Thursday, November 17, 2016

Roflumilast

Roflumilast (Daliresp)
  • phosphodiesterase inhibitor --> increase levels of intracellular cAMP in lung cells --> decreased neutrophil and eosinophil cell counts
    • decrease inflammation, promote airway smooth muscle relaxation
  • used for COPD associated with chronic bronchitis
    • demonstrated significant improvement in FEV1 and reduction of rate of COPD exacerbations in comparison to placebo
    • failed to show benefit in patients with emphysema
    • has not been compared to other phosphodiesterase inhibitors
    • has been studied as add-on therapy to long-acting beta agonist and long-acting anti-muscarinic
    • uncertain in asthma
  • 500 mcg orally once daily
  • no renal dose adjustments, use caution in mild hepatic impairment, contraindicated in mod-severe hepatic impairment
    • metabolized by liver, cyp 3A4 and 1A2
  • take with or without food
  • avoid use with strong cyp450 inducers
  • may increase risk of depression/suicidal thoughts
  • may cause diarrhea, nausea, headache, back pain
  • can cause weight LOSS/decreased appetite
  • initial response takes approx. 4 weeks
    • NOT for ACUTE bronchospasm -- this is not a bronchodilator
    • roflumilast PREVENTS exacerbations
  • should be reserved for refractory disease
    • data is less convincing than the effects of standard of care LABA and LAMA
    • can be used as add-on to standard of care prevention
  • cost 30 day supply = $354.17

References:
Product Information: DALIRESP(TM) oral tablets, roflumilast oral tablets. Forest Laboratories, Inc., St. Louis, MO, 2011.
Stoller J. Management of exacerbations of chronic obstructive pulmonary disease. UpToDate. Barnes P (Ed). Accessed on: 17 November 2016. 
Ferguson G. Management of stable chronic obstructive pulmonary disease. UpToDate. Stoller J (Ed). Accessed on: 17 November 2016.
 

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