Beclomethasone Oral Inhalation

Pharmacology: Has potent anti-inflammatory effect on respiratory tract and in nasal passages. 

Pharmacokinetics

Absorption

Rapidly absorbed. 

Oral  inhalation

Systemic bioavailability  from lungs is about 20%. 

Nasal inhalation:  Primarily deposited in  the nasal passage; majority of the drug is eventually swallowed. Bioavailability following administration is 44%. 

Distribution: 87% protein bound. 

Metabolism: Metabolized to beclomethasone 17-monopropionate (active) and free beclomethasone (very weak activity). 

Elimination:  Primarily excreted in feces. Less than 10% excreted in urine. The t ½  is 2.8 h for beclomethasone 17-monopropionate. 

Onset: Within 24 h (oral inhalation). Within 3 days (nasal inhalation) 

Indications and Usage:  Oral inhalation 

Maintenance prophylactic treatment  of asthma in patients 5 yr of age  and older;  asthma patients requiring systemic corticosteroid administration  in which adding an inhaled corticosteroid may reduce or eliminate need for systemic  corticosteroids.

Nasal inhalation: Relief of symptoms of seasonal or perennial allergic and nonallergic rhinitis; prevention of recurrence of nasal polyps following surgical removal. 

Contraindications 

Oral inhalation:  Primary treatment of status asthmaticus  or acute episodes of asthma; hypersensitivity  to any of the ingredients. 

Nasal inhalation:  Standard considerations. 

Dosage and Administration: 

Bronchial Asthma 
Adults and children 12 yr  of age and older 

PO Oral inhalation If previous therapy consisted of bronchodilators alone, start  with 40  or 80 mcg twice daily (max dose, 320 mcg twice daily); if previous therapy consisted of inhaled corticosteroids, start with 40  to 160 mcg twice daily (max dose, 320 mcg twice daily). 

Children 5  to 11 yr of age 

PO Oral inhalation If previous therapy consisted of bronchodilators alone or inhaled corticosteroids, start with 40 mcg twice daily (max dose, 80 mcg twice daily). 

Seasonal or Perennial Allergic and Nonallergic Rhinitis; Prevention of Recurrence of Nasal Polyps after Surgical Removal 

Adults and Children 12 yr of age and older 

Nasal inhalation 1 or 2 inhalations (42  to 84 mcg) in each nostril twice daily (168 to 336 mcg/day). 

Children 6 to 12 yr of age 

Nasal inhalation 1 inhalation in each nostril twice daily (168 mcg/day). Patients not adequately responding or those with more severe symptoms may use 2 inhalations in each nostril twice daily (336 mcg/day). Once adequate control is achieved, decrease dose to 1 inhalation in each nostril twice daily (168 mcg/day). Max total daily dosage should not exceed 2 sprays in each nostril twice daily (336 mcg/day). 

General Advice 

• If patient is also receiving a bronchodilator by inhalation, administer bronchodilator 5 min before beclomethasone to enhance penetration of latter drug into bronchial tree. 
• Oral inhalation 
• Have patient place inhaler in mouth and close  lips around mouthpiece, keeping tongue below  mouthpiece. Tilt patient's head back slightly. Instruct patient to take  a slow, deep breath while inhaler  is being activated and  to hold breath for 5  to 10 sec, and then breathe out slowly. A spacing device (eg, Aerochamber ) may  be used to enhance delivery of medication. Have patient rinse mouth after inhalations are complete. 
• The aerosol is  for oral inhalation only. Avoid spraying into  the nose or eyes. 
• Aerosol does not need to be shaken before use. 
• Test aerosol by spraying  2 times into  the air before using the first time and/or when the  inhaler has not been used for more than 10 days. 
• Nasal inhalation 
• If excessive nasal mucous secretion or edema are present, nasal inhalation may not reach intended site of action. In such cases, it may be necessary to use a nasal vasoconstrictor during first 2 or 3 days of therapy with nasal spray. 
• The nasal spray should be shaken  well before use. 

Storage/Stability

Oral inhalation: Store at 59° to 86°F  on the concave end of the canister with the plastic actuator on top. For optimal results, canister should be at room temperature when used. Do not use actuator with any other inhalation drug product. Do not puncture canister or use near heat or open flame or discard into fire or incinerator. Nasal inhalation: Store between 59° and 86°F. 

Drug Interactions:  None well documented. 

Laboratory Test Interactions: None well documented. 

Adverse Reactions: CNS 

Oral inhalation:  Headache (at least 3%). 

Nasal inhalation:  Headache, light-headedness (less than 5%). 

EENT 
Oral inhalation 

Pharyngitis, rhinitis, sinusitis (at least 3%). 

