A long-acting muscarinic antagonist called Yupelri (revefenacin) relaxes the bronchial smooth muscle by competitively and irreversibly blocking the action of acetylcholine at type 3 muscarinic (M-3) receptors.

Yupelri (revefenacin) Uses (Indications):

• It is used in the maintenance treatment of chronic obstructive pulmonary disease (COPD)

Yupelri (revefenacin) dose in adults:

Yupelri dose for treating Chronic obstructive pulmonary disease:

• Nebulization solution dose is  175 mcg (1 unit-dose vial) once daily

Yupelri (revefenacin) dose in children:

Not recommended for use in children.

Pregnancy Risk Factor: Not Assigned

• Animal reproduction studies did not show any adverse events.
• Original studies did not include females with reproductive potential.

Revefenacin use during breastfeeding:

• It is unknown if revefenacin can be found in breast milk, or if it is absorbed through oral inhalation.
• According to the manufacturer breastfeeding during therapy should be considered in light of the risks to infants and the benefits to mothers.

Yupelri dose in Kidney disease:

• No dosage adjustment required

Yupelri dose in mild, moderate, or severe liver impairment:

• Use is not advised.

Side Effects of Revefenacin (Yupelri):

• Cardiovascular:

  • Hypertension

• Central Nervous System:

  • Headache
  • Dizziness

• Neuromuscular & Skeletal:

  • Back Pain

• Respiratory:

  • Nasopharyngitis
  • Upper Respiratory Tract Infection
  • Bronchitis
  • Oropharyngeal Pain

Contraindications to Revefenacin (Yupelri):

• Hypersensitivity to revefenacin, or any part thereof

Warnings and precautions

• Bronchospasm

  • Inhaled bronchodilating agent can cause paradoxical bronchospasm, which can be fatal.
  • This should be distinguished from an inadequate response.
  • Paradoxical bronchospasm can be treated with a short-acting bronchodilator.
  • If this does not work, you should discontinue revefenacin and seek alternative treatment.

• CNS effects

  • Dizziness and blurred vision can also be caused by anticholinergic agents
  • Patients must be made aware of activities requiring mental attentiveness, such as operating machinery or a vehicle. 

• Hypersensitivity

  • Also, hypersensitivity reactions can occur immediately.
  • If you experience an allergic reaction, stop taking any medication immediately.

• Glaucoma:

  • Patients with narrow-angle Glaucoma should be cautious; it may raise intraocular pressure.

• Hepatic impairment

  • Patients with hepatic impairment should not use this medication.

• Prostatic hyperplasia, bladder neck obstruction

  • Patients with bladder neck obstruction or prostatic hyperplasia should be cautious.
  • It can cause or worsen urinary retention.

• Renal impairment

  • It is important to keep an eye out for any systemic antimuscarinic adverse effects in patients with severe renal impairment.

Revefenacin: Drug Interaction

Monitor:

• FEV
• peak flow (or other pulmonary function tests)
• liver function tests (at baseline).
• Keep an eye out for urine retention, hypersensitivity responses, and acute narrow-angle glaucoma signs and symptoms.
• In individuals with severe renal impairment, look out for systemic antimuscarinic side effects.

How to administer Revefenacin (Yupelri)?

• Nebulization solution: For inhalation only
• Do not inject or swallow the solution.
• Use an ordinary jet nebulizer with a mouthpiece linked to an air compressor to administer through oral inhalation.
• Additionally, take the unit-dose vial out of the foil pouch right before using it.
• Prior to delivery, revefenacin does not require dilution.
• In the nebulizer, do not combine any other drugs.
• Discard any used drug.

Mechanism of action of Revefenacin (Yupelri):

• It is a long-acting muscarinic antagonist that blocks acetylcholine (M-3) receptor activity in bronchial smooth muscles in a competitive and reversible manner.
• This causes bronchodilation.

Initial:

• The onset of bronchodilation occurs within 45 minutes following a single dose. Peak FEV effect takes 2 to 3 hours after a single dosage.

Duration: Bronchodilation:

• Takes up to 24 hours

Absorption: Rapid

Protein binding:

• Revefenacin: almost 71%
• Active metabolite: almost 42%

Metabolism:

• The main amide is hydrolyzed to produce carboxylic acid as the principal mode of metabolism (to the major active metabolite)

Bioavailability:

• less than 3%

Half-life elimination:

• It takes 22 - 70 hours (revefenacin and active metabolite)

Time to peak:

• It takes 14 - 41 minutes (after the start of nebulization)

Excretion:  

• By Feces (primarily) & Urine (<1%, as revefenacin and active metabolite)

International Brands of Revefenacin:

• Yupelri

Revefenacin Brand Names in Pakistan:

No Brands Available in Pakistan.