Usage
Indacaterol + Mometasone is prescribed for the maintenance treatment of asthma in adults and adolescents 12 years and older whose asthma is not adequately controlled with inhaled corticosteroids and short-acting beta2-agonists and who experienced one or more asthma exacerbations in the previous year. It is not indicated for the relief of acute bronchospasm (i.e., a sudden asthma attack).
Pharmacological Classification:
This drug is a combination product containing:
- Indacaterol: Long-acting beta2-adrenergic agonist (LABA)
- Mometasone: Inhaled corticosteroid (ICS)
Mechanism of Action:
Indacaterol relaxes the muscles of the small airways in the lungs, making breathing easier. Mometasone reduces inflammation (swelling and irritation) in the airways. Together, these two actions help to prevent and control asthma symptoms.
Alternate Names
International and regional variations may exist.
Brand Names: Atectura Breezhaler, Enerzair Breezhaler (when combined with glycopyrronium).
How It Works
Pharmacodynamics:
- Indacaterol: Stimulates beta2-adrenergic receptors, leading to bronchodilation (relaxation of airway smooth muscle). This increases airflow to the lungs. The onset of action is rapid (within 5 minutes), and the effect lasts for 24 hours.
- Mometasone: Exhibits anti-inflammatory effects by binding to glucocorticoid receptors in the airways, reducing swelling, mucus production, and airway hyperresponsiveness.
Pharmacokinetics:
- Indacaterol: Administered via inhalation. Peak plasma concentrations are reached in approximately 15 minutes. Metabolized primarily by UGT1A1. Eliminated through renal and fecal routes.
- Mometasone: Administered via inhalation. Peak plasma concentrations are reached in approximately 1 hour. Metabolized by CYP3A4. Eliminated through hepatic and renal routes.
Receptor Binding/Enzyme Inhibition/Neurotransmitter Modulation:
- Indacaterol: Beta2-adrenergic receptor agonist.
- Mometasone: Glucocorticoid receptor agonist.
Elimination Pathways:
- Indacaterol: Renal/hepatic excretion, metabolism by UGT1A1.
- Mometasone: Hepatic/renal excretion, metabolism by CYP3A4.
Dosage
Standard Dosage
Adults:
One capsule inhaled once daily using the Breezhaler inhaler. Administer at the same time each day.
Available strengths (indacaterol/mometasone):
- 150 mcg / 80 mcg
- 150 mcg / 160 mcg
- 150 mcg / 320 mcg
The appropriate strength depends on asthma severity.
Children:
Not recommended for children under 12 years of age.
Special Cases:
- Elderly Patients: No dose adjustment required.
- Patients with Renal Impairment: No dose adjustment required.
- Patients with Hepatic Dysfunction: No dose adjustment required for mild to moderate impairment. Caution is advised in patients with severe hepatic impairment. Monitor for increased systemic exposure of mometasone.
- Patients with Comorbid Conditions: Use with caution in patients with cardiovascular disorders (e.g., coronary artery disease, cardiac arrhythmias, hypertension), convulsive disorders, diabetes, hyperthyroidism, infections (e.g., tuberculosis, herpes), eye problems (e.g., cataracts, glaucoma), osteoporosis, and seizures.
Clinical Use Cases
This medication is not indicated for use in:
- Intubation
- Surgical Procedures
- Mechanical Ventilation
- Intensive Care Unit (ICU) Use
- Emergency Situations
Dosage Adjustments
Dosage adjustments may be necessary for patients with severe hepatic impairment.
Side Effects
Common Side Effects:
Headache, nasopharyngitis, upper respiratory tract infection, bronchitis, oral thrush (candidiasis), hoarseness, throat irritation, cough.
Rare but Serious Side Effects:
Worsening of asthma, pneumonia, paradoxical bronchospasm, hypersensitivity reactions (including anaphylaxis), hyperglycemia, hypokalemia, increased risk of infections, glaucoma, cataracts, osteoporosis, adrenal suppression (with long-term use).
Long-Term Effects:
Adrenal suppression, osteoporosis, growth retardation in children and adolescents.
Adverse Drug Reactions (ADR):
Severe allergic reactions (anaphylaxis), paradoxical bronchospasm.
Contraindications
Hypersensitivity to indacaterol, mometasone, milk proteins, or any component of the formulation.
