Prevent an allergic reaction from happening at school.

Beclomethasone Dipropionate eent

Pronunciation

Class: Corticosteroids
VA Class: NT200
Molecular Formula: C28H37ClO7
CAS Number: 5534-09-8
Brands: Beconase AQ

Introduction

Synthetic corticosteroid.a

Uses for Beclomethasone Dipropionate

Seasonal and Perennial Rhinitis

Symptomatic treatment of seasonal or perennial rhinitis.103

Generally provides symptomatic relief of watery rhinorrhea, nasal congestion, sneezing (including morning sneezing attacks), and nasal and pharyngeal itching.a

Generally does not relieve signs and symptoms of conjunctivitis or those involving the lower respiratory tract (e.g., coughing), although improvement in ophthalmic and respiratory manifestations may occur.a

Slideshow: 2014 Update - First Time Brand-to-Generic Switches

Relieves symptoms in both allergic and nonallergic rhinitis, although intranasal route appears to provide greater relief in allergic rhinitis.a

Continuous concomitant therapies (e.g., oral or orally inhaled corticosteroids, bronchodilators, antihistamines, decongestants) may be required for optimum symptomatic relief, especially in patients with concurrent asthmatic conditions.a

Symptomatic relief is usually evident within several days of initiating continuous intranasal therapy; however, up to 2 weeks may be required for optimum effectiveness.a

Nasal Polyposis

Used principally to prevent nasal polyp recurrence after surgical removal.a

May delay need for subsequent surgery, but should not preclude polypectomy when polyp size prevents adequate penetration of drug into nasal passages.a

May reduce polyp size and the degree of nasal obstruction, but apparently does not alter underlying disease; manifestations usually recur when the drug is discontinued.a

Periodically monitor patients receiving prolonged intranasal corticosteroid therapy with rhinoscopic examinations, since risk for atrophic rhinitis is increased.a

Beclomethasone Dipropionate Dosage and Administration

Administration

Intranasal Inhalation

Administer by nasal inhalation only using a metered-dose nasal spray pump.103 104 a

Prime spray pump prior to initial use (6 actuations or until a fine spray appears) and after ≥7days of non-use (until a fine spray appears).104

Shake spray pump well immediately prior to use.104

Avoid contact with the eyes.104

Blow nose to clear nasal passages prior to administration.104 Adequate penetration of the drug may require a topical nasal vasoconstrictor in patients with blocked nasal passages during the first 2–3 days of therapy.103

For each inhalation, support the base of the spray bottle with the thumb and place the middle finger and forefinger on the white collar of the bottle.104 Tilt the head slightly forward, keep the bottle upright, and insert the nasal applicator into one nostril while holding the other nostril closed.104

Spray the drug into one nostril by pressing down firmly on the white collar of the bottle and concurrently inhaling gently through the nose, then exhale through the mouth.104

Repeat procedure for the other nostril.104

To clean nasal applicator, remove dust cap and safety clip and press applicator collar gently upward to free applicator.104 Wash dust cap and nasal applicator in cold water, then dry and replace applicator, safety clip, and dust cap.104

To unblock nasal applicator, remove dust cap, unscrew complete pump mechanism, and soak in warm water for a few minutes.104 Rinse with cold water, dry, replace on bottle, and reprime the pump.104

Dosage

Available as beclomethasone dipropionate monohydrate; dosage expressed in terms of the anhydrous salt.103

After initial priming, each actuation of the nasal aqueous suspension spray pump delivers a 100-mg dose of beclomethasone dipropionate suspension equivalent to 42 mcg of anhydrous beclomethasone dipropionate.103 Each 25-g spray bottle delivers 180 metered doses, after which the correct amount of drug in each spray cannot be assured.103 104 Discard the bottle after 180 sprays have been used.103 104

Adjust dosage according to individual requirements and response.a

Therapeutic effects of intranasal corticosteroids, unlike those of decongestants, are not immediate.103

