Concise Prescribing Info
Severe COPD associated with chronic bronchitis and history of exacerbations.
Dosage/Direction for Use
Adult : PO Combined with bronchodilators: 500 mcg/day.
Dosage Details
Chronic obstructive pulmonary disease
Adult: In combination with bronchodilators in patient with severe cases associated with chronic bronchitis and history of exacerbations: 500 mcg once daily.
Hepatic Impairment
Moderate to severe (Child-Pugh B or C): Contraindicated.
May be taken with or without food.
Moderate to severe hepatic impairment (Child-Pugh B or C).
Special Precautions
Patient with history of suicidal ideation and behaviour, depression; <60 kg body weight. Mild hepatic impairment (Child-Pugh A). Pregnancy and lactation. Not indicated for the relief of acute bronchospasm.
Adverse Reactions
Significant: Weight loss, anxiety, depression, insomia. Rarely, suicidal ideation and behaviour.
Gastrointestinal disorders: Nausea, diarrhoea, abdominal pain.
Infections and infestations: Influenza.
Metabolism and nutrition disorders: Decreased appetite.
Musculoskeletal and connective tissue disorders: Back pain.
Nervous system disorders: Headache, dizziness.
Psychiatric disorders: Nervousness.
Monitor weight, LFTs; signs and symptoms of suicidal ideation and behaviour.
Symptoms: Headache, dizziness, lightheadedness, palpitations, arterial hypertension, gastrointestinal disturbances, clamminess. Management: Supportive treatment.
Drug Interactions
Increased exposure and adverse reactions with CYP enzyme inhibitors (e.g. cimetidine, erythromycin, fluvoxamine, ketoconazole, theophylline), oral contraceptives (e.g. ethinylestradiol). Decreased serum concentration with strong CYP enzyme inducers (e.g. rifampicin).
Description: Roflumilast is an inhibitor of phosphodiesterase type-4 (PDE4), an enzyme that metabolises cyclic adenosine-3’, 5’-monophosphate (cAMP), leading to accumulation of intracellular cAMP in the lungs which inhibits some inflammatory mediators (e.g. leukotriene) and reduces sputum neutrophils in patient with COPD.
Absorption: Absolute bioavailability: Approx 80%. Time to peak plasma concentration: 0.5-2 hours (roflumilast); 4-13 hours (roflumilast N-oxide).
Distribution: Food delays the rate of absorption. Volume of distribution: 2.9 L/kg. Plasma protein binding: Approx 99% (roflumilast); approx 97% (roflumilast N-oxide).
Metabolism: Extensively metabolised via phase I reactions including pyridine N-oxidation by CYP3A4 and CYP1A2 into active metabolite, roflumilast N-oxide; further metabolised via phase II reactions (conjugation).
Excretion: Mainly via urine (approx 70% as metabolites); faeces (approx 20%). Plasma elimination half-life: Approx 17 hours (roflumilast); approx 30 hours (roflumilast N-oxide).
Chemical Structure

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Store between 20-25°C.
ATC Classification
R03DX07 - roflumilast ; Belongs to the class of other systemic drugs used in the treatment of obstructive airway diseases.
Disclaimer: This information is independently developed by MIMS based on Roflumilast from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by
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