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Namespace Prefixes

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Statements

Subject Item
n2:DB08906
rdf:type
n3:Drug
n3:description
Fluticasone furoate is a synthetic trifluorinated corticosteroid with potent anti-inflammatory activity. Despite the similarity in the names, fluticasone furoate and fluticasone propionate are different drugs with different properties. It is marketed under the brand name, Veramyst in the US by GlaxoSmithKline for the management of chronic obstructive pulmonary disease (COPD). FDA approved on April 27, 2007.
n3:dosage
n7:271B5BFF-363D-11E5-9242-09173F13E4C5 n7:271B5C00-363D-11E5-9242-09173F13E4C5 n7:271B5BFD-363D-11E5-9242-09173F13E4C5 n7:271B5BFE-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# FDA label # Allen A, Schenkenberger I, Trivedi R, Cole J, Hicks W, Gul N, Jacques L: Inhaled fluticasone furoate/vilanterol does not affect hypothalamic-pituitary-adrenal axis function in adolescent and adult asthma: randomised, double-blind, placebo-controlled study. Clin Respir J. 2013 Apr 12. doi: 10.1111/crj.12026. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23578031 # Tamm M, Richards DH, Beghe B, Fabbri L: Inhaled corticosteroid and long-acting beta2-agonist pharmacological profiles: effective asthma therapy in practice. Respir Med. 2012 Dec;106 Suppl 1:S9-19. doi: 10.1016/S0954-6111(12)70005-7. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23273165 # Allen A, Bareille PJ, Rousell VM: Fluticasone furoate, a novel inhaled corticosteroid, demonstrates prolonged lung absorption kinetics in man compared with inhaled fluticasone propionate. Clin Pharmacokinet. 2013 Jan;52(1):37-42. doi: 10.1007/s40262-012-0021-x. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23184737
n3:group
approved
n3:halfLife
Elimination phase half-life, IV dose = 15.1 hours; Elimination phase half-life, inhaled = 17 - 24 hours;
n3:indication
Fluticasone furoate nasal spray is indicated for the treatment of the symptoms of seasonal and perennial allergic rhinitis in patients aged 2 years and older. Breo Ellipta, a mixture of fluticasone furoate and vilanterol is indicated for the management of COPD.
owl:sameAs
n10:DB08906
dcterms:title
Fluticasone furoate
adms:identifier
n16:54868-6168-0 n17:Fluticasone_furoate n18:DB08906 n19:D06315
n3:mechanismOfAction
Fluticasone furoate is a synthetic trifluorinated corticosteroid with potent anti-inflammatory activity. The precise mechanism through which fluticasone furoate affects rhinitis symptoms is not known. Corticosteroids have been shown to have a wide range of actions on multiple cell types (e.g., mast cells, eosinophils, neutrophils, macrophages, lymphocytes) and mediators (e.g., histamine, eicosanoids, leukotrienes, cytokines) involved in inflammation. Specific effects of fluticasone furoate demonstrated in in vitro and in vivo models included activation of the glucocorticoid response element, inhibition of pro-inflammatory transcription factors such as NFkB, and inhibition of antigen-induced lung eosinophilia in sensitized rats. Fluticasone is also found to increase airway retention of long-acting beta adrenergic agonist, thus potentiating its beneficial effects for the treatment of asthma.
n3:routeOfElimination
Fluticasone furoate and its metabolites are eliminated primarily in the feces, accounting for approximately 101% and 90% of the orally and intravenously administered dose, respectively. Urinary excretion accounted for approximately 1% and 2% of the orally and intravenously administered dose, respectively. Fluticasone furoate is extensively metabolized so very little is excreted unchanged.
n3:synonym
GSK 685698 Furoate de fluticasone Furoato de fluticasona Veramyst Fluticasonum furoas
n3:toxicity
The most common adverse reactions (>1% incidence) included headache, epistaxis, pharyngolaryngeal pain, nasal ulceration, back pain, pyrexia, and cough.
n3:volumeOfDistribution
Steady state, IV administration = 608 L
n3:mixture
n14:271B5BFC-363D-11E5-9242-09173F13E4C5
n3:proteinBinding
>99% protein bound.
n3:synthesisReference
Adrienne KOVACSNE-MEZEI, Roman Gabriel, Alexandr Jegorov, "POLYMORPHS OF FLUTICASONE FUROATE AND PROCESSES FOR PREPARATION THEREOF." U.S. Patent US20100240629, issued September 23, 2010.
foaf:page
n6:fluticasone-furoate-spray.html n8:veramyst-drug.htm
n3:IUPAC-Name
n4:271B5C05-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B5C0B-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B5C0A-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B5C07-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B5C08-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B5C09-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B5C03-363D-11E5-9242-09173F13E4C5 n4:271B5C1B-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B5C01-363D-11E5-9242-09173F13E4C5 n4:271B5C04-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B5C02-363D-11E5-9242-09173F13E4C5
n3:pKa
n4:271B5C1C-363D-11E5-9242-09173F13E4C5
n11:hasATCCode
n12:R01AD12 n12:R03BA09
n3:H-Bond-Acceptor-Count
n4:271B5C11-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B5C12-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B5C0C-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B5C0D-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B5C0F-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B5C0E-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B5C10-363D-11E5-9242-09173F13E4C5
n3:absorption
Following intranasal administration of fluticasone furoate, most of the dose is eventually swallowed and undergoes incomplete absorption and extensive first-pass metabolism in the liver and gut, resulting in negligible systemic exposure. Even at the highest recommended intranasal dose of 110 mcg once daily, plasma concentrations were not quantifiable. This is an especially useful feature as it lowers the incidence of adverse events associated with corticosteroid use. If administered using oral solution and intravenous dosing, 30% of the drug is absorbed and rapidly cleared from the plasma. Absolute bioavailability, intranasal route = 0.5%; Absolute bioavailability, oral route = 1.26%; Mean lung absorption time = 7 hours (regardless of formulation);
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
397864-44-7
n3:category
n3:clearance
Total plasma clearance = 58.7 L/h
n3:Bioavailability
n4:271B5C17-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B5C19-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B5C1A-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B5C16-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B5C15-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B5C18-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B5C06-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n4:271B5C13-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B5C14-363D-11E5-9242-09173F13E4C5