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Identification
NameCiclesonide
Accession NumberDB01410
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionCiclesonide is a glucocorticoid used to treat obstructive airway diseases. It is marketed under the brand name Alvesco.
Structure
Thumb
SynonymsNot Available
External Identifiers
  • BI54903
  • RPR-251526
  • RPR251526
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Alvescoaerosol, metered dose100 mcginhalationTakeda Canada Inc2006-09-27Not applicableCanada
Alvescoaerosol, metered80 ug/1respiratory (inhalation)Physicians Total Care, Inc.2009-02-19Not applicableUs
Alvescoaerosol, metered80 ug/1respiratory (inhalation)Sunovion Pharmaceuticals Inc.2008-10-01Not applicableUs
Alvescoaerosol, metered dose200 mcginhalationTakeda Canada Inc2006-09-27Not applicableCanada
Alvescoaerosol, metered160 ug/1respiratory (inhalation)Physicians Total Care, Inc.2009-02-23Not applicableUs
Alvescoaerosol, metered160 ug/1respiratory (inhalation)Sunovion Pharmaceuticals Inc.2008-10-01Not applicableUs
Alvescoaerosol, metered dose50 mcginhalationTakeda Canada IncNot applicableNot applicableCanada
Omnarisspray50 ug/1nasalREMEDYREPACK INC.2013-07-16Not applicableUs
Omnarisspray, metered dose50 mcgnasalTakeda Canada Inc2008-04-10Not applicableCanada
Omnarisspray50 ug/1nasalSunovion Pharmaceuticals Inc.2008-03-01Not applicableUs
Omnarisspray50 ug/1nasalPhysicians Total Care, Inc.2009-04-15Not applicableUs
Omnaris HFAaerosol, metered dose50 mcgnasalTakeda Canada Inc2013-08-07Not applicableCanada
Zetonnaaerosol, metered37 ug/1nasalSunovion Pharmaceuticals Inc.2012-07-30Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-ciclesonidespray, metered dose50 mcgnasalApotex IncNot applicableNot applicableCanada
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
OmniairNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIS59502J185
CAS number126544-47-6
WeightAverage: 540.697
Monoisotopic: 540.308703757
Chemical FormulaC32H44O7
InChI KeyLUKZNWIVRBCLON-GXOBDPJESA-N
InChI
InChI=1S/C32H44O7/c1-18(2)28(36)37-17-25(35)32-26(38-29(39-32)19-8-6-5-7-9-19)15-23-22-11-10-20-14-21(33)12-13-30(20,3)27(22)24(34)16-31(23,32)4/h12-14,18-19,22-24,26-27,29,34H,5-11,15-17H2,1-4H3/t22-,23-,24-,26+,27+,29+,30-,31-,32+/m0/s1
IUPAC Name
2-[(1S,2S,4R,6R,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
SMILES
[H][C@@]12C[C@@]3([H])[C@]4([H])CCC5=CC(=O)C=C[C@]5(C)[C@@]4([H])[C@@H](O)C[C@]3(C)[C@@]1(O[C@@H](O2)C1CCCCC1)C(=O)COC(=O)C(C)C
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as gluco/mineralocorticoids, progestogins and derivatives. These are steroids with a structure based on a hydroxylated prostane moiety.
KingdomOrganic compounds
Super ClassLipids and lipid-like molecules
ClassSteroids and steroid derivatives
Sub ClassPregnane steroids
Direct ParentGluco/mineralocorticoids, progestogins and derivatives
Alternative Parents
Substituents
  • Progestogin-skeleton
  • 20-oxosteroid
  • 3-oxo-delta-1,4-steroid
  • 3-oxosteroid
  • 11-hydroxysteroid
  • 11-beta-hydroxysteroid
  • Oxosteroid
  • Hydroxysteroid
  • Delta-1,4-steroid
  • Alpha-acyloxy ketone
  • Meta-dioxolane
  • Cyclic alcohol
  • Carboxylic acid ester
  • Cyclic ketone
  • Secondary alcohol
  • Ketone
  • Acetal
  • Carboxylic acid derivative
  • Oxacycle
  • Organoheterocyclic compound
  • Monocarboxylic acid or derivatives
  • Carbonyl group
  • Organic oxide
  • Hydrocarbon derivative
  • Organic oxygen compound
  • Organooxygen compound
  • Alcohol
  • Aliphatic heteropolycyclic compound
Molecular FrameworkAliphatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of nasal symptoms associated with seasonal and perennial allergic rhinitis in adults and adolescents 12 years of age and older.
