roflumilast (Rx)

Brand and Other Names:Daliresp
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Dosing & Uses

AdultPediatric

Dosing Form & Strengths

tablet

  • 250mcg
  • 500mcg

Chronic Obstructive Pulmonary Disease

Indicated to reduce the risk of COPD exacerbations in patients with severe COPD associated with chronic bronchitis and a history of exacerbations

500 mcg PO qDay

Starting treatment with 250 mcg PO qDay for 4 weeks and increasing to 500 mcg qDay thereafter may reduce the rate of treatment discontinuation in some patients

NOTE: 250 mcg/day is not the effective (therapeutic) dose

Also see Administration

Dosage Modifications

Renal impairment

  • No dosage adjustment required

Hepatic impairment

  • 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

Safety and efficacy not established

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Interactions

Interaction Checker

and roflumilast

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            1-10%

            Diarrhea (9.5%)

            Weight loss (7.5%)

            Nausea (4.7%)

            Headache (4.4%)

            Back pain (3.2%)

            Insomnia (2.4%)

            Decreased appetite (2.1%)

            Dizziness (2.1%)

            1-10%

            Abdominal pain (1-2%)

            Anxiety (1-2%)

            Depression (1-2%)

            Dyspepsia (1-2%)

            Gastritis (1-2%)

            Muscle spasms (1-2%)

            Rhinitis (1-2%)

            Sinusitis (1-2%)

            Tremor (1-2%)

            Urinary tract infection (1-2%)

            Vomiting (1-2%)

            Frequency Not Defined

            Suicidality

            Postmarketing Reports

            Hypersensitivity reactions including angioedema, urticaria, rash

            Gynecomastia

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            Warnings

            Contraindications

            Hypersensitivity

            Moderate-to-severe liver impairment (Child-Pugh class B or C)

            Cautions

            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

            Drug interaction overview

            • Strong CYP3A4 inducers may reduce therapeutic effectiveness of roflumilast; coadministration not recommended
            • CYP P450 enzyme inhibitors
              • CYP3A4 inhibitors or dual inhibitors that inhibit both CYP3A4 and CYP1A2 simultaneously may increase roflumilast systemic exposure and increase risk for adverse effects
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            Pregnancy & Lactation

            Pregnancy

            Data are not available regarding use in pregnant women

            Lactation

            Probable that roflumilast, its metabolites, or both are excreted into milk; avoid use

            Pregnancy Categories

            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.

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            Pharmacology

            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

            Absorption

            80% absorbed

            Peak plasma time: 1 hr (range, 0.5-2 hr); active metabolite, 8 hr

            Distribution

            Protein bound: 99%  

            Vd: 2.9 L/kg

            Metabolism

            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

            Elimination

            Half-life: Roflumilast, 17 hr; N-oxide metabolite, 30 hr

            Clearance: 9.6 L/hr

            Excretion: Urine (70%)

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            Administration

            Oral Administration

            May take with or without food

            May titrate dose from 250 mcg/day to 500 mcg/day (therapeutic dose) over 4 weeks to improve tolerability (see Dosing)

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            Formulary

            FormularyPatient Discounts

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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.

            Tier Description
            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.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
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            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
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            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.