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QuickView for Ciclesonide (compound)

Name: ciclesonide
PubChem Compound ID: 3081298
Molecular formula: C32H44O7
Molecular weight: 540.688 g/mol
(R)-11beta,16alpha,17,21-Tetrahydroxypregna-1,4-diene-3,20-dione, cyclic 16,17-acetal with cyclohexanecarboxaldehyde, 21-isobutyrate; 141845-82-1; Ciclesonide [INN]; Alvesco; Ciclesonide
Name: ciclesonide
Name (isomeric): DB01410
Drug Type: small molecule
Brand: Alvesco
Category: Anti-Allergic Agents, Glucocorticoids
CAS number: 141845-82-1
Indication: For the treatment of nasal symptoms associated with seasonal and perennial allergic rhinitis in adults and adolescents 12 years of age and older.
Ciclesonide is a pro-drug that is enzymatically hydrolyzed to a pharmacologically active metabolite, C21-desisobutyryl-ciclesonide (des-ciclesonide or RM1) following intranasal application. Des-ciclesonide has anti-inflammatory activity with affinity for the glucocorticoid receptor that is 120 times higher than the parent compound. The precise mech...
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Mechanism of Action:
Glucocorticoids such as ciclesonide can inhibit leukocyte infiltration at the site of inflammation, interfere with mediators of inflammatory response, and suppress humoral immune responses. The antiinflammatory actions of glucocorticoids are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of pote...
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Absorption: Ciclesonide and des-ciclesonide have negligible oral bioavailability (both less than 1%) due to low gastrointestinal absorption and high first-pass metabolism. The intranasal administration of ciclesonide at recommended doses results in negligible serum concentrations of ciclesonide.
Protein binding: The percentage of ciclesonide and des-ciclesonide bound to human plasma proteins averaged ≥ 99% each, with ≤ 1% of unbound drug detected in the systemic circulation.
Biotransformation: Des-ciclesonide undergoes metabolism in the liver to additional metabolites mainly by the cytochrome P450 (CYP) 3A4 isozyme and to a lesser extent by CYP 2D6.
Clearance: 152 L/hr [Following IV administration of 800 mcg of ciclesonide]
Affected organisms: Humans and other mammals
Drug interaction:
TelithromycinTelithromycin may reduce clearance of Ciclesonide. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Ciclesonide if Telithromycin is initiated, discontinued or dose changed.
KetoconazoleIncreased effects/toxicity of ciclesonide
ItraconazoleIncreased effects/toxicity of ciclesonide
RitonavirIncreased effects/toxicity of ciclesonide
NelfinavirIncreased effects/toxicity of ciclesonide
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