mometasone and indacaterol

Action and Spectrum

Actions and Spectrum: 

Mechanism of action: 

• mometasone is a synthetic corticosteroid with potent anti-inflammatory and immunosuppressive properties. It acts as a glucocorticoid receptor agonist, binding to glucocorticoid receptors inside the cells. Once activated, the glucocorticoid-receptor complex binds to specific DNA sequences, modulating the transcription of inflammatory genes.  
• indacaterol is a long-acting beta-2 adrenergic agonist (LABA) that acts on beta-2 adrenergic receptors in the airway smooth muscles. By binding to these receptors, indacaterol activates the enzyme adenylate cyclase, which leads to increased levels of cyclic adenosine monophosphate (cAMP). Elevated cAMP levels trigger a series of intracellular events that result in bronchodilation.  

Spectrum of activity: 

mometasone’s spectrum of activity is mainly focused on its anti-inflammatory effects. It is commonly used for the treatment of the following conditions: 

• Asthma: mometasone is used as an inhaled corticosteroid (ICS) in managing asthma, particularly in patients with persistent asthma. It helps reduce airway inflammation and bronchial hyperresponsiveness, improving asthma control and reducing exacerbations. 
• Allergic Rhinitis: mometasone is used as an intranasal corticosteroid for treating allergic rhinitis, including seasonal and perennial allergic rhinitis.  
• Dermatitis and Eczema: Topical mometasone formulations manage inflammatory skin conditions like dermatitis and eczema.  

indacaterol’s spectrum of activity is centered on its bronchodilatory effects. It is used in the management of chronic obstructive pulmonary disease (COPD) and, in some cases, in asthma management: 

• Chronic Obstructive Pulmonary Disease (COPD): indacaterol is indicated for the long-term maintenance treatment of COPD, including chronic bronchitis and emphysema. By providing sustained bronchodilation improves lung function, reduces symptoms like shortness of breath and cough, and enhances exercise tolerance in patients with COPD. 
• Asthma: While indacaterol is not typically a first-line treatment for asthma, it may be used as an add-on therapy for adult patients with severe asthma who require additional bronchodilation. In such cases, indacaterol is usually combined with an inhaled corticosteroid. 

Drug Interaction

Adverse Reaction

Frequency defined 

1-10% 

Hypersensitivity reaction  

Musculoskeletal pain  

Headache 

Oropharyngeal pain 

<1% 

Pruritis 

Oropharyngeal candidiasis 

Muscle spasm 

Tachycardia 

Hyperglycemia 

Angioedema 

Black Box Warning

Black box warning: 

None 

Contraindication / Caution

Contraindications/caution: 

Contraindications: 

• Hypersensitivity or Allergy: mometasone should not be used in patients with known hypersensitivity or allergy to mometasone or corticosteroids.  
• Untreated Infections: mometasone should not be applied to areas of the skin with active infections, such as bacterial, viral, or fungal infections.  
• Tuberculosis of the Skin: mometasone should not be used in patients with skin tuberculosis, as topical corticosteroids can exacerbate the condition. 
• Hypersensitivity or allergy: indacaterol should not be used in patients with known hypersensitivity or allergy to indacaterol or other long-acting beta-2 adrenergic agonists (LABAs). 
• Status Asthmaticus: indacaterol is not appropriate for treating acute episodes of bronchospasm or status asthmaticus. It is not a rescue medication and should not be used as a substitute for short-acting bronchodilators during acute asthma attacks. 
• Severe Cardiovascular Disease: indacaterol is contraindicated in patients with severe cardiovascular diseases, such as severe hypertension, cardiac arrhythmias, or coronary artery disease, as it may exacerbate these conditions. 

Caution: 

• Cardiovascular Effects: Both mometasone (a corticosteroid) and indacaterol (a long-acting beta-2 adrenergic agonist) can potentially affect the cardiovascular system.  
• Hypersensitivity and Allergic Reactions: Patients receiving a combination of mometasone and indacaterol should be closely monitored for signs of hypersensitivity reactions or allergic responses. 
• Adrenal Suppression: Systemic corticosteroids like mometasone can lead to adrenal suppression, especially when used at higher doses or for prolonged periods. When combined with indacaterol, which may also have systemic effects, the risk of adrenal suppression may be increased. 

