Products
Indacaterol is commercially available as hard capsules with a powder for inhalation (Onbrez Breezhaler) and has been approved since 2010. It is also combined fixed with the LAMA glycopyrronium bromide (Ultibro Breezhaler, approved 2014). The fixed combination with mometasone furoate (Atectura Breezhaler) was registered for asthma therapy in 2020. Finally, a combination of indacaterol with glycopyrronium bromide and mometasone furoate was also registered for asthma treatment in 2020 (Enerzair Breezhaler).
Structure and properties
Indacaterol (C24H28N2O3, Mr = 392.49 g/mol) is chiral and is present in the drug as -enantiomer and indacaterol maleate, a white to light gray or light yellow powder that is sparingly soluble in water. Later, a drug containing indacaterol acetate was also approved. Indacaterol is a derivative of 8-hydroxyquinoline and 2-aminoindan and has some structural similarity to other beta2-sympathomimetics, for example, salbutamol. Indacaterol is lipophilic, which is a prerequisite for its long duration of action.
Effects
Indacaterol (ATC R03AC18) has bronchospasmolytic properties. It is an ultra-long-acting, beta2-specific sympathomimetic with relaxing effects on bronchial smooth muscle. The onset of action is rapid, within 5 minutes, and persists for a long time, during 24 hours. Indacaterol has a comparably rapid onset of action as salbutamol, but at the same time a significantly longer duration of action. It needs to be inhaled only once daily, unlike the LABA salmeterol or formoterol, which are also long-acting.
Indications
Indications depend on the drug and the combination:
- For bronchodilator maintenance therapy of airway obstruction in adults with chronic obstructive pulmonary disease (COPD).
- In combination with mometasone furoate for maintenance therapy of asthma.
Dosage
According to the professional information. The contents of the capsules are inhaled once a day and always at the same time of day. The capsules must be removed from the blister only immediately before use. They must not be swallowed!
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Indacaterol is a substrate of CYP3A4, UGT1A1, and P-glycoprotein. Drug-drug interactions have been described with the following drugs:
- Agents that prolong the QT interval.
- Sympathomimetics, MAO inhibitors, tricyclic antidepressants.
- Drugs that increase hypokalemia
- Beta-blockers
Adverse effects
The most common possible adverse effects include nasopharyngitis, upper respiratory tract infections, cough, headache, and muscle cramps.
