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Namespace Prefixes

PrefixIRI
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n6http://bio2rdf.org/drugbank:
n25http://linked.opendata.cz/resource/drugbank/drug/DB01656/identifier/chemspider/
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n8http://www.drugs.com/mtm/
n23http://linked.opendata.cz/resource/drugbank/drug/DB01656/identifier/chebi/
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n4http://linked.opendata.cz/resource/drugbank/property/
xsdhhttp://www.w3.org/2001/XMLSchema#
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n24http://linked.opendata.cz/resource/atc/
n13http://linked.opendata.cz/ontology/sukl/drug/

Statements

Subject Item
n2:DB01656
rdf:type
n3:Drug
n3:description
Roflumilast is a phosphodiesterase-4 (PDE-4) inhibitor. Due to its selective inhibition of the PDE4 isoenzyme in lung cells, roflumilast is indicated for the management of chronic obstrtuctive pulmonary disease (COPD) exacerbations. Treatment with Roflumilast is associated with an increase in psychiatric adverse reactions, including suicide and suicidal attempts.
n3:dosage
n9:271B60CD-363D-11E5-9242-09173F13E4C5 n9:271B60CE-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Meyers JA, Taverna J, Chaves J, Makkinje A, Lerner A: Phosphodiesterase 4 inhibitors augment levels of glucocorticoid receptor in B cell chronic lymphocytic leukemia but not in normal circulating hematopoietic cells. Clin Cancer Res. 2007 Aug 15;13(16):4920-7. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17699872 # Sanz MJ, Cortijo J, Taha MA, Cerda-Nicolas M, Schatton E, Burgbacher B, Klar J, Tenor H, Schudt C, Issekutz AC, Hatzelmann A, Morcillo EJ: Roflumilast inhibits leukocyte-endothelial cell interactions, expression of adhesion molecules and microvascular permeability. Br J Pharmacol. 2007 Oct;152(4):481-492. Epub 2007 Aug 20. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17704822 # Barone FC, Barton ME, White RF, Legos JJ, Kikkawa H, Shimamura M, Kuratani K, Kinoshita M: Inhibition of Phosphodiesterase Type 4 Decreases Stress-Induced Defecation in Rats and Mice. Pharmacology. 2007 Aug 28;81(1):11-17. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17726343 # Chong J, Poole P, Leung B, Black PN: Phosphodiesterase 4 inhibitors for chronic obstructive pulmonary disease. Cochrane Database Syst Rev. 2011 May 11;(5):CD002309. doi: 10.1002/14651858.CD002309.pub3. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/21563134 # Grootendorst DC, Gauw SA, Verhoosel RM, Sterk PJ, Hospers JJ, Bredenbroker D, Bethke TD, Hiemstra PS, Rabe KF: Reduction in sputum neutrophil and eosinophil numbers by the PDE4 inhibitor roflumilast in patients with COPD. Thorax. 2007 Dec;62(12):1081-7. Epub 2007 Jun 15. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17573446 # Thappali SR, Varanasi KV, Veeraraghavan S, Vakkalanka SK, Mukkanti K: Simultaneous quantitation of IC87114, roflumilast and its active metabolite roflumilast N-oxide in plasma by LC-MS/MS: application for a pharmacokinetic study. J Mass Spectrom. 2012 Dec;47(12):1612-9. doi: 10.1002/jms.3103. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23280750
n3:group
approved
n3:halfLife
Plasma half-life of roflumilast is 17 hours and its metabolite is 30 hours (oral dose).
n3:indication
Roflumilast is indicated as a treatment to reduce the risk of COPD exacerbations in patients with severe COPD associated with chronic bronchitis and a history of exacerbations. Roflumilast is not a bronchodilator and is not indicated for the relief of acute bronchospasm.
owl:sameAs
n6:DB01656
dcterms:title
Roflumilast
adms:identifier
n11:Roflumilast n15:14774 n17:449193 n18:10300323 n19:0456-0095-30 n20:ROF n21:DB01656 n22:D05744 n23:47657 n25:395793
n3:mechanismOfAction
Roflumilast is a phosphodiesterase-4 (PDE-4) inhibitor which, due to its selective inhibition of the PDE4 isoenzyme, has potential antiinflammatory and antimodulatory effects in the pulmonary system. It is thought that the increased levels of intracellular cyclic AMP are responsible for the therapeutic actions of Roflumilast.
n3:patent
n16:5712298
n3:routeOfElimination
Roflumilast is excreted 70% in the urine as roflumilast N-oxide.
n3:synonym
Roflumilastum ROF Daliresp
n3:toxicity
Headache, weight loss, GI upset, insomnia, and loose stools.
n3:volumeOfDistribution
Roflumilast has a Vd of 2.9L/kg with a dose of 500mcg. Permeability of roflumilast across the blood-brain barrier appears to be poor in rat studies.
n13:hasAHFSCode
n14:48-32
n3:proteinBinding
Roflumilast is 99% plasma protein bound.
n3:synthesisReference
http://en.wikipedia.org/wiki/File:Roflumilast_syn.png
foaf:page
n8:roflumilast.html
n3:IUPAC-Name
n4:271B60D3-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B60D9-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B60D8-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B60D5-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B60D6-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B60D7-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B60D1-363D-11E5-9242-09173F13E4C5 n4:271B60E9-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B60CF-363D-11E5-9242-09173F13E4C5 n4:271B60D2-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B60D0-363D-11E5-9242-09173F13E4C5
n3:pKa
n4:271B60EB-363D-11E5-9242-09173F13E4C5
n13:hasATCCode
n24:R03DX07
n3:H-Bond-Acceptor-Count
n4:271B60DF-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B60E0-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B60DA-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B60DB-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B60DD-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B60DC-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B60DE-363D-11E5-9242-09173F13E4C5
n3:absorption
After a 500mcg dose, the bioavailability of roflumilast is about 80%. In the fasted state, maximum plasma concentrations are reached in 0.5 to 2 hours. While in the fed state, Cmax is reduced by 40%, Tmax is increased by one hour, and total absorption is unchanged.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
162401-32-3
n3:clearance
~9.6 L/hour.
n3:Bioavailability
n4:271B60E5-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B60E7-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B60E8-363D-11E5-9242-09173F13E4C5
n3:Melting-Point
n4:271B60EA-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B60E4-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B60E3-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B60E6-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B60D4-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n4:271B60E1-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B60E2-363D-11E5-9242-09173F13E4C5