roflumilast topical (Rx)

Brand and Other Names:Zoryve

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

topical cream

  • 0.3%

Plaque Psoriasis

Indicated for plaque psoriasis, including intertriginous areas

Apply once daily to affected areas and rub in completely

Wash hands after application, unless application is for treatment of hands

Dosage Forms & Strengths

topical cream

  • 0.3%

Plaque Psoriasis

Indicated for plaque psoriasis, including intertriginous areas, in patients aged ≥12 years

<12 years: Safety and efficacy not established

≥12 years

  • Apply once daily to affected areas and rub in completely
  • Wash hands after application, unless application is for treatment of hands
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Interactions

Interaction Checker

and roflumilast topical

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Contraindicated (0)

              Serious - Use Alternative (0)

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                  Minor (0)

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                    Adverse Effects

                    1-10%

                    Diarrhea (3.1%)

                    Headache (2.4%)

                    Insomnia (1.4%)

                    Nausea (1.2%)

                    Application site pain (1%)

                    Upper respiratory tract infection (1%)

                    Urinary tract infection (1%)

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                    Warnings

                    Contraindications

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

                    Cautions

                    Hepatic impairment

                    • Contraindicated with moderate-to-severe impairment (Child-Pugh B or C)
                    • No studies were conducted with topical roflumilast in patients with hepatic impairment; however, oral roflumilast 250 mcg/day for 14 days was studied in mild-to-moderate hepatic impairment (Child-Pugh A and B)
                    • AUC of roflumilast and roflumilast N-oxide were increased by 51% and 24%, respectively, in Child-Pugh A and by 92% and 41%, respectively, in Child-Pugh B, as compared to age-, weight-, and gender-matched healthy individuals
                    • Peak plasma concentration of roflumilast and roflumilast N-oxide were increased by 3% and 26%, respectively, in Child-Pugh A and by 26% and 40%, respectively, in Child-Pugh B, as compared to healthy individuals

                    Drug interaction overview

                    • No formal drug-drug interaction studies were conducted with topical roflumilast
                    • CYP Inhibitors
                      • Caution, monitor
                      • Coadministration of roflumilast with systemic CYP3A4 inhibitors or dual inhibitors that inhibit both CYP3A4 and CYP1A2 simultaneously (eg, erythromycin, ketoconazole, fluvoxamine, cimetidine) may increase roflumilast systemic exposure
                    • Oral contraceptives
                      • Caution, monitor
                      • Coadministration of roflumilast with oral contraceptives containing ethinyl estradiol may increase roflumilast systemic exposure
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                    Pregnancy & Lactation

                    Pregnancy

                    There are no randomized clinical trials of oral or topical roflumilast in pregnant females

                    Animal studies

                    • Oral administration to pregnant rats and rabbits during organogenesis produced no fetal structural abnormalities at doses up to 9 and 8 times the maximum recommended human dose (MRHD), respectively
                    • Roflumilast induced post-implantation loss in rats at oral doses ≥3x MRHD
                    • Roflumilast induced stillbirth and decreased pup viability in mice at oral doses 5x and 15x MRHD, respectively
                    • Shown to adversely affect pup post-natal development when dams were treated with oral dose 15x MRHD during pregnancy and lactation periods in mice

                    Clinical considerations

                    • Do not use during labor and delivery
                    • There are no human studies that have investigated effects on preterm labor or labor at term; however, animal studies showed roflumilast PO disrupted labor and delivery process in mice

                    Lactation

                    Data are not available regarding presence in human milk, effects on breastfed infants, or effects on milk production

                    Roflumilast and/or its metabolites are excreted into the milk of lactating rats; when a drug is present in animal milk, it is likely that to be present in human milk

                    Consider developmental and health benefits of breastfeeding along with the mother’s clinical need for treatment and any potential adverse effects on the breastfed infant

                    Clinical considerations

                    • Minimize potential exposure to breastfeeding infants via breast milk by applying to smallest area of skin and for the shortest duration possible
                    • Advise breastfeeding women not to apply cream directly to the nipple and areola to avoid direct infant exposure

                    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

                    Roflumilast and its active metabolite (roflumilast N-oxide) are inhibitors of phosphodiesterase (PDE)-4

                    Inhibition of PDE4 (a major cyclic 3′,5′-adenosine monophosphate (cyclic AMP) metabolizing enzyme) activity leads to accumulation of intracellular cyclic AMP

                    Specific mechanism(s) by which roflumilast exerts its therapeutic action is not well defined

                    Absorption

                    Following application of mean BSA 26.8% and 13% in adults (n = 18) and adolescents (n = 6) respectively, plasma concentrations were quantifiable in all but 2 individuals at Day 15

                    AUC (adults): 72.7 h⋅ng/mL (roflumilast); 628 h⋅ng/mL (N-oxide metabolite)

                    AUC (adolescents): 25.1 h⋅ng/mL (roflumilast); 140 h⋅ng/mL (N-oxide metabolite)

                    Distribution

                    Protein bound: 99% (roflumilast); 97% (N-oxide metabolite)

                    Metabolism

                    Extensively metabolized by cytochrome P450, then it undergoes conjugation

                    Elimination

                    Half-life (topical): 4 days (roflumilast); 4.6 days (N-oxide metabolite)

                    Plasma clearance (IV): 9.6 L/hr

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                    Administration

                    Topical Administration

                    For topical use only

                    Not for ophthalmic, oral, or intravaginal use

                    Wash hands after application, unless application is for treatment of hands

                    Storage

                    Store at 20-25ºC (68-77ºF); excursions permitted to 15-30ºC (59-86ºF)

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                    Images

                    No images available for this drug.
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                    Patient Handout

                    A Patient Handout is not currently available for this monograph.
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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.
                    QL Quantity Limits
                    Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
                    ST Step Therapy
                    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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                    Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each 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.