worthwhile [12:<1%) because of low GI absorption and high first-pass metabolism. 1 4 7 9 11 Following oral inhalation, absolute bioavailability of ciclesonide is 22%; relative systemic exposure of des-ciclesonide is 63%. 1 Special Populations In patients with moderate to severe hepatic impairment, increased systemic exposure of des-ciclesonide (i.e., peak plasma concentrations, AUC). 1 Distribution Extent Glucocorticoids cross the placenta. a Not known whether ciclesonide is distributed into milk; 1 however, other corticosteroids are distributed into milk. 1 Plasma Protein Binding 99%; 1 3 7 8 9 11 12 des-ciclesonide is not appreciably bound to human transcortin. 1 8 12 Elimination Metabolism Hydrolyzed by esterases to the active metabolite C21-desisobutyryl-ciclesonide (des-ciclesonide). 1 3 4 7 8 9 11 Des-ciclesonide is metabolized in the liver principally by CYP3A4 and, to a lesser extent, by CYP2D6. 1 4 11 Elimination Route Excreted principally in feces (66%) as ciclesonide and to a lesser extent ( 20%) in urine as des-ciclesonide. 1 Half-life The mean elimination half-lives of ciclesonide and des-ciclesonide are 0.71 and 6 7 hours, respectively, following IV administration. 1 12 Special Populations In patients with renal impairment, pharmacokinetics not evaluated. 1 Stability Storage Oral Inhalation Inhalation Solution 25 C (may be exposed to 15 30 C). 1 Contents of oral inhaler are under pressure; do not puncture, use or store aerosol container near heat or an open flame, expose to temperatures> 49 C, or place into a fire or incinerator for disposal. 1 Actions Prodrug with little pharmacologic activity until hydrolyzed to active metabolite des-ciclesonide. 1 3 4 7 8 9 11 Des-ciclesonide exhibits anti-inflammatory activity, with affinity for glucocorticoid receptors that is 120 times that of ciclesonide. 1 4 7 11 Exact mechanism(s) of action not known; however, may reduce inflammatory asthmatic response by inhibiting multiple cell types (e.g., mast cells, eosinophils, neutrophils, macrophages, lymphocytes, basophils) and mediators (e.g., histamine, eicosanoids, leukotrienes, cytokines) involved in the asthmatic response. 1 Improves lung function (e.g., FEV 1 , morning PEFR). 1 Advice to Patients Importance of providing the patient a copy of the manufacturer s patient information and medication guide. 1 6 Importance of adequate understanding of proper storage, preparation, and inhalation techniques, including use of the inhalation delivery system. 1 6 Importance of pediatric patients receiving therapy under adult supervision. 12 Risk of localized candidal infections of the mouth and pharynx. 1 6 Importance of rinsing the mouth with water without swallowing after oral inhalation. 1 6 Importance of advising patients that ciclesonide oral inhalation must be used at regular intervals to be therapeutically effective. 1 6 Importance of advising patients that at least 4 weeks of continuous therapy may be required for optimum effects to be achieved. 1 6 Importance of not exceeding the recommended dosage and of contacting a clinician immediately if symptoms of asthma worsen or fail to improve. 1 6 Importance of not discontinuing therapy with ciclesonide abruptly and of contacting a clinician immediately if use of ciclesonide is discontinued as symptoms may recur. 1 6 Importance of advising patients that orally inhaled ciclesonide should not be used as a bronchodilator and that the drug is not indicated for emergency use (e.g., relief of acute bronchospasm). 1 6 Importance of availability and use of a short-acting β 2 -adrenergic agonist for relief of acute asthma symptoms. 1 6 Importance of contacting a clinician immediately when asthmatic attacks are not controlled by current bronchodilator therapy. 1 6 Importance of gradual withdrawal from systemic corticosteroids during transfer to orally inhaled ciclesonide and of monitoring by a clinician during such transfer of therapy. 1 6 Importance of advising patients being transferred from systemic corticosteroid to ciclesonide oral inhalation therapy to carry special identification (e.g., card) indicating the need for supplementary systemic corticosteroids during periods of stress or severe exacerbation of asthma. 1 Importance of advising patients to immediately resume therapy with large doses of systemic corticosteroids and to contact their clinician for further instructions during stressful periods (e.g., stress, severe asthmatic attack, surgery, trauma, infection). 1 6 Risk of systemic corticosteroid effects (e.g., hypercorticism, potentially life-threatening adrenal suppression). 1 6 Importance of informing a clinician of fatigue, weakness, nausea, vomiting, dizziness, or fainting. 