Use of topical nasal decongestants or oral antihistamines may be necessary until the effects of intranasal beclomethasone dipropionate are fully manifested.103

Symptomatic relief is usually evident within several days of continuous therapy; however, up to 2 weeks may be required for relief in some patients.103

Do not continue therapy beyond 3 weeks in the absence of substantial symptomatic improvement.103

Pediatric Patients

Seasonal Rhinitis
Intranasal Inhalation

Children 6–12 years of age: Initially, 1 spray (42 mcg) in each nostril twice daily (total dosage: 168 mcg/day).103

Increase dosage to 2 sprays (84 mcg) in each nostril twice daily (total dosage: 336 mcg/day) if response is inadequate or symptoms are severe.103

Reduce dosage to 1 spray in each nostril twice daily (total dosage: 168 mcg/day) once adequate symptom control is achieved.103

Adolescents ≥12 years of age: 1 or 2 sprays (42–84 mcg) in each nostril twice daily (total dosage: 168–336 mcg/day).103

Perennial Rhinitis
Intranasal Inhalation

Children 6–12 years of age: Initially, 1 spray (42 mcg) in each nostril twice daily (total dosage: 168 mcg/day).103

Increase dosage to 2 sprays (84 mcg) in each nostril twice daily (total dosage: 336 mcg/day) if response is inadequate or symptoms are severe.103

Reduce dosage to 1 spray in each nostril twice daily (total dosage: 168 mcg/day) once adequate symptom control is achieved.103

Adolescents ≥12 years of age: 1 or 2 sprays (42–84 mcg) in each nostril twice daily (total dosage: 168–336 mcg/day).103

Nasal Polyposis
Intranasal Inhalation

Children 6–12 years of age: Initially, 1 spray (42 mcg) in each nostril twice daily (total dosage: 168 mcg/day).103

Increase dosage to 2 sprays (84 mcg) in each nostril twice daily (total dosage: 336 mcg/day) if response is inadequate or symptoms are severe.103

Reduce dosage to 1 spray in each nostril twice daily (total dosage: 168 mcg/day) once adequate symptom control is achieved.103

Adolescents ≥12 years of age: 1 or 2 sprays (42–84 mcg) in each nostril twice daily (total dosage: 168–336 mcg/day).103

Adults

Seasonal Rhinitis
Intranasal Inhalation

1 or 2 sprays (42–84 mcg) in each nostril twice daily (total dosage: 168–336 mcg/day).103

Perennial Rhinitis
Intranasal Inhalation

1 or 2 sprays (42–84 mcg) in each nostril twice daily (total dosage: 168–336 mcg/day).103

Nasal Polyposis
Intranasal Inhalation

1 or 2 sprays (42–84 mcg) in each nostril twice daily (total dose: 168–336 mcg/day).103

Prescribing Limits

No evidence that higher than recommended dosages or increased frequency of administration is beneficial.103

Exceeding the maximum recommended daily dosage may only increase the risk of adverse systemic effects (e.g., HPA-axis suppression, Cushing’s syndrome) and should be avoided.103

Pediatric Patients

Seasonal Rhinitis
Intranasal Inhalation

Children 6–12 years of age: Maximum 84 mcg (2 sprays) in each nostril twice daily (total dosage: 336 mcg/day).103

Adolescents ≥12 years of age: Maximum 84 mcg (2 sprays) in each nostril twice daily (total dosage: 336 mcg/day).103

Perennial Rhinitis
Intranasal Inhalation

Children 6–12 years of age: Maximum 84 mcg (2 sprays) in each nostril twice daily (total dosage: 336 mcg/day).103

Adolescents ≥12 years of age: Maximum 84 mcg (2 sprays) in each nostril twice daily (total dosage: 336 mcg/day).103

Nasal Polyposis
Intranasal Inhalation

Children 6–12 years of age: Maximum 84 mcg (2 sprays) in each nostril twice daily (total dosage: 336 mcg/day).103