PharmacodynamicsCiclesonide 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 mechanism through which ciclesonide affects allergic rhinitis symptoms is not known. Corticosteroids have been shown to have a wide range of effects on multiple cell types (e.g., mast cells, eosinophils, neutrophils, macrophages, and lymphocytes) and mediators (e.g., histamine, eicosanoids, leukotrienes, and cytokines) involved in allergic inflammation.
Mechanism of actionGlucocorticoids 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 potent mediators of inflammation such as prostaglandins and leukotrienes. Ciclesonide reduces inflammatory reaction by limiting the capillary dilatation and permeability of the vascular structures. These compounds restrict the accumulation of polymorphonuclear leukocytes and macrophages and reduce the release of vasoactive kinins. Recent research suggests that corticosteroids may inhibit the release of arachidonic acid from phospholipids, thereby reducing the formation of prostaglandins. Ciclesonide is a glucocorticoid receptor agonist. On binding, the corticoreceptor-ligand complex translocates itself into the cell nucleus, where it binds to many glucocorticoid response elements (GRE) in the promoter region of the target genes. The DNA bound receptor then interacts with basic transcription factors, causing an increase or decrease in expression of specific target genes, including suppression of IL2 (interleukin 2) expression.
Related Articles
AbsorptionCiclesonide 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.
Volume of distributionNot Available
Protein bindingThe percentage of ciclesonide and des-ciclesonide bound to human plasma proteins averaged ≥ 99% each, with ≤ 1% of unbound drug detected in the systemic circulation.
Metabolism

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.

Route of eliminationNot Available
Half lifeNot Available
Clearance
  • 152 L/hr [Following IV administration of 800 mcg of ciclesonide]
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9907
Blood Brain Barrier+0.9439
Caco-2 permeable-0.6847
P-glycoprotein substrateSubstrate0.7787
P-glycoprotein inhibitor IInhibitor0.8247
P-glycoprotein inhibitor IIInhibitor0.9476
Renal organic cation transporterNon-inhibitor0.7744
CYP450 2C9 substrateNon-substrate0.8232
CYP450 2D6 substrateNon-substrate0.915
CYP450 3A4 substrateSubstrate0.774
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorNon-inhibitor0.7104
CYP450 2D6 inhibitorNon-inhibitor0.9407
CYP450 2C19 inhibitorNon-inhibitor0.9151
CYP450 3A4 inhibitorNon-inhibitor0.6192
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8478
Ames testNon AMES toxic0.9032
CarcinogenicityNon-carcinogens0.9367
BiodegradationNot ready biodegradable0.9897
Rat acute toxicity3.5547 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9738
hERG inhibition (predictor II)Non-inhibitor0.595
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Aerosol, meteredrespiratory (inhalation)160 ug/1
Aerosol, meteredrespiratory (inhalation)80 ug/1
Aerosol, metered doseinhalation100 mcg
Aerosol, metered doseinhalation200 mcg
Aerosol, metered doseinhalation50 mcg
Spraynasal50 ug/1
Spray, metered dosenasal50 mcg
Aerosol, metered dosenasal50 mcg
Aerosol, meterednasal37 ug/1
Prices
Unit descriptionCostUnit
Alvesco 160 mcg/act Aerosol 6.1 gm Inhaler162.24USD inhaler
Alvesco 80 mcg/act Aerosol 6.1 gm Inhaler162.24USD inhaler
Alvesco 160 mcg inhaler31.1USD g
Alvesco 80 mcg inhaler31.1USD g
Omnaris 50 mcg nasal spray11.01USD g
Alvesco 200 mcg/dose Metered Dose Aerosol0.66USD dose
Alvesco 100 mcg/dose Metered Dose Aerosol0.4USD dose
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2050812 No2003-07-292011-09-06Canada
CA2388325 No2007-09-182020-10-20Canada
