Indarol

• Chronic Obstructive Pulmonary Disease (COPD)
• Long-term, once-daily maintenance treatment of airflow obstruction in patients with COPD, including chronic bronchitis and/or emphysema.
• Improves lung function, reduces symptoms such as breathlessness, and enhances quality of life.
• Not for Acute Relief
• Not indicated for the relief of acute bronchospasm or sudden breathing problems.
• Asthma
• Not approved for asthma monotherapy in most regions due to safety concerns with long-acting β₂-agonists (LABAs).
• If used for asthma, it must be in combination with an inhaled corticosteroid (ICS) where approved.

Route: Inhalation only, using the specific inhaler supplied with the product.

• Adults (COPD):
• US formulation: 75 mcg once daily (Arcapta® Neohaler).
• EU/Other regions: 150 mcg or 300 mcg once daily, based on severity and tolerability.
• Pediatric use: Not established; not recommended in children.
• Elderly: No adjustment needed; monitor for cardiovascular effects.
• Renal impairment: No dose adjustment generally required.
• Hepatic impairment: Use with caution in severe impairment; no standard adjustment for mild to moderate cases.

Administration Notes:

• Use the inhaler device as instructed; do not swallow capsules.
• If a dose is missed, take as soon as remembered on the same day; do not double the dose.

Indacaterol is an ultra-long-acting β₂-adrenergic receptor agonist. It selectively stimulates β₂-receptors in bronchial smooth muscle, activating adenylate cyclase and increasing intracellular cAMP. Elevated cAMP levels relax airway smooth muscle, producing bronchodilation. Indacaterol has a rapid onset of action (within minutes) and provides sustained bronchodilation for at least 24 hours due to its high affinity and prolonged receptor binding.

• Absorption: Rapid onset with peak bronchodilation typically within 30 minutes.
• Bioavailability: Low systemic bioavailability; therapeutic action is primarily local in the lungs.
• Distribution: Moderate plasma protein binding; high lung tissue exposure.
• Metabolism: Extensively metabolized via direct glucuronidation (UGT1A1, UGT2B7, UGT2B17) and oxidative pathways involving CYP3A4.
• Elimination: Predominantly via feces; minor renal excretion.
• Half-life: Functional bronchodilation supports once-daily dosing; terminal elimination half-life ~40–52 hours.

• Pregnancy: Use only if potential benefits outweigh risks. Limited human data; animal studies show potential fetal risk at high exposures.
• Lactation: Unknown if excreted in human milk; caution advised. Monitor infants for β₂-agonist effects such as tachycardia or irritability.

• Primary: Long-acting β₂-adrenergic agonist (LABA).
• Subclass: Ultra-long-acting inhaled bronchodilator.

• Hypersensitivity to indacaterol, indacaterol maleate, or formulation components.
• Use as monotherapy in asthma (unless combined with ICS in regions where approved).
• Acute episodes of bronchospasm.

• Not for acute symptoms — always have a rescue inhaler available.
• Increased risk of asthma-related death if used without ICS in asthma patients.
• Use with caution in cardiovascular disorders, seizure disorders, thyrotoxicosis, and diabetes mellitus.
• May cause paradoxical bronchospasm — discontinue immediately if it occurs.
• Monitor potassium levels in patients at risk of hypokalemia.

Common:

• Cough
• Nasopharyngitis
• Headache
• Oropharyngeal pain
• Muscle cramps
• Tremor

Uncommon/Rare:

• Tachycardia, palpitations
• Hypersensitivity reactions (rash, urticaria, angioedema)
• Paradoxical bronchospasm
• Hypokalemia

• β-blockers: May reduce efficacy; avoid non-selective agents.
• Other adrenergic agents: Increased cardiovascular risk.
• Potassium-lowering drugs (diuretics, corticosteroids): Increased risk of hypokalemia.
• CYP3A4 inhibitors/inducers: May alter systemic exposure.
• QT-prolonging drugs: Risk of additive cardiac effects.

• Emphasis from international COPD guidelines on once-daily LABAs for maintenance therapy.
• Regulatory bodies continue to warn against LABA monotherapy in asthma.
• Indacaterol available in fixed-dose combinations with long-acting muscarinic antagonists (LAMA) in many countries for improved symptom control.

• Store at 20°C to 30°C in original packaging.
• Protect from moisture and light.
• Keep capsules in the blister until immediately before use.
• Do not freeze.
• Keep out of reach of children.