beclomethasone, intranasal

Action and Spectrum

Actions and Spectrum: 

The mechanism of action of beclomethasone involves its anti-inflammatory and immunosuppressive effects. 

• Anti-inflammatory Effects: It acts by binding to glucocorticoid receptors present in the nasal mucosal cells. Once bound to these receptors, it regulates the transcription of several genes involved in the inflammatory response. This leads to decreased production and release of pro-inflammatory cytokines and mediators, such as histamine, leukotrienes, and prostaglandins. By suppressing inflammation in the nasal passages, beclomethasone reduces the swelling, redness, and congestion associated with allergic rhinitis and other nasal conditions. 
• Immunosuppressive Effects: It has immunosuppressive properties, which can dampen the immune response. This action helps to decrease hypersensitivity reactions to allergens, preventing the exaggerated immune response that leads to symptoms like sneezing, itching, and a runny nose in allergic rhinitis. 

Drug Interaction

Adverse Reaction

Frequency defined 

>10% 

Nasopharyngeal irritation (24%) 

1-10% 

Nausea (<5%) 

Sneezing attacks after administration (4%) 

Nose bleeds (<3%) 

Increased lacrimation (<3%) 

Epistaxis (<3%) 

Headache (<5%) 

Lightheadedness (<5%) 

Nasal congestion (<3%) 

Rhinorrhea (<3%) 

Frequency Not Defined 

Nasal septum perforation 

Nasal mucosa ulceration 

Black Box Warning

Black box warning: 

None 

Contraindication / Caution

Contraindications/caution: 

Contraindications: 

• Hypersensitivity: Individuals with known hypersensitivity or allergy to beclomethasone or other corticosteroids should not use this medication. 
• Active Nasal Infections: beclomethasone should not be used in individuals with active untreated nasal infections, as it may worsen or interfere with the body’s immune response. 
• Untreated Fungal Infections: If there is evidence of untreated fungal infections in the nasal passages, intranasal corticosteroids like beclomethasone should be avoided, as they may exacerbate the infection. 
• Recent Nasal Surgery or Injury: beclomethasone should be used cautiously in individuals who have recently undergone or experienced nasal injury, as it may interfere with wound healing. 
• Tuberculosis: Intranasal corticosteroids should not be used in patients with active or latent tuberculosis (TB) unless there is adequate anti-TB treatment, as corticosteroids can suppress the immune system and potentially worsen TB. 
• Children Under 6 Years: The safety and efficacy of beclomethasone in children under 6 years of age have not been established, so its use in this age group may not be recommended. 

Caution: 

• Local Effects: beclomethasone is a corticosteroid, and like all steroids, it can have local effects on the nasal mucosa. Prolonged or excessive use of intranasal corticosteroids may cause nasal irritation, dryness, and sometimes nasal bleeding.  
• Systemic Absorption: While intranasal corticosteroids like beclomethasone primarily act locally in the nasal passages, some medications can be absorbed into the bloodstream. In some cases, systemic absorption can lead to systemic corticosteroid effects, mainly if higher doses are used for an extended period.  
• Immunosuppression: Corticosteroids, including beclomethasone, have immunosuppressive effects, which can suppress the immune system.  
• Cataracts and Glaucoma: Prolonged use of intranasal corticosteroids may be 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: 

The pharmacology of beclomethasone intranasal: 

