclesonide is 2.7 or 5.9 hours, respectively. Following IV administration of 800 mcg of ciclesonide, approximately 66% of radiolabeled ciclesonide was detected in feces and 20% or less detected in urine.
Generic name: ciclesonide
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Zetonna
Indications
The following indications are listed for Zetonna:
- Allergic Rhinitis
- Perennial Allergic Rhinitis
- Seasonal Allergic Rhinitis
Also known as: Atopic Rhinitis, Intermittent Allergic Rhinitis, Non-Seasonal Allergic Rhinitis, Periodic Runny Nose, Seasonal Allergy.
Dosing
For the symptomatic management of seasonal allergic rhinitis, the recommended dosage of intranasal ciclesonide in adults and children 6 years of age and older is 100 mcg (2 sprays) in each nostril once daily (total daily dosage of 200 mcg).
For the symptomatic management of perennial allergic rhinitis, the recommended dosage of intranasal ciclesonide in adults and children 12 years of age and older is 100 mcg (2 sprays) in each nostril once daily (total daily dosage of 200 mcg).
The maximum dosage should not exceed 200 mcg daily (2 sprays in each nostril once daily).
Ciclesonide is administered by nasal inhalation as a hypotonic aqueous suspension using a metered-dose spray pump.
Prior to initial use of the inhaler, the bottle should be shaken gently, and the pump should be primed by pressing downward on the shoulders of the applicator 8 times. After initial priming (8 sprays), the nasal spray delivers about 50 mcg of ciclesonide per metered spray and about 120 metered sprays. If the pump is unused for 4 consecutive days, the bottle should be shaken gently, and the pump should be reprimed by actuating once or until a fine spray appears.
Prior to administration of the nasal suspension using the spray pump, patients should blow the nose as needed to clear their nasal passages. The bottle should be shaken gently. Patients should tilt the head slightly forward and insert the spray tip into one nostril, keeping the bottle upright. The drug suspension should be sprayed quickly and firmly into one nostril (away from the nasal septum) while holding the other nostril closed and concurrently inspiring through the nose. This procedure should be repeated for the other nostril. The applicator should be wiped with a clean tissue after daily use.
To unblock or thoroughly clean the applicator, patients should be advised to remove the dust cap and gently pull upward to free the applicator. The dust cap and applicator should be washed in warm water and then dried, and then the applicator should be replaced on the bottle. The pump should be reprimed by actuating once or until a fine spray appears; then the dust cap should be replaced.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
Based on results of in vitro studies, des-ciclesonide does not appear to inhibit or induce the metabolism of other drugs metabolized by cytochrome P-450 (CYP) isoenzymes. The inhibitory potential of ciclesonide on CYP isoenzymes has not been studied.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
Known hypersensitivity to ciclesonide or any ingredient of the formulation.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects occurring in 1% or more of patients receiving ciclesonide nasal spray and more frequently than with placebo include headache, epistaxis, nasopharyngitis, nasal discomfort, pharyngolaryngeal pain, and ear pain.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety of intranasal ciclesonide has not been established in children younger than 2 years of age.
Efficacy of intranasal ciclesonide has not been established in children younger than 6 years of age for the treatment of seasonal allergic rhinitis or younger than 12 years of age for the treatment of perennial allergic rhinitis.
Intranasal corticosteroids may cause growth suppression in children or adolescents, and clinicians should routinely monitor (e.g., via stadiometry) the growth of pediatric patients receiving these drugs. See Cautions: Pediatric Precautions, in the Corticosteroids General Statement 68:04.
Category C. (See Users Guide.) Hypoadrenalism may occur in infants of mothers receiving corticosteroid therapy during pregnancy. These infants should be carefully monitored.
Ciclesonide is distributed into milk in rats. It is not known whether ciclesonide is distributed into human milk. Because other corticosteroids are distributed into human milk, caution is advised if ciclesonide is administered in nursing women.
Clinical studies of ciclesonide nasal spray did not include sufficient numbers of patients 65 years of age and older to determine whether geriatric patients respond differently than younger patients. Other reported clinical experience has not revealed age-related differences in response. In general, dosage should be selected cautiously in geriatric patients because of age-related decreases in hepatic, renal, and/or cardiac function and of concomitant disease and drug therapy.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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