Indacaterol

Patient with CV disorders (e.g. coronary artery disease, acute MI, hypertension, cardiac arrhythmia, known or suspected QT interval prolongation); diabetes mellitus, hyperthyroidism, hypokalaemia, seizure disorder. Patients who are unusually responsive to β₂-adrenergic agonists. Not indicated for the treatment of asthma or acute bronchospastic episodes of COPD. Pregnancy and lactation.

Significant: Immediate hypersensitivity reactions (e.g. skin rash, urticaria, swelling of tongue, lips, and face, difficulty in breathing or swallowing); increased pulse rate or blood pressure, ECG changes (e.g. flattening of T wave, prolonged QT interval, ST segment depression); increased plasma glucose, exacerbation of pre-existing diabetes mellitus and ketoacidosis; hypokalaemia (usually transient).
General disorders and administration site conditions: Chest pain, peripheral oedema.
Musculoskeletal and connective tissue disorders: Muscle spasms, musculoskeletal pain.
Nervous system disorders: Headache, dizziness.
Respiratory, thoracic and mediastinal disorders: Nasopharyngitis, sinusitis, URTI, cough, rhinorrhoea, oropharyngeal pain (including throat irritation).
Skin and subcutaneous tissue disorders: Pruritus.
Potentially Fatal: Paradoxical bronchospasm.

Monitor FEV₁, forced vital capacity (FVC) and other pulmonary function tests; blood pressure, heart rate, serum glucose and potassium levels.

Symptoms: Moderately increased pulse rate, systolic blood pressure, and QT interval; headache, drowsiness, nausea, vomiting, tremor, palpitations, ventricular arrhythmias, hypokalaemia, hyperglycaemia, and metabolic acidosis.

Management: Symptomatic and supportive treatment. May consider use of cardioselective β-blockers with extreme caution.

May potentiate adverse effects with other sympathomimetic agents. Hypokalaemic effect may be potentiated by concomitant use with methylxanthine derivatives, corticosteroids or non-potassium-sparing diuretics. Antagonistic effect with β-adrenergic blockers. Increased serum concentration with inhibitors of CYP3A4 and P-glycoprotein (e.g. ketoconazole, erythromycin, verapamil, ritonavir). May increase the risk of QT interval prolongation with MAOIs, TCAs and other agents known to prolong the QT interval.

Description:
Overview: Indacaterol, a bronchodilator, is a long-acting β₂-adrenergic agonist that acts locally in the lung.
Mechanism of Action: Indacaterol relaxes the bronchial smooth muscle by selectively acting on β₂-adrenergic receptors. It stimulates the intracellular adenyl cyclase, the enzyme that catalyses the conversion of ATP to cAMP, thus increasing cAMP levels.
Pharmacodynamics: Studies have shown that indacaterol reduces both dynamic and resting lung hyperinflation, which leads to increased peak inspiratory capacity during exercise and at rest. Additionally, significant increases in resting respiratory capacity and FEV₁ were also demonstrated.
Onset: 5 minutes.
Duration: 24 hours.
Pharmacokinetics:
Absorption: Absolute bioavailability: 43-45%. Time to peak plasma concentration: Approx 15 minutes.
Distribution: Plasma protein binding: Approx 95%.
Metabolism: Metabolised in the liver by CYP3A4 (main), CYP2D6, and CYP1A1 into hydroxylated indacaterol and by UGT1A1 into phenolic O-glucuronides.
Excretion: Via faeces (>90%; 54% as unchanged drug, 23% as hydroxylated metabolites); urine (<2% as unchanged drug). Elimination half-life: 40-56 hours.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 6918554, Indacaterol. https://pubchem.ncbi.nlm.nih.gov/compound/Indacaterol. Accessed June 27, 2025.

Store below 30°C. Protect from moisture.

Antiasthmatic & COPD Preparations

R03AC18 - indacaterol ; Belongs to the class of adrenergic inhalants, selective beta-2-adrenoreceptor agonists. Used in the treatment of obstructive airway diseases.

Brayfield A, Cadart C (eds). Indacaterol. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/10/2025.

Indacaterol. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 01/10/2025.

Joint Formulary Committee. Indacaterol. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/10/2025.

Novartis New Zealand Limited. Onbrez Breezhaler 150 microgram Inhalation Powder, Hard Capsules data sheet 24 September 2020. Medsafe. http://www.medsafe.govt.nz. Accessed 01/10/2025.

Onbrez Breezhaler 150 mcg and 300 mcg Inhalation Powder Hard Capsules (Novartis Corporation [Malaysia] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 01/10/2025.

Onbrez Breezhaler 150 microgram Inhalation Powder, Hard Capsules (Novartis Pharmaceuticals UK Limited). MHRA. https://products.mhra.gov.uk. Accessed 01/10/2025.