Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Substrate of
  • Inhibits
  • Induces
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names


Bulgaria: Daxas; Czech Republic: Daxas; Denmark: Daxas; Estonia: Daxas; Finland: Daxas; Germany: Daxas; Greece: Daxas; Hungary: Daxas; Ireland: Daxas; Latvia: Daxas; Lithuania: Daxas; Luxembourg: Daxas; Malta: Daxas; Netherlands: Daxas; Poland: Daxas; Portugal: Daxas; Romania: Daxas; Slovakia: Daxas; Slovenia: Daxas; Spain: Daxas; Sweden: Daxas; UK: Daxas.

North America

Canada: Daxas.

Drug combinations


Roflumilast: C~17~H~14~Cl~2~F~2~N~2~O~3~. Mw: 403.21. 3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide. CAS-162401-32-3.

Pharmacologic Category

Respiratory Tract Agents; Anti-inflammatory Agents; Leukotriene Modifiers. Selective Inhibitor of PDE4; Other Systemic Drugs for Obstructive Airway Diseases. (ATC-Code: R03DX07).

Mechanism of action

Roflumilast is a PDE4 inhibitor, a non-steroid, anti-inflammatory agent designed to target both the systemic and pulmonary inflammation associated with chronic obstructive pulmonary disease (COPD). Its mechanism of action is the inhibition of PDE4, a major cyclic adenosine monophosphate (cAMP)-metabolizing enzyme found in structural and inflammatory cells important to the pathogenesis of COPD. This mechanism of action and the selectivity also apply to roflumilast N-oxide, which is the major active metabolite of roflumilast. Inhibition of PDE4 leads to elevated intracellular cAMP levels and mitigates COPD-related malfunctions of leukocytes, airway and pulmonary vascular smooth muscle cells, endothelial and airway epithelial cells and fibroblasts in experimental models. Upon in vitro stimulation of human neutrophils, monocytes, macrophages or lymphocytes, roflumilast and roflumilast N-oxide suppress the release of inflammatory mediators, e.g. leukotriene B~4~, Reactive Oxygen Species, tumor necrosis factor α, interferon γ and granzyme B. In patients with COPD, roflumilast reduced sputum neutrophils. Furthermore, roflumilast attenuated influx of neutrophils and eosinophils into the airways of endotoxin-challenged healthy volunteers.

Therapeutic use

Indicated for maintenance treatment of severe COPD (FEV~1~ post-bronchodilator less than 50% predicted), associated with chronic bronchitis in adult patients with a history of frequent exacerbations, as an add-on to bronchodilator treatment.

Pregnancy and lactiation implications

Not recommended during pregnancy and in women of childbearing potential not using contraception. Should not be used during breast-feeding. Roflumilast has been demonstrated to cross the placenta and to be excreted in milk in animal studies.

Unlabeled use


Hypersensitivity to roflumilast or to any of the excipients. Moderate or severe hepatic impairment.

Warnings and precautions

Not indicated as rescue medicinal product for the relief of acute bronchospasms. A decrease in body weight has been reported. Treatment with roflumilast should not be initiated or existing treatment should be stopped in patients with severe immunological diseases (e.g. HIV infection, multiple sclerosis, lupus erythematosus, progressive multifocal leukoencephalopathy), severe acute infectious diseases, cancers (except basal cell carcinoma), or patients being treated with immunosuppressive medicinal products (e.g. methotrexate, azathioprine, infliximab, etanercept, or oral corticosteroids to be taken long-term; except short-term systemic corticosteroids). Not recommended in patients with congestive heart failure (NYHA grades 3 and 4). Associated with an increased risk of psychiatric disorders such as insomnia, anxiety, nervousness and depression. Rare instances of suicidal ideation and behavior, including completed suicide, have been observed. While adverse reactions like diarrhea, nausea, abdominal pain and headache mainly occur within the first weeks of therapy and mostly resolve on continued treatment, treatment should be reassessed in case of persistent intolerability, particularly in special populations that may have higher exposure, such as in black, non-smoking females or in patients concomitantly treated with the CYP1A2 inhibitor fluvoxamine or the dual CYP3A4/1A2 inhibitors enoxacin and cimetidine. Concomitant treatment with theophylline is not recommended. Tablets contain lactose (patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicinal product).



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