Revefenacin (2 brand names, 1 dosage form, 1 route)
Available dosage forms: SOLUTION.
Routes of administration: INHALATION.
Brand Names
- REVEFENACIN
- YUPELRI
Indications and Usage
YUPELRI is indicated for the maintenance treatment of patients with chronic obstructive pulmonary disease (COPD).
Dosage and Administration
The recommended dosage is 175 mcg YUPELRI (one 175 mcg unit‑dose vial) administered by oral inhalation once daily by nebulizer using a mouthpiece. Administration Overview YUPELRI should be administered by the orally inhaled route via a standard jet nebulizer connected to an air compressor (See Instructions for Use). The safety and efficacy of YUPELRI have been established in clinical trials when administered using the PARI LC® Sprint nebulizer with a mouthpiece and the PARI Trek® S compressor. The safety and efficacy of YUPELRI delivered from non‑compressor based nebulizer systems have not been established. The YUPELRI unit-dose vial should only be removed from the foil pouch and opened IMMEDIATELY BEFORE USE. The vial and any residual content should be discarded after use. No dosage adjustment is required for geriatric patients, or patients with renal impairment [see Use in Specific Populations (8.5, 8.7) and Clinical Pharmacology (12.3)]. The drug compatibility (physical and chemical), efficacy, and safety of YUPELRI when mixed with other drugs in a nebulizer have not been established.
Contraindications
YUPELRI is contraindicated in patients with hypersensitivity to revefenacin or any component of this product.
Adverse Reactions
The following clinically significant adverse reactions are described elsewhere in labeling: •Paradoxical bronchospasm [see Warnings and Precautions (5.2)] •Worsening of narrow-angle glaucoma [see Warnings and Precautions (5.3)] •Worsening of urinary retention [see Warnings and Precautions (5.4)] •Immediate hypersensitivity reactions [see Warnings and Precautions (5.5) ]
Mechanism of Action
Revefenacin is a long-acting muscarinic antagonist, which is often referred to as an anticholinergic. It has similar affinity to the subtypes of muscarinic receptors M1 to M5. In the airways, it exhibits pharmacological effects through inhibition of M3 receptor at the smooth muscle leading to bronchodilation. The competitive and reversible nature of antagonism was shown with human and animal origin receptors and isolated organ preparations. In preclinical in vitro as well as in vivo models, prevention of methacholine- and acetylcholine-induced bronchoconstrictive effects was dose-dependent and lasted longer than 24 hours. The clinical relevance of these findings is unknown. The bronchodilation following inhalation of revefenacin is predominantly a site-specific effect.
Overdosage
An overdosage of YUPELRI may lead to anticholinergic signs and symptoms such as nausea, vomiting, dizziness, lightheadedness, blurred vision, increased intraocular pressure (causing pain, vision disturbances, or reddening of the eye), obstipation or difficulties in voiding. Treatment of overdosage consists of discontinuation of YUPELRI along with institution of appropriate symptomatic and/or supportive therapy.