US5482934 No1997-10-242017-10-24Us
US5695743 No1993-07-062010-07-06Us
US5775321 No1995-07-072015-07-07Us
US6006745 No1996-12-282016-12-28Us
US6120752 No1998-05-132018-05-13Us
US6264923 No1998-05-132018-05-13Us
US6767901 No2000-10-212020-10-21Us
US6939559 No1999-04-212019-04-21Us
US7235247 No1999-04-212019-04-21Us
US8371292 No2008-02-012028-02-01Us
US8383611 No2000-10-202020-10-20Us
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.00157 mg/mLALOGPS
logP4.08ALOGPS
logP5.32ChemAxon
logS-5.5ALOGPS
pKa (Strongest Acidic)14.78ChemAxon
pKa (Strongest Basic)-2.9ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area99.13 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity146.28 m3·mol-1ChemAxon
Polarizability60.18 Å3ChemAxon
Number of Rings6ChemAxon
Bioavailability0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
References
Synthesis Reference

Beate Schmidt, “Process for preparing crystalline ciclesonide with defined particle size.” U.S. Patent US20060128954, issued June 15, 2006.

US20060128954
General References
  1. Mutch E, Nave R, McCracken N, Zech K, Williams FM: The role of esterases in the metabolism of ciclesonide to desisobutyryl-ciclesonide in human tissue. Biochem Pharmacol. 2007 May 15;73(10):1657-64. Epub 2007 Jan 28. [PubMed:17331475 ]
External Links
ATC CodesR03BA08R01AD13
AHFS Codes
  • 68:04.00
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
1,10-PhenanthrolineThe risk or severity of adverse effects can be increased when Ciclesonide is combined with 1,10-Phenanthroline.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Ciclesonide.
AldesleukinCiclesonide may decrease the antineoplastic activities of Aldesleukin.
Aluminum hydroxideThe bioavailability of Ciclesonide can be decreased when combined with Aluminum hydroxide.
Aluminum phosphateThe bioavailability of Ciclesonide can be decreased when combined with Aluminum phosphate.
AmbenoniumThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Ambenonium.
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Ciclesonide.
AmiodaroneThe serum concentration of Ciclesonide can be increased when it is combined with Amiodarone.
Amphotericin BCiclesonide may increase the hypokalemic activities of Amphotericin B.
AprepitantThe serum concentration of Ciclesonide can be increased when it is combined with Aprepitant.
AtazanavirThe serum concentration of Ciclesonide can be increased when it is combined with Atazanavir.
AtomoxetineThe metabolism of Ciclesonide can be decreased when combined with Atomoxetine.
Atracurium besylateAtracurium besylate may increase the adverse neuromuscular activities of Ciclesonide.
BazedoxifeneThe serum concentration of Ciclesonide can be increased when it is combined with Bazedoxifene.
BendroflumethiazideCiclesonide may increase the hypokalemic activities of Bendroflumethiazide.
Benzoic AcidThe therapeutic efficacy of Benzoic Acid can be decreased when used in combination with Ciclesonide.
BexaroteneThe serum concentration of Ciclesonide can be decreased when it is combined with Bexarotene.
Bismuth SubcitrateThe bioavailability of Ciclesonide can be decreased when combined with Bismuth Subcitrate.
BoceprevirThe serum concentration of Ciclesonide can be increased when it is combined with Boceprevir.
BortezomibThe metabolism of Ciclesonide can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Ciclesonide can be decreased when it is combined with Bosentan.
BumetanideCiclesonide may increase the hypokalemic activities of Bumetanide.
CalcitriolThe therapeutic efficacy of Calcitriol can be decreased when used in combination with Ciclesonide.
Calcium carbonateThe bioavailability of Ciclesonide can be decreased when combined with Calcium carbonate.
