beclomethasone inhaled

Action and Spectrum

Actions and Spectrum: 

beclomethasone is a corticosteroid medication commonly used as an inhaled treatment for asthma and other respiratory conditions. When inhaled, beclomethasone acts locally in the airways to reduce inflammation and improve breathing.  

Action: 

• Anti-inflammatory: beclomethasone works by suppressing the inflammatory response in the airways. It reduces the production of inflammatory mediators, such as cytokines and leukotrienes, which contribute to the swelling and narrowing of the air passages in asthma. 
• Immunosuppressive: beclomethasone also has immunosuppressive properties, suppressing the immune response in the airways. This helps to prevent excessive immune reactions that can lead to inflammation and bronchoconstriction. 

Spectrum: 

• Prevention of Asthma Symptoms: beclomethasone is primarily used as a preventive medication for asthma. Regular use of beclomethasone inhalers can reduce the frequency and severity of asthma symptoms, including coughing, wheezing, and shortness of breath. 
• Long-Term Control: beclomethasone is considered a long-term control medication for asthma. It is not intended for immediate relief of acute asthma attacks but rather for ongoing management and prevention of symptoms. 
• Allergic and Non-Allergic Asthma: beclomethasone is effective in both allergic and non-allergic types of asthma. It helps control the underlying inflammation and reduce the hypersensitivity of the airways to various triggers, like pollen, dust mites, pet dander, or exercise. 
• Chronic Obstructive Pulmonary Disease (COPD): beclomethasone may also be prescribed to treat chronic obstructive pulmonary disease (COPD). This progressive lung condition includes chronic bronchitis and emphysema. It can help reduce inflammation and improve lung function in some individuals with COPD. 
• Other Respiratory Conditions: In addition to asthma and COPD, beclomethasone may be used to manage other respiratory conditions characterized by airway inflammation, such as bronchitis and certain forms of chronic cough. 

Drug Interaction

Adverse Reaction

Frequency defined 

>10% 

Pharyngitis (5-27%) 

URT infection (5-11%) 

Headache (8-25%) 

1-10% 

Vomiting (1.6%) 

Headache (1.6%) 

Pharyngitis (3.2%) 

Nasopharyngitis (4%) 

Viral URI (4%) 

Pyrexia (3.2%) 

Nasopharyngitis (8.8%) 

Cough (2.4%) 

URI (2.4%) 

Headache (4%) 

<1% 

Sinusitis (<1%) 

Viral URI (<1%) 

Oropharyngeal pain (<1%) 

Cough (0.8%) 

URI (0.8%) 

Rhinitis allergic (<1%) 

Pyrexia (0.8%) 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

Some common contraindications of inhaled beclomethasone: 

• Hypersensitivity: beclomethasone inhalers should not be used in individuals with known hypersensitivity or allergy to beclomethasone or any other component of the medication. Allergic reactions may include skin rash, itching, swelling, or difficulty breathing. 
• Active Tuberculosis (TB): beclomethasone should not be used during active tuberculosis or other untreated respiratory infections. Corticosteroids can suppress the immune system, potentially worsening the infection. 
• Fungal Infections: Inhaled corticosteroids like beclomethasone can increase the risk of developing or worsening fungal infections in the mouth (oral candidiasis or thrush) or throat. If someone has an active fungal infection, treating it before starting beclomethasone or using additional medications to prevent or manage the infection may be necessary. 
• Untreated Infections: beclomethasone should not be initiated during an untreated bacterial, viral, or parasitic infection, as corticosteroids can mask or exacerbate the symptoms of the infection. 
• Diabetic Ketoacidosis: beclomethasone inhalers should be used with caution in individuals with diabetes, particularly during episodes of diabetic ketoacidosis. Corticosteroids can affect blood glucose levels, so careful monitoring is important. 
• Systemic Effects: Inhaled beclomethasone has fewer systemic effects than oral corticosteroids, but it may still have some effects on the whole body when used in high doses for a long duration. These effects may include adrenal suppression, bone loss, decreased growth velocity in children, and increased susceptibility to infections. Close monitoring and appropriate dosage adjustments are essential when using high-dose or long-term beclomethasone therapy. 

