ANORO ELLIPTA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ANORO ELLIPTA (ANORO ELLIPTA).
ANORO ELLIPTA is a combination of umeclidinium, a long-acting muscarinic antagonist (LAMA), and vilanterol, a long-acting beta2-adrenergic agonist (LABA). Umeclidinium inhibits acetylcholine at M3 receptors in bronchial smooth muscle, causing bronchodilation. Vilanterol stimulates beta2-adrenergic receptors, leading to relaxation of bronchial smooth muscle and increased cyclic AMP.
| Metabolism | Umeclidinium is primarily metabolized by cytochrome P450 isoenzyme 2D6 (CYP2D6) and is a substrate of P-glycoprotein (P-gp). Vilanterol is primarily metabolized by CYP3A4. |
| Excretion | Umeclidinium: 0.7% unchanged in urine, 58% as metabolites in feces; vilanterol: 26% unchanged in urine, 70% as metabolites in feces. Total elimination: renal (30-40% for vilanterol metabolites) and fecal (primary). |
| Half-life | Umeclidinium: 11 hours (terminal); vilanterol: 2.5 hours (terminal). Steady-state achieved by day 14 once-daily dosing. |
| Protein binding | Umeclidinium: 89% bound to albumin; vilanterol: 94% bound to albumin and acid glycoprotein. |
| Volume of Distribution | Umeclidinium: 86 L (extensive tissue distribution); vilanterol: 165 L (highly distributed). Mean Vd following IV administration. |
| Bioavailability | Inhalation: 13% (umeclidinium) and 3% (vilanterol) of the metered dose. Absolute bioavailability not determined due to low systemic exposure. |
| Onset of Action | Inhalation: FEV1 improvement within 6 minutes (vilanterol), 30 minutes (umeclidinium). |
| Duration of Action | 24 hours (once-daily dosing) for both bronchodilation and symptom control, with sustained effect over 24 hours per phase III trials. |
One inhalation (umeclidinium 62.5 mcg / vilanterol 25 mcg) once daily, orally inhaled.
| Dosage form | POWDER |
| Renal impairment | No dosage adjustment required for any degree of renal impairment. |
| Liver impairment | No dosage adjustment required for mild or moderate hepatic impairment (Child-Pugh A or B). Not studied in severe hepatic impairment (Child-Pugh C); use caution. |
| Pediatric use | Not approved for pediatric use; safety and efficacy not established in children. |
| Geriatric use | No dosage adjustment required in elderly patients. Monitor for anticholinergic effects and cardiovascular events due to beta-agonist. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ANORO ELLIPTA (ANORO ELLIPTA).
| Breastfeeding | No data on presence in human milk. Umeclidinium: likely excreted; vilanterol: expected in milk. No M/P ratio available. Consider developmental benefits of breastfeeding vs. maternal need for drug and potential infant effects (e.g., tachycardia). |
| Teratogenic Risk | Pregnancy Category C. Inhaled umeclidinium/vilanterol: no adequate human studies. Animal studies show fetal harm at high systemic doses. First trimester: theoretical risk based on sympathomimetic effects. Second/third trimesters: risk of preterm labor and fetal tachycardia due to beta-agonist activity. Use only if benefit outweighs risk. |
■ FDA Black Box Warning
LABA use increases the risk of asthma-related death. ANORO ELLIPTA is not approved for asthma. In asthma patients, LABA monotherapy (without an inhaled corticosteroid) is associated with an increased risk of asthma-related death.
| Serious Effects |
["Hypersensitivity to umeclidinium, vilanterol, or any ingredient in the formulation","Asthma (without concomitant inhaled corticosteroid due to increased risk of asthma-related death)"]
| Precautions | ["Not indicated for asthma or acute deterioration of COPD","Paradoxical bronchospasm","Cardiovascular effects (e.g., increased heart rate, blood pressure, arrhythmias)","Hypersensitivity reactions including anaphylaxis, angioedema, and urticaria","Worsening of narrow-angle glaucoma","Worsening of urinary retention"] |
| Food/Dietary | No clinically significant food interactions. Avoid grapefruit juice as it may increase systemic exposure of vilanterol. |
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| Fetal Monitoring | Monitor maternal blood pressure, heart rate, and signs of preterm labor. Fetal monitoring: assess growth and heart rate via ultrasound if prolonged use. Assess for maternal hypokalemia and hyperglycemia. |
| Fertility Effects | No human data on fertility. Animal studies: no impairment with umeclidinium/vilanterol at exposures multiples of MRHD. Potential for beta-agonist-induced ovarian effects in animals, but clinical relevance unknown. |
| Clinical Pearls | ANORO ELLIPTA (umeclidinium/vilanterol) is a once-daily LAMA/LABA combination for maintenance treatment of COPD. It should not be used for acute bronchospasm. Monitor for paradoxical bronchospasm, cardiovascular effects (e.g., increased heart rate, hypertension), and anticholinergic effects (e.g., urinary retention, narrow-angle glaucoma). Assess patient's inhaler technique regularly to ensure dose delivery. Taper corticosteroids if switching from ICS. |
| Patient Advice | Use one inhalation once daily at the same time each day; do not use more often. · Do not use for sudden breathing problems; have a rescue inhaler (e.g., albuterol) available. · Rinse mouth with water after each dose to reduce dry mouth, but do not swallow. · Seek immediate medical help if symptoms worsen or if you experience chest pain, rapid heartbeat, or allergic reactions. · Avoid spraying into eyes; if contact occurs, rinse with water and seek medical attention. · Inform healthcare provider about all medications, especially other anticholinergics or beta-blockers. · Store at room temperature; keep inhaler in the sealed tray until ready to use. |