CarbamazepineThe serum concentration of Ciclesonide can be decreased when it is combined with Carbamazepine.
CeritinibThe serum concentration of Ciclesonide can be increased when it is combined with Ceritinib.
CeritinibCiclesonide may increase the hyperglycemic activities of Ceritinib.
ChlorothiazideCiclesonide may increase the hypokalemic activities of Chlorothiazide.
ChlorotrianiseneThe serum concentration of Ciclesonide can be increased when it is combined with Chlorotrianisene.
ChlorthalidoneCiclesonide may increase the hypokalemic activities of Chlorthalidone.
CholestyramineCholestyramine can cause a decrease in the absorption of Ciclesonide resulting in a reduced serum concentration and potentially a decrease in efficacy.
ClarithromycinThe serum concentration of Ciclesonide can be increased when it is combined with Clarithromycin.
ClemastineThe metabolism of Ciclesonide can be decreased when combined with Clemastine.
ClotrimazoleThe metabolism of Ciclesonide can be decreased when combined with Clotrimazole.
CobicistatThe serum concentration of Ciclesonide can be increased when it is combined with Cobicistat.
ColesevelamColesevelam can cause a decrease in the absorption of Ciclesonide resulting in a reduced serum concentration and potentially a decrease in efficacy.
ColestipolColestipol can cause a decrease in the absorption of Ciclesonide resulting in a reduced serum concentration and potentially a decrease in efficacy.
ConivaptanThe serum concentration of Ciclesonide can be increased when it is combined with Conivaptan.
Conjugated Equine EstrogensThe serum concentration of Ciclesonide can be increased when it is combined with Conjugated Equine Estrogens.
Corticorelin ovine triflutateThe therapeutic efficacy of Corticorelin ovine triflutate can be decreased when used in combination with Ciclesonide.
CoumaphosThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Coumaphos.
CrizotinibThe metabolism of Ciclesonide can be decreased when combined with Crizotinib.
CyclosporineThe metabolism of Ciclesonide can be decreased when combined with Cyclosporine.
DabrafenibThe serum concentration of Ciclesonide can be decreased when it is combined with Dabrafenib.
DarunavirThe serum concentration of Ciclesonide can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Ciclesonide can be increased when it is combined with Dasatinib.
DecamethoniumThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Decamethonium.
DeferasiroxThe serum concentration of Ciclesonide can be decreased when it is combined with Deferasirox.
DeferasiroxThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Deferasirox.
DelavirdineThe metabolism of Ciclesonide can be decreased when combined with Delavirdine.
DemecariumThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Demecarium.
DexamethasoneThe serum concentration of Ciclesonide can be decreased when it is combined with Dexamethasone.
DichlorvosThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Dichlorvos.
DienestrolThe serum concentration of Ciclesonide can be increased when it is combined with Dienestrol.
DiethylstilbestrolThe serum concentration of Ciclesonide can be increased when it is combined with Diethylstilbestrol.
DiflunisalThe risk or severity of adverse effects can be increased when Diflunisal is combined with Ciclesonide.
DihydroergotamineThe metabolism of Ciclesonide can be decreased when combined with Dihydroergotamine.
DihydrotestosteroneCiclesonide may increase the fluid retaining activities of Dihydrotestosterone.
DiltiazemThe metabolism of Ciclesonide can be decreased when combined with Diltiazem.
DonepezilThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Donepezil.
DoxycyclineThe metabolism of Ciclesonide can be decreased when combined with Doxycycline.
DronedaroneThe metabolism of Ciclesonide can be decreased when combined with Dronedarone.
EchothiophateThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Echothiophate.
EdrophoniumThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Edrophonium.
EfavirenzThe serum concentration of Ciclesonide can be decreased when it is combined with Efavirenz.
EnzalutamideThe serum concentration of Ciclesonide can be decreased when it is combined with Enzalutamide.
ErythromycinThe metabolism of Ciclesonide can be decreased when combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Ciclesonide can be decreased when it is combined with Eslicarbazepine acetate.
