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Brand Name :
Yupelri
Synonyms :
revefenacin
Class :
Inhaled Anticholinergics
Brand Name :
Yupelri
Synonyms :
revefenacin
Class :
Inhaled Anticholinergics
Dosage Forms & StrengthsÂ
Oral Inhalation SolutionÂ
175mcg/3ml vialÂ
Chronic Obstructive Pulmonary Disease (COPD)Â
Using a mouthpiece on a nebulizer, inhale 175 mcg orally every day
Administer every day at the same time
Do not exceed 175mg daily once
Dose Adjustments
Renal impairment
Any level of impairment: No change in dose is necessary.
Patients with COPD with substantial renal impairment should be monitored for systemic antimuscarinic side effects.
Hepatic impairment
Mild-to-severe: Safety has not been determined; individuals with any degree of hepatic impairment are not recommended
Not suggestedÂ
Refer adult dosingÂ
may decrease the therapeutic effect of Anticholinergic Agents
may enhance the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
revefenacin: they may increase the bradycardic effect of Bradycardia-Causing Agents
revefenacin: they may increase the bradycardic effect of Bradycardia-Causing Agents
revefenacin: they may increase the bradycardic effect of Bradycardia-Causing Agents
revefenacin: they may increase the bradycardic effect of Bradycardia-Causing Agents
revefenacin: they may increase the bradycardic effect of Bradycardia-Causing Agents
OATP1B1/1B3 inhibitors increase the concentration of active metabolites of revefenacin in the serum
OATP1B1/1B3 inhibitors increase the concentration of active metabolites of revefenacin in the serum
OATP1B1/1B3 inhibitors increase the concentration of active metabolites of revefenacin in the serum
OATP1B1/1B3 inhibitors increase the concentration of active metabolites of revefenacin in the serum
OATP1B1/1B3 inhibitors increase the concentration of active metabolites of revefenacin in the serum
may increase the anticholinergic effect of Anticholinergic Agents
may increase the anticholinergic effect of each other when combined
may increase the anticholinergic effect of each other when combined
may increase the anticholinergic effect of each other when combined
may increase the anticholinergic effect of each other when combined
may increase the anticholinergic effect of each other when combined
may decrease the therapeutic effect of Long-acting muscarinic antagonists
may increase the anticholinergic effect of Anticholinergic Agents
may increase the anticholinergic effect of Anticholinergic Agents
BCRP/ABCG2 inhibitors increase the concentration of pazobanib in the serum
BCRP/ABCG2 inhibitors increase the concentration of pazobanib in the serum
revefenacin: they may decrease the therapeutic effect of antihistamines
revefenacin: they may decrease the therapeutic effect of antihistamines
revefenacin: they may decrease the therapeutic effect of antihistamines
revefenacin: they may decrease the therapeutic effect of antihistamines
revefenacin: they may decrease the therapeutic effect of antihistamines
it increases the effect of anticholinergic agents
it increases the effect of anticholinergic agents
it increases the effect of anticholinergic agents
it increases the effect of anticholinergic agents
it increases the effect of anticholinergic agents
revefenacin: they may increase the CNS depressant effect of CNS Depressants
revefenacin: they may increase the CNS depressant effect of CNS Depressants
revefenacin: they may increase the CNS depressant effect of CNS Depressants
revefenacin: they may increase the CNS depressant effect of CNS Depressants
revefenacin: they may increase the CNS depressant effect of CNS Depressants
may increase the anticholinergic effect of anticholinergic agents
may enhance the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors
may enhance the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors
may increase the anticholinergic effect of anticholinergic agents
may increase the anticholinergic effect of anticholinergic agents
may increase the anticholinergic effect of Anticholinergic Agents
may increase the anticholinergic effect of Anticholinergic Agents
acetaminophen/doxylamine/dextromethorphanÂ
may increase the anticholinergic effect of Anticholinergic Agents
may enhance the concentration of serum when combined with OAT1/3 substrates
may decrease the therapeutic effect of Anticholinergic Agents
may decrease the therapeutic effect of Anticholinergic Agents
may decrease the therapeutic effect of Anticholinergic Agents
may increase the adverse effect of Anticholinergic Agents
may enhance the serum concentration of Anticholinergic Agents
may enhance the serum concentration of Anticholinergic Agents
may enhance the serum concentration of Anticholinergic Agents
may enhance the serum concentration of Anticholinergic Agents
may increase the adverse effect of Anticholinergic Agents
revefenacin: they may increase the hypertensive effect of sympathomimetics
