Generic
Revefenacin
2 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)
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.
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.
Contraindications
- Hypersensitivity to revefenacin or any component
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%)
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.
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
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.
Therapeutic class
Anticholinergic bronchodilators
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