revefenacin (Rx)

Brand and Other Names:Yupelri

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

solution for oral inhalation

  • 175mcg/3mL vial

Chronic Obstructive Pulmonary Disease

Indicated for maintenance treatment of chronic obstructive pulmonary disease (COPD)

175 mcg inhaled PO qDay via nebulizer using a mouthpiece

Administer at the same time every day

Not to exceed 175 mg once daily

Dosage Modifications

Renal impairment

  • Any degree of impairment: No dosage adjustment is required
  • Monitor for systemic antimuscarinic adverse effects in COPD patients with severe renal impairment

Hepatic impairment

  • Mild-to-severe: Safety not evaluated; not recommended in patients with any degree of hepatic impairment

Not indicated

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Interactions

Interaction Checker

and revefenacin

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      Serious - Use Alternative

        Significant - Monitor Closely

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            Contraindicated (0)

              Serious - Use Alternative (37)

              • aclidinium

                revefenacin and aclidinium both decrease cholinergic effects/transmission. Avoid or Use Alternate Drug. Coadministration may cause additive anticholinergic effects.

              • atropine

                revefenacin and atropine both decrease cholinergic effects/transmission. Avoid or Use Alternate Drug. Coadministration may cause additive anticholinergic effects.

              • benztropine

                revefenacin and benztropine both decrease cholinergic effects/transmission. Avoid or Use Alternate Drug. Coadministration may cause additive anticholinergic effects.

              • cyclosporine

                cyclosporine increases levels of revefenacin by Other (see comment). Avoid or Use Alternate Drug. Comment: OATP1B1 and OATP1B3 transport inhibitors may increase systemic exposure of revefenacin's active metabolite. Coadministration not recommended.

              • darifenacin

                revefenacin and darifenacin both decrease cholinergic effects/transmission. Avoid or Use Alternate Drug. Coadministration may cause additive anticholinergic effects.

              • dicyclomine

                revefenacin and dicyclomine both decrease cholinergic effects/transmission. Avoid or Use Alternate Drug. Coadministration may cause additive anticholinergic effects.

              • erythromycin base

                erythromycin base increases levels of revefenacin by Other (see comment). Avoid or Use Alternate Drug. Comment: OATP1B1 and OATP1B3 transport inhibitors may increase systemic exposure of revefenacin's active metabolite. Coadministration not recommended.

              • erythromycin ethylsuccinate

                erythromycin ethylsuccinate increases levels of revefenacin by Other (see comment). Avoid or Use Alternate Drug. Comment: OATP1B1 and OATP1B3 transport inhibitors may increase systemic exposure of revefenacin's active metabolite. Coadministration not recommended.

              • erythromycin lactobionate

                erythromycin lactobionate increases levels of revefenacin by Other (see comment). Avoid or Use Alternate Drug. Comment: OATP1B1 and OATP1B3 transport inhibitors may increase systemic exposure of revefenacin's active metabolite. Coadministration not recommended.

              • erythromycin stearate

                erythromycin stearate increases levels of revefenacin by Other (see comment). Avoid or Use Alternate Drug. Comment: OATP1B1 and OATP1B3 transport inhibitors may increase systemic exposure of revefenacin's active metabolite. Coadministration not recommended.

              • fesoterodine

                revefenacin and fesoterodine both decrease cholinergic effects/transmission. Avoid or Use Alternate Drug. Coadministration may cause additive anticholinergic effects.

              • gemfibrozil

                gemfibrozil increases levels of revefenacin by Other (see comment). Avoid or Use Alternate Drug. Comment: OATP1B1 and OATP1B3 transport inhibitors may increase systemic exposure of revefenacin's active metabolite. Coadministration not recommended.

              • glecaprevir/pibrentasvir

                glecaprevir/pibrentasvir increases levels of revefenacin by Other (see comment). Avoid or Use Alternate Drug. Comment: OATP1B1 and OATP1B3 transport inhibitors may increase systemic exposure of revefenacin's active metabolite. Coadministration not recommended.

              • glycopyrrolate

                revefenacin and glycopyrrolate both decrease cholinergic effects/transmission. Avoid or Use Alternate Drug. Coadministration may cause additive anticholinergic effects.

              • glycopyrrolate inhaled

                revefenacin and glycopyrrolate inhaled both decrease cholinergic effects/transmission. Avoid or Use Alternate Drug. Coadministration may cause additive anticholinergic effects.

              • hyoscyamine

                revefenacin and hyoscyamine both decrease cholinergic effects/transmission. Avoid or Use Alternate Drug. Coadministration may cause additive anticholinergic effects.

              • hyoscyamine spray

                revefenacin and hyoscyamine spray both decrease cholinergic effects/transmission. Avoid or Use Alternate Drug. Coadministration may cause additive anticholinergic effects.

              • ipratropium

                revefenacin and ipratropium both decrease cholinergic effects/transmission. Avoid or Use Alternate Drug. Coadministration may cause additive anticholinergic effects.

