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Expert Opinion on Pharmacotherapy 2015Allergic rhinitis (AR) is a common chronic disorder, affecting 10 -30% of populations. AR has significant morbidity and expense. AR patients treat themselves with... (Review)
Review
INTRODUCTION
Allergic rhinitis (AR) is a common chronic disorder, affecting 10 -30% of populations. AR has significant morbidity and expense. AR patients treat themselves with over-the-counter medications. However the usual H1 antihistamines are often inadequate. Intranasal corticosteroids effectively diminish AR symptoms. Beclomethasonedipropionate (BDP) was reported to effectively treat adults and children with AR. BDP was a chlorofluorocarbon (CFC) propellant pressurized metered dose inhaler (pMDI). Subsequently BDP appeared in an aqueous format. Some patients preferred the dryer sensation of pMDI to aqueous formulations. The protocol of Montréal, removed CFC devices from medical practice. The remaining intranasal steroids were in aqueous format. Many patients did not like the sensory perceptions using liquids intranasal. They were unlikely to be compliant. BDP hydrofluoroalkanepMDI (BDP HFA) was developed.
AREAS COVERED
The need of active treatment of AR will be reviewed. Chemistry, pharmacokinetics and pharmacodynamics of BDP HFA will be presented. Clinical efficacy studies and safety data which led to the approval of BDP for use in adults and children will be reviewed.
EXPERT OPINION
BDP HFA is an option to treat AR, demonstrating a favorable therapeutic index in large double-blind placebo-controlled studies. BDP HFA appeals to select AR patients.
Topics: Administration, Inhalation; Administration, Intranasal; Beclomethasone; Chronic Disease; Glucocorticoids; Humans; Metered Dose Inhalers; Patient Compliance; Rhinitis, Allergic
PubMed: 26653155
DOI: 10.1517/14656566.2015.1115014 -
Annals of Internal Medicine Oct 1981Experience with beclomethasone dipropionate during the past 5 years has confirmed and extended the original observation that it is an effective, topically active...
Experience with beclomethasone dipropionate during the past 5 years has confirmed and extended the original observation that it is an effective, topically active corticosteroid of great value in treating asthma. Most steroid-dependent asthmatic patients can be successfully controlled with the drug, at least most of the time, and the therapeutic effect is dose dependent. Although high doses may be associated with some adrenal suppression such doses do not cause systemic symptoms, and side effects are of little consequence. It is important that patients treated with steroid aerosols continue to receive other effective therapeutic agents, notably adrenergic drugs, particularly by aerosol, and theophylline compounds; that they learn how to inhale the aerosol properly; and, most important, that they promptly start taking oral steroids when they experience an exacerbation of asthma.
Topics: Aerosols; Asthma; Beclomethasone; Candidiasis, Oral; Humans; Long-Term Care; Lung Diseases, Obstructive
PubMed: 6792963
DOI: 10.7326/0003-4819-95-4-464 -
The Cochrane Database of Systematic... 2000Inhaled steroids play a central role in the management of childhood asthma. There is concern about their side effects, especially on growth. However asthma may also... (Review)
Review
BACKGROUND
Inhaled steroids play a central role in the management of childhood asthma. There is concern about their side effects, especially on growth. However asthma may also cause growth retardation. Growth rates are not stable, so randomised controlled parallel group studies are needed to assess the impact of inhaled steroids on growth. This review is confine to one inhaled steroid, beclomethasone, that is known to have significant levels of systemic absorption.
OBJECTIVES
To determine whether inhaled beclomethasone cause significant delay in the linear growth of children with asthma.
SEARCH STRATEGY
The Cochrane Airways Group asthma register was searched. Bibliographies from included studies, and known reviews were searched for additional citations. Personal contact with colleagues and researchers working in the field of asthma were made to identify potentially relevant trials.
SELECTION CRITERIA
Randomized, controlled trials comparing the effects of beclamethasone to non-steroidal medication (placebo or non-steroidal therapy) on the linear growth of children with asthma.
DATA COLLECTION AND ANALYSIS
Data related to the clinical outcome "change in growth" were extracted by two reviewers working independently
MAIN RESULTS
One hundred and fifty-nine citations were identified by the search strategy and bibliography review. Three studies met the inclusion criteria. All used beclomethasone 200 mcg twice daily delivered by dry powder Diskhaler to treat children with mild-moderate asthma. Study duration was 7-12 months. In all three studies, a significant decrease in linear growth occurred in children treated with beclomethasone compared to those receiving placebo or non-steroidal asthma therapy. The average decrease, calculated through meta-analysis, was -1.54 cm per year (95% CI -1.15, -1.94).
