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Roflumilast: Wikis


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Systematic (IUPAC) name
CAS number 162401-32-3
ATC code R03DX07
PubChem 449193
Chemical data
Formula C 17H14Cl2F2N2O3  
Mol. mass 403.207 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes Oral

Roflumilast is a drug which acts as a selective, long-acting inhibitor of the phosphodiesterase enzyme PDE-4. It has antiinflammatory effects and is under development as an orally administered drug for the treatment of inflammatory conditions of the lungs such as asthma, chronic obstructive pulmonary disease and emphysema.[1][2][3][4] While roflumilast was found to be effective in clinical trials, it produced several dose-limiting side effects including nausea, diarrhoea and headache, and development is continuing in an attempt to minimise the incidence of side effects while retaining clinical efficacy.[5]


  1. ^ Boswell-Smith V, Spina D. PDE4 inhibitors as potential therapeutic agents in the treatment of COPD-focus on roflumilast. International Journal of Chronic Obstructive Pulmonary Disease. 2007;2(2):121-9. PMID 18044684
  2. ^ Herbert C, Hettiaratchi A, Webb DC, Thomas PS, Foster PS, Kumar RK. Suppression of cytokine expression by roflumilast and dexamethasone in a model of chronic asthma. Clinical and Experimental Allergy. 2008 May;38(5):847-56. PMID 18307529
  3. ^ Hohlfeld JM, Schoenfeld K, Lavae-Mokhtari M, Schaumann F, Mueller M, Bredenbroeker D, Krug N, Hermann R. Roflumilast attenuates pulmonary inflammation upon segmental endotoxin challenge in healthy subjects: a randomized placebo-controlled trial. Pulmonary Pharmacology and Therapeutics. 2008 Aug;21(4):616-23. PMID 18374614
  4. ^ Field SK. Roflumilast: an oral, once-daily selective PDE-4 inhibitor for the management of COPD and asthma. Expert Opinion on Investigational Drugs. 2008 May;17(5):811-8. PMID 18447606
  5. ^ Spina D. PDE4 inhibitors: current status. British Journal of Pharmacology. 2008 Jul 28. PMID 18660825


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