              • leniolisib

                leniolisib will increase the level or effect of revefenacin by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates

              • methscopolamine

                revefenacin and methscopolamine both decrease cholinergic effects/transmission. Avoid or Use Alternate Drug. Coadministration may cause additive anticholinergic effects.

              • ombitasvir/paritaprevir/ritonavir & dasabuvir (DSC)

                ombitasvir/paritaprevir/ritonavir & dasabuvir (DSC) increases levels of revefenacin by Other (see comment). Avoid or Use Alternate Drug. Comment: OATP1B1 and OATP1B3 transport inhibitors may increase systemic exposure of revefenacin's active metabolite. Coadministration not recommended.

              • pazopanib

                pazopanib increases levels of revefenacin by Other (see comment). Avoid or Use Alternate Drug. Comment: OATP1B1 and OATP1B3 transport inhibitors may increase systemic exposure of revefenacin's active metabolite. Coadministration not recommended.

              • propantheline

                revefenacin and propantheline both decrease cholinergic effects/transmission. Avoid or Use Alternate Drug. Coadministration may cause additive anticholinergic effects.

              • rifampin

                rifampin increases levels of revefenacin by Other (see comment). Avoid or Use Alternate Drug. Comment: OATP1B1 and OATP1B3 transport inhibitors may increase systemic exposure of revefenacin's active metabolite. Coadministration not recommended.

              • rifamycin

                rifamycin increases levels of revefenacin by Other (see comment). Avoid or Use Alternate Drug. Comment: OATP1B1 and OATP1B3 transport inhibitors may increase systemic exposure of revefenacin's active metabolite. Coadministration not recommended.

              • ritonavir

                ritonavir increases levels of revefenacin by Other (see comment). Avoid or Use Alternate Drug. Comment: OATP1B1 and OATP1B3 transport inhibitors may increase systemic exposure of revefenacin's active metabolite. Coadministration not recommended.

              • solifenacin

                revefenacin and solifenacin both decrease cholinergic effects/transmission. Avoid or Use Alternate Drug. Coadministration may cause additive anticholinergic effects.

              • tacrolimus

                tacrolimus increases levels of revefenacin by Other (see comment). Avoid or Use Alternate Drug. Comment: OATP1B1 and OATP1B3 transport inhibitors may increase systemic exposure of revefenacin's active metabolite. Coadministration not recommended.

              • telmisartan

                telmisartan increases levels of revefenacin by Other (see comment). Avoid or Use Alternate Drug. Comment: OATP1B1 and OATP1B3 transport inhibitors may increase systemic exposure of revefenacin's active metabolite. Coadministration not recommended.

              • tiotropium

                revefenacin and tiotropium both decrease cholinergic effects/transmission. Avoid or Use Alternate Drug. Coadministration may cause additive anticholinergic effects.

              • tolterodine

                revefenacin and tolterodine both decrease cholinergic effects/transmission. Avoid or Use Alternate Drug. Coadministration may cause additive anticholinergic effects.

              • trihexyphenidyl

                revefenacin and trihexyphenidyl both decrease cholinergic effects/transmission. Avoid or Use Alternate Drug. Coadministration may cause additive anticholinergic effects.

              • trofinetide

                trofinetide will increase the level or effect of revefenacin by Other (see comment). Avoid or Use Alternate Drug. rofinetide (an OATP131 and OATP13B inhibitor) may increase plasma levels of OATP131 or OATP13B substrates. Avoid coadministration with sensitive substrates.

              • trospium chloride

                revefenacin and trospium chloride both decrease cholinergic effects/transmission. Avoid or Use Alternate Drug. Coadministration may cause additive anticholinergic effects.

              • umeclidinium bromide

                revefenacin and umeclidinium bromide both decrease cholinergic effects/transmission. Avoid or Use Alternate Drug. Coadministration may cause additive anticholinergic effects.

              • umeclidinium bromide/vilanterol inhaled

                revefenacin and umeclidinium bromide/vilanterol inhaled both decrease cholinergic effects/transmission. Avoid or Use Alternate Drug. Coadministration may cause additive anticholinergic effects.

              • velpatasvir

                velpatasvir increases levels of revefenacin by Other (see comment). Avoid or Use Alternate Drug. Comment: OATP1B1 and OATP1B3 transport inhibitors may increase systemic exposure of revefenacin's active metabolite. Coadministration not recommended.

              Monitor Closely (3)

              • donepezil transdermal

                donepezil transdermal, revefenacin. Either decreases effects of the other by pharmacodynamic antagonism. Use Caution/Monitor.

              • encorafenib

                encorafenib will increase the level or effect of revefenacin by Other (see comment). Modify Therapy/Monitor Closely. Encorafenib (a OATP1B1 and OATP1B3 inhibitor) may increase the concentration and toxicities of OATP1B1 and OATP1B3 substrates. Closely monitor for signs and symptoms of increased exposure and consider adjusting the dose of these substrates.