Drug Interactions
- Beta-blockers: May reduce the bronchodilating effects of indacaterol. Avoid concomitant use unless absolutely necessary. If beta-blockers are required, use cardioselective beta-blockers with caution.
- CYP3A4 Inhibitors (e.g., ketoconazole, itraconazole, ritonavir): May increase systemic exposure to mometasone. Use with caution.
- Monoamine oxidase inhibitors (MAOIs), tricyclic antidepressants (TCAs), drugs that prolong the QT interval: Use with caution as they may potentiate the QT-prolonging effects of indacaterol.
- Other LABAs or LAMAs: Avoid concomitant use as it may increase the risk of adverse effects.
Pregnancy and Breastfeeding
Pregnancy: There are insufficient data on the use of Indacaterol + Mometasone during pregnancy. Use only if the potential benefit outweighs the potential risk to the fetus. Indacaterol may inhibit labor due to its relaxant effect on uterine smooth muscle.
Breastfeeding: It is unknown if indacaterol or mometasone are excreted in human milk. Consult with a physician before breastfeeding.
Drug Profile Summary
- Mechanism of Action: Indacaterol: LABA (bronchodilation). Mometasone: ICS (anti-inflammatory).
- Side Effects: Headache, nasopharyngitis, upper respiratory tract infection, oral thrush, worsening of asthma, paradoxical bronchospasm.
- Contraindications: Hypersensitivity, acute asthma attacks.
- Drug Interactions: Beta-blockers, CYP3A4 inhibitors, MAOIs, TCAs, QT-prolonging drugs, other LABAs or LAMAs.
- Pregnancy & Breastfeeding: Insufficient data for pregnancy. Unknown if excreted in breast milk.
- Dosage: One capsule inhaled once daily.
- Monitoring Parameters: Lung function (FEV1), asthma control, blood glucose levels, potassium levels, eye exams (for glaucoma/cataracts), growth in children.
Popular Combinations
No popular combinations exist. Indacaterol + Mometasone is itself a combination product. Combining it with other LABAs or LAMAs is generally not recommended.
Precautions
- General Precautions: Assess for allergies, pre-existing medical conditions (cardiovascular disease, diabetes, infections, glaucoma, osteoporosis, seizures), and concomitant medications before initiating therapy.
- Specific Populations:
- Pregnant Women: Use with caution. Potential for fetal harm. May inhibit labor.
- Breastfeeding Mothers: Unknown if excreted in breast milk. Use with caution.
- Children & Elderly: Not recommended for children under 12. No dose adjustment required for elderly patients.
- Lifestyle Considerations: Advise patients to avoid smoking and to limit alcohol intake. No specific dietary restrictions are generally necessary. No driving restrictions are typically associated with this medication.
FAQs (Frequently Asked Questions)
A: One capsule inhaled once daily using the Breezhaler inhaler. Different strengths are available depending on individual needs.
A: No, this medication is not indicated for the relief of acute bronchospasm. Patients should use a rescue inhaler (short-acting beta2-agonist) for acute asthma attacks.
A: Headache, nasopharyngitis, upper respiratory tract infection, oral thrush, hoarseness, and throat irritation.
Q4: Are there any drug interactions I should be aware of?
A: Yes, Indacaterol + Mometasone can interact with beta-blockers, CYP3A4 inhibitors, MAOIs, TCAs, QT-prolonging drugs, and other LABAs or LAMAs.
Q5: Can this medication be used during pregnancy or breastfeeding?
A: Use during pregnancy only if the potential benefit outweighs the potential risk. Consult with a physician before breastfeeding, as it’s unknown if the drug is excreted in breast milk.
Q6: How should I instruct patients to use the Breezhaler inhaler?
A: Patients should be instructed to not swallow the capsule, and to inhale rapidly and deeply through the mouthpiece to ensure delivery of medication. It is important to clean the inhaler regularly.
A: Monitor lung function, asthma control, blood glucose, potassium levels, and look out for any signs of infections, glaucoma, or cataracts. Monitor growth in pediatric patients.
Q8: Is there a risk of adrenal suppression with this medication?
A: Long-term use of inhaled corticosteroids like mometasone can lead to adrenal suppression, especially at higher doses.
Q9: Can patients stop taking this medication once their asthma is controlled?
A: No, Indacaterol + Mometasone is a maintenance medication. Patients should continue taking it regularly even when they are asymptomatic to maintain asthma control. Discontinuation should be done gradually and under the supervision of a physician.
