Roflumilast
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Trade names | Daxas, Daliresp, others |
AHFS/Drugs.com | Monograph |
MedlinePlus | a611034 |
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Routes of administration | By mouth |
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Pharmacokinetic data | |
Bioavailability | 79%[2][1][4][5] |
Protein binding | 99%[2][1][4][5] |
Metabolism | Hepatic via CYP1A2 & CYP3A4[2][1][4][5] |
Elimination half-life | 17 hours (30 hours [active metabolite])[2][1][4][5] |
Excretion | Urine (70%)[2][1][4][5] |
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ECHA InfoCard | 100.210.960 ![]() |
Chemical and physical data | |
Formula | C17H14Cl2F2N2O3 |
Molar mass | 403.21 g·mol−1 |
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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).[6][7][8][9]
In June 2010, it was approved in the European Union for severe COPD associated with chronic bronchitis.[3][10] In February 2011, it gained FDA approval in the United States for reducing COPD exacerbations.[11][12]
Medical uses[]
Its primary clinical use is in the prevention of exacerbations (lung attacks) in severe chronic obstructive pulmonary disease (COPD).[1][2][3][4][5]
Adverse effects[]
Common (1–10% incidence) adverse effects include:[2][1][4][5][13]
- Diarrhea
- Weight loss
- Nausea
- Headache
- Insomnia
- Decreased appetite
- Abdominal pain
- Rhinitis
- Sinusitis
- Urinary tract infection
- Depression
References[]
- ^ a b c d e f g h "Daxas 250 micrograms tablets - Summary of Product Characteristics (SmPC)". (emc). 11 June 2020. Retrieved 28 September 2020.
- ^ a b c d e f g h "Daliresp- roflumilast tablet". DailyMed. 12 March 2020. Retrieved 28 September 2020.
- ^ a b c "Daxas EPAR". European Medicines Agency. Retrieved 28 September 2020.
- ^ a b c d e f g "Daliresp : EPAR - Product Information" (PDF). European Medicines Agency. Takeda GmbH. 26 September 2013. Retrieved 18 November 2013.
- ^ a b c d e f g "roflumilast (Rx) - Daliresp". Medscape Reference. WebMD. Retrieved 18 November 2013.
- ^ Boswell-Smith V, Spina D (2007). "PDE4 inhibitors as potential therapeutic agents in the treatment of COPD-focus on roflumilast". International Journal of Chronic Obstructive Pulmonary Disease. 2 (2): 121–9. PMC 2695611. PMID 18044684.
- ^ Herbert C, Hettiaratchi A, Webb DC, Thomas PS, Foster PS, Kumar RK (May 2008). "Suppression of cytokine expression by roflumilast and dexamethasone in a model of chronic asthma". Clinical and Experimental Allergy. 38 (5): 847–56. doi:10.1111/j.1365-2222.2008.02950.x. PMID 18307529. S2CID 19050454.
- ^ Hohlfeld JM, Schoenfeld K, Lavae-Mokhtari M, Schaumann F, Mueller M, Bredenbroeker D, et al. (August 2008). "Roflumilast attenuates pulmonary inflammation upon segmental endotoxin challenge in healthy subjects: a randomized placebo-controlled trial" (PDF). Pulmonary Pharmacology & Therapeutics. 21 (4): 616–23. doi:10.1016/j.pupt.2008.02.002. PMID 18374614.
- ^ Field SK (May 2008). "Roflumilast: an oral, once-daily selective PDE-4 inhibitor for the management of COPD and asthma". Expert Opinion on Investigational Drugs. 17 (5): 811–8. doi:10.1517/13543784.17.5.811. PMID 18447606. S2CID 73241684.
- ^ "Nycomed's Anti-Inflammatory Gains Approval in EU for COPD"
- ^ "Drug Approval Package: Daliresp Tablets (roflumilast) NDA #022522". U.S. Food and Drug Administration (FDA). 24 December 1999. Retrieved 28 September 2020. Lay summary (PDF).
- ^ "FDA approves new drug to treat chronic obstructive pulmonary disease" (Press release). U.S. Food and Drug Administration (FDA). March 1, 2011.[dead link]
- ^ Spina D (October 2008). "PDE4 inhibitors: current status". British Journal of Pharmacology. 155 (3): 308–15. doi:10.1038/bjp.2008.307. PMC 2567892. PMID 18660825.
External links[]
- "Roflumilast". Drug Information Portal. U.S. National Library of Medicine.
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