Daliresp (roflumilast) is an advanced oral phosphodiesterase-4 (PDE4) inhibitor specifically indicated to reduce the risk of COPD exacerbations in patients with severe COPD associated with chronic bronchitis and a history of exacerbations. Unlike conventional bronchodilators, it targets underlying inflammation, offering a novel mechanism for long-term disease control. This medication represents a significant addition to maintenance therapy, particularly for high-risk patient populations seeking to minimize flare-ups and preserve lung function. Its systemic anti-inflammatory action complements standard care, providing a strategic option for pulmonologists and patients navigating complex COPD management.

Features

• Active ingredient: Roflumilast 500 mcg per tablet
• Pharmacologic class: Selective phosphodiesterase-4 (PDE4) inhibitor
• Administration: Oral, once-daily dosing
• Presentation: Film-coated, non-scored tablets
• Mechanism: Reduces airway inflammation via inhibition of PDE4, decreasing cytokines, chemokines, and other inflammatory mediators
• Prescription status: Rx-only

Benefits

• Reduces frequency of moderate-to-severe COPD exacerbations
• Decreases systemic and airway inflammation contributing to disease progression
• Offers convenient once-daily oral dosing, supporting adherence
• Complements existing bronchodilator therapy without significant pharmacokinetic interactions
• May help preserve lung function over time in high-risk patient subsets
• Provides a non-steroidal anti-inflammatory option for long-term management

Common use

Daliresp is indicated as a treatment to reduce the risk of COPD exacerbations in patients with severe COPD associated with chronic bronchitis and a history of exacerbations. It is not a bronchodilator and is not indicated for the relief of acute bronchospasm. It is generally prescribed as part of a comprehensive COPD management plan that includes smoking cessation, pulmonary rehabilitation, vaccination, and appropriate rescue and maintenance inhalers.

Dosage and direction

The recommended dosage of Daliresp is one 500 mcg tablet taken orally once daily, with or without food. It is important to initiate treatment with a dose escalation scheme to improve gastrointestinal tolerability: 250 mcg once daily for 4 weeks, followed by the maintenance dose of 500 mcg once daily thereafter. Tablets should be swallowed whole and not crushed, chewed, or broken. If gastrointestinal adverse reactions occur during treatment, temporary dose reduction to 250 mcg once daily may be considered, followed by re-escalation to 500 mcg once daily.

Precautions

• Daliresp is not a bronchodilator and should not be used for the relief of acute bronchospasm.
• Weight loss and decreased appetite have been reported; monitor body weight regularly and evaluate unexplained or clinically significant weight loss.
• Psychiatric events including insomnia, anxiety, depression, and rarely suicidal ideation have been observed. Patients and caregivers should be advised to report any new or worsening psychiatric symptoms.
• Use with caution in patients with a history of depression or suicidal thoughts/behavior.
• Not recommended for use in patients with moderate to severe liver impairment (Child-Pugh B or C).
• Pregnancy Category C: Use during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Contraindications

• Hypersensitivity to roflumilast or any component of the formulation.
• Moderate to severe liver impairment (Child-Pugh B or C).
• Concomitant use with strong cytochrome P450 enzyme inducers (e.g., rifampicin, phenobarbital, carbamazepine, phenytoin), which may significantly reduce roflumilast exposure and efficacy.

Possible side effects

Common adverse reactions (≥2% and greater than placebo) include:

• Diarrhea
• Weight decrease
• Nausea
• Headache
• Back pain
• Influenza
• Insomnia
• Dizziness
• Decreased appetite
• Vomiting
• Rhinitis
• Sinusitis
• Tremor
• Abdominal pain
• Dyspepsia
• Fatigue
• Muscle spasms
• Tooth abscess
• Gastroenteritis
• Anxiety
• Depression

Drug interaction

• Strong CYP450 inducers (e.g., rifampicin, phenobarbital, carbamazepine, phenytoin): May significantly decrease roflumilast exposure; concomitant use is contraindicated.
• Oral contraceptives containing gestodene and ethinyl estradiol: May increase roflumilast exposure by approximately 40%; clinical significance unknown.
• CYP3A4 inhibitors or CYP1A2 inhibitors: May increase roflumilast exposure, but dose adjustment is not recommended.

Missed dose

If a dose is missed, it should be taken as soon as remembered on the same day. If missed entirely for that day, the patient should resume the regular dosing schedule the following day. Do not double the dose to make up for a missed dose.

Overdose

There is limited experience with overdose. In clinical trials, doses up to 2500 mcg daily (5 times the recommended dose) were administered and were associated with increased incidence of adverse events, including gastrointestinal disturbances, headache, dizziness, palpitations, and lightheadedness. There is no specific antidote for roflumilast overdose. Treatment should be supportive and symptomatic. Hemodialysis is not expected to enhance elimination as roflumilast is highly protein-bound.

Storage

Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C (59°F and 86°F). Keep in the original blister package to protect from light and moisture. Keep out of reach of children and pets.

Disclaimer

This information is provided for educational purposes only and does not constitute medical advice. Daliresp is a prescription medication that should be used only under the supervision of a qualified healthcare professional. Patients should not initiate, adjust, or discontinue medication without consulting their physician. Individual results may vary, and not all patients will experience the same benefits or side effects.

Reviews

Clinical trials have demonstrated that Daliresp significantly reduces the rate of moderate-to-severe exacerbations compared to placebo in patients with severe COPD associated with chronic bronchitis. In pooled analyses, roflumilast-treated patients showed a 17% reduction in exacerbation rate. Pulmonary specialists note its value as an add-on therapy for specific patient populations, particularly those with frequent exacerbations despite optimized standard care. Many experts emphasize the importance of patient education regarding the delayed onset of effect (typically 4-8 weeks) and management of gastrointestinal side effects during treatment initiation. Real-world evidence continues to support its role in comprehensive COPD management strategies.