REVIEWER'S CONCLUSIONS
In children with mild-moderate asthma, beclomethasone 200 mcg twice daily caused a decrease in linear growth of -1.54 cm per year. These studies lasted a maximum of 54 weeks, so it remains unclear whether the decrease in growth is sustained or whether it reverses with 'catch up' after therapy is discontinued. We are unable to comment on growth effects of other inhaled steroids that have potentially less systemic effects. If inhaled steroids are required to control a child's asthma, we recommend using the minimum dose that effectively controls the child's asthma and closely following growth.
Topics: Age Factors; Anti-Asthmatic Agents; Asthma; Beclomethasone; Child; Child Development; Growth; Humans
PubMed: 10796632
DOI: 10.1002/14651858.CD001282 -
Drugs 1975At doses similar to those used in the treatment of chronic bronchial asthma, intranasal beclomethasone dipropionate is effective in alleviating nasal symptoms of... (Clinical Trial)
Clinical Trial Review
At doses similar to those used in the treatment of chronic bronchial asthma, intranasal beclomethasone dipropionate is effective in alleviating nasal symptoms of seasonal allergic and perennial rhinitis in about three-quarters of patients. Eye symptoms are not relieved. The carry-over effect of the evening dose is useful in preventing early morning attacks of sneezing. Intranasal beclomethasone dipropionate is useful in controlling symptoms persisting after polypectomy and may possibly delay or eliminate the need for the surgical removal of nasal polyps, which may shrink after several weeks or months of treatment.
Topics: Administration, Intranasal; Adrenal Glands; Adult; Beclomethasone; Child; Chronic Disease; Clinical Trials as Topic; Cromolyn Sodium; Drug Evaluation; Humans; Hydrocortisone; Methylprednisolone; Nasal Polyps; Placebos; Rhinitis, Allergic, Seasonal; Seasons
PubMed: 811455
DOI: 10.2165/00003495-197510030-00003 -
Steroids Jan 2022Beclomethasone dipropionate (1) is a synthetic corticosteroid with anti-inflammatory, antipruritic, and anti-allergy properties. It is widely used to treat asthma,...
Beclomethasone dipropionate (1) is a synthetic corticosteroid with anti-inflammatory, antipruritic, and anti-allergy properties. It is widely used to treat asthma, allergic rhinitis, and dermatoses. However, existing synthetic routes to this active pharmaceutical ingredient (API) contain steps resulting in low and/or inconsistent yields, and use obsolete reagents. Such inconsistencies coupled with a lack of reliable experimental data makes laboratory-scale and large-scale synthesis of this API difficult and time-consuming. In this paper, we report a practical and scalable approach to synthesize 1 from the readily available steroidal intermediate, 16β-methyl epoxide (3, DB-11). A gram-scale to kilogram-scale synthesis of 1 was achieved with 82% yield, using a cost-effective and scalable methodology. Selective propionylation of the hydroxyl groups at C and C demonstrate the fact that this approach can be conveniently implemented in fine chemical industries.
Topics: Beclomethasone; Molecular Conformation; Stereoisomerism
PubMed: 34871605
DOI: 10.1016/j.steroids.2021.108948 -
Drugs Aug 1984Inhaled beclomethasone dipropionate is now well established in the management of asthma. Studies conducted over the last decade, and since the drug was previously... (Review)
Review
Inhaled beclomethasone dipropionate is now well established in the management of asthma. Studies conducted over the last decade, and since the drug was previously reviewed in the Journal, have confirmed that inhaled beclomethasone dipropionate 400 to 800 micrograms daily can reduce the need for oral maintenance corticosteroids in the majority of asthmatic patients requiring such therapy, and that increasing the dosage to 2000 micrograms daily may provide additional clinical benefit in some patients unresponsive to usual therapeutic dosages. Follow-up over a period of several years has confirmed that the initial response to inhaled beclomethasone can be maintained in most patients. Recent studies indicate that beclomethasone dipropionate 400 micrograms daily is equally effective when administered in 2 or 4 divided doses in patients with stable asthma, but it is likely that the lower frequency of administration will be less effective when the asthma is unstable. Recent studies have established the usefulness and good tolerability of intranasal beclomethasone dipropionate in the treatment of perennial and seasonal rhinitis, where the drug has been shown to be more effective than intranasal sodium cromoglycate and similar in efficacy to flunisolide. Nasal polyps decrease in size during continuous treatment with intranasal beclomethasone dipropionate, but enlarge again during periods of respiratory infection. After a decade of treatment with inhaled and intranasal beclomethasone dipropionate, there is no evidence that the drug damages the tracheobronchial lining or the nasal mucosa. Thus, the initial promise of beclomethasone dipropionate has been fulfilled. It has had an important role in asthma therapy over the past decade, which will continue into the future.
