Roflumilast

Information about Roflumilast

Roflumilast is a selective inhibitor of phosphodiesterase-4 (PDE-4) that has unique antiinflammatory activity and is used to treat and prevent exacerbations of chronic obstructive pulmonary disease (COPD).

Liver safety of Roflumilast

Roflumilast has not been linked to significant serum enzyme elevations during therapy or to instances of clinically apparent acute liver injury.

Mechanism of action of Roflumilast

Roflumilast (roe flue' mi last) is a long acting inhibitor of the enzyme, phosphodiesterase-4 (PDE-4), an oral antiinflammatory agent that is used to treat chronic obstructive pulmonary disease (COPD). PDE-4 is responsible for the metabolism of cyclic adenosine monophosphate (cAMP) and its inhibition results in increased intracellular concentrations of cAMP, an important mediator of inflammatory pathways. Roflumilast has been shown to decrease pro-inflammatory cytokines and reduce inflammatory responses in chronic pulmonary conditions including chronic bronchitis. In large controlled trials, roflumilast therapy was associated with a decrease in the numbers of severe, acute exacerbations of COPD and a modest improvement in pulmonary function test results.

FDA approval information for Roflumilast

Roflumilast was approved is 2011 for use in patients with COPD to prevent acute exacerbations of chronic bronchitis. It is currently available in tablets of 500 µg under the brand name Daliresp and the recommended dose in 500 µg once daily.

Side effects of Roflumilast

Side effects are generally mild and include diarrhea, nausea, vomiting, decreased appetite, weight loss, headache, dizziness, insomnia and back and joint pain. Rare, but potentially severe adverse reactions include depression, suicidality and hypersensitivity reactions, including angioedema.

Pulmonary Disease Agents

• Chronic Obstructive Pulmonary Disease (COPD) Agents
  • Anticholinergic Agents
    • Ipratropium, Tiotropium, Aclidinium
  • Beta-2 Adrenergic Agonists
    • Albuterol, Formoterol, Salmeterol, Terbutaline
  • Corticosteroids
    • Budesonide, Fluticasone
  • Miscellaneous
    • Roflumilast, Theophylline

• Pulmonary Arterial Hypertension Agents
  

• • Endothelin Receptor Antagonists
    • • Ambrisentan, Bosentan, Macitentan
  • Phosphodiesterase Type 5 (PDE5) Inhibitors
    • Avanafil, Sildenafil, Tadalafil, Vardenafil
  •  Prostacyclin Analogs
    • Epoprostenol, Iloprost, Treprostinil
  •  Miscellaneous
    • Riociguat, Selexipag

• Pulmonary Fibrosis Agents
  • Nintedanib, Pirfenidone

• Dailymed label info on Roflumilast
• FDA Roflumilast

Roflumilast

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  Roflumilast structure
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  Roflumilast ball-and-stick model