EstradiolThe serum concentration of Ciclesonide can be increased when it is combined with Estradiol.
EstriolThe serum concentration of Ciclesonide can be increased when it is combined with Estriol.
EstroneThe serum concentration of Ciclesonide can be increased when it is combined with Estrone.
Etacrynic acidCiclesonide may increase the hypokalemic activities of Etacrynic acid.
Ethinyl EstradiolThe serum concentration of Ciclesonide can be increased when it is combined with Ethinyl Estradiol.
EtravirineThe serum concentration of Ciclesonide can be decreased when it is combined with Etravirine.
FenthionThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Fenthion.
FluconazoleThe metabolism of Ciclesonide can be decreased when combined with Fluconazole.
FluoxymesteroneCiclesonide may increase the fluid retaining activities of Fluoxymesterone.
FluvoxamineThe metabolism of Ciclesonide can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Ciclesonide can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Ciclesonide can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Ciclesonide can be decreased when it is combined with Fosphenytoin.
FurosemideCiclesonide may increase the hypokalemic activities of Furosemide.
Fusidic AcidThe serum concentration of Ciclesonide can be increased when it is combined with Fusidic Acid.
GalantamineThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Galantamine.
Gallamine TriethiodideThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Gallamine Triethiodide.
GenisteinThe serum concentration of Ciclesonide can be increased when it is combined with Genistein.
Ginkgo bilobaThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Ginkgo biloba.
Glycerol PhenylbutyrateThe therapeutic efficacy of Glycerol Phenylbutyrate can be decreased when used in combination with Ciclesonide.
HexestrolThe serum concentration of Ciclesonide can be increased when it is combined with Hexestrol.
Huperzine AThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Huperzine A.
HyaluronidaseThe therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Ciclesonide.
HydrochlorothiazideCiclesonide may increase the hypokalemic activities of Hydrochlorothiazide.
HydroflumethiazideCiclesonide may increase the hypokalemic activities of Hydroflumethiazide.
IdelalisibThe serum concentration of Ciclesonide can be increased when it is combined with Idelalisib.
ImatinibThe metabolism of Ciclesonide can be decreased when combined with Imatinib.
IndacaterolIndacaterol may increase the hypokalemic activities of Ciclesonide.
IndapamideCiclesonide may increase the hypokalemic activities of Indapamide.
IndinavirThe serum concentration of Ciclesonide can be increased when it is combined with Indinavir.
IsavuconazoniumThe metabolism of Ciclesonide can be decreased when combined with Isavuconazonium.
IsoflurophateThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Isoflurophate.
IsoniazidThe serum concentration of Isoniazid can be decreased when it is combined with Ciclesonide.
IsradipineThe metabolism of Ciclesonide can be decreased when combined with Isradipine.
ItraconazoleThe serum concentration of Ciclesonide can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Ciclesonide can be increased when it is combined with Ivacaftor.
KetoconazoleThe serum concentration of Ciclesonide can be increased when it is combined with Ketoconazole.
LopinavirThe serum concentration of Ciclesonide can be increased when it is combined with Lopinavir.
LovastatinThe metabolism of Ciclesonide can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Ciclesonide can be increased when it is combined with Luliconazole.
MagaldrateThe bioavailability of Ciclesonide can be decreased when combined with Magaldrate.
Magnesium carbonateThe bioavailability of Ciclesonide can be decreased when combined with Magnesium carbonate.
Magnesium hydroxideThe bioavailability of Ciclesonide can be decreased when combined with Magnesium hydroxide.
Magnesium oxideThe bioavailability of Ciclesonide can be decreased when combined with Magnesium oxide.
Magnesium TrisilicateThe bioavailability of Ciclesonide can be decreased when combined with Magnesium Trisilicate.
MalathionThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Malathion.
MefloquineThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Mefloquine.
MemantineThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Memantine.
MesalazineThe risk or severity of adverse effects can be increased when Mesalazine is combined with Ciclesonide.
MestranolThe serum concentration of Ciclesonide can be increased when it is combined with Mestranol.
