About: Roflumilast     Goto   Sponge   NotDistinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

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rdf:type
http://linked.open...gbank/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. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...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 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
http://linked.open...drugbank/halfLife
  • Plasma half-life of roflumilast is 17 hours and its metabolite is 30 hours (oral dose). (en)
http://linked.open...ugbank/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. (en)
sameAs
Title
  • Roflumilast (en)
adms:identifier
http://linked.open...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. (en)
http://linked.open...y/drugbank/patent
http://linked.open...outeOfElimination
  • Roflumilast is excreted 70% in the urine as roflumilast N-oxide. (en)
http://linked.open.../drugbank/synonym
  • Daliresp (en)
  • ROF (en)
  • Roflumilastum (en)
http://linked.open...drugbank/toxicity
  • Headache, weight loss, GI upset, insomnia, and loose stools. (en)
http://linked.open...umeOfDistribution
  • 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. (en)
http://linked.open.../drug/hasAHFSCode
http://linked.open...nk/proteinBinding
  • Roflumilast is 99% plasma protein bound. (en)
http://linked.open...ynthesisReference
  • http://en.wikipedia.org/wiki/File:Roflumilast_syn.png (en)
foaf:page
http://linked.open...ugbank/IUPAC-Name
http://linked.open...gy/drugbank/InChI
http://linked.open...Molecular-Formula
http://linked.open.../Molecular-Weight
http://linked.open...noisotopic-Weight
http://linked.open...y/drugbank/SMILES
http://linked.open.../Water-Solubility
http://linked.open...ogy/drugbank/logP
http://linked.open...ogy/drugbank/logS
http://linked.open...logy/drugbank/pKa
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http://linked.open...urface-Area--PSA-
http://linked.open...nk/Polarizability
http://linked.open...bank/Refractivity
http://linked.open...atable-Bond-Count
http://linked.open...ugbank/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. (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 162401-32-3 (en)
http://linked.open...rugbank/clearance
  • ~9.6 L/hour. (en)
http://linked.open...k/Bioavailability
http://linked.open...bank/Ghose-Filter
http://linked.open...nk/MDDR-Like-Rule
http://linked.open...ank/Melting-Point
http://linked.open...k/Number-of-Rings
http://linked.open...siological-Charge
http://linked.open...bank/Rule-of-Five
http://linked.open...tional-IUPAC-Name
http://linked.open...strongest-acidic-
http://linked.open...-strongest-basic-
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