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roflumilast (Daliresp)

Indications: - add on therapy to reduce COPD exacerbations in patients with severe COPD associated with chronic bronchitis - topical roflumilast 0.15% 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) Pregnancy category: C Safety in lactation: - Dosage: - 250-500 ug PO QD - cream 0.15% for atopic dermatitis Pharmacokinetics: - metabolized by CYP3A4 & CYP1A2; roflumilast is converted to roflumilast N-oxide Adverse effects: 1) well tolerated 2) diarrhea (6-9%) generally within 4 weeks 3) nausea 4) headache 5) insomnia 6) back pain 7) decreased appetite 8) dizziness 9) 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

Specific

Roflumilast Topical

General

phosphodiesterase-4 inhibitor

Database Correlations

PUBCHEM cid=449193

References

  1. 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: 16099292
  2. 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. Prescriber's Letter 18(7): 2011 New Drug: Daliresp (Roflumilast) Detail-Document#: 270709 (subscription needed) http://www.prescribersletter.com
  4. 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: 23117188
  5. Medical Knowledge Self Assessment Program (MKSAP) 18, American College of Physicians, Philadelphia 2018
  6. 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: 19716961 Clinical Trial.
  7. 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: 25684586 Clinical Trial.
  8. 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 - Bunk D Roflumilast Cream 0.15% Approved for Eczema in Patients Aged 6 or Older. Medscape. July 10, 2024 https://www.medscape.com/viewarticle/roflumilast-cream-approved-eczema-patients-2024a1000cpx