Dosing & Uses
Dosing Form & Strengths
Chronic Obstructive Pulmonary Disease
Reduction of frequency of exacerbations or worsening of symptoms
500 mcg PO once daily
- No dosage adjustment required
- Mild (Child-Pugh class A): Not sufficiently studied; AUCs of roflumilast and roflumilast N-oxide are increased by 51% and 24%, respectively; benefits of administration must be weighed against risks
- Moderate-to-severe (Child-Pugh class B or C): Contraindicated
May be taken with or without food
Safety and efficacy not established
Serious - Use Alternative
Significant - Monitor Closely
Weight loss (7.5%)
Back pain (3.2%)
Decreased appetite (2.1%)
Abdominal pain (1-2%)
Muscle spasms (1-2%)
Urinary tract infection (1-2%)
Frequency Not Defined
Hypersensitivity reactions including angioedema, urticaria, rash
Moderate-to-severe liver impairment (Child-Pugh class B or C)
Not indicated for relief of acute bronchospasm; drug is not bronchodilator
Psychiatric events, including suicidality, reported (monitor for emergence or worsening of insomnia, mood disturbance, or anxiety)
Monitor for clinically significant weight loss; this may be reversible upon discontinuance
Use with strong cytochrome P450 enzyme inducers (eg, rifampicin, phenobarbital, carbamazepine, phenytoin) not recommended
Pregnancy & Lactation
Pregnancy category: C
Lactation: Probable that roflumilast, its metabolites, or both are excreted into milk; avoid use
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Mechanism of Action
Selective phosphodiesterase (PDE)-4 inhibitor; PDE-4 inhibition leads to accumulation of intracellular cyclic adenosine monophosphate (cAMP) in lung tissue and is thought to be underlying mechanism of action
Peak plasma time: 1 hr (range, 0.5-2 hr); active metabolite, 8 hr
Protein bound: 99%
Vd: 2.9 L/kg
Extensively metabolized via phase I (CYP450) and phase II (conjugation) reactions; N-oxide metabolite is only major metabolite observed in human plasma; together, roflumilast and roflumilast N-oxide account for 87.5% of total dose administered in plasma
Biotransformation of roflumilast to N-oxide metabolite is mediated by CYP1A2 and CYP3A4
Half-life: Roflumilast, 17 hr; N-oxide metabolite, 30 hr
Clearance: 9.6 L/hr
Excretion: Urine (70%)
Adding plans allows you to compare formulary status to other drugs in the same class.
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The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.
|1||This drug is available at the lowest co-pay. Most commonly, these are generic drugs.|
|2||This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.|
|3||This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.|
|4||This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.|
|5||This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.|
|6||This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.|
|NC||NOT COVERED – Drugs that are not covered by the plan.|
Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.