Caution 

Certain cautions associated with inhaled beclomethasone: 

• Local Effects: Inhaled corticosteroids like beclomethasone can cause local side effects in the mouth and throat, such as oral candidiasis (thrush) or hoarseness. To minimize the risk of these side effects, it’s important to rinse the mouth with water after each use and spit it out. A spacer device can also help deliver the medication directly to the lungs, reducing the amount reaching the mouth and throat. 
• Systemic Effects: Although inhaled beclomethasone has fewer systemic effects than oral corticosteroids, high doses or long-term use can still increase the risk of systemic effects. These may include adrenal suppression (reduced production of natural steroid hormones by the adrenal glands), decreased bone mineral density, cataracts, and glaucoma.  
• Growth in Children: Inhaled corticosteroids, including beclomethasone, may affect children’s growth. It’s important to monitor children’s growth using beclomethasone long-term and consider alternative treatment options if there are concerns about growth suppression. 
• Interactions with Other Medications: beclomethasone may interact with certain medications, such as other corticosteroids, ketoconazole, ritonavir, and some HIV medications. It’s important to inform the healthcare professional about all medications, including over-the-counter drugs and supplements, to ensure no potential interactions. 
• Adrenal Insufficiency: Prolonged use of high doses of inhaled corticosteroids, including beclomethasone, may lead to adrenal insufficiency. This is more likely to occur when high doses are used for extended periods and in stress, trauma, or surgery situations. In such cases, additional systemic corticosteroid coverage may be required. 
• Eye Conditions: beclomethasone should be used cautiously in individuals with eye conditions, such as cataracts or glaucoma, as corticosteroids can potentially worsen these conditions. Regular eye examinations may be recommended in these cases. 

Pregnancy / Lactation

Pregnancy consideration:  

AU TGA pregnancy category: B3
US FDA pregnancy category: Not assigned. 

Lactation:   

Excreted into human milk: Not known. 

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: 

When administered via inhalation, beclomethasone exerts its pharmacological effects through local action in the respiratory system. It is a synthetic corticosteroid with potent anti-inflammatory properties. Upon inhalation, beclomethasone diffuses into the airways and binds to glucocorticoid receptors present in the target cells, leading to the activation or repression of specific genes. This suppresses inflammatory mediators, such as cytokines and leukotrienes, thereby reducing airway inflammation. 

Pharmacodynamics: 

Mechanism of action: The action occurs as a potent glucocorticoid; it exhibits strong anti-inflammatory properties by suppressing inflammatory cells and releasing inflammatory mediators. 

Pharmacokinetics: 

Absorption 

The bioavailability, or the percentage of the substance that reaches the systemic circulation, is 20%. The onset of action may occur within 24 hours of initiating the treatment, with the expected timeframe being the first or second week. However, the maximum therapeutic benefit is not anticipated until 3 to 4 weeks into the treatment. The duration of action is 6 hours. The peak plasma concentration, which represents the highest level of the substance in the bloodstream, is measured at 88 pg/mL. The peak plasma concentration is significantly higher for the specific compound BDP (beclomethasone dipropionate), reaching 6635 pg/mL. It takes to reach the highest plasma concentration for BDP is 2 minutes. Additionally, the active metabolite of the substance demonstrates a peak plasma concentration of 1464 pg/mL, reached after approximately 10 minutes. 

Distribution 

The drug substance exhibits high protein binding, with approximately 94-96% binding to proteins. This binding occurs over a 1000-5000 pg/mL concentration range. 

Metabolism 

the major metabolites are produced through the action of esterases, specific enzymes responsible for breaking down esters. These major metabolites include beclomethasone-17-mono propionate (17-BMP), beclomethasone-21-mono propionate (21-BMP), and beclomethasone (BOH). 