1 6 Importance of informing patients that corticosteroids may decrease BMD. 1 6 Risk of reduction in growth velocity in children and adolescents with orally inhaled corticosteroids. 1 Importance of immunosuppressed patients avoiding exposure to chickenpox and measles, and, if exposed, of immediately consulting their clinician. 1 Importance of advising immunosuppressed patients of potential worsening of existing tuberculosis; fungal, bacterial, parasitic, or viral infections; or ocular herpes simplex. 1 6 Importance of immunosuppressed patients informing clinician of a history of infections. 6 Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed. 1 6 Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses (e.g., infections). 1 6 Importance of informing patients of other important precautionary information. 1 (See Cautions.) Preparations Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details. Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations. Ciclesonide Routes Dosage Forms Strengths Brand Names Manufacturer Oral Inhalation Aerosol 80 mcg/metered spray Alvesco Sepracor 160 mcg/metered spray Alvesco Sepracor AHFS DI Essentials. Copyright 2017, Selected Revisions July 12, 2012. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814. References 1. Sepracor Inc. Alvesco (ciclesonide) inhalation aerosol prescribing information. Marlborough, MA; 2008 Jun. 2. Bateman E, Karpel J, Casale T et al. Ciclesonide reduces the need for oral steroid use in adult patients with severe, persistent asthma. Chest . 2006; 129:1176-87. [PubMed 16685007] 3. . Ciclesonide (Alvesco)-a new inhaled corticosteroid for asthma. Med Lett Drugs Ther . 2008; 50:75-6. [PubMed 18800024] 4. Reynolds NA, Scott LJ. Ciclesonide. Drugs . 2004; 64:511-9; discussion 520-1. [PubMed 14977388] 5. National Asthma Education and Prevention Program. Expert panel report 3: Guidelines for the diagnosis and management of asthma. Full report 2007. Bethesda, MD: National Institutes of Health, National Heart, Lung and Blood Institute. 2007 Aug 28. Available from website. Accessed 2008 Nov 7. 6. Sepracor Inc. Alvesco (ciclesonide) inhalation aerosol patient instructions for use. Marlborough, MA; 2008 Jun. 7. Deeks ED, Perry CM. Ciclesonide: a review of its use in the management of asthma. Drugs . 2008; 68:1741-70. [PubMed 18681495] 8. Rohatagi S, Luo Y, Shen L et al. Protein binding and its potential for eliciting minimal systemic side effects with a novel inhaled corticosteroid, ciclesonide. Am J Ther . 2005 May-Jun; 12:201-9. 9. Nave R, Drollmann A, Steinijans VW et al. Lack of pharmacokinetic drug-drug interaction between ciclesonide and erythromycin. Int J Clin Pharmacol Ther . 2005; 43:264-70. [PubMed 15968883] 10. Chu V, Zeng Z, Pan J et al. In vitro assessment of cytochrome P450 metabolic drug-drug interaction potential of ciclesonide [abstract no. 552]. Drug Metab Rev . 2004; 36 (Suppl 1):276. 11. Böhmer GM, Drollmann A, Gleiter CH et al. Effect of coadministered ketoconazole, a strong cytochrome P450 3A4 enzyme inhibitor, on the pharmacokinetics of ciclesonide and its active metabolite desisobutyryl-ciclesonide. Clin Pharmacokinet . 2008; 47:343-9. [PubMed 18399715] 12. Sepracor, Inc, Marlborough, MA: Personal communication. a. AHFS Drug Information 2011. McEvoy GK, ed. Corticosteroids General Statement. Bethesda, MD: American Society of Health-System Pharmacists; 2011:3047-62. Next Interactions Print this page Add to My Med List More about ciclesonide Side Effects During Pregnancy or Breastfeeding Dosage Information Drug Interactions Support Group En Español 15 Reviews Add your own review/rating Drug class: inhaled corticosteroids Consumer resources Ciclesonide inhalation Ciclesonide (Oral Inhalation) Ciclesonide Inhalation (Advanced Reading) Professional resources Ciclesonide (Oral Inhalation) (Wolters Kluwer) Other brands: Alvesco Related treatment guides Asthma Asthma, Maintenance ]} FEATURED: CAR-T Cell Therapy Overview Mechanism of Action KTE-C19 Studies KTE-C19 Cancer Targets Adverse Events Manufacturing Drug Status Rx Availability Prescription only C Pregnancy Category Risk cannot be ruled out N/A CSA Schedule Not a controlled drug Approval History Drug history at FDA Drug Class Inhaled corticosteroids Related Drugs Asthma, Maintenance Symbicort , albuterol , fluticasone , montelukast , ProAir HFA , Singulair , Advair Diskus , budesonide , Breo Ellipta , Ventolin , Medrol , methylprednisolone , More... Asthma prednisone , triamcinolone , montelukast , Singulair , ipratropium , Breo Ellipta , Medrol , dexamethasone , methylprednisolone , Dulera , Medrol Dosepak , Xopenex , More... Ciclesonide Rating 15 User Reviews 7.4 /10 15 User Reviews 7.4 Rate it!} } locate
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