roflumilast

Common name: roflumilast

Trade name: Daxas

All names: roflumilast, roflumilast film tablets, roflumilast tablets, roflumilast, Daxas, Daliresp

Indications:

Chronic Obstructive Pulmonary Disease (COPD)

Dosage:

The recommended dose for patients with COPD is 500 mcg once daily, with or without food.

Adverse reactions:

The most common adverse reactions (≥2%): diarrhea, weight loss, nausea, headache, back pain, influenza, insomnia, dizziness and decreased appetite.

Contraindications:

Moderate to severe hepatic impairment (Child-Pugh classification B or C)

Precautions:

Acute bronchospasm: Do not use to relieve acute bronchospasm.

Psychiatric events including suicidal behavior: Advise patients, their caregivers, and families to be alert to the emergence or worsening of insomnia, anxiety, depression, suicidal thoughts, or other mood changes, and to contact their health care provider if such changes occur. Carefully weigh the risks and benefits of treatment with DALIRESP in patients with a history of depression and/or suicidal thoughts or behaviors.

Weight loss: Monitor your weight regularly. If unexplained or clinically significant weight loss occurs, evaluate weight loss and consider discontinuing use.

Drug interactions: It is not recommended to use with strong cytochrome P450 enzyme inducers (such as rifampicin, phenobarbital, carbamazepine, phenytoin).

Storage:

Keep away from light and sealed.

Mechanism of action:

Roflumilast is a long-acting inhibitor of selective phosphodiesterase type 4 (PDE-4) and has anti-inflammatory effects. Phosphodiesterases are a family of enzymes including at least 11 subtypes of enzymes that catalyze the decomposition of the messenger molecules cyclic adenosine monophosphate and/or cyclic guanosine monophosphate. Phosphodiesterase-4 is a major cyclic adenosine monophosphate metabolic enzyme in inflammatory and immune cells, and phosphodiesterase-4 inhibitors have broad anti-inflammatory activities including inhibiting the release of inflammatory mediators and inhibiting immune cell activation. In addition, phosphodiesterase-4 inhibitors have also been shown to have therapeutic effects in animal models of airway inflammation.

Safety and efficacy:

The EU approved the marketing of roflumilast (Daxas) in July 2010 for the treatment of chronic obstructive pulmonary disease (COPD). This product is a selective phosphodiesterase 4 (PDE4) inhibitor and is the first new class of COPD treatment drug approved by the EU in more than ten years. This product is a once-daily oral tablet that must be combined with other bronchodilators. It is suitable for the maintenance treatment of severe COPD related to chronic bronchitis (post-diastolic FEV1 less than 50% of the expected value) in adult patients with a history of frequent exacerbations. As a new type of COPD treatment drug, this product is expected to be launched on the European market soon. The first countries to be launched will be Germany and the United Kingdom.

Four phase III clinical studies laid the foundation for the approval of this product. More than 3,000 COPD patients were included in two pivotal placebo-controlled clinical studies. Studies have proven that this product can significantly improve patients with moderate to severe exacerbations and prediastolic FEV1, regardless of whether it is combined with a long-acting β2 agonist. Studies have also proven that this product can significantly improve patients' lung function compared with placebo.