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Clinical data | |
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Trade names | Daxas, Daliresp, Zoryve, others |
AHFS/Drugs.com | Monograph |
MedlinePlus | a611034 |
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Routes of administration | By mouth, topical |
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Pharmacokinetic data | |
Bioavailability | 79%[2][1][5][6] |
Protein binding | 99%[2][1][5][6] |
Metabolism | Hepatic via CYP1A2 & CYP3A4[2][1][5][6] |
Elimination half-life | 17 hours (30 hours [active metabolite])[2][1][5][6] |
Excretion | Urine (70%)[2][1][5][6] |
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ECHA InfoCard | 100.210.960 |
Chemical and physical data | |
Formula | C17H14Cl2F2N2O3 |
Molar mass | 403.21 g·mol−1 |
3D model (JSmol) | |
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Roflumilast, sold under the trade name Daxas among others, is a drug that acts as a selective, long-acting inhibitor of the enzyme phosphodiesterase-4 (PDE-4). It has anti-inflammatory effects and is used as an orally administered drug for the treatment of inflammatory conditions of the lungs such as chronic obstructive pulmonary disease (COPD).[7][8][9][10]
In June 2010, it was approved in the European Union for severe COPD associated with chronic bronchitis.[4][11] In February 2011, it gained FDA approval in the United States for reducing COPD exacerbations.[12][13] It is available as a generic medication.[14]
Roflumilast is indicated for the treatment of severe chronic obstructive pulmonary disease (COPD)[2] and for the treatment of plaque psoriasis.[3][15]
It is used in the prevention of exacerbations (lung attacks) in severe chronic obstructive pulmonary disease (COPD).[1][2][4][5][6]
Common (1–10% incidence) adverse effects include:[2][1][5][6][16]