Topics: Adrenal Glands; Aerosols; Asthma; Beclomethasone; Bronchi; Drug Therapy, Combination; Glucocorticoids; Humans; Immunity; Kinetics; Nasal Mucosa; Rhinitis
PubMed: 6381025
DOI: 10.2165/00003495-198428020-00002 -
Recenti Progressi in Medicina Nov 2017
Review
Topics: Administration, Inhalation; Aerosol Propellants; Anti-Asthmatic Agents; Asthma; Beclomethasone; Glucocorticoids; Humans; Nebulizers and Vaporizers
PubMed: 29255325
DOI: 10.1701/2813.28446 -
The British Journal of Psychiatry : the... Dec 1989
Topics: Aged; Beclomethasone; Bipolar Disorder; Humans; Lung Diseases, Obstructive; Male
PubMed: 2620226
DOI: 10.1192/bjp.155.6.871 -
Clinical Therapeutics 1995There is an increasing trend toward topical intranasal corticosteroids as the preferred treatment for seasonal or perennial allergic rhinitis. This trend is based on the... (Review)
Review
There is an increasing trend toward topical intranasal corticosteroids as the preferred treatment for seasonal or perennial allergic rhinitis. This trend is based on the fact that the chronic, mucosal inflammation that accompanies allergic rhinitis responds to anti-inflammatory drugs such as topical corticosteroids. Intranasal corticosteroids, given before the natural antigen challenge, reverse preexisting inflammation and prevent nasal priming by antigens. One intranasal corticosteroid, beclomethasone dipropionate, has been available by prescription in the United States for more than a decade and has an established efficacy and safety profile in patients with allergic rhinitis. Beclomethasone dipropionate has become the standard to which other intranasal corticosteroid preparations are compared. In comparison with earlier corticosteroids (eg, hydrocortisone, prednisolone, dexamethasone, betamethasone) that caused adrenal suppression and other systemic adverse reactions, the actions of new corticosteroids, including beclomethasone dipropionate, are confined to the site of application. These drugs are also more rapidly metabolized, less irritating to the nasal mucosa, and have a longer duration of action. When given intranasally to relieve the sneezing, congestion, and rhinorrhea associated with seasonal and perennial allergic rhinitis, the newer corticosteroids have proved safe and effective. Despite the fact that topical nasal corticosteroids such as beclomethasone dipropionate are responsible for important improvements in the treatment of both allergic and nonallergic rhinitis as well as nasal polyposis and chronic sinusitis, these drugs may be underused, particularly in the pediatric population. Because of the concern of systemic side effects in younger children, less effective therapies are sometimes used.
Topics: Anti-Asthmatic Agents; Beclomethasone; Humans; Rhinitis, Allergic, Perennial; Rhinitis, Allergic, Seasonal
PubMed: 8750396
DOI: 10.1016/0149-2918(95)80082-4 -
Mini Reviews in Medicinal Chemistry Dec 2008Corticosteroids have represented the mainstay of medical treatment for induction of remission in inflammatory bowel disease. Aim of this paper is to review mechanisms of... (Review)
Review
Corticosteroids have represented the mainstay of medical treatment for induction of remission in inflammatory bowel disease. Aim of this paper is to review mechanisms of action, safety and efficacy of beclomethasone dipropionate, a steroid with enhanced topical intestinal activity and low systemic activity, in the treatment of inflammatory bowel disease.
Topics: Administration, Oral; Beclomethasone; Drug Tolerance; Drug-Related Side Effects and Adverse Reactions; Humans; Inflammatory Bowel Diseases
PubMed: 19075804
DOI: 10.2174/138955708786786444