Pregnancy / Lactation

Pregnancy consideration: Insufficient data available 

Lactation: Excretion of the drug in human breast milk is unknown 

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

• mometasone is a synthetic corticosteroid with potent anti-inflammatory and immunosuppressive properties. mometasone acts as a glucocorticoid receptor agonist, binding to glucocorticoid receptors inside cells. This activates the glucocorticoid-receptor complex, leading to the regulation of inflammatory genes. mometasone inhibits the synthesis of pro-inflammatory mediators involved in the inflammatory response, such as cytokines, chemokines, and prostaglandins. 
• indacaterol is a long-acting beta-2 adrenergic agonist (LABA) that acts as a bronchodilator. indacaterol binds to beta-2 adrenergic receptors on airway smooth muscle cells. This activation stimulates adenylate cyclase, increasing intracellular cyclic adenosine monophosphate (cAMP) levels. Elevated cAMP levels cause relaxation of airway smooth muscles, resulting in bronchodilation and improved airflow. 

Pharmacokinetics: 

Absorption 

mometasone is administered as an inhaled corticosteroid. indacaterol is administered as an inhaled long-acting beta-2 adrenergic agonist. When inhaled, it is absorbed through the airway mucosa and lung tissues, reaching the beta-2 adrenergic receptors in the bronchial smooth muscles to exert its bronchodilatory effects.  

Distribution 

After absorption, mometasone may enter systemic circulation, but its distribution is limited due to significant first-pass metabolism in the liver. Systemic levels are generally low when mometasone is used in recommended doses via inhalation. After absorption, indacaterol may enter systemic circulation, but its distribution is limited due to low oral bioavailability and significant binding to plasma proteins.  

Metabolism 

mometasone is extensively metabolized in the liver by various enzymes, mainly CYP3A4. The metabolites are primarily inactive or have reduced glucocorticoid activity. indacaterol undergoes minimal hepatic metabolism, primarily via glucuronidation. It is mainly eliminated unchanged in the feces.  

Elimination and Excretion 

Metabolites of mometasone are excreted primarily in the urine and feces. The majority of indacaterol is excreted unchanged in the feces. 

Adminstartion

Administration: 

Breezhaler inhaler  

• Prepare the Inhaler: Open the Breezhaler inhaler and load a single indacaterol capsule from the blister card. Do not remove the capsule from the blister until just before use. 
• Inhaling the Medication: Exhale fully to empty the lungs. Do not exhale into the inhaler. Close your lips tightly around the mouthpiece of the Breezhaler inhaler. 
• Inhale deeply and forcefully through the mouthpiece to pull the medication into your lungs. 
• Hold your breath for up to 5 seconds to allow the medication to reach deep into your lungs. 
• Checking for Remaining Medication: After inhaling, check the capsule to ensure it is empty. If any powder remains in the capsule, repeat the inhaling process until the capsule is empty. 
• Handling of Capsules and Inhalers: Do not push the capsule through the foil or remove the capsule from the blister until just before use. 
• Never wash the Breezhaler inhaler with water. Wipe the mouthpiece with a dry, lint-free cloth if needed. 
• Keep the inhaler dry and avoid handling capsules with wet hands. 
• Rinse Mouth After Use: After using the inhaler, rinse your mouth with water (do not swallow) to minimize the risk of oral thrush. 
• Discarding the Breezhaler Inhaler: Once all capsules have been used, discard the Breezhaler inhaler. It is designed for single use only. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: mometasone and indacaterol 

Why do we use mometasone and indacaterol? 

mometasone is a corticosteroid used for reducing inflammation, while indacaterol is a long-acting beta-agonist used as a bronchodilator to relax the airway muscles. The main uses of mometasone and indacaterol include: 

• Asthma Management: Both mometasone and indacaterol are used to manage asthma, a chronic respiratory condition characterized by airway inflammation and bronchoconstriction. mometasone reduces airway inflammation, while indacaterol provides long-acting bronchodilation, helping to control asthma symptoms and prevent exacerbations. 
• Chronic Obstructive Pulmonary Disease (COPD): mometasone and indacaterol are also used to manage COPD, a progressive lung disease involving chronic bronchitis and emphysema. Combining mometasone’s anti-inflammatory properties and indacaterol’s bronchodilation can improve lung function, reduce symptoms, and enhance exercise tolerance in patients with COPD. 
• Long-term Maintenance Therapy: Both medications are typically used as part of long-term maintenance therapy for patients with asthma or COPD to achieve optimal disease control and reduce the risk of exacerbations.