Generic Daliresp (Roflumilast)

Introduction

Daliresp is a prescription medication whose active ingredient is roflumilast, a selective phosphodiesterase-4 (PDE-4) inhibitor. It is supplied as an oral tablet of 500 µg and is indicated for the long-term maintenance treatment of patients with severe chronic obstructive pulmonary disease (COPD) associated with chronic bronchitis, who have frequent exacerbations despite optimal bronchodilator therapy. The drug belongs to the class of anti-inflammatory agents used in respiratory disease. In addition to its primary indication, roflumilast has been explored in clinical research for several other inflammatory and dermatologic conditions, although these uses remain off-label.

What is Daliresp?

Daliresp is a brand-name formulation of roflumilast, developed and marketed by Takeda Pharmaceutical Company. The product is supplied as a film-coated tablet containing 500 µg of roflumilast. Roflumilast is the chemical entity that confers the therapeutic activity; Daliresp is the commercial name under which it is sold in many regulatory regions, including the United States, the European Union, and Japan. Other market identifiers for roflumilast include the generic name “roflumilast” itself and, in some territories, the brand “Daliresp®.”

How Daliresp Works

Roflumilast exerts its effect by selectively inhibiting the enzyme phosphodiesterase-4 (PDE-4), which is highly expressed in inflammatory cells of the airway such as neutrophils, macrophages, and T-lymphocytes. PDE-4 normally degrades cyclic adenosine monophosphate (cAMP); by blocking this enzyme, roflumilast increases intracellular cAMP levels. Elevated cAMP dampens the release of pro-inflammatory cytokines (e.g., TNF-α, IL-8, IL-6) and reduces the recruitment of inflammatory cells to the bronchial wall. The net result is a decrease in chronic airway inflammation, which translates into fewer COPD exacerbations and a slower decline in lung function.

Pharmacokinetic data show that roflumilast is absorbed rapidly after oral administration, reaching peak plasma concentrations within 1 hour. It is extensively metabolized by the cytochrome P450 enzyme CYP3A4 to an active metabolite (roflumilast N-oxide) that contributes to the overall anti-inflammatory effect. The terminal half-life of the parent drug is approximately 20 hours, permitting once-daily dosing. Steady-state concentrations are achieved after 4-5 days of continuous therapy.

Conditions Treated with Daliresp

• Severe COPD with a chronic bronchitis phenotype - Clinical trials (e.g., the “REACT” and “HORIZON” studies) demonstrated that daily roflumilast reduced the rate of moderate-to-severe exacerbations by 15-20 % when added to inhaled bronchodilators. The drug is therefore indicated for patients who continue to experience exacerbations despite optimized inhaled therapy.

• COPD patients with a history of frequent exacerbations - The indication specifically includes individuals who have had at least two exacerbations in the previous year, reflecting the drug’s role in secondary prevention.

The therapeutic benefit arises from roflumilast’s anti-inflammatory mechanism, which targets a pathogenic pathway not addressed by bronchodilators alone. By decreasing airway inflammation, the medication helps maintain lung capacity and improves overall disease stability.

Off-Label and Investigational Uses of Daliresp

• Psoriasis - Small-scale studies have shown that roflumilast can reduce the severity of plaque psoriasis, likely through the same cAMP-mediated anti-inflammatory pathway. However, the formulation is not approved for dermatologic use, and larger randomized trials are pending.

• Asthma with eosinophilic inflammation - Early-phase research suggests that PDE-4 inhibition may suppress eosinophil activation, offering a potential adjunctive therapy for severe asthma. Regulatory approval for this indication has not been granted.

• Chronic rhinosinusitis with nasal polyps - Case series have reported symptom improvement when roflumilast is added to standard nasal steroids, but evidence remains anecdotal.

• Peripheral artery disease - Pre-clinical models indicate that roflumilast may improve endothelial function, yet clinical translation is still investigational.

All off-label applications should be pursued only under the direct supervision of a qualified healthcare professional, as safety and efficacy have not been formally established by regulatory agencies such as the FDA or EMA.