The prodrug occurs rapidly through hydrolysis, facilitated by the action of enzymes, resulting in the formation of the active monoester, 17-BMP. The liver assumes a crucial role in the metabolism of this substance, specifically through the involvement of the enzyme CYP450-3A. 

Elimination and Excretion 

The half-life, or the time it takes for half of the substance to be eliminated, is 30 minutes, while 17-BMP has a half-life of 2.8 hours. On the other hand, the beclomethasone has a half-time of 4 hours. Excretion, the primary route of elimination, occurs primarily through the feces, with a smaller percentage excreted in the urine (less than 10%). 

Adminstartion

Administration: 

Oral administration 

beclomethasone inhalers are typically administered using an inhalation device called an “inhaler” or a “metered-dose inhaler (MDI). 

• Shake the Inhaler: Before using the inhaler, shake it gently to ensure the medication is properly mixed. 
• Prepare the Inhaler: Remove the cap from the inhaler mouthpiece and ensure it is clean and free from debris. If it is a new inhaler or has not been used for a while, you may need to prime it according to the manufacturer’s instructions. 
• Breathe Out: Exhale fully to empty your lungs. 
• Position the Inhaler: Hold the inhaler upright with your index finger and thumb on the bottom. Alternatively, you can use a spacer device, which attaches to the inhaler and helps to deliver the medication effectively. 
• Form a Seal: Place the mouthpiece between your teeth, ensuring a tight seal around it with your lips.  
• Start Inhaling: While pressing down firmly on the top of the inhaler, start inhaling slowly and deeply through your mouth. This should be done simultaneously by activating the inhaler, which releases the medication. If you use a spacer device, press down on the inhaler and then inhale through the spacer. 
• Breathe In Slowly: Continue inhaling slowly until your lungs are full. This allows the drug to reach deep into your lungs. 
• Hold Your Breath: Once you have inhaled fully, remove the inhaler from your mouth (or stop inhaling through the spacer) and hold your breath for about 10 seconds, or as long as it is comfortable. 
• Exhale Slowly: Finally, exhale slowly and gently from the inhaler. 
• Repeat if Necessary: If your healthcare professional has prescribed more than one puff, wait for the recommended interval (usually 30 seconds to 1 minute) before repeating the process. 
• Rinse Your Mouth: After using the inhaler, it is important to rinse your mouth with water and spit it out. This helps reduce the risk of oral candidiasis (thrush) and other potential side effects. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: beclomethasone, inhaled 

Pronounced: [ be-kloe-METH-a-sone ] 

Why do we use beclomethasone, inhaled? 

beclomethasone inhalers are primarily used to treat and manage various respiratory conditions, particularly asthma. Here are some common uses of inhaled beclomethasone: 

• Asthma: beclomethasone is widely prescribed as a controller medication for asthma. It helps to reduce airway inflammation, prevent asthma symptoms, and improve overall lung function. It is typically used as a long-term maintenance therapy to manage and control persistent asthma. 
• Allergic Rhinitis: beclomethasone inhalers can also treat allergic rhinitis, commonly known as hay fever. It helps to reduce nasal inflammation, congestion, and other allergy symptoms associated with allergic rhinitis. 
• Chronic Obstructive Pulmonary Disease: In certain cases, beclomethasone might be used to treat chronic obstructive pulmonary disease. It can help reduce airway inflammation and improve symptoms like coughing and shortness of breath. 
• Exercise-Induced Bronchoconstriction: People who experience exercise-induced bronchoconstriction, also known as exercise-induced asthma, may benefit from using beclomethasone inhalers. It can help prevent or minimize airway narrowing and symptoms triggered by physical exertion. 
• Other Respiratory Conditions: beclomethasone inhalers may treat other respiratory conditions, such as bronchitis, chronic cough, and certain forms of interstitial lung diseases to which airway inflammation contributes.