Adolescents ≥12 years of age: Maximum 84 mcg (2 sprays) in each nostril twice daily (total dosage: 336 mcg/day).103

Adults

Seasonal Rhinitis
Intranasal Inhalation

Maximum 84 mcg (2 sprays) in each nostril twice daily (total dosage: 336 mcg/day).103

Perennial Rhinitis
Intranasal Inhalation

Maximum 84 mcg (2 sprays) in each nostril twice daily (total dosage: 336 mcg/day).103

Nasal Polyposis
Intranasal Inhalation

Maximum 84 mcg (2 sprays) in each nostril twice daily (total dosage: 336 mcg/day).103

Cautions for Beclomethasone Dipropionate

Contraindications

  • Known hypersensitivity to beclomethasone or any ingredient in the formulation.103

  • Do not use in the presence of untreated localized nasal mucosa infections.103

Warnings/Precautions

Warnings

Withdrawal of Systemic Corticosteroid Therapy

Patients being switched from prolonged systemic corticosteroids to intranasal therapy should be monitored carefully since corticosteroid withdrawal symptoms (e.g., joint pain, muscular pain, lassitude, depression), acute adrenal insufficiency, and/or severe symptomatic exacerbation of asthma or other clinical conditions may occur.103

In patients being switched to intranasal therapy, systemic corticosteroid dosage should be tapered and patients carefully monitored during dosage reduction.103

Systemic Corticosteroid Effects

Excessive intranasal dosages or use in patients who are particularly sensitive to corticosteroid effects may cause systemic corticosteroid effects (e.g., menstrual irregularities, acneiform lesions, cataracts, cushingoid features).103

Avoid larger than recommended dosages; potential for systemic effects increases with excessive dosage.103

If systemic effects occur, therapy with the drug should gradually be withdrawn (tapered).103

Immunosuppression

Although risk with intranasal use is unknown, consider the possibility that corticosteroid-induced immunosuppression could occur.a Avoid exposure to varicella and measles in previously unexposed patients and those who have not been properly immunized.103

If exposure to varicella or measles occurs in such individuals, administration of varicella zoster immune globulin (VZIG) or immune globulin, respectively, may be indicated.103 If varicella develops, treatment with an antiviral agent may be considered.103

Sensitivity Reactions

Immediate or delayed hypersensitivity reactions, including anaphylactoid/anaphylactic reactions, urticaria, angioedema, rash, wheezing, and bronchospasm, have occurred rarely.103

General Precautions

Nasopharyngeal Effects

Persistent nasopharyngeal irritation may require discontinuance of beclomethasone therapy.103

Rarely, nasal septal perforations.103

Rarely, localized candidal infections of the nose and/or pharynx.103 Treat suspected infection with appropriate local therapy;103 may require discontinuance of beclomethasone therapy.103

Avoid use until healing occurs in patients with recurrent epistaxis, recent nasal septal ulcers, nasal surgery, or nasal trauma.103

Ophthalmic Effects

Increased intraocular pressure (IOP), glaucoma, cataracts, and conjunctivitis have been reported rarely.103

Hypothalamic-Pituitary-Adrenal Axis Suppression

Avoid higher than recommended dosages since suppression of hypothalamic-pituitary-adrenal (HPA) function may occur.103

Reductions in plasma cortisol concentrations have occurred when intranasal and orally inhaled beclomethasone dipropionate were used concomitantly.a

Cases of growth suppression also have been reported.103 (See Pediatric Use under Cautions.)

