Usage
- Medical Conditions: Glycopyrronium + Indacaterol + Mometasone is prescribed as a maintenance treatment for asthma in adult patients not adequately controlled with a maintenance combination of a long-acting beta2-agonist (LABA) and a medium or high dose of an inhaled corticosteroid (ICS) who experienced one or more asthma exacerbations in the previous year. It is not for the relief of acute bronchospasm or asthma attacks.
- Pharmacological Classification: This drug is a combination product containing a LABA (indacaterol), a long-acting muscarinic antagonist (LAMA) (glycopyrronium), and an ICS (mometasone furoate).
- Mechanism of Action: Indacaterol, a LABA, relaxes bronchial smooth muscle by stimulating beta2-adrenergic receptors. Glycopyrronium, a LAMA, blocks the bronchoconstricting effects of acetylcholine by antagonizing muscarinic receptors. Mometasone, an ICS, exerts anti-inflammatory effects by binding to glucocorticoid receptors, reducing airway inflammation and hyperresponsiveness.
Alternate Names
- International Nonproprietary Name (INN): indacaterol/glycopyrronium/mometasone furoate
- Brand Name(s): Enerzair Breezhaler, Zimbus Breezhaler
How It Works
- Pharmacodynamics: The combination of the three drugs provides bronchodilation (indacaterol and glycopyrronium) and reduces airway inflammation (mometasone).
- Pharmacokinetics:
- Absorption: All three components are absorbed into the systemic circulation after inhalation. However, due to the targeted delivery to the lungs and subsequent metabolism, plasma concentrations achieved after inhaled dosing are low.
- Metabolism: Indacaterol is primarily metabolized by CYP3A4. Glycopyrronium undergoes minimal metabolism. Mometasone is extensively metabolized.
- Elimination: All three components are eliminated through a combination of renal and hepatic pathways.
Dosage
Standard Dosage
Adults:
- One capsule inhaled once daily using the Breezhaler inhaler device.
- The maximum recommended dose is 114 mcg indacaterol/46 mcg glycopyrronium/136 mcg mometasone furoate once daily.
- Administer at the same time each day.
Children:
- Not recommended for use in patients under 18 years of age. Safety and efficacy have not been established in this population.
Special Cases:
- Elderly Patients: No dose adjustment is required.
- Patients with Renal Impairment: No dose adjustment is required in mild to moderate renal impairment. Caution is advised in patients with severe renal impairment.
- Patients with Hepatic Dysfunction: No dose adjustment is specifically recommended, but caution is advised due to the potential for altered drug metabolism.
- Patients with Comorbid Conditions: Caution should be exercised in patients with cardiovascular disease, diabetes, glaucoma, seizures, hypokalemia, hyperthyroidism, pulmonary tuberculosis, or chronic/untreated infections.
Clinical Use Cases
- The drug is not indicated for use in intubation, surgical procedures, mechanical ventilation, the intensive care unit (ICU), or emergency situations like cardiac arrest or status epilepticus.
Dosage Adjustments
- Dose adjustments may be necessary based on individual patient response and tolerability.
Side Effects
Common Side Effects:
- Nasopharyngitis
- Upper respiratory tract infection
- Headache
- Cough
- Hoarseness
- Dry throat
- Oral candidiasis (thrush)
Rare but Serious Side Effects:
- Hypersensitivity reactions (e.g., angioedema, urticaria)
- Paradoxical bronchospasm
- Cardiovascular effects (e.g., tachycardia, palpitations, arrhythmias)
- Pneumonia
- Hyperglycemia
- Hypokalemia
- Glaucoma or cataracts
- Immunosuppression
Contraindications
- Hypersensitivity to indacaterol, glycopyrronium, mometasone, or any of the excipients.
Drug Interactions
- Beta-blockers: May antagonize the bronchodilatory effects of indacaterol. Cardioselective beta-blockers should be used with extreme caution, if at all.
- MAO inhibitors, tricyclic antidepressants, QT-prolonging drugs: Use with caution as these may potentiate the effects of indacaterol on the QT interval.
