Pharmacokinetic and pharmacodynamic properties of inhaled beclometasone dipropionate delivered via hydrofluoroalkane-containing devices. 2005

Eric Derom, and Romain A Pauwels
Department of Respiratory Diseases, Ghent University Hospital, De pintelaan 185, B-9000 Gent, Belgium. eric.derom@Ugent.be

Inhaled corticosteroids have a key role in the treatment of asthma and chronic obstructive pulmonary disease. In recent times, beclometasone dipropionate has been reformulated in pressurised metered dose inhalers (pMDIs), using hydrofluoroalkanes (HFAs) as a propellant. Extensive toxicological testing has shown that HFA-propellants are well tolerated. Among the reformulated beclometasone dipropionate-containing pMDIs, only the characteristics of the two Qvar formulations have been thoroughly explored. Compared to the reference beclometasone dipropionate formulation, the mass median aerodynamic diameter of the Qvar formulations are substantially smaller (1.1 vs 4.0 microm), whereas that of Modulite averages 2.6 microm. Scintigraphic and pharmacokinetic studies indicate a higher lung deposition for both the Qvar and the Beclazone formulations, compared with reference beclometasone dipropionate formulation. Since the 2- to 3-fold increase in pulmonary deposition results in a 2.6- to 3-fold difference in relative efficacy for Qvar, half the dose of the reference beclometasone dipropionate formulation has been currently recommended in adult patients with asthma, a recommendation that is supported by a large number of clinical trials. Conversely, the design of the studies conducted to compare the efficacy of Qvar with fluticasone propionate and budesonide does not allow establishing their equivalence on a milligram per milligram basis. Good studies on the bioequivalence between the reference beclometasone dipropionate formulation and the Modulite or Beclazone formulations are not available.

UI MeSH Term Description Entries
D005938 Glucocorticoids A group of CORTICOSTEROIDS that affect carbohydrate metabolism (GLUCONEOGENESIS, liver glycogen deposition, elevation of BLOOD SUGAR), inhibit ADRENOCORTICOTROPIC HORMONE secretion, and possess pronounced anti-inflammatory activity. They also play a role in fat and protein metabolism, maintenance of arterial blood pressure, alteration of the connective tissue response to injury, reduction in the number of circulating lymphocytes, and functioning of the central nervous system. Glucocorticoid,Glucocorticoid Effect,Glucorticoid Effects,Effect, Glucocorticoid,Effects, Glucorticoid
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D006845 Hydrocarbons, Fluorinated Inert liquid or gaseous halocarbon compounds in which FLUORINE replaces some or all HYDROGEN atoms. Fluorinated Hydrocarbons
D000280 Administration, Inhalation The administration of drugs by the respiratory route. It includes insufflation into the respiratory tract. Drug Administration, Inhalation,Drug Administration, Respiratory,Drug Aerosol Therapy,Inhalation Drug Administration,Inhalation of Drugs,Respiratory Drug Administration,Aerosol Drug Therapy,Aerosol Therapy, Drug,Drug Therapy, Aerosol,Inhalation Administration,Administration, Inhalation Drug,Administration, Respiratory Drug,Therapy, Aerosol Drug,Therapy, Drug Aerosol
D000335 Aerosol Propellants Compressed gases or vapors in a container which, upon release of pressure and expansion through a valve, carry another substance from the container. They are used for cosmetics, household cleaners, and so on. Examples are BUTANES; CARBON DIOXIDE; FLUOROCARBONS; NITROGEN; and PROPANE. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed) Propellants, Aerosol
D000893 Anti-Inflammatory Agents Substances that reduce or suppress INFLAMMATION. Anti-Inflammatory Agent,Antiinflammatory Agent,Agents, Anti-Inflammatory,Agents, Antiinflammatory,Anti-Inflammatories,Antiinflammatories,Antiinflammatory Agents,Agent, Anti-Inflammatory,Agent, Antiinflammatory,Agents, Anti Inflammatory,Anti Inflammatories,Anti Inflammatory Agent,Anti Inflammatory Agents
D001249 Asthma A form of bronchial disorder with three distinct components: airway hyper-responsiveness (RESPIRATORY HYPERSENSITIVITY), airway INFLAMMATION, and intermittent AIRWAY OBSTRUCTION. It is characterized by spasmodic contraction of airway smooth muscle, WHEEZING, and dyspnea (DYSPNEA, PAROXYSMAL). Asthma, Bronchial,Bronchial Asthma,Asthmas
D001507 Beclomethasone An anti-inflammatory, synthetic glucocorticoid. It is used topically as an anti-inflammatory agent and in aerosol form for the treatment of ASTHMA. Beclomethasone Dipropionate,AeroBec Forte,Aerobec,Aldecin,Apo-Beclomethasone,Ascocortonyl,Asmabec Clickhaler,Beclamet,Beclazone,Beclazone Easy Breathe,Beclo AZU,Beclo Asma,Beclocort,Becloforte,Beclomet,Beclometasone,Beclorhinol,Becloturmant,Beclovent,Becodisk,Becodisks,Beconase,Beconase AQ,Becotide,Bemedrex Easyhaler,Bronchocort,Ecobec,Filair,Filair Forte,Junik,Nasobec Aqueous,Prolair,Propaderm,Qvar,Respocort,Sanasthmax,Sanasthmyl,Vancenase,Vanceril,Ventolair,Viarin,Dipropionate, Beclomethasone
D013810 Therapeutic Equivalency The relative equivalency in the efficacy of different modes of treatment of a disease, most often used to compare the efficacy of different pharmaceuticals to treat a given disease. Bioequivalence,Clinical Equivalency,Equivalency, Therapeutic,Generic Equivalency,Clinical Equivalencies,Equivalencies, Clinical,Equivalencies, Therapeutic,Equivalency, Clinical,Therapeutic Equivalencies,Bioequivalences,Equivalencies, Generic,Equivalency, Generic,Generic Equivalencies
D018927 Anti-Asthmatic Agents Drugs that are used to treat asthma. Anti-Asthmatic,Anti-Asthmatic Agent,Anti-Asthmatic Drug,Antiasthmatic,Antiasthmatic Agent,Antiasthmatic Drug,Anti-Asthmatic Drugs,Anti-Asthmatics,Antiasthmatic Agents,Antiasthmatic Drugs,Antiasthmatics,Agent, Anti-Asthmatic,Agent, Antiasthmatic,Agents, Anti-Asthmatic,Agents, Antiasthmatic,Anti Asthmatic,Anti Asthmatic Agent,Anti Asthmatic Agents,Anti Asthmatic Drug,Anti Asthmatic Drugs,Anti Asthmatics,Drug, Anti-Asthmatic,Drug, Antiasthmatic,Drugs, Anti-Asthmatic,Drugs, Antiasthmatic

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