roflumilast (Daliresp)
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Indications
- add on therapy to reduce COPD exacerbations in patients with severe COPD associated with chronic bronchitis
- topical roflumilast effective for atopic dermatitis[8]
Contraindications
- not for treatment of acute bronchospasm
- treatment of pulmonary emphysema[4]
- moderate-severe hepatic impairment (Child-Pugh Class B or C)
Dosage
Pharmacokinetics
- metabolized by CYP3A4 & CYP1A2; roflumilast is converted to roflumilast N-oxide
Adverse effects
- well tolerated
- diarrhea (6-9%) generally within 4 weeks
- nausea
- headache
- insomnia
- back pain
- decreased appetite
- dizziness
- depression
Drug interactions
- drugs that inhibit CYP3A4 (erythromycin, ketoconazole, fluvoxamine, enoxacin, cimetidine) may increase levels of roflumilast
- drugs that induce CYP3A4 (rifampicin, phenobarbital, carbamazepine, phenytoin) may decrease effectiveness of roflumilast
Mechanism of action
- inhibits phosphodiesterase-4 in neutrophils
- attenuates influx of neutrophils & eosinophils into the airways[3]
- not a bronchodilator
Notes
- the FDA approved roflumilast in March 2011 with a medication guide informing patients of the potential risks of mental health problems, including changes in mood, thinking, or behavior, or unexplained weight loss
More general terms
References
- ↑ Rabe KF et al Roflumilast - An oral anti-inflammatory treatment for chronic obstructive pulmonary disease: A randomised controlled trial. Lancet 2005 Aug 13; 366:563-71. PMID: https://www.ncbi.nlm.nih.gov/pubmed/16099292
- ↑ FDA NEWS RELEASE, March 1, 2011 FDA approves new drug to treat chronic obstructive pulmonary disease http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm244989.htm
- ↑ 3.0 3.1 Prescriber's Letter 18(7): 2011 New Drug: Daliresp (Roflumilast) Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=270709&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 4.0 4.1 Wedzicha JA, Rabe KF, Martinez FJ et al Efficacy of roflumilast in the COPD frequent exacerbator phenotype. Chest. 2013 May;143(5):1302-11 PMID: https://www.ncbi.nlm.nih.gov/pubmed/23117188
- ↑ Medical Knowledge Self Assessment Program (MKSAP) 18, American College of Physicians, Philadelphia 2018
- ↑ Fabbri LM, Calverley PM, Izquierdo-Alonso JL et al Roflumilast in moderate-to-severe chronic obstructive pulmonary disease treated with longacting bronchodilators: two randomised clinical trials. Lancet. 2009 Aug 29;374(9691):695-703. PMID: https://www.ncbi.nlm.nih.gov/pubmed/19716961 Clinical Trial.
- ↑ Martinez FJ, Calverley PM, Goehring UM et al Effect of roflumilast on exacerbations in patients with severe chronic obstructive pulmonary disease uncontrolled by combination therapy (REACT): a multicentre randomised controlled trial. Lancet. 2015 Mar 7;385(9971):857-66. PMID: https://www.ncbi.nlm.nih.gov/pubmed/25684586 Clinical Trial.
- ↑ 8.0 8.1 Bankhead C Rapid Improvement in Atopic Dermatitis With Topical PDE4 Inhibitor. Disease status, itch improved significantly within 1 to 2 weeks with roflumilast cream. MedPage Today March 20, 2023 https://www.medpagetoday.com/meetingcoverage/aad/103615