ARCAPTA NEOHALER
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ARCAPTA NEOHALER (ARCAPTA NEOHALER).
Umeclidinium is a long-acting muscarinic antagonist (LAMA) that inhibits acetylcholine at M3 receptors in bronchial smooth muscle, leading to bronchodilation. Vilanterol is a long-acting beta2-agonist (LABA) that stimulates beta2-adrenergic receptors, increasing cyclic AMP and producing bronchodilation.
| Metabolism | Umeclidinium is primarily metabolized by CYP2D6 and is also a substrate for P-glycoprotein. Vilanterol is primarily metabolized by CYP3A4. |
| Excretion | Primarily hepatic metabolism; 13.5% of the dose excreted unchanged in urine over 24 hours; 62.9% recovered in feces (mostly as metabolites). |
| Half-life | Terminal elimination half-life approximately 15-19 hours; supports once-daily dosing. |
| Protein binding | Approximately 85% bound to human plasma proteins (primarily albumin). |
| Volume of Distribution | Approximately 5.6 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Inhalation: approximately 30% systemic bioavailability; oral bioavailability negligible (<1%) due to first-pass metabolism. |
| Onset of Action | Inhalation: bronchodilation observed within 30 minutes. |
| Duration of Action | Bronchodilation maintained for 24 hours with once-daily dosing; clinically relevant over the dosing interval. |
Inhalation: 55 mcg once daily (two sprays of 27.5 mcg each).
| Dosage form | POWDER |
| Renal impairment | No dose adjustment required for renal impairment. |
| Liver impairment | No dose adjustment required for mild to moderate hepatic impairment (Child-Pugh A or B). Not studied in severe impairment (Child-Pugh C). |
| Pediatric use | Not approved for use in pediatric patients (safety and efficacy not established). |
| Geriatric use | No specific dose adjustment; use with caution due to potential for increased systemic exposure and reduced renal function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ARCAPTA NEOHALER (ARCAPTA NEOHALER).
| Breastfeeding | No human data on excretion in breast milk. M/P ratio unknown. Beclomethasone dipropionate is excreted in milk of lactating rats. Caution should be exercised when administered to nursing women; consider developmental and health benefits of breastfeeding along with mother’s clinical need and potential adverse effects on breastfed child. |
| Teratogenic Risk | FDA Pregnancy Category C. In animal studies, inhaled beclomethasone dipropionate (the active ingredient) caused teratogenic effects at doses less than the maximum recommended human daily inhalation dose. No adequate and well-controlled studies in pregnant women. Risk cannot be ruled out; should be used during pregnancy only if potential benefit justifies potential risk to the fetus. First trimester: potential for malformations, though data limited. Second and third trimesters: risk of fetal adrenal suppression with prolonged use. |
■ FDA Black Box Warning
LABA use increases the risk of asthma-related death. ARCAPTA NEOHALER is not indicated for asthma.
| Serious Effects |
["Hypersensitivity to umeclidinium, vilanterol, or any ingredient.","Use of LABA in asthma without concomitant ICS.","Severe hypersensitivity to milk proteins."]
| Precautions | ["LABA increases risk of asthma-related death (not approved for asthma).","Paradoxical bronchospasm.","Cardiovascular effects (e.g., increased heart rate, hypertension).","Worsening of narrow-angle glaucoma.","Urinary retention.","Hypersensitivity reactions."] |
| Food/Dietary | No specific food interactions. Avoid excessive caffeine or stimulants as they may increase cardiovascular side effects. |
Loading safety data…
| Fetal Monitoring | Monitor maternal respiratory status (peak expiratory flow, FEV1, symptoms). Monitor for signs of adrenal insufficiency in the neonate if mother used high doses during pregnancy. Assess fetal growth and development via ultrasound if prolonged use. |
| Fertility Effects | No human data on fertility. In animal studies, no impairment of fertility was observed with inhaled beclomethasone dipropionate at doses up to 16 times the maximum recommended human daily inhalation dose. |
| Clinical Pearls | Arcapta Neohaler (indacaterol) is a once-daily long-acting beta2-agonist (LABA) for maintenance treatment of COPD. It should not be used for acute bronchospasm. Administer via the Neohaler device only; capsules are for inhalation and should not be swallowed. Monitor for paradoxical bronchospasm, cardiovascular effects (tachycardia, hypertension), and hypokalemia. Educate patients that it is not a rescue inhaler. |
| Patient Advice | Use exactly as prescribed; do not exceed one capsule daily. · Do not use for sudden breathing problems; have a rescue inhaler (e.g., albuterol) available. · Swallow the capsule? No! Insert into Neohaler, pierce, and inhale deeply. · Rinse mouth with water after each use to prevent thrush. · Store capsules in blister pack; remove only before use. · Seek medical help if symptoms worsen or you have chest pain, fast heartbeat, or allergic reactions. |