Roflumilast
From Wikipedia, the free encyclopedia
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| Systematic (IUPAC) name | |
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3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide
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| Clinical data | |
| Trade names | Daxas,Daliresp |
| AHFS/Drugs.com | Consumer Drug Information |
| MedlinePlus | a611034 |
| Licence data | EMA:Link, US FDA:link |
| Pregnancy category |
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| Routes of administration |
Oral |
| Pharmacokinetic data | |
| Bioavailability | 79%[1][2][3][4] |
| Protein binding | 99%[1][2][3][4] |
| Metabolism | Hepatic via CYP1A2 & CYP3A4[1][2][3][4] |
| Biological half-life | 17 hours (30 hours [active metabolite])[1][2][3][4] |
| Excretion | Urine (70%)[1][2][3][4] |
| Identifiers | |
| CAS Registry Number | 162401-32-3  |
| ATC code | R03DX07 |
| PubChem | CID: 449193 |
| IUPHAR/BPS | 6962 |
| ChemSpider | 395793 |
| UNII | 0P6C6ZOP5U  |
| ChEBI | CHEBI:47657 |
| ChEMBL | CHEMBL193240 |
| Chemical data | |
| Formula | C17H14Cl2F2N2O3 |
| Molecular mass | 403.207 g/mol |
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Roflumilast (trade names Daxas, Daliresp) is a drug that acts as a selective, long-acting inhibitor of the enzyme 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).[5][6][7][8]
In June 2010, Daxas was approved in the EU for severe COPD associated with chronic bronchitis.[9] In March 2011, Daliresp gained FDA approval in the US for reducing COPD exacerbations.[10]
Medical uses[edit]
Its primary clinical use is in the prevention of exacerbations (lung attacks) in severe COPD.[1][2][3][4]
Adverse effects[edit]
Common (1–10% incidence) adverse effects include:[1][2][3][4][11]
- Diarrhea
- Weight decreased
- Nausea
- Headache
- Insomnia
- Decreased appetite
- Abdominal pain
- Rhinitis
- Sinusitis
- Urinary tract infection
- Depression
References[edit]
- ^ a b c d e f g "DALIRESP (roflumilast) tablet [Forest Laboratories, Inc.]" (PDF). DailyMed. Forest Laboratories, Inc. August 2013. Retrieved 18 November 2013.
- ^ a b c d e f g "DAXAS 500 micrograms film-coated tablets". electronic Medicines Compendium. Takeda UK Ltd. 9 September 2013. Retrieved 18 November 2013.
- ^ 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. ISSN 1178-2005. 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 & Experimental Allergy 38 (5): 847–56. doi:10.1111/j.1365-2222.2008.02950.x. ISSN 1365-2222. PMID 18307529.
- ^ Hohlfeld, JM; Schoenfeld, K; Lavae-Mokhtari, M; Schaumann, F; Mueller, M; Bredenbroeker, D; Krug, N; Hermann, R (August 2008). "Roflumilast attenuates pulmonary inflammation upon segmental endotoxin challenge in healthy subjects: a randomized placebo-controlled trial". Pulmonary Pharmacology & Therapeutics 21 (4): 616–23. doi:10.1016/j.pupt.2008.02.002. ISSN 1094-5539. 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. ISSN 1354-3784. PMID 18447606.
- ^ "Nycomed's Anti-Inflammatory Gains Approval in EU for COPD"
- ^ "FDA approves new drug to treat chronic obstructive pulmonary disease" (Press release). U.S. Food and Drug Administration (FDA). March 1, 2011.
- ^ Spina, D (October 2008). "PDE4 inhibitors: current status". British Journal of Pharmacology 155 (3): 308–15. doi:10.1038/bjp.2008.307. ISSN 1476-5381. PMC 2567892. PMID 18660825.
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