Is Daliresp the Right Medication for You?

Daliresp is most appropriate for adults with a confirmed diagnosis of severe COPD who continue to experience frequent exacerbations despite maximal inhaled therapy (long-acting bronchodilators and inhaled corticosteroids). Patients who demonstrate a chronic bronchitis phenotype-characterized by persistent cough and sputum production-derive the greatest benefit.

Contraindications include:

• Known hypersensitivity to roflumilast or any excipients in the tablet.
• Severe hepatic impairment (Child-Pugh class C) because roflumilast exposure can increase markedly.
• Pregnancy or lactation, where the risk-benefit ratio has not been established.

Caution is advised in individuals with moderate liver disease, a history of depression or suicidal ideation, and in those receiving strong CYP3A4 inhibitors (e.g., ketoconazole) or inducers (e.g., rifampin), as drug levels may be altered.

Risks, Side Effects, and Interactions

Common

• Diarrhea - Occurs in up to 30 % of patients; usually mild to moderate and resolves with continued therapy.
• Nausea and abdominal pain - Frequently reported early in treatment.
• Weight loss - A modest decrease in body weight (average 1-2 kg) can be observed, particularly in patients with lower baseline BMI.

Rare

• Psychiatric events - Including anxiety, insomnia, and, rarely, depressive symptoms. Patients with a prior history of mood disorders should be monitored closely.
• Elevated liver enzymes - Transient increases in ALT/AST have been documented in <5 % of users; routine hepatic monitoring is recommended.

Serious

• Severe gastrointestinal hemorrhage - Though uncommon, reports of gastrointestinal bleeding warrant immediate medical attention.
• Severe hepatotoxicity - Rare cases of clinically significant liver injury have been described; cessation of the drug is required if liver enzymes rise >3 × upper limit of normal with symptoms.

Drug-Drug Interactions

• CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin) - May increase roflumilast plasma concentrations, raising the risk of adverse events. Dose adjustment is not formally recommended, but close monitoring is advised.
• CYP3A4 inducers (e.g., rifampin, carbamazepine) - Can reduce efficacy by lowering drug exposure.
• Strong P-glycoprotein (P-gp) inhibitors - May modestly increase roflumilast levels.

Drug-Food Interactions

• Roflumilast can be taken with or without food; however, taking the tablet with a meal may lessen gastrointestinal discomfort for some patients.
• Alcohol ingestion does not impact the pharmacokinetics of roflumilast but should be limited because of the additive risk of hepatic stress.

Use: Dosing, Missed Dose, Overdose

• Standard dosing - The recommended regimen is one 500 µg tablet taken orally once daily, preferably in the morning to align with daily routines. No titration is required.
• Missed dose - If a dose is forgotten and the scheduled time for the next dose is more than 12 hours away, the missed tablet should be taken as soon as remembered. If the next dose is imminent, skip the missed tablet and continue with the regular dosing schedule. Do not double-dose.
• Overdose - Acute overdose of roflumilast is rare. Symptoms may include severe nausea, vomiting, diarrhea, and abdominal pain. Management is supportive; there is no specific antidote. Contact emergency services or a poison-information center promptly.
• Practical considerations - Roflumilast should be stored at room temperature, protected from moisture and heat. Avoid crushing or splitting the tablet, as the film coating ensures consistent drug release. Patients should refrain from operating heavy machinery until they know how the medication affects them, especially during the first few days of therapy.

FAQ

• Can I travel internationally with Daliresp? You may transport a personal supply of Daliresp in its original pharmacy-labeled container. Carry a copy of the prescribing information or a physician’s letter if you anticipate customs screening, as the medication is prescription-only in most jurisdictions.

• Does Daliresp interact with grapefruit juice? Roflumilast is metabolized predominantly by CYP3A4, an enzyme that grapefruit juice can inhibit. While documented interactions are limited, it is prudent to avoid large amounts of grapefruit or grapefruit juice to prevent a potential increase in drug exposure.

