Usage
Indacaterol is prescribed for the long-term, once-daily maintenance bronchodilator treatment of airflow obstruction in patients with chronic obstructive pulmonary disease (COPD), including chronic bronchitis and/or emphysema. It belongs to the pharmacological classification of long-acting beta2-adrenergic agonists (LABA). Indacaterol relaxes the muscles in the airways, which allows them to open up and makes breathing easier.
Alternate Names
The International Nonproprietary Name (INN) is indacaterol. Brand names include Arcapta Neohaler, Onbrez Breezhaler, and Oslif Breezhaler. Indacaterol is also available in combination inhalers like Utibron Neohaler (with glycopyrrolate) and Atectura Breezhaler (with mometasone).
How It Works
Pharmacodynamics: Indacaterol acts as a selective agonist at beta2-adrenergic receptors, predominantly found in bronchial smooth muscle. Stimulation of these receptors activates intracellular signaling pathways, leading to smooth muscle relaxation and bronchodilation, improving airflow in the lungs.
Pharmacokinetics:
- Absorption: Following oral inhalation, indacaterol is absorbed through the lungs and the gastrointestinal tract. Absolute bioavailability is approximately 43-45%.
- Distribution: Data on distribution are limited.
- Metabolism: Indacaterol is primarily metabolized by uridine diphosphate glucuronosyltransferase 1 family, polypeptide A1 (UGT1A1) via glucuronidation, resulting in the formation of phenolic O-glucuronide metabolites.
- Elimination: Indacaterol and its metabolites are mainly excreted in the feces. Elimination half-life is approximately 45-57 hours. Steady-state plasma concentrations are typically reached within 12-14 days of once-daily dosing.
Dosage
Standard Dosage
Adults:
The recommended dose is 75 mcg (one capsule) inhaled orally once daily, using the Neohaler inhaler device, at the same time each day. The maximum dose is 75 mcg once daily. In some cases, 150 mcg or 300 mcg dosages (via Breezhaler inhaler) are prescribed. However, the 75 mcg dosage is more commonly used.
Children:
Use is not recommended in children under 18 years old as safety and efficacy have not been established.
Special Cases:
- Elderly Patients: No dosage adjustment is required.
- Patients with Renal Impairment: No dosage adjustment is required.
- Patients with Hepatic Dysfunction: No dosage adjustment is required for mild to moderate hepatic impairment. No data are available for severe hepatic impairment.
- Patients with Comorbid Conditions: Use with caution in patients with cardiovascular disease, diabetes, hyperthyroidism, hypokalemia, seizures, or a history of QT interval prolongation.
Clinical Use Cases
Indacaterol is not indicated for:
- Intubation
- Surgical Procedures
- Mechanical Ventilation
- Intensive Care Unit (ICU) Use
- Emergency Situations (e.g., status epilepticus, cardiac arrest).
It is specifically for the long-term maintenance treatment of COPD and is not for acute exacerbations or asthma.
Dosage Adjustments
No dose adjustment is required based on age, renal impairment, or mild to moderate hepatic impairment.
Side Effects
Common Side Effects:
- Upper respiratory tract infection (nasopharyngitis, sinusitis)
- Cough
- Headache
- Nasal congestion
- Muscle spasms
- Musculoskeletal pain
Rare but Serious Side Effects:
- Paradoxical bronchospasm
- Hypersensitivity reactions (angioedema, urticaria)
- Cardiac arrhythmias (QT prolongation)
- Worsening hypokalemia
- Hyperglycemia
Long-Term Effects:
Long-term effects are primarily related to the progression of COPD itself rather than the drug.
Contraindications
- Hypersensitivity to indacaterol or any of the excipients
- Asthma (monotherapy)
- Concomitant use with other LABAs
Drug Interactions
- Beta-blockers: May interfere with the bronchodilating effect of indacaterol and can induce bronchospasm in COPD patients.
- CYP3A4 and P-gp inhibitors (e.g., ketoconazole, ritonavir): May increase systemic exposure to indacaterol.
- Sympathomimetic agents: May potentiate adrenergic effects.
- Xanthine derivatives, steroids: May potentiate hypokalemia.
Pregnancy and Breastfeeding
- Pregnancy: Pregnancy Safety Category C. Use only if the potential benefit justifies the potential risk to the fetus. May inhibit labor due to relaxant effects on uterine smooth muscle.
- Breastfeeding: It is unknown if indacaterol is excreted in human milk. Use caution and consider the risks and benefits.
Drug Profile Summary
- Mechanism of Action: Selective beta2-adrenergic agonist, causing bronchodilation.
- Side Effects: Cough, headache, nasal congestion, upper respiratory tract infections; rarely, paradoxical bronchospasm, hypersensitivity reactions, cardiac arrhythmias.
- Contraindications: Hypersensitivity, asthma (monotherapy), concomitant LABA use.
- Drug Interactions: Beta-blockers, CYP3A4/P-gp inhibitors, sympathomimetics, xanthines, steroids.
- Pregnancy & Breastfeeding: Category C; use with caution. Excretion in breast milk unknown.
- Dosage: 75 mcg inhaled once daily.
- Monitoring Parameters: FEV1, FVC, other pulmonary function tests; serum potassium, blood glucose, blood pressure, heart rate.
Popular Combinations
Indacaterol is commonly combined with a long-acting muscarinic antagonist (LAMA), like glycopyrrolate (Utibron Neohaler) or with a corticosteroid like mometasone furoate (Atectura Breezhaler), for enhanced bronchodilation and improved COPD management.
Precautions
- General Precautions: Monitor for paradoxical bronchospasm, cardiovascular effects, and metabolic changes (potassium, glucose).
- Specific Populations: Caution in pregnancy and breastfeeding. Not recommended for children.
- Lifestyle Considerations: Advise patients about proper inhaler technique.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Indacaterol?
A: 75 mcg inhaled once daily for adults. Not recommended for children.
Q2: Can Indacaterol be used to treat asthma?
A: No, indacaterol as monotherapy is not indicated for the treatment of asthma.
Q3: What are the most common side effects of Indacaterol?
A: The most common side effects are upper respiratory tract infections, cough, headache, and nasal congestion.
Q4: Are there any serious side effects associated with Indacaterol?
A: Yes, though rare, serious side effects include paradoxical bronchospasm, hypersensitivity reactions, and cardiac arrhythmias.
Q5: Can Indacaterol be used with other COPD medications?
A: Yes, indacaterol can be combined with other COPD medications, such as LAMAs or inhaled corticosteroids, for enhanced bronchodilation. Do not use with other LABAs.
Q6: What should I do if a patient misses a dose of Indacaterol?
A: Instruct the patient to take the missed dose as soon as possible but not to exceed one dose in a 24-hour period.
Q7: How should Indacaterol be administered?
A: Indacaterol should be administered via oral inhalation using the Neohaler inhaler device. Capsules should not be swallowed.
Q8: Does indacaterol interact with any medications?
A: Yes. Clinically significant interactions include those with beta-blockers, CYP3A4/P-gp inhibitors, and sympathomimetic agents.
Q9: What are the contraindications for Indacaterol?
A: Contraindications include hypersensitivity to indacaterol, asthma (as monotherapy), and concomitant use with other LABAs.
