The potential role of roflumilast: the new phosphodiesterase-4 inhibitor.
OBJECTIVE
To review the pharmacology, pharmacokinetics, efficacy, and safety of roflumilast in the treatment of asthma and chronic obstructive pulmonary disease (COPD).


METHODS
Studies, review articles, and meeting abstracts evaluating roflumilast were obtained from MEDLINE (1966-May 16, 2006), EMBASE (1980-May 16, 2006), and International Pharmaceutical Abstracts (1970-May 16, 2006) databases. Key terms used in all of the database searches were roflumilast, phosphodiesterase-4 inhibitor, asthma, chronic obstructive pulmonary disease, and COPD. Company Web sites were reviewed, and bibliographies of selected articles were evaluated for pertinent articles.


METHODS
In vitro, in vivo, and animal studies were selected, as were published human studies on the efficacy and safety of roflumilast. Due to limited published data on its safety, efficacy, pharmacokinetics, and drug interactions, meeting abstracts were also selected. Data retrieved from abstracts only is indicated in the references.


RESULTS
Roflumilast is a phosphodiesterase-4 (PDE-4) inhibitor which, due to its selective inhibition of the PDE 4 isoenzyme, has potential antiinflammatory and antimodulatory effects in the pulmonary system. It has been studied as an oral tablet in doses of 250 or 500 microg/day. Animal data and clinical trials have demonstrated roflumilast's efficacy and safety as an antiinflammatory and antimodulatory agent for use in asthma and COPD, with no documented drug interactions and a favorable adverse effect profile.


CONCLUSIONS
Roflumilast may be an additional option in the treatment of asthma and COPD due to its ease of administration and a seemingly favorable adverse event profile. However, more research is needed to solidify roflumilast's place in therapy.
Karish
Sarah B
SB
Pharmacy Practice, Massachusetts College of Pharmacy and Health Sciences, Boston, 02115, USA. skarish@bos.mcphs.edu
Gagnon
James M
JM
D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000037:antagonists & inhibitors*; D000631:Aminopyridines / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use* / Q000633:toxicity; D018927:Anti-Asthmatic Agents / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use* / Q000633:toxicity; D001249:Asthma / Q000188:drug therapy*; D001549:Benzamides / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use* / Q000633:toxicity; D002986:Clinical Trials as Topic; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4; D003521:Cyclopropanes / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use / Q000633:toxicity; D016527:Drug Costs; D004347:Drug Interactions; D006801:Humans; D010726:Phosphodiesterase Inhibitors / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use* / Q000633:toxicity; D029424:Pulmonary Disease, Chronic Obstructive / Q000188:drug therapy*
D000631:Aminopyridines; D018927:Anti-Asthmatic Agents; D001549:Benzamides; D003521:Cyclopropanes; D010726:Phosphodiesterase Inhibitors; C424423:Roflumilast; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4