MethyclothiazideCiclesonide may increase the hypokalemic activities of Methyclothiazide.
MethyltestosteroneCiclesonide may increase the fluid retaining activities of Methyltestosterone.
MetolazoneCiclesonide may increase the hypokalemic activities of Metolazone.
MifepristoneThe therapeutic efficacy of Ciclesonide can be decreased when used in combination with Mifepristone.
MinaprineThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Minaprine.
MitotaneThe serum concentration of Ciclesonide can be decreased when it is combined with Mitotane.
MivacuriumMivacurium may increase the adverse neuromuscular activities of Ciclesonide.
ModafinilThe serum concentration of Ciclesonide can be decreased when it is combined with Modafinil.
NafcillinThe serum concentration of Ciclesonide can be decreased when it is combined with Nafcillin.
NefazodoneThe serum concentration of Ciclesonide can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Ciclesonide can be increased when it is combined with Nelfinavir.
NeostigmineThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Neostigmine.
NetupitantThe serum concentration of Ciclesonide can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Ciclesonide can be decreased when combined with Nevirapine.
NicorandilThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Nicorandil.
NilotinibThe metabolism of Ciclesonide can be decreased when combined with Nilotinib.
OlaparibThe metabolism of Ciclesonide can be decreased when combined with Olaparib.
OsimertinibThe serum concentration of Ciclesonide can be increased when it is combined with Osimertinib.
OxandroloneCiclesonide may increase the fluid retaining activities of Oxandrolone.
OxymetholoneCiclesonide may increase the fluid retaining activities of Oxymetholone.
PalbociclibThe serum concentration of Ciclesonide can be increased when it is combined with Palbociclib.
PentobarbitalThe serum concentration of Ciclesonide can be decreased when it is combined with Pentobarbital.
PhenobarbitalThe serum concentration of Ciclesonide can be decreased when it is combined with Phenobarbital.
Phenylacetic acidThe therapeutic efficacy of Phenylacetic acid can be decreased when used in combination with Ciclesonide.
PhenytoinThe serum concentration of Ciclesonide can be decreased when it is combined with Phenytoin.
PhysostigmineThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Physostigmine.
PiretanideCiclesonide may increase the hypokalemic activities of Piretanide.
Polyestradiol phosphateThe serum concentration of Ciclesonide can be increased when it is combined with Polyestradiol phosphate.
PolythiazideCiclesonide may increase the hypokalemic activities of Polythiazide.
PosaconazoleThe serum concentration of Ciclesonide can be increased when it is combined with Posaconazole.
PrimidoneThe serum concentration of Ciclesonide can be decreased when it is combined with Primidone.
PyridostigmineThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Pyridostigmine.
QuinestrolThe serum concentration of Ciclesonide can be increased when it is combined with Quinestrol.
QuinethazoneCiclesonide may increase the hypokalemic activities of Quinethazone.
Rabies vaccineThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Rabies vaccine.
RanolazineThe metabolism of Ciclesonide can be decreased when combined with Ranolazine.
RapacuroniumRapacuronium may increase the adverse neuromuscular activities of Ciclesonide.
RifabutinThe serum concentration of Ciclesonide can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Ciclesonide can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Ciclesonide can be decreased when it is combined with Rifapentine.
RitonavirThe serum concentration of Ciclesonide can be increased when it is combined with Ritonavir.
RivastigmineThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Rivastigmine.
Salicylic acidThe risk or severity of adverse effects can be increased when Salicylic acid is combined with Ciclesonide.
SaquinavirThe serum concentration of Ciclesonide can be increased when it is combined with Saquinavir.
SildenafilThe metabolism of Ciclesonide can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Ciclesonide can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Ciclesonide can be increased when it is combined with Simeprevir.
Sodium phenylbutyrateThe therapeutic efficacy of Sodium phenylbutyrate can be decreased when used in combination with Ciclesonide.
St. John's WortThe serum concentration of Ciclesonide can be decreased when it is combined with St. John's Wort.
StanozololCiclesonide may increase the fluid retaining activities of Stanozolol.