revefenacin: they may increase the hypertensive effect of sympathomimetics
revefenacin: they may increase the hypertensive effect of sympathomimetics
revefenacin: they may increase the hypertensive effect of sympathomimetics
revefenacin: they may increase the hypertensive effect of sympathomimetics
revefenacin: they may enhance the serum concentration of CYP3A4 Inhibitors
revefenacin: they may enhance the serum concentration of CYP3A4 Inhibitors
revefenacin: they may enhance the serum concentration of CYP3A4 Inhibitors
revefenacin: they may enhance the serum concentration of CYP3A4 Inhibitors
revefenacin: they may enhance the serum concentration of CYP3A4 Inhibitors
aminohippuric acid may result in a decreased excretion rate of revefenacin, potentially causing elevated serum levels
may increase the anti-cholinergic effect
may increase the serum concentration of OAT1/3 substrates
may result in a significant increase in zavegepant exposure
may diminish the serum concentration of each other when combined
long-acting muscarinic antagonists decrease the efficacy of methacholine
Actions and Spectrum:Â
Mechanism of Action:Â
Spectrum of Activity:Â
Frequency definedÂ
1-10%Â
Nasopharyngitis (4%)Â
Upper respiratory tract infection (3%)Â
Hypertension (1-2%)Â
Oropharyngeal pain (1-2%)Â
Cough (4%)Â
Headache (4%)Â
Back pain (2%)Â
Dizziness (1-2%)Â
Bronchitis (1-2%)Â
Frequency not definedÂ
Worsening narrow-angle glaucomaÂ
Immediate hypersensitivity reactionsÂ
Dry mouthÂ
Paradoxical bronchospasmÂ
Worsening urinary retentionÂ
Contraindications/caution:Â
Contraindications:Â
Caution:Â
Â
Pregnancy consideration: Insufficient data availableÂ
Lactation: Excretion of the drug in human breast milk is unknownÂ
Pregnancy category:Â
Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.Â
Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.Â
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   Â
Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   Â
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.   Â
Category N: There is no data available for the drug under this categoryÂ
Pharmacology:Â
revefenacin is a long-acting muscarinic antagonist (LAMA) used as a bronchodilator for treating chronic obstructive pulmonary disease (COPD). The medication works by blocking the action of acetylcholine at muscarinic receptors in the airways, leading to the relaxation of the smooth muscle and dilation of the airways.Â
Specifically, revefenacin is a selective antagonist of the M3 muscarinic receptor subtype found primarily in the airway smooth muscle. By blocking the M3 receptor, revefenacin reduces bronchoconstriction and increases airflow, making breathing easier for individuals with COPD.Â
Pharmacodynamics:Â
The pharmacodynamics of revefenacin are primarily related to its action as a long-acting muscarinic antagonist (LAMA). Here are the vital pharmacodynamic effects of revefenacin:Â
Pharmacokinetics:Â
AbsorptionÂ
revefenacin is administered via inhalation using a handheld inhaler device. When inhaled, the medication reaches the lungs, which are absorbed through the respiratory epithelium and into the bloodstream. The inhalation route allows for targeted lung delivery while minimizing systemic absorption. Â
DistributionÂ
After absorption, revefenacin is distributed throughout the body. It primarily targets the muscarinic receptors in the smooth muscles of the airways, exerting bronchodilatory effects. The exact extent of distribution to other tissues and organs needs to be better characterized. Â
MetabolismÂ
revefenacin undergoes metabolism primarily through hydrolysis, which is the breakdown of the molecule by adding water. The specific enzymes involved in the metabolism of revefenacin have yet to be fully elucidated. The metabolites formed because of hydrolysis are pharmacologically inactive. Â
Elimination and ExcretionÂ
The elimination of revefenacin and its metabolites occurs primarily through renal excretion. After metabolism, the drug and its metabolites are eliminated from the body through the urine. The exact proportion of revefenacin excreted unchanged versus as metabolites need to be better established.Â
Administration:Â
Oral Inhalation:Â
Storage:Â
Patient information leafletÂ
Generic Name: revefenacinÂ
Why do we use revefenacin? Â
revefenacin is a medication used for the maintenance treatment of chronic obstructive pulmonary disease (COPD) in adults. Here are the specific uses of revefenacin:Â
Maintenance Treatment of COPD: revefenacin is indicated as a long-term maintenance treatment for patients with COPD. It improves symptoms and prevents exacerbations (flare-ups) in individuals with COPD, including chronic bronchitis and emphysema.Â
The medication helps to alleviate symptoms such as shortness of breath, coughing, and wheezing by promoting bronchodilation and improving airflow.Â
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