New Drug Update 2010-2011 Faculty Disclaimer - CME Conferences

2 nd Annual Essentials in Primary Care
Fall Conference
Friday, November 11, 2011
Roflumilast - Daliresp
by Forest Labs • Dose 500 mcg QD with
or without food
• Indicated as a treatment to
reduce the risk of COPD
exacerbations in patients with
severe COPD associated with
chronic bronchitis and a
history of exacerbations
• Neutrophils, eosinophils, and
monocytes contain PDE4.
Roflumilast is believed to
exert an anti-inflammatory
effect through inhibition of
PDE4 in these cell types
• Cost $211.50/30 tabs
WAC
Roflumilast - Daliresp
• The pharmacologically active N-oxide metabolite is
estimated to account for about 90% of roflumilast’s
overall pharmacologic effects. The elimination halflife
of the N-oxide metabolite is approximately 21 to
27 hours. Roflumilast N-oxide is predominantly
metabolized via CYP3A4
• Drug Interactions: Use with strong cytochrome P450
enzyme inducers (e.g. rifampicin, phenobarbital,
carbamazepine, phenytoin) is not recommended.
• CYP3A4 inhibitors or dual inhibitors that inhibit both
CYP3A4 and CYP1A2 simultaneously (e.g.,
erythromycin, ketoconazole, fluvoxamine, enoxacin,
cimetidine) may increase roflumilast systemic
exposure and may result in increased adverse
reactions. The risk of such concurrent use should be
weighed carefully against benefit.
Wayne Weart
New Drug Update Part I