PRESCRIBING HIGHLIGHTS: Please see package insert for additional information and possible updates
to ensure safe and effective use of this medication. The authors make no claims of the accuracy of the information contained herein; and these suggested doses are not a substitute for clinical judgment. Neither GlobalRPh
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Initial U.S. Approval: 2011 DESCRIPTION
The active ingredient in DALIRESP tablets is roflumilast. Roflumilast
and its active metabolite (roflumilast N-oxide) are selective
phosphodiesterase 4 (PDE4) inhibitors.
The drug substance is a white to off-white non-hygroscopic powder with a
melting point of 160°C. It is practically insoluble in water and hexane,
sparingly soluble in ethanol and freely soluble in acetone.
DALIRESP is supplied as white to off-white, round tablets, embossed with
'D' on one side and '500' on the other side. Each tablet contains 500
mcg of roflumilast.
Each tablet of DALIRESP for oral administration contains the following
inactive ingredients: lactose monohydrate, corn starch, povidone and
CLINICAL PHARMACOLOGY Mechanism of Action
Roflumilast and its active metabolite (roflumilast N-oxide) are
selective inhibitors of phosphodiesterase 4 (PDE4). Roflumilast and
roflumilast N-oxide inhibition of PDE4 (a major cyclic-3',5'-adenosine
monophosphate (cyclic AMP)-metabolizing enzyme in lung tissue) activity
leads to accumulation of intracellular cyclic AMP. While the specific
mechanism(s) by which DALIRESP exerts its therapeutic action in COPD
patients is not well defined, it is thought to be related to the effects
of increased intracellular cyclic AMP in lung cells.
Acute bronchospasm: Do not use for the relief of acute
Psychiatric Events including Suicidality: Advise
patients , their caregivers, and families to be alert for
the emergence or worsening of insomnia, anxiety, depression,
suicidal thoughts or other mood changes, and if such changes
occur to contact their healthcare provider. Carefully weigh
the risks and benefits of treatment with DALIRESP in
patients with a history of depression and/or suicidal
thoughts or behavior.
Weight Decrease: Monitor weight regularly. If
unexplained or clinically significant weight loss occurs,
evaluate weight loss and consider discontinuation of
Drug Interactions: Use with strong cytochrome P450
enzyme inducers (e.g. rifampicin, phenobarbital,
carbamazepine, phenytoin) is not recommended.
Use with inhibitors of CYP3A4 or dual inhibitors of CYP3A4 and
CYP1A2 (e.g, erythromycin, ketoconazole, fluvoxamine, enoxacin,
cimetidine) will increase roflumilast systemic exposure and may
result in increased adverse reactions. The risk of such
concurrent use should be weighed carefully against benefit.
USE IN SPECIFIC POPULATIONS
Nursing Mothers: DALIRESP should not be used by women who are
nursing as excretion of roflumilast and/or its metabolites into
human milk is probable and there are no human studies that have
investigated effects of DALIRESP on breast-fed infants.