Nasal inhalation:  Nasopharyngeal irritation (24%); sneezing attacks (4%); nasal stuffiness, nosebleeds, rhinorrhea, tearing eyes (less than 3%); dryness, irritation of  the nose and throat, unpleasant taste and smell. 

GI
Oral inhalation 

Nausea (at least 3%). 

Nasal inhalation 

Nausea (less than 5%). 

Genitourinary 
Oral inhalation 

Dysmenorrhea (1% to 3%). 

Metabolic: Suppression of hypothalamic-pituitary-adrenal (HPA) function. 

Respiratory 
Oral inhalation 

Increased asthma symptoms, upper respiratory tract infections (at least 3%); coughing (1% to 3%). 

Miscellaneous:  Growth velocity reduction  in children; rare cases  of immediate  and delayed hypersensitivity reaction with angioedema, bronchospasm, rash,  and urticaria; weight gain. 

Oral inhalation:  Back pain, dysphonia, oral symptoms, pain (at least 3%). 

Precautions 

Monitor: If change  is made from systemic (oral) corticosteroids  to inhaled or intranasal corticosteroids, observe patient carefully for signs  of adrenal insufficiency (eg, depression, dizziness, fatigue, hypotension, nausea, or abdominal, joint, or muscle pain). Deaths caused by adrenal insufficiency have occurred during  and after conversion to aerosol corticosteroids. If nasal spray is used for several months  or longer, periodically examine for changes in the nasal mucosa. 

Pregnancy: Category C . 

Lactation: Undetermined. Because other corticosteroids are excreted in human milk, use caution. 

Children: Safety and efficacy in children younger than 5 yr of age not established (oral inhalation). Safety and efficacy in children younger than 6 yr of age not established (nasal inhalation). Corticosteroids may suppress growth in children and adolescents, particularly  with higher doses over extended periods. 

Hypersensitivity:  Immediate  and delayed hypersensitivity reactions have occurred. 

Acute asthma:  Not indicated for relief of bronchospasm. 

Fungal infections:  Antifungal treatment  or discontinuance of corticosteroid therapy may be necessary. 

Immunology: Patients receiving immunosuppressant agents are more susceptible to infections than healthy adults.  If a patient is exposed  to measles  or chickenpox, appropriate prophylaxis and treatment  may be indicated. 

Systemic effects:  Use cautiously in patients taking daily or alternate-day prednisone; may increase likelihood  of HPA function suppression. Exceeding recommended dose may cause systemic effects. 

Transfer: Use extreme caution when transferring patient  from systemic corticosteroid to less systemically available inhaled corticosteroid because death caused by adrenal insufficiency has occurred in asthmatic patients. 

Wound healing:  Patients who have experienced recent nasal septal ulcers, nasal surgery, or nasal trauma should  not use a nasal corticosteroid until healing has occurred. 

Patient Information 

• Advise patient to read the patient information leaflet before starting therapy and again with each refill. 
• Warn patient that drug is an asthma controller and is not to be used to treat an acute asthma attack. Patient must use rescue medication (bronchodilator) to obtain rapid relief of asthma symptoms. 
• Instruct patient to carry medical identification (eg, card, bracelet) if experiencing acute, severe asthma attacks requiring rapid systemic treatment. 
• Advise patient to continue taking other medications for asthma as prescribed by health care provider. 
• Review proper administration technique. Have patient demonstrate technique. 
• Advise patient to rinse mouth with water after inhalations are complete. Instruct patient to spit rinse water out and not to swallow it. 
• Advise patient to report following symptoms to health care provider: cough, dry mouth, facial swelling, rash, sore throat or mouth, worsening asthma symptoms (increasing need for bronchodilator). 
• Advise patient to notify health care provider if oral, nasal, or pharyngeal irritation occurs, or if symptoms worsen. 
• Advise patient that dose may be changed periodically depending on how well symptoms are controlled. 
• Instruct patient not to exceed prescribed dose. 
• Explain that effects of drug are not immediate. Benefit requires daily use as instructed and usually occurs after 1 to 2 days, but full relief may take 1 to 2 wk. 
• Instruct patient not to stop the medication once symptoms have been controlled. Continued daily use is necessary to control symptoms. 
• Advice patient to use nasal spray at regular intervals since effectiveness depends on regular use. 
• Advise patient not to increase dose on own and to inform health care provider if symptoms do not improve or if they worsen. 
• If patient is being converted from oral corticosteroids to inhaled corticosteroids, review signs and symptoms of adrenal insufficiency, which may occur days or wk after conversion is complete. Advise patient to carry medical identification (eg, card, bracelet) indicating that supplemental systemic corticosteroids during periods of stress or a severe asthma attack may be needed. 
• Advise patient to discard the aerosol canister when the labeled number of doses have been used. 
• Advise patient to avoid exposure to chickenpox and measles, and to seek medical advice immediately if exposed.