indacaterol
Brand: Arcapta Neohaler, Onbrez Breezhaler
Prototype: salmeterol
Drug Class: beta-2 adrenergic agonist (LABA)
Drug Family: bronchodilator
Subclass: ultra-long-acting beta-2 agonist
Organ Systems: respiratory
Mechanism of Action
Ultra-long-acting beta-2 agonist with both high intrinsic efficacy and fast onset; activates beta-2 receptors in bronchial smooth muscle to stimulate adenylyl cyclase, elevating cAMP and causing sustained bronchodilation for 24 hours.
beta-2 adrenergic receptors (bronchial smooth muscle)
Indications
- COPD maintenance bronchodilator therapy (not indicated for asthma)
Contraindications
- asthma (not approved for asthma; increased asthma-related death risk as LABA monotherapy)
- acutely deteriorating COPD or as rescue therapy
- hypersensitivity to indacaterol or lactose
Adverse Effects
Common
- cough (characteristic — occurs shortly after inhalation and resolves within minutes)
- nasopharyngitis
- headache
- oropharyngeal pain
Serious
- cardiovascular effects (arrhythmia, QTc prolongation)
- paradoxical bronchospasm
- hypokalemia (high doses)
Pharmacokinetics (ADME)
| Absorption | inhaled; Cmax at 15 minutes post-dose; absolute systemic bioavailability approximately 43-45% |
| Distribution | Vd approximately 2361-2557 L; 95% protein bound |
| Metabolism | hepatic hydroxylation via CYP3A4 and CYP2D6; glucuronidation by UGT1A1 and UGT2B7 |
| Excretion | fecal (approximately 54% unchanged) and renal (approximately 2-7%) |
| Half-life | approximately 40-56 hours |
| Onset | 5 minutes |
| Peak | 15 minutes |
| Duration | 24 hours |
| Protein Binding | 95% |
| Vd | approximately 2361 L |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| strong CYP3A4 and P-gp inhibitors (ketoconazole, erythromycin) | may increase indacaterol AUC; increased cardiovascular adverse effects | moderate |
| non-selective beta-blockers | antagonize bronchodilatory effects | major |
| QTc-prolonging drugs | additive QTc prolongation risk | moderate |
Nursing Considerations
- Administer once daily at the same time each day; instruct patients to pierce the capsule in the Neohaler device and inhale rapidly and deeply through the device — do not swallow capsules.
- Warn patients that a characteristic cough occurs within 15 seconds of inhalation in many patients; this brief cough does not indicate therapeutic failure and typically resolves within 15 minutes.
- Indacaterol is not approved for asthma in the United States; confirm the diagnosis is COPD before prescribing; have a SABA rescue inhaler available for acute symptoms.
- Monitor heart rate and QTc interval, particularly in patients with pre-existing cardiac conditions; reassess at each visit whether bronchodilator therapy remains adequate for symptom control.
Clinical Pearls
- Indacaterol's rapid onset (5 minutes) is unusual for a LABA and approaches the speed of a SABA, making it preferred over other once-daily LABAs when patients need both rapid relief and sustained bronchodilation in COPD.
- The post-inhalation cough associated with indacaterol is due to transient sensory nerve stimulation in the upper airway and does not represent bronchospasm or inadequate drug delivery; patient education prevents unnecessary discontinuation.
Safety Profile
Pregnancy use-with-caution
Lactation use-with-caution
Renal Adjustment Not required
Hepatic Adjustment Required
TDM Not required
Concordance Terms
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