Infection

Use cautiously, if at all, in patients with clinical tuberculosis or asymptomatic Mycobacterium tuberculosis infections of the respiratory tract; untreated local or systemic fungal or bacterial infections; systemic viral or parasitic infections; or ocular herpes simplex infections.103

Nasal Polyposis

Treatment with beclomethasone should be considered adjunctive to surgical removal and/or use of other drugs that will permit effective penetration of the drug into the nose; polyps may recur after any treatment.103

Nasal Mucosal Changes

During long-term intranasal therapy (several months or longer), periodically examine nasal passages for mucosal changes.103

Specific Populations

Pregnancy

Category C.103

Lactation

Other corticosteroids known to be distributed into milk.103 Caution if used in nursing women.103

Corticosteroids may cause adverse effects (e.g., growth suppression) in nursing infants if distributed into milk.a

Pediatric Use

May be a useful therapeutic alternative to oral corticosteroids in children ≥6 years of age with seasonal or perennial allergic rhinitis, since intranasal administration is associated with a decreased risk of adverse systemic effects.a

Intranasal corticosteroids, including beclomethasone, may reduce growth velocity in pediatric patients; use lowest effective dosage and monitor growth routinely.103 In a placebo-controlled, 1-year study, approximately 50% of beclomethasone dipropionate-treated children were below the 10th percentile for growth velocity.103

Safety and efficacy not established in children <6 years of age.103

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether such patients respond differently than younger adults; select dosage with caution due to greater frequency of decreased hepatic, renal, and/or cardiac function and of concomitant disease and drug therapy observed in geriatric patients.103

Common Adverse Effects

Mild nasopharyngeal irritation, sneezing attacks, headache, nausea, lightheadedness, nasal stuffiness, nosebleeds, rhinorrhea, tearing eyes.103

Beclomethasone Dipropionate Pharmacokinetics

Absorption

Bioavailability

Most of an intranasal dose is swallowed.103 105

Systemic bioavailability (as active metabolite) is 44% (43% from swallowed portion, 1% from nasal mucosa).103 105

Distribution

Extent

Moderate distribution, more extensive for active metabolite.103 105 Beclomethasone dipropionate and its metabolites are not stored in tissues.103

Not known whether beclomethasone crosses the placenta or is distributed into milk; other corticosteroids are distributed into milk.a 103

Plasma Protein Binding

Approximately 87%.103

Elimination

Metabolism

Beclomethasone dipropionate is a weakly active prodrug, rapidly hydrolyzed to highly active beclomethasone-17-monopropionate (B-17-MP) by esterase enzymes found in most tissues.a 103 105

Elimination Route

Excreted mainly as metabolites in feces (60%) and in urine (12%) following oral administration.103

Half-life

Not determined following intranasal administration.a Terminal half-life averages 0.5 hours (beclomethasone dipropionate) and 2.7 hours (active metabolite) following IV administration.103

Stability

Storage

Nasal Suspension

15–30°C.103

Discard the nasal pump spray after 180 sprays.103 104

Actions

  • Potent glucocorticoid and weak mineralocorticoid effects.a

  • Topical anti-inflammatory potency of beclomethasone dipropionate is about 5000 times greater than hydrocortisone; 500 times greater than beclomethasone, betamethasone, or dexamethasone; and about 5 times greater than fluocinolone or the acetonides of fluocinolone or triamcinolone, as measured by vasoconstrictor assay.a Beclomethasone dipropionate is 6–7 times more potent as a glucocorticoid than hydrocortisone when administered orally or subcutaneously.a

  • Local anti-inflammatory and vasoconstrictor effects following topical application to the nasal mucosa.a 103

  • Reduces number of mediator cells (basophil leukocytes and mast cells) at the epithelial level, number of eosinophils, sensitivity of sensory nerves to mechanical stimuli, secretory response to cholinergic receptor stimulation, and fibroblast activity.a

  • May inhibit capillary dilation and permeability, stabilize lysosomal membranes and prevent proteolytic enzyme release.a

  • Adrenal suppression has not been observed when beclomethasone dipropionate inhalation aerosol (no longer commercially available in the US) was administered in clinical trials,103 but decreases in nocturnal cortisol secretion have been reported with usual dosages of beclomethasone oral inhalation in children.103 (See Hypothalamic-Pituitary-Adrenal Axis Suppression under Cautions.)

