Roflumilast: Difference between revisions

Latest revision as of 11:05, 23 March 2025

Roflumilast[edit]

Roflumilast is a phosphodiesterase-4 inhibitor used as an anti-inflammatory agent in the treatment of chronic obstructive pulmonary disease (COPD). It is marketed under the brand name Daliresp, among others. Roflumilast is specifically indicated to reduce the risk of COPD exacerbations in patients with severe COPD associated with chronic bronchitis and a history of exacerbations.

Mechanism of Action[edit]

Roflumilast works by inhibiting the enzyme phosphodiesterase-4 (PDE4), which leads to an increase in intracellular cyclic adenosine monophosphate (cAMP) levels. The elevation of cAMP results in a broad range of anti-inflammatory effects, including the suppression of the release of pro-inflammatory cytokines and the inhibition of inflammatory cell infiltration into the lungs. This mechanism helps to reduce the chronic inflammation associated with COPD.

Pharmacokinetics[edit]

Roflumilast is administered orally and is well absorbed from the gastrointestinal tract. It undergoes extensive metabolism in the liver, primarily by the cytochrome P450 enzymes CYP3A4 and CYP1A2, to form its active metabolite, roflumilast N-oxide. The drug and its metabolites are excreted mainly via the urine.

Clinical Use[edit]

Roflumilast is used as a maintenance treatment to reduce the frequency of exacerbations in patients with severe COPD. It is not a bronchodilator and should not be used for the relief of acute bronchospasm. The drug is typically prescribed to patients who have a history of frequent exacerbations despite the use of long-acting bronchodilators.

Side Effects[edit]

Common side effects of roflumilast include diarrhea, weight loss, nausea, headache, and insomnia. Some patients may experience psychiatric symptoms such as anxiety, depression, and insomnia. Due to the potential for weight loss, regular monitoring of body weight is recommended during treatment.

Contraindications and Precautions[edit]

Roflumilast is contraindicated in patients with moderate to severe liver impairment. Caution is advised when prescribing roflumilast to patients with a history of depression or suicidal thoughts. It is important to monitor patients for any changes in mood or behavior.

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Related Pages[edit]

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-{{intro}}
+== 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).
+[[File:Roflumilast_structure.svg|Structure of Roflumilast|thumb|right]]
+'''Roflumilast''' is a [[phosphodiesterase-4 inhibitor]] used as an [[anti-inflammatory]] agent in the treatment of [[chronic obstructive pulmonary disease]] (COPD). It is marketed under the brand name Daliresp, among others. Roflumilast is specifically indicated to reduce the risk of COPD exacerbations in patients with severe COPD associated with chronic bronchitis and a history of exacerbations.
+== Mechanism of Action ==
+Roflumilast works by inhibiting the enzyme [[phosphodiesterase-4]] (PDE4), which leads to an increase in intracellular cyclic adenosine monophosphate (cAMP) levels. The elevation of cAMP results in a broad range of anti-inflammatory effects, including the suppression of the release of pro-inflammatory cytokines and the inhibition of inflammatory cell infiltration into the lungs. This mechanism helps to reduce the chronic inflammation associated with COPD.
+== Pharmacokinetics ==
+Roflumilast is administered orally and is well absorbed from the gastrointestinal tract. It undergoes extensive metabolism in the liver, primarily by the [[cytochrome P450]] enzymes CYP3A4 and CYP1A2, to form its active metabolite, roflumilast N-oxide. The drug and its metabolites are excreted mainly via the urine.
-{{livtox}}
+== Clinical Use ==
-Roflumilast has not been linked to significant serum enzyme elevations during therapy or to instances of clinically apparent acute liver injury.
-{{moa}}
-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}}
+Roflumilast is used as a maintenance treatment to reduce the frequency of exacerbations in patients with severe COPD. It is not a bronchodilator and should not be used for the relief of acute bronchospasm. The drug is typically prescribed to patients who have a history of frequent exacerbations despite the use of long-acting bronchodilators.
-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.
-{{se}}
+== Side Effects ==
-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.
+Common side effects of roflumilast include diarrhea, weight loss, nausea, headache, and insomnia. Some patients may experience psychiatric symptoms such as anxiety, depression, and insomnia. Due to the potential for weight loss, regular monitoring of body weight is recommended during treatment.
-{{pulmonary agents}}
-{{coststubd}}
+== Contraindications and Precautions ==
-== Roflumilast ==
-<gallery>
+Roflumilast is contraindicated in patients with moderate to severe liver impairment. Caution is advised when prescribing roflumilast to patients with a history of depression or suicidal thoughts. It is important to monitor patients for any changes in mood or behavior.
-File:Roflumilast structure.svg|Roflumilast structure
-File:Roflumilast ball-and-stick model.png|Roflumilast ball-and-stick model
+== [[File:Roflumilast_ball-and-stick_model.png|Ball-and-stick model of Roflumilast|thumb|left]]
-</gallery>
+== Related Pages ==
+* [[Chronic obstructive pulmonary disease]]
+* [[Phosphodiesterase inhibitor]]
+* [[Anti-inflammatory]]
+[[Category:Phosphodiesterase inhibitors]]
+[[Category:Anti-inflammatory agents]]
+[[Category:Drugs used in respiratory diseases]]