Roflumilast

Roflumilast tablets 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. Limitations of Use Roflumilast tablets is not a bronchodilator and is not indicated for the relief of acute bronchospasm. Roflumilast tablets 250 mcg is a starting dose, for the first 4 weeks of treatment only and is not the effective (therapeutic) dose. Roflumilast tablets is a selective phosphodiesterase 4 inhibitor 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. …

• The maintenance dose of roflumilast tablets is one 500 micrograms (mcg) tablet per day, with or without food
• Starting treatment with a dose of Roflumilast tablets 250 mcg once daily for 4 weeks and increasing to Roflumilast tablets 500 mcg once daily thereafter may reduce the rate of treatment discontinuation in some patients [ see Clinical Studies ]
• However, 250 mcg per day is not the effective (therapeutic) dose
• The maintenance dose for patients with COPD is one 500 mcg tablet per day, with or without food
• Starting treatment with a dose of Roflumilast tablets 250 mcg once daily for 4 weeks and increasing to roflumilast tablets 500 mcg once daily thereafter may reduce the rate of treatment discontinuation in some patients

Roflumilast tablets 250 mcg are White to off-white, round shaped, uncoated tablets debossed with 'R' on one side and '250' on the other side. Roflumilast tablets 500 mcg are white to off-white, round shaped, uncoated tablets debossed with "R" on one side and "500" on the other side. Tablets: 250 mcg, 500 mcg ( 3 )

• COPD does not normally occur in children
• The safety and effectiveness of roflumilast tablets
• In pediatric patients have not been established

Of the 4438 COPD subjects exposed to roflumilast tablets for up to 12 months in 8 controlled clinical trials, 2022 were greater than 65 years of age and 471 were greater than 75 years of age. No overall differences in safety or effectiveness were observed between these subjects and younger subjects and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity o …

• Advise the patient to read the FDA-approved patient labeling (Medication Guide)
• Bronchospasm Roflumilast tablets is not a bronchodilator and should not be used for immediate relief of breathing problems (i.e., as a rescue medication)
• Psychiatric Events including Suicidality Treatment with roflumilast tablets is associated with an increase in psychiatric adverse reactions
• Cases of suicidal ideation and behavior, including completed suicide, have been observed in the post-marketing setting in patients with or without a history of depression. …

• The use of roflumilast tablets is contraindicated in the following condition: Moderate to severe liver impairment (Child-Pugh B or C) [see Clinical Pharmacology and Use in Specific Populations ]
• Moderate to severe liver impairment (Child-Pugh B or C)

A major step in roflumilast metabolism is the N-oxidation of roflumilast to roflumilast N-oxide by CYP3A4 and CYP1A2 [see Clinical Pharmacology (12.3) ]. Use with inhibitors of CYP3A4 or dual inhibitors of CYP3A4 and CYP1A2 (e.g., erythromycin, ketoconazole, fluvoxamine, enoxacin, cimetidine) will increase roflumilast systemic exposure and may result in increased adverse reactions. The risk of such concurrent use should be weighed carefully against benefit.( 7.2 ) 7.1 Drugs that Induce Cytochrome P450 (CYP) Enzymes Strong cytochrome P450 enzyme inducers decrease systemic exposure to roflumilast and may reduce the therapeutic effectiveness of roflumilast tablets. …

Acute Bronchospasm: Do not use for the relief of acute bronchospasm. ( 5.1 ) Psychiatric Events including Suicidality: Advise patients, their caregivers, and families to be alert for the emergence or worsening of insomnia, anxiety, depression, suicidal thoughts or other mood changes, and if such changes occur to contact their healthcare provider. Carefully weigh the risks and benefits of treatment with roflumilast tablets in patients with a history of depression and/or suicidal thoughts or behavior. ( 5.2 ) Weight Decrease: Monitor weight regularly. If unexplained or clinically significant weight loss occurs, evaluate weight loss and consider discontinuation of roflumilast tablets. …

The following adverse reactions are described in greater detail in other sections: Psychiatric Events Including Suicidality [see Warnings and Precautions (5.2) ] Weight Decrease [see Warnings and Precautions (5.3) ] Most common adverse reactions (≥2%) are diarrhea, weight decrease, nausea, headache, back pain, influenza, insomnia, dizziness and decreased appetite. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Ascend Laboratories, LLC at 1-877-272-7901 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . …

8.1 Pregnancy Risk Summary There are no randomized clinical studies of roflumilast tablets in pregnant women. In animal reproductive toxicity studies, roflumilast tablets administered to pregnant rats and rabbits during the period of organogenesis produced no fetal structural abnormalities. The highest roflumilast tablets dose in these studies was approximately 30 and 26 times, respectively, the maximum recommended human dose (MRHD). …

10.1 Human Experience No case of overdose has been reported in clinical studies with roflumilast tablets. During the Phase I studies of roflumilast tablets, the following symptoms were observed at an increased rate after a single oral dose of 2500 mcg and a single dose of 5000 mcg: headache, gastrointestinal disorders, dizziness, palpitations, lightheadedness, clamminess, and arterial hypotension 10.2 Management of Overdose In case of overdose, patients should seek immediate medical help. Appropriate supportive medical care should be provided. …

Take it when you remember, unless it is nearly time for the next dose. Then skip the missed one. Never take two doses at once to make up for it. Check your leaflet, as some medicines are different.