Roflumilast

Roflumilast

Structure of Roflumilast

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.

Clinical Use

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

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

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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Ball-and-stick model of Roflumilast

Related Pages

• Chronic obstructive pulmonary disease
• Phosphodiesterase inhibitor
• Anti-inflammatory