              • fostemsavir

                fostemsavir will increase the level or effect of revefenacin by Other (see comment). Modify Therapy/Monitor Closely. Fostemsavir inhibits OATP1B1/3 transporter. If possible, avoid coadministration or modify dose of OATP1B1/3 substrates coadministered with fostemsavir.

              Minor (0)

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                Adverse Effects

                1-10%

                Cough (4%)

                Nasopharyngitis (4%)

                Headache (4%)

                Upper respiratory tract infection (3%)

                Back pain (2%)

                Hypertension (1-2%)

                Dizziness (1-2%)

                Oropharyngeal pain (1-2%)

                Bronchitis (1-2%)

                Frequency Not Defined

                Paradoxical bronchospasm

                Worsening narrow-angle glaucoma

                Worsening urinary retention

                Immediate hypersensitivity reactions

                Dry mouth

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                Warnings

                Contraindications

                Hypersensitivity

                Cautions

                Do not initiate during acutely deteriorating or life-threatening COPD episodes; intended as maintenance treatment and not for relief of acute symptoms

                Inhalers can produce paradoxical bronchospasm that may be life-threatening; if this occurs, treat immediately with an inhaled, short-acting bronchodilator and discontinue revefenacin

                Caution with narrow-angle glaucoma; instruct patients to contact physician if symptoms occur (eg, eye pain, blurred vision, visual halos, colored images, red eyes from congestion, corneal edema)

                May worsen urinary retention, especially with history of prostatic hyperplasia or bladder-neck obstruction

                Immediate hypersensitivity reported; discontinue drug immediately

                Reevaluate COPD treatment immediately if

                • Therapy no longer controls bronchoconstriction symptoms
                • Inhaled short-acting beta2-agonist becomes less effective
                • More inhalations of a short-acting beta2-agonist are needed or exceed recommended maximum dose

                Drug interaction overview

                • Avoid coadministration with other anticholinergic drugs, owing to additive effects
                • OATP1B1 and OATP1B3 inhibitors may increase systemic exposure of revefenacin’s active metabolite; coadministration not recommended
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                Pregnancy

                Pregnancy

                There are no available data regarding use in pregnant women

                Advise women to contact their physician if they become pregnant while taking revefenacin

                Lactation

                Data are not available regarding presence of revefenacin in human milk, effects on breastfed infant, or effects on milk production

                Present in milk of lactating rats following dosing during pregnancy and lactation

                Consider the development and health benefits of breastfeeding along with the mother’s clinical need for the drug and any potential adverse effects on the breastfed child or from the underlying maternal condition

                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

                Long-acting muscarinic antagonist (LAMA), which is often referred to as an anticholinergic; blocks action of acetylcholine at muscarinic receptors (M1 to M5); in the bronchial airways, it elicits pharmacologic effect by inhibiting M3 at the smooth muscle, leading to bronchodilation

                Absorption

                Absolute oral bioavailability: <3%

                Peak plasma concentration: 0.16 ng/mL; 0.2 ng/mL (active metabolite)

                AUC: 0.22 ng·hr/mL; 0.69 ng·hr/mL (active metabolite)

                Steady-state achieved: Within 7 days

                Distribution

                Protein bound (IV): 71%; 42% (active metabolite)

                Vd (IV): 218 L

                Metabolism

                Primarily metabolized via hydrolysis of the primary amide to a carboxylic acid forming its major active metabolite

                Conversion to active metabolite occurred rapidly after inhalation, and plasma exposures of the active metabolite exceeded those of revefenacin by ~4- to 6-fold (based on AUC)

                Elimination

                Half-life: 22-70 hr

                Excretion

                • IV: 54% (19% active metabolite) feces; 27% urine
                • PO: 88% feces; <5% urine
                • Inhaled: <1% urine
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                Administration

                Oral Inhalation

                Do not swallow or inject solution

                Orally inhale using a standard jet nebulizer connected to air compressor; safety and efficacy not established for administration via noncompressor nebulizer systems

                Immediately before use, remove unit-dose vial from the foil pouch and open; discard vial and any residual content after use

                Drug compatibility (physical and chemical), efficacy, and safety of revefenacin when mixed with other drugs in a nebulizer have not been established

                Storage

                Store at room temperature between 68-77°F (20-25°C); excursions permitted from 59-86°F (15-30°C)

                Store in foil pouch until administered; protect from direct light

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                Images

                BRAND FORM. UNIT PRICE PILL IMAGE
                Yupelri inhalation
                -
                175 mcg/3 mL nebulizer soln
                Yupelri inhalation
                -
                175 mcg/3 mL nebulizer soln

                Copyright © 2010 First DataBank, Inc.

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                A Patient Handout is not currently available for this monograph.
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                Formulary

                FormularyPatient Discounts

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                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.
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                NC NOT COVERED – Drugs that are not covered by the plan.
                Code Definition
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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.