Generic
Revefenacin
1 brands available in the market
At a glance
Revefenacin is a long-acting muscarinic antagonist (LAMA) used for the maintenance treatment of chronic obstructive pulmonary disease (COPD). It is inhaled once daily via nebulizer and provides bronchodilation.
Description
Revefenacin is a long-acting muscarinic antagonist (anticholinergic) with similar affinity for M1-M5 muscarinic receptors. In the airways, it inhibits M3 receptors on smooth muscle, causing bronchodilation. Competitive and reversible antagonism has been demonstrated in animal and human receptor models.
Indications
- Maintenance treatment of chronic obstructive pulmonary disease (COPD)
Therapeutic class
Anticholinergic bronchodilators
Pharmacological class
Long-acting Muscarinic Antagonist (LAMA)
Pharmacology
Revefenacin is a long-acting muscarinic antagonist with similar affinity for M1-M5 receptors. It inhibits M3 receptors on airway smooth muscle, causing bronchodilation. Preclinical models showed dose-dependent prevention of methacholine- and acetylcholine-induced bronchoconstrictive effects lasting over 24 hours.
Mechanism of action
Provides bronchodilation by inhibiting M3 receptors on airway smooth muscle.
Dosage
Adult Dose (Inhalation):
- COPD maintenance: 175 mcg (one unit-dose vial) once daily via nebulizer using a mouthpiece
- Administer at the same time each day
- Hepatic impairment: Safety not evaluated; not recommended in any degree of hepatic impairment
- Renal impairment: No dosage adjustment required
Administration
- Inhale orally; do not swallow or inject
- Use a standard jet nebulizer connected to an air compressor
- Remove the unit-dose vial from the foil pouch and open immediately before use
- Discard vial and any residual content after use
Missed dose
If you miss a dose, consult your doctor.
Side effects
Side 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%)
Precautions & warnings
- Do not initiate during acutely deteriorating or life-threatening COPD episodes
- Intended for maintenance treatment; not for relief of acute symptoms
- Paradoxical bronchospasm may occur (life-threatening); treat with short-acting bronchodilator and discontinue
- Caution in narrow-angle glaucoma (eye pain, blurred vision, visual halos) and urinary retention (prostatic hyperplasia)
- Immediate hypersensitivity reactions: Discontinue
Contraindications
- Hypersensitivity to revefenacin or any component
Drug interactions
- Additive interaction with other anticholinergic drugs; avoid co-administration
- OATP1B1/1B3 inhibitors (rifampicin, cyclosporine): Increased exposure of active metabolite; co-administration not recommended
Food interactions
Not food-related (inhalation); it is not known whether it is safe to consume alcohol.
Use in pregnancy
Use in Pregnancy: No data on use in pregnant women; advise to contact physician if pregnancy occurs; animal studies showed no evidence of fetal harm.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: No data on presence in human milk; present in milk of lactating rats; consider developmental and health benefits of breastfeeding.
Pediatric use
Safety and efficacy not established in children and adolescents under 18 years.
Geriatric use
No dose adjustment necessary for geriatric patients.
Renal / hepatic impairment
Renal Impairment: No dose adjustment required for any degree of impairment; monitor for systemic antimuscarinic adverse effects in severe renal impairment; consult your doctor.
Hepatic Impairment: Not recommended in any degree of hepatic impairment; safety not evaluated; consult your doctor.
Overdose effects
Overdose: Anticholinergic signs and symptoms (nausea, vomiting, dizziness, blurred vision, increased intraocular pressure, fatigue, difficulty voiding); treatment: symptomatic supportive care.
Storage conditions
Store below 30°C in a dry place, protected from direct sunlight; discard ampoule and other part after use; keep out of reach of children.
Chemical structure
Revefenacin