Yupelri (revefenacin)

Anticholinergic Agents Long-Acting (Inhaled) Inhalation Vial, Nebulizer (Ml)

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Last reviewed · Source: First Databank (FDB) drug data

Overview

Revefenacin, a synthetic tertiary amine antimuscarinic agent, is a long-acting orally inhaled bronchodilator.

Revefenacin is a synthetic tertiary amine antimuscarinic agent used as a long-acting, orally inhaled bronchodilator. The drug is a nonselective competitive antagonist at muscarinic (M1-M5) receptors. Revefenacin competitively and reversibly inhibits the actions of acetylcholine and other cholinergic stimuli at M3 receptors in the smooth muscle of the respiratory tract leading to bronchodilation.

Following oral inhalation in healthy individuals or in patients with chronic obstructive pulmonary disease (COPD), peak plasma concentrations of revefenacin and its active metabolite are reached within 14-41 minutes after initiation of nebulization. The absolute bioavailability following an oral dose of revefenacin is low (less than 3%). The peak effect on FEV1 following oral inhalation is 2-3 hours post dose.

Following repeated dosing of orally inhaled revefenacin, steady-state plasma concentrations are achieved within 7 days. In vitro revefenacin and its active metabolite are 71 and 42% bound to plasma proteins, respectively. Revefenacin is principally metabolized via hydrolysis of the primary amide to a carboxylic acid forming its major active metabolite.

Following oral inhalation of revefenacin, the conversion to its active metabolite occurs rapidly; plasma exposures of the active metabolite exceed those of revefenacin by approximately 4- to 6-fold (based on area under the serum concentration-time curve (AUC)). The active metabolite possesses activity at target muscarinic receptors that is lower (approximately one-third to one-tenth) than that of revefenacin.

Following IV administration in healthy individuals, approximately 54 and 27% of the radiolabeled dose was recovered in feces and urine, respectively. Approximately 19% of the radiolabeled dose was recovered in feces as the active metabolite. Following oral administration, 88 and less than 5% of a radiolabeled dose of revefenacin, was recovered in feces and urine, respectively, suggesting low oral absorption.

Following oral inhalation in patients with COPD, there is minimal renal excretion (less than 1%) of revefenacin and its active metabolite. The terminal half-life of the drug and its active metabolite after once-daily oral inhalation in patients with COPD is 22-70 hours. Age, sex, weight, and smoking status do not affect revefenacin exposure.

USES: Revefenacin is a long-term medication used to treat an ongoing lung disease, chronic obstructive pulmonary disease (COPD). It must be used regularly to reduce and prevent symptoms such as shortness of breath, cough, and wheezing. This medication belongs to a class of drugs known as anticholinergics.

It works by relaxing the muscles around the airways so that they open up and you can breathe more easily. Revefenacin does not work right away and should not be used to relieve sudden breathing problems. If wheezing or sudden shortness of breath occurs, use your quick-relief inhaler as prescribed.

Generic name: revefenacin
Pronunciation: (REV-e-FEN-a-sin)
Drug class: Anticholinergic Agents Long-Acting (Inhaled)
Therapeutic class: Respiratory Therapy Agents

Reference product & biosimilars

No reference, biosimilar or interchangeable associated with this drug.

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Indications

The following indications are listed for Yupelri:

  • Chronic Obstructive Pulmonary Disease

Dosing

No dosing information is available for this tab.

Drug interactions

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Contraindications

Revefenacin is contraindicated in patients with known hypersensitivity to the drug or any ingredient in the formulation.

Adverse reactions

Adverse events occurring in at least 2% of patients receiving revefenacin include cough, nasopharyngitis, upper respiratory tract infection, headache, and back pain.

Precautions

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ICD codes

CodeTypeDescription
Chronic obstructive pulmonary disease
J44ICD10CMOther chronic obstructive pulmonary disease
J44.8ICD10CMOther specified chronic obstructive pulmonary disease
J44.89ICD10CMOther specified chronic obstructive pulmonary disease
J44.9ICD10CMChronic obstructive pulmonary disease, unspecified

ICD code information from First Databank (FDB).

Formulary status

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Last reviewed · Source: First Databank (FDB) drug data