Advice to Patients

  • Importance of giving patient a copy of the manufacturer’s patient instructions.103 104

  • Importance of instructing patient about proper techniques for assembly and priming of nasal spray pump and for administration and storage of the nasal solution.103 104

  • Importance of shaking nasal spray well prior to each use.104

  • Importance of discarding container after 180 actuations or once the expiration date on the label is reached.103 104

  • Avoid spraying into eyes.104

  • Importance of advising patient that effects are not immediate; full benefit may require ≤2 weeks of continuous use.103

  • Importance of using at regular intervals as directed.103

  • Importance of not continuing therapy for longer than 3 weeks in the absence of substantial symptomatic improvement.103

  • Importance of informing clinician if symptoms fail to improve or worsen or if sneezing or nasal irritation occurs.103

  • Importance of not increasing dosage unless directed by a clinician.103

  • Importance of using concomitant nasal vasoconstrictor and/or oral antihistamines for 1–2 weeks if needed until the effects of beclomethasone are optimal.103

  • Importance of avoiding exposure to chickenpox or measles if receiving immunosuppressive doses of corticosteroids; if exposed, notify a clinician.103

  • Importance of patients with severe allergies avoiding exposure to allergens during intranasal beclomethasone dipropionate therapy to prevent the occurrence of severe allergic symptoms in the eyes and/or lower respiratory tract.a

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.103

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.103

  • Importance of informing patients of other important precautionary information.103 (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Beclomethasone dipropionate inhalation aerosols containing chlorofluorocarbon (CFC) propellants are no longer marketed in the US.

Beclomethasone Dipropionate (Monohydrate)

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Nasal

Suspension

equivalent to Beclomethasone Dipropionate 42 mcg/metered dose

Beconase AQ Nasal Spray (with benzalkonium chloride and phenylethyl alcohol)

GlaxoSmithKline

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 02/2014. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Beconase AQ 42MCG/SPRAY Suspension (GLAXO SMITH KLINE): 25/$149.99 or 75/$415.97

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions October 1, 2007. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

Only references cited for selected revisions after 1984 are available electronically.

100. Schering. Vancenase (beclomethasone dipropionate) Pockethaler nasal inhaler prescribing information. In: Physicians’ desk reference. 53rd ed. Montvale, NJ: Medical Economics Company Inc; 1999(Suppl A):A292-4.

101. Schering. Vancenase (beclomethasone dipropionate) AQ 84 mcg double strength prescribing information. Kenilworth, NJ. 1996 Jun.

102. Schering. Vancenase (beclomethasone dipropionate) nasal inhaler prescribing information (dated 1997 Apr). In: Physicians’ desk reference. 54th ed. Montvale, NJ: Medical Economics Company Inc; 2000:2844-5.

103. GlaxoSmithKline. Beconase AQ (beclomethasone dipropionate monohydrate) nasal spray prescribing information. Research Triangle Park, NC; 2005 Apr.

104. GlaxoSmithKline. Beconase AQ (beclomethasone dipropionate monohydrate) nasal spray patient instructions for use. Research Triangle Park, NC; 2005 Apr.

105. Daley-Yates PT, Price AC, Sisson JR et al. Beclomethasone dipropionate: absolute bioavailability, pharmacokinetics and metabolism following intravenous, oral, intranasal and inhaled administration in man. Br J Clin Pharmacol. 2001; 51:400-9. [PubMed 11421996]

a. AHFS drug information 2005. McEvoy GK, ed. Beclomethasone dipropionate. Bethesda, MD: American Society of Health-System Pharmacists; 2005:2676-80.

c. Anon. FDA publishes final rule on chlorofluorocarbons in metered dose inhalers. FDA talk paper. Rockville, MD: Food and Drug Administration; 2005 Mar 31.

Hide
(web3)