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Ciclesonide: Wikis

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Ciclesonide
Systematic (IUPAC) name
2-[(1S, 2S, 4R, 8S, 9S,11S, 12S, 13R)-6-cyclohexyl-11-hydroxy-9, 13-dimethyl-16-oxo-5, 7-dioxapentacyclo [10.8.0.02,9.04, 8.013,18] icosa-14, 17-dien-8-yl]- 2-oxoethyl 2-methylpropanoate
Identifiers
CAS number 141845-82-1
ATC code R03BA08
PubChem 444033
Chemical data
Formula C 32H44O7  
Mol. mass 540.688 g/mol
Synonyms (11β, 16α)-16, 17-[[(R)-cyclohexylmethylene]bis(oxy)]-11-hydroxy-21- (2-methyl-1-oxopropoxy)- pregna-1, 4-diene-3, 20-dione
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat. B3(AU) C(US)
Legal status Prescription Only (S4) (AU) POM (UK) -only (US)
Routes  ?

Ciclesonide is a glucocorticoid used to treat obstructive airway diseases. It is marketed under the brand name Alvesco for asthma and Omnaris/Omniair for hayfever in the US & Canada. Phase 3 trials for the hayfever indication outside the US are ongoing.[1]

Contents

Indications

Maintenance treatment in persistent asthma; hayfever.

Specific Considerations

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Pregnancy

No data as yet exists, Other inhaled glucocorticoids are considered ADEC category B3.

Breastfeeding

Should be safe to use. Consult your medical professional.

Practice Points

  • Appears to be as effective as budesonide or fluticasone for maintenance treatment in persistent asthma although long term data on clinical outcomes are lacking.
  • In short term studies ciclesonide had a minimal effect on markers of adrenal suppression but data with long term use is lacking. The US Food and Drug Administration (FDA) announced October 2006 the approval of ciclesonide nasal spray for the treatment of nasal symptoms associated with seasonal and perennial allergic rhinitis in adults and children 12 years of age and older.[2]

The safety and efficacy of the nasal spray, manufactured by ALTANA Pharma US, Inc. of Florham Park, NJ, were studied in randomized placebo controlled clinical trials. The studies showed that patients treated with nasal spray had an 8-10 percent greater reduction in nasal symptoms compared to placebo, with difference between ciclesonide nasal spray and placebo significant, i.e. p<0.05.

The highest level of conversion was found in the liver, the site of inactivation of des-CIC through rapid oxidation by cytochrome P450. Carboxylesterases in bronchial epithelial cells probably contribute significantly to the conversion to des-CIC in the target organ, whereas low systemic levels of des-CIC are a result of the high metabolic clearance by the liver following CIC inhalation.

The most common side effects were headache, nosebleeds, and inflammation of the nose and throat linings.[3]

References

  • Rossi S (Ed.) (2006). Australian Medicines Handbook 2006. Adelaide: Australian Medicines Handbook. ISBN 0-9757919-2-3

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