StiripentolThe serum concentration of Ciclesonide can be increased when it is combined with Stiripentol.
SulfisoxazoleThe metabolism of Ciclesonide can be decreased when combined with Sulfisoxazole.
Synthetic Conjugated Estrogens, AThe serum concentration of Ciclesonide can be increased when it is combined with Synthetic Conjugated Estrogens, A.
Synthetic Conjugated Estrogens, BThe serum concentration of Ciclesonide can be increased when it is combined with Synthetic Conjugated Estrogens, B.
TacrineThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Tacrine.
TelaprevirThe serum concentration of Telaprevir can be decreased when it is combined with Ciclesonide.
TelaprevirThe serum concentration of Ciclesonide can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Ciclesonide can be increased when it is combined with Telithromycin.
TestosteroneCiclesonide may increase the fluid retaining activities of Testosterone.
TiboloneThe serum concentration of Ciclesonide can be increased when it is combined with Tibolone.
TiclopidineThe metabolism of Ciclesonide can be decreased when combined with Ticlopidine.
TocilizumabThe serum concentration of Ciclesonide can be decreased when it is combined with Tocilizumab.
TorasemideCiclesonide may increase the hypokalemic activities of Torasemide.
TrichlorfonThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Trichlorfon.
TrichlormethiazideCiclesonide may increase the hypokalemic activities of Trichlormethiazide.
TubocurarineThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Tubocurarine.
VenlafaxineThe metabolism of Ciclesonide can be decreased when combined with Venlafaxine.
VerapamilThe metabolism of Ciclesonide can be decreased when combined with Verapamil.
VoriconazoleThe serum concentration of Ciclesonide can be increased when it is combined with Voriconazole.
WarfarinCiclesonide may increase the anticoagulant activities of Warfarin.
ZeranolThe serum concentration of Ciclesonide can be increased when it is combined with Zeranol.
ZiprasidoneThe metabolism of Ciclesonide can be decreased when combined with Ziprasidone.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Zinc ion binding
Specific Function:
Receptor for glucocorticoids (GC). Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modulator of other transcription factors. Affects inflammatory responses, cellular proliferation and differentiation in target tissues. Could act as a coactivator for STAT5-dependent transcription upon grow...
Gene Name:
NR3C1
Uniprot ID:
P04150
Molecular Weight:
85658.57 Da
References
  1. Barnes NC: The properties of inhaled corticosteroids: similarities and differences. Prim Care Respir J. 2007 Jun;16(3):149-54. [PubMed:17530144 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Peet CF, Enos T, Nave R, Zech K, Hall M: Identification of enzymes involved in phase I metabolism of ciclesonide by human liver microsomes. Eur J Drug Metab Pharmacokinet. 2005 Oct-Dec;30(4):275-86. [PubMed:16435573 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Triglyceride lipase activity
Specific Function:
Involved in the detoxification of xenobiotics and in the activation of ester and amide prodrugs. Hydrolyzes aromatic and aliphatic esters, but has no catalytic activity toward amides or a fatty acyl-CoA ester. Hydrolyzes the methyl ester group of cocaine to form benzoylecgonine. Catalyzes the transesterification of cocaine to form cocaethylene. Displays fatty acid ethyl ester synthase activity,...
Gene Name:
CES1
Uniprot ID:
P23141
Molecular Weight:
62520.62 Da
References
  1. Mutch E, Nave R, McCracken N, Zech K, Williams FM: The role of esterases in the metabolism of ciclesonide to desisobutyryl-ciclesonide in human tissue. Biochem Pharmacol. 2007 May 15;73(10):1657-64. Epub 2007 Jan 28. [PubMed:17331475 ]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
binder
General Function:
Steroid binding
Specific Function:
Major transport protein for glucocorticoids and progestins in the blood of almost all vertebrate species.
Gene Name:
SERPINA6
Uniprot ID:
P08185
Molecular Weight:
45140.49 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Comments
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Drug created on July 17, 2007 06:38 / Updated on October 01, 2016 02:23