• What does the Daliresp tablet look like? The tablet is a white, film-coated, round tablet bearing the imprint “RFL 500”. It is scored in the middle, allowing the tablet to be split if a lower dose is ever prescribed, though routine splitting is not recommended.

• Are there any excipients that could trigger allergies? Inactive ingredients include lactose, microcrystalline cellulose, and magnesium stearate. Patients with documented lactose intolerance or severe hypersensitivity to any of these components should discuss alternatives with their clinician.

• How long does it take to see a reduction in COPD exacerbations? Clinical trials reported a measurable decline in exacerbation rates after approximately 12 weeks of continuous therapy. Full therapeutic benefit is generally observed after 6 months of consistent use.

• Is Daliresp safe for patients with mild kidney disease? Roflumilast is eliminated primarily via hepatic pathways, and dose adjustment is not required for mild to moderate renal impairment. Severe renal failure has not been extensively studied, so clinicians should exercise caution.

• Can I take Daliresp together with inhaled corticosteroids? Yes. In fact, the approved indication for Daliresp requires that patients are already on optimal bronchodilator therapy, which often includes inhaled corticosteroids. No pharmacokinetic interaction has been identified.

• What should I do if I experience persistent weight loss? A gradual decline in body weight of more than 5 % of baseline over several weeks should be reported to a healthcare professional. Nutritional counseling and periodic weight monitoring are recommended during therapy.

• Does Daliresp affect blood glucose levels? Roflumilast does not have a direct impact on glucose metabolism. However, weight loss or gastrointestinal side effects could indirectly influence glycemic control in diabetic patients; monitoring is advisable.

• Is there a generic version of roflumilast available? Yes, roflumilast is marketed in generic form by several licensed manufacturers. The generic tablets contain the same 500 µg dose and are bioequivalent to Daliresp, offering a cost-effective alternative for eligible patients.

Glossary

Phosphodiesterase-4 (PDE-4)

An enzyme that breaks down cyclic AMP in inflammatory cells; inhibition leads to increased cAMP and reduced cytokine release.

Exacerbation

A worsening of COPD symptoms (increased dyspnea, cough, sputum) that often requires additional treatment such as antibiotics or steroids.

CYP3A4

A major liver enzyme responsible for metabolizing many drugs; substances that inhibit or induce CYP3A4 can respectively increase or decrease levels of roflumilast.

N-oxide metabolite

The primary active metabolite of roflumilast formed by oxidation; it contributes significantly to the drug’s overall anti-inflammatory effect.

Buying Daliresp from Our Online pharmacy

Patients who encounter limited access to Daliresp through conventional retail pharmacies or face high out-of-pocket costs can obtain the medication from our online pharmacy. We partner exclusively with licensed, overseas pharmaceutical distributors that source the product directly from the manufacturer or authorized wholesalers, ensuring that every tablet meets regulatory quality standards.

Because the supply chain is tightly vetted, you receive a product that is chemically identical to the brand-name version, yet offered at a price that closely reflects the manufacturer’s cost. Our discreet packaging protects your privacy, and we ship with reliable carriers that provide tracking and delivery confirmation. Typical shipping options include a 7-day express service for urgent needs and a regular airmail service that arrives in approximately three weeks, both with a guarantee of on-time arrival.

Operating as a pharmacy-broker service, we simplify the logistics of acquiring international medications while maintaining full compliance with import regulations. The process is secure, confidential, and supported by a dedicated customer-care team that can answer any questions about product verification, shipping status, or payment methods.

Disclaimer

The information presented about Daliresp is intended solely for general educational purposes and does not substitute for professional medical advice. Treatment choices, including any off-label applications, must be made under the direct supervision of a qualified healthcare provider. Readers are presumed to be competent adults capable of evaluating health-related information. Our online pharmacy provides access to Daliresp for individuals who may experience limited availability through traditional pharmacy channels, insurance formularies, or who are seeking cost-effective generic alternatives. Always consult a qualified clinician before initiating, adjusting, or discontinuing any medication.