Dosing & Uses
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
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
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)
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
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
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.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
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
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Yupelri inhalation - | 175 mcg/3 mL nebulizer soln |  | |
| Yupelri inhalation - | 175 mcg/3 mL nebulizer soln |  |
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