- Methylxanthines, steroids, non-potassium-sparing diuretics: May potentiate the hypokalemic effects of indacaterol.
- CYP3A4 inhibitors/inducers: May affect the metabolism of indacaterol, requiring dose adjustments.
- Other long-acting muscarinic antagonists or long-acting beta2-adrenergic agonists: Concomitant use is not recommended as it may potentiate adverse effects.
Pregnancy and Breastfeeding
- Pregnancy: Insufficient data are available to determine the safety of this drug during pregnancy. Use only if the potential benefit outweighs the potential risk to the fetus.
- Breastfeeding: It is unknown if indacaterol, glycopyrronium, or mometasone are present in human milk. Other inhaled corticosteroids similar to mometasone are transferred into human milk. A decision should be made whether to discontinue breastfeeding or discontinue/abstain from therapy, taking into account the benefit of breastfeeding for the child and the benefit of therapy for the woman.
Drug Profile Summary
- Mechanism of Action: LABA/LAMA/ICS combination providing bronchodilation and anti-inflammatory effects.
- Side Effects: Nasopharyngitis, upper respiratory tract infection, headache, cough.
- Contraindications: Hypersensitivity to any component of the drug.
- Drug Interactions: Beta-blockers, MAO inhibitors, tricyclic antidepressants, QT-prolonging drugs.
- Pregnancy & Breastfeeding: Insufficient safety data available, use with caution.
- Dosage: One inhalation once daily.
- Monitoring Parameters: Lung function (FEV1), blood pressure, heart rate, blood glucose, serum potassium, eye examinations for glaucoma/cataracts if using long-term.
Popular Combinations
- This drug itself is a triple combination, therefore adding other medications for asthma control requires careful consideration to avoid duplicate therapy or increased side effects. The use of a short-acting beta2-agonist (SABA) as needed for acute bronchospasm is appropriate.
Precautions
- Regular monitoring of asthma control is necessary.
- Do not use for acute asthma symptoms.
- Caution in patients with cardiovascular disease, diabetes, glaucoma, seizures, hypokalemia, hyperthyroidism, pulmonary tuberculosis, or infections.
- Patients with lactose intolerance should not take this drug.
FAQs (Frequently Asked Questions)
A: The recommended dosage for adults is one inhalation (one capsule via Breezhaler inhaler) once daily. Not recommended for children under 18.
Q2: Can this medicine be used to treat an acute asthma attack?
A: No, this medication is for maintenance treatment of asthma and should not be used to treat acute asthma attacks. A rescue inhaler (SABA) should be used for acute symptoms.
Q3: Are there any specific precautions for elderly patients?
A: No dose adjustment is generally necessary for elderly patients. However, they may be more susceptible to side effects and should be monitored closely.
Q4: What are the common side effects of this medication?
A: Common side effects include nasopharyngitis, upper respiratory tract infections, headache, cough, dry/sore throat, and oral thrush.
Q5: Can patients with renal or hepatic impairment use this medication?
A: No dose adjustment is needed for mild to moderate renal impairment. Caution is advised for severe renal impairment. No specific dose adjustment is recommended for hepatic impairment, but caution is advised and monitoring is recommended.
Q6: Are there any drug interactions I should be aware of?
A: Yes, this medication can interact with beta-blockers, MAO inhibitors, tricyclic antidepressants, QT prolonging drugs, and certain other asthma medications. It is important to inform your doctor of all medications you are taking.
Q7: Can this medication be used during pregnancy or breastfeeding?
A: There are limited data regarding safety during pregnancy and breastfeeding. Use only if the potential benefit outweighs the risk. Discuss with your doctor about the risks and benefits, and consider alternatives if appropriate.
Q8: What should I do if I miss a dose?
A: Inhale the missed dose as soon as possible, but do not take more than one dose in a day. Return to your regular dosing schedule the next day.
Q9: Can I stop taking this medication if my asthma symptoms improve?
A: Do not stop taking this medication or any other asthma controller medications without consulting your doctor. Stopping this medication abruptly can worsen asthma symptoms.
