Daliresp (roflumilast) is a selective phosphodiesterase-4 (PDE4) inhibitor indicated to reduce the risk of COPD exacerbations in patients with severe COPD associated with chronic bronchitis and a history of exacerbations. It represents a distinct class of oral maintenance therapy targeting underlying inflammation in the airways, rather than simply providing symptomatic bronchodilation. By modulating intracellular cyclic AMP levels, it exerts anti-inflammatory effects that can lead to a significant reduction in the frequency of flare-ups, thereby improving long-term disease management and patient quality of life.

Features

• Active Pharmaceutical Ingredient: Roflumilast 500 mcg
• Pharmacologic Class: Selective Phosphodiesterase-4 (PDE4) Inhibitor
• Dosage Form: Film-coated, unscored tablet
• Administration Route: Oral
• Mechanism of Action: Inhibition of PDE4 enzyme, leading to increased intracellular cyclic AMP (cAMP), which mediates broad anti-inflammatory effects within lung tissue.

Benefits

• Reduces the frequency of moderate or severe exacerbations (flare-ups) in high-risk COPD patients.
• Targets the underlying inflammatory pathophysiology of COPD, offering a mechanism distinct from bronchodilators.
• Oral administration provides a convenient, once-daily dosing regimen that integrates easily into a patient’s existing treatment plan.
• Can be used as an add-on therapy to bronchodilator treatment, providing a complementary approach to disease management.
• Helps improve lung function over time by mitigating the inflammatory processes that contribute to disease progression.
• May contribute to an enhanced quality of life by reducing hospitalizations and the need for rescue medications.

Common use

Daliresp is prescribed for the maintenance treatment of severe Chronic Obstructive Pulmonary Disease (COPD). It is specifically indicated to reduce the risk of COPD exacerbations in adult patients with COPD associated with chronic bronchitis and a history of exacerbations. It is not indicated for the relief of acute bronchospasm and is intended as a chronic, daily therapy to manage the inflammatory component of the disease. It is often used concomitantly with bronchodilators.

Dosage and direction

The recommended dosage of Daliresp is one 500 mcg tablet taken orally once daily, with or without food. To improve tolerability, particularly with regard to gastrointestinal side effects, a dose escalation scheme is recommended: 250 mcg once daily for the first 4 weeks of treatment, followed by an increase to the maintenance dose of 500 mcg once daily. The tablet should be swallowed whole; it should not be crushed, split, or chewed. Treatment should be continued on a long-term basis as prescribed to achieve the full therapeutic effect on exacerbation reduction.

Precautions

• Weight Monitoring: Patients should have their body weight monitored regularly. Clinically significant weight loss has been observed; management may include nutritional support or discontinuation of therapy.
• Psychiatric Events: Use with caution in patients with a history of depression or underlying psychiatric illness. Patients and caregivers should be advised to report any new or worsening psychiatric symptoms (e.g., depression, suicidal thoughts/behavior, anxiety, insomnia).
• Nausea and Diarrhea: These are common side effects, especially upon initiation. These symptoms often decrease over time. Dose escalation is used to mitigate these effects.
• Pregnancy and Lactation: Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is not known if roflumilast is excreted in human milk; a decision should be made to discontinue nursing or discontinue the drug.
• Hepatic Impairment: Not recommended for patients with severe hepatic impairment (Child-Pugh C).

Contraindications

Daliresp is contraindicated in patients with a known hypersensitivity to roflumilast or any excipients in the product. Its use is also contraindicated in patients with moderate to severe liver impairment (Child-Pugh B or C).

Possible side effect

The most common adverse reactions (>2% and greater than placebo) include:

• Diarrhea
• Weight decrease
• Nausea
• Headache
• Insomnia
• Back pain
• Decreased appetite
• Dizziness
• Influenza Less common but serious side effects can include psychiatric events including depression, suicidal ideation, and anxiety, as well as persistent and severe weight loss.

Drug interaction

• CYP450 Enzyme Inducers: Strong cytochrome P450 enzyme inducers (e.g., rifampicin, phenobarbital, carbamazepine, phenytoin) may reduce the systemic exposure and efficacy of roflumilast. Concomitant use is not recommended.
• Oral Corticosteroids: While often used together in clinical practice, no formal pharmacokinetic interaction has been observed.
• Bronchodilators: (e.g., salmeterol, tiotropium) No clinically significant interactions have been observed; Daliresp is designed for concomitant use.
• Other CYP3A4/1A2 Inhibitors: While not contraindicated, fluvoxamine and enoxacin (CYP1A2 inhibitors) or ketoconazole (CYP3A4 inhibitor) may increase roflumilast exposure. Clinical monitoring is advised.

Missed dose

If a dose is missed, it should be taken as soon as remembered on the same day. If a day has been missed, the patient should not take a double dose to make up for the missed dose. Instead, they should resume the usual schedule of one tablet once daily the following day.

Overdose

There is limited experience with overdose in humans. Based on its mechanism and pharmacological profile, symptoms of overdose may be an extension of its adverse reaction profile, particularly severe nausea, vomiting, diarrhea, dizziness, palpitations, and lightheadedness. There is no known specific antidote. Treatment should consist of general supportive measures, including monitoring of vital signs and ECG. Gastric lavage may be considered if performed soon after ingestion.

Storage

Store Daliresp tablets at room temperature, between 20°C to 25°C (68°F to 77°F), with excursions permitted between 15°C and 30°C (59°F and 86°F). Keep the bottle tightly closed to protect from moisture and light. Keep out of reach of children and pets. Do not use after the expiration date printed on the bottle.

Disclaimer

This information is for educational and informational purposes only and does not constitute medical advice. It is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or before starting any new treatment. Never disregard professional medical advice or delay in seeking it because of something you have read here. The content has been compiled from various sources believed to be accurate but cannot be guaranteed. The manufacturer’s official prescribing information is the ultimate authority.

Reviews

“Since adding Daliresp to my patient’s regimen of LABA/ICS and a SAMA, we have seen a marked reduction in his exacerbation frequency. The initial GI side effects were managed with the stepped dosing approach and subsided after a few weeks. A valuable tool for targeting inflammation.” – Pulmonologist, Northeast US

“While the efficacy in reducing exacerbations is clear from the trials, patient selection and management are key. The weight loss and potential psychiatric effects require vigilant monitoring and a strong patient-doctor dialogue. It’s not a first-line agent, but for the right patient, it fills an important therapeutic niche.” – Clinical Pharmacist Specialist, Respiratory

“My patients who have stayed on it long-term have truly benefited from fewer flare-ups and hospital visits. The key is setting expectations upfront about the first month and providing strong support during the dose-escalation phase.” – Nurse Practitioner, COPD Clinic