• Anti-inflammatory Effects: beclomethasone is a synthetic glucocorticoid, a type of corticosteroid that mimics the action of natural cortisol produced by the body. When administered intranasally, beclomethasone binds to glucocorticoid receptors in the nasal mucosal cells. 
• Inhibition of Pro-inflammatory Mediators: Once bound to these receptors, beclomethasone regulates the transcription of several genes involved in the inflammatory response. It inhibits the expression of pro-inflammatory cytokines (e.g., interleukins, tumor necrosis factor-alpha) and other inflammatory mediators (e.g., histamine, leukotrienes, prostaglandins). 
• Reduction of Vasodilation and Vascular Permeability: By suppressing the production and release of inflammatory mediators, beclomethasone reduces vasodilation (dilation of blood vessels) and vascular permeability in the nasal mucosa. This action decreases nasal congestion and fluid leakage into the tissues, relieving nasal swelling and runny nose. 
• Modulation of Immune Response: beclomethasone has immunosuppressive properties, which can dampen the immune response. It inhibits the activation and migration of immune cells to the nasal mucosa, preventing the exaggerated immune response that leads to symptoms like sneezing and itching in allergic rhinitis. 
• Local action: beclomethasone intranasal acts mainly locally on the nasal mucosa, reducing the potential for systemic side effects compared to systemic corticosteroids like oral prednisone.  

Pharmacokinetics: 

Absorption 

Only about 44% of the drug is absorbed into the body when administered intranasally. Of this, 43% is absorbed through the swallowing portion of the intranasal dose (i.e., it may drip down the throat), and only 1% is absorbed through the nasal mucosa directly. After intranasal administration, the peak plasma concentration of beclomethasone is undetectable. 

Distribution 

Once absorbed into the bloodstream, approximately 87% of beclomethasone is bound to proteins in the blood. Protein binding can influence the drug’s distribution and availability for action. The apparent volume of distribution of beclomethasone is 20 liters, and for the active metabolite B-17-MP, it is 424 liters.  

Metabolism 

beclomethasone is metabolized in the body to its active metabolite B-17-MP (also known as 17-BMP or 17-beta-methylprednisolone), responsible for its anti-inflammatory effects in the nasal mucosa. beclomethasone is metabolized by esterase enzymes found in most tissues. 

Elimination and Excretion 

The half-life of beclomethasone is approximately 0.3 hours. After administration, beclomethasone is primarily excreted in the feces (60%) and the urine (12%). The fecal excretion indicates the drug’s elimination in an unchanged form and as metabolites, while the urinary excretion reflects the elimination of metabolites. 

Adminstartion

Administration: 

Intranasal administration 

Beconase AQ 

• Shake vigorously before using. 
• Before the first usage, prime the pump 6 times into the air. 
• Reprime the pump until a fine spray occurs if it hasn’t been used for 7 days. 

QNASL 

• Spray into the air four times away from your eyes to prime the pump before your first usage; the dosage meter on the canister should display 120 after priming.  
• Hold the gadget upright between your thumb and index finger, with the canister pointing down at the top.  
• Reprime the pump with two sprays if it has been seven days since usage. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: beclomethasone intranasal 

Why do we use beclomethasone intranasal? 

beclomethasone intranasal is a corticosteroid medication used for various nasal conditions, particularly inflammation associated. Its primary use is for treating allergic rhinitis, both seasonal and perennial. Here are the primary uses of beclomethasone intranasal: 

• Allergic rhinitis: beclomethasone intranasal is highly effective in managing the symptoms of allergic rhinitis, which is an inflammatory condition caused by an allergic reaction to airborne allergens like pollen, pet dander, dust mites, or mold spores. It helps reduce nasal inflammation, sneezing, itching, nasal congestion, and runny nose associated with allergic rhinitis. 
• Perennial Allergic Rhinitis: This form of allergic rhinitis occurs year-round and is usually triggered by allergens throughout the year, such as dust mites, pet dander, or mold spores. beclomethasone intranasal helps manage symptoms in individuals with perennial allergic rhinitis. 
• Seasonal Allergic Rhinitis: Seasonal allergic rhinitis, commonly known as hay fever, is triggered by allergens that are present during specific seasons, such as pollen during spring or fall. beclomethasone intranasal is effective in alleviating symptoms during the peak allergy seasons. 
• Nasal Polyps: beclomethasone intranasal may also be used to manage nasal polyps, which are small non-cancerous growths that can develop in the nasal passages. The medication helps reduce inflammation in the nasal mucosa and shrink nasal polyps, relieving nasal obstruction and congestion.