budesonide inhaled

Action and Spectrum

Actions and Spectrum: 

Mechanism of Action:  

budesonide works by reducing the inflammation in the airways. It has potent anti-inflammatory properties due to its ability to bind to glucocorticoid receptors within cells. Once bound to these receptors, budesonide regulates the transcription of various genes involved in the inflammatory response, decreasing the production of pro-inflammatory substances, such as cytokines and leukotrienes.  

Spectrum of Activity:  

budesonide has a local effect on the airways and is mainly used as an inhaled medication. Its primary therapeutic use is in the management of asthma, including both the treatment of persistent asthma and the prevention of asthma exacerbations.  

Drug Interaction

Adverse Reaction

Frequency defined 

>10% 

Rhinitis (7-12%) 

Respiratory infection (34-38%) 

Otitis media (1-12%) 

1-10% 

Nasal congestion (3%) 

Allergic rhinitis (2%) 

Nasopharyngitis (10%) 

Pharyngitis (3%) 

Viral gastroenteritis (2%) 

Black Box Warning

Black box warning: 

None 

Contraindication / Caution

Contraindications/caution: 

Contraindications: 

• Hypersensitivity: budesonide inhalation should not be used in individuals with known hypersensitivity or allergy to budesonide or any other inhaler component. Hypersensitivity reactions can range from mild skin reactions to severe allergic reactions, including anaphylaxis. 
• Active Infections: Inhaled corticosteroids like budesonide may increase the risk of respiratory infections.  

Caution: 

• Respiratory Infections: Inhaled corticosteroids, including budesonide, may enhance the risk of respiratory infections, such as bronchitis or pneumonia.  
• Immunosuppression: Inhaled corticosteroids can suppress the immune system locally in the lungs. This may increase the risk of infections, including mouth and throat fungal infections.  
• Adrenal Insufficiency: Prolonged use of high doses of inhaled corticosteroids, including budesonide, may potentially suppress the function of the adrenal glands, leading to adrenal insufficiency. Adrenal insufficiency is a condition where the body’s natural production of corticosteroids is reduced.  
• Growth Retardation in Children: Long-term use of high doses of inhaled corticosteroids, particularly in children, has been associated with a potential decrease in growth velocity. 
• Ocular Effects: In rare cases, inhaled corticosteroids is associated with an increased risk of developing cataracts or glaucoma.

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: 

budesonide exerts its therapeutic effects by binding to glucocorticoid receptors within cells. This binding leads to the modulation of gene expression and the subsequent inhibition of various inflammatory mediators. budesonide reduces the production of pro-inflammatory cytokines, such as interleukins (IL-1, IL-2, IL-4, IL-5, IL-6), tumor necrosis factor-alpha (TNF-alpha), and other substances involved in the inflammatory response. 

Pharmacodynamics: 

• Anti-inflammatory Effects: budesonide exerts its pharmacological actions by binding to glucocorticoid receptors in target cells, leading to the modulation of gene expression. This suppresses inflammatory mediators involved in the pathogenesis of respiratory diseases. 
• Reduction of Airway Hyperresponsiveness: Airway hyperresponsiveness refers to the exaggerated bronchoconstrictive response to various triggers, such as allergens or irritants. By decreasing airway hyperresponsiveness, budesonide helps to prevent and control bronchoconstriction, thus improving airflow and reducing respiratory symptoms. 
• Mucus Production: budesonide has an inhibitory effect on mucus production in the respiratory system. It reduces mucus secretion from goblet cells and decreases the thickness and viscosity of mucus.  
• Local Activity in the Respiratory System: Inhaled budesonide acts locally in the respiratory system, with minimal systemic effects when used at recommended doses. The drug is delivered directly to the airways, where it exerts its anti-inflammatory and other pharmacological effects. 

Pharmacokinetics: 

Absorption 

Bioavailability: 6 to 13% 

Peak plasma time: 1 to 2 hours  

Onset: 24 hours to 2 weeks 

Distribution 

Protein-bound: 85 to 90% (the extent to which budesonide binds to plasma proteins) 

Volume of distribution (Vd): 3 L/kg (average volume of distribution, indicating distribution throughout the body) 

Metabolism 

budesonide is metabolized in the liver by the enzyme CYP3A4. The primary metabolites of budesonide are 16-Alpha hydroxyprednisolone and 6-beta hydroxybudesonide. These metabolites have negligible glucocorticoid activity. 

Elimination and Excretion 

Half-life: 2 to 3 hours 

budesonide and its metabolites are excreted primarily through the urine (60%) and feces (40%). 

Adminstartion

Administration: 

An air compressor with sufficient airflow and a jet nebulizer with a mouthpiece or an appropriate face mask is required for suspension administration; an ultrasonic nebulizer is not recommended. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: budesonide inhaled 

Why do we use budesonide inhaled? 

budesonide inhalation is commonly used to treat respiratory conditions, particularly asthma and COPD-chronic obstructive pulmonary disease. Here are some specific uses of inhaled budesonide: 

• Asthma: budesonide inhalation is an effective controller medication for asthma. It helps reduce inflammation and swelling in the airways, making breathing easier and preventing asthma attacks. 
• Chronic Obstructive Pulmonary Disease (COPD): budesonide inhalation is also used to manage COPD, including chronic bronchitis and emphysema.  
• Allergic Rhinitis: budesonide nasal spray is sometimes prescribed for treating allergic rhinitis, commonly known as hay fever. 
• Eosinophilic Esophagitis: budesonide inhalation can be used off-label to treat eosinophilic esophagitis, a chronic inflammatory condition that affects the esophagus.