Corticosteroids beclomethasone dipropionate

Corticosteroids beclomethasone dipropionate budesonide fluticasone propionate... 

The determination of corticosteroid beclomethasone dipropionate, the prodrag of beclomethasone used in the treatment of respiratory disorders in horses, in equine plasma and mine was reported by Guan et al. [59]. The dosing is only 325 pg per horse, posing challenges to the detection of this drag with restricted use. After LLE with methyl i-butyl ether (MTBE), the analytes and its metabolites were analysed by positive-ion LC-ESl-MS. The LOQ was 13 pg/ml for the analyte and between 25 and 50 pg/ml for its three major metabolites, which allowed detection in equine plasma up to 4 h post administration. 

Corticosteroids — Beclomethasone dipropionate (17) aerosol has been tested extensively clinically. It is used prophylactically (400 fig per day), not therapeutically, in the treatment of chronic asthma, particularly in children.52 An evaluation of the drug has been published.53 One of the most important clinical advantages is that 1 7 effectively can replace oral corticosteroids in steroid-dependent patients and avoid many of the adverse effects of adrenal suppression.52,54 Most patients with impaired adrenal function due to oral corticosteroids show recovery of adrenal function within 6 months.55 The combination of 17 and disodium cromoglycate (DSCG) showed no additive therapeutic effects.5 Flunisolide (18), when administered as a nasal spray for 4 weeks during the hay fever season in 51 patients, showed significant symptomatic improvement with no systemic steroid effects observed.57... 

CB s asthma is currently being treated with a low-dose of the inhaled corticosteroid beclomethasone dipropionate (QVAR, 40 pg b.i.d.). She is in your pharmacy now with prescriptions for both chronic medications written by her new provider. After taking her medical history and reviewing her psychosocial situation, you recognize that she has many risk factors for near-fatal asthma" and believe she should have ready access to rescue therapy in case she experiences an acute episode of severe bronchoconstriction. Consider the structures of the adrenergic agents drawn below, and prepare to make a therapeutic recommendation to CB s new physician. 

The corticosteroids are effective in most children and adults with asthma. They are beneficial for the treatment of both acute and chronic aspects of the disease. Inhaled corticosteroids, including triamcinolone ace-tonide (Azmflcort),beclomethasone dipropionate (Beclo-vent, Vancerit), flunisolide AeroBid), and fluticasone (Flovent), are indicated for maintenance treatment of asthma as prophylactic therapy. Inhaled corticosteroids are not effective for relief of acute episodes of severe bronchospasm. Systemic corticosteroids, including prednisone and prednisolone, are used for the short-term treatment of asthma exacerbations that do not respond to (32-adrenoceptor agonists and aerosol corticosteroids. Systemic corticosteroids, along with other treatments, are also used to control status asthmaticus. Because of the side effects produced by systemically administered corticosteroids, they should not be used for maintenance therapy unless all other treatment options have been exhausted. 

The active component of inhalation aerosol is beclomethasone dipropionate, an anti-inflammatory corticosteroid having the chemical name 9-chloro-ll(beta),17,21-trihy-droxy-16(beta)-methylpregna-l,4-diene-3,20-dione 17,21-dipropionate. It is a pressurized, metered-dose aerosol intended for oral inhalation only. Each unit contains a solution of beclomethasone dipropionate in propellant HFA-134a (1,1,1,2 tetrafluoroethane) and ethanol. The 40-mcg strength delivers 40 meg of beclomethasone dipropionate from the actuator and 50 meg from the valve. The... 

Gregson RK, Rao R, Murrills AJ, Taylor PA, Warner JO. Effect of inhaled corticosteroids on bone mineral density in childhood asthma comparison of fluticasone propionate with beclomethasone dipropionate. Osteoporos Int 1998 8(5) 418-22. 

Beclomethasone dipropionate is a corticosteroid with mainly glucocorticoid activity that is started to exert a topical effect on the lungs, without significant systemic activity. It is used by inhalation, generally from a metered-dose aerosol, for the prophylaxis of asthma. Inhalation of nebulized beclomethasone dipropionate has also been used in the management of asthma in children. 

Beclomethasone dipropionate and budesonide Modulite formulations have been compared with equivalent chlorofluorocarbon products in small groups of healthy volunteers and asthmatic patients (18) there was no significant difference in morning serum cortisol or urinary cortisol excretion, suggesting that the systemic availability of the inhaled corticosteroids with different propellants is similar. Moreover, plasma profiles of beclomethasone dipropionate and B17MP were similar after inhalation of beclomethasone dipropionate Modulite and beclomethasone dipropionate-chlorofluorocarbon, suggesting that pulmonary delivery to the lung is comparable with the two propellants (18). 

The ICSs beclomethasone dipropionate, budesonide, flunisolide, fluticasone propionate, and triamcinolone acetonide that are currently available for use are compared and listed in Table 26-12. The ICSs have pharmacokinetic differences that result in different topical/ systemic activity. Most evidence is consistent with log-linear dose-response curves for both indirect and direct responses. The log-linear nature of the dose-response curve for corticosteroid activity raises the issue of how much of a difference in dose (or lung delivery) or potency is detectable. The dose-response curves for the ICSs are relatively flat primarily because all the measures used to assess efficacy (lung function, BHR, symptoms, and as-needed short-acting inhaled /32-agonist use) are downstream events from the anti-inflammatory activity. In general, it takes a fourfold difference in potency or dose to detect clinically significant differences. The table of comparative doses (see Table 26-12) is based on extensive comparative clinical trials. Clinical comparative doses take into consideration potency differences as well as lung delivery differences from the various devices. 

Corticosteroids (Table 11) are synthetic adrenocortical steroids with antiinflammatory actions and effects, and are used in numerous disorders including bronchial asthma. For example, beclomethasone dipropionate (Beclovent, 85 meg 3 to 4 times daily), dexamethasone sodium phosphate (Decadron phosphate), and triamcinolone acetonide (Azmacort), which are not bronchodilators and are not indicated for rapid rehef of acute asthma, are used in bronchospastic states intractable to an adequate trial of conventional therapy. 

In order to increase their Upid solubility, corticosteroids have been esterified with monocarboxylic (fatty) acids. Examples include hydrocortisone acetate, beclomethasone dipropionate and betamethasone isovalerate. For triamcinolone, the following method has been developed to make the substance lipophilic the hydroxyl groups at the C16 and C17-position of triamcinolone are used to form a cyclic acetal (Fig. 18.4). Although the formed substance, triamcinolone acetonide, is not a fatty acid ester, with regard to lipid solubility it behaves as such. 

Corticosteroid therapy, oral or parenteral (by inhalation) may offer dramatic relief from asthma when other less dangerous measures have failed. At least one of the inhalant preparations (beclomethasone dipropionate) seems to compete favourably with other anti-asthmatics as far as the risks involved are concerned. Recent data on the corticosteroids in all their forms can be found in Chapter 37. 

Corticosteroids - Corticosteroids have a number of side effects that can restrict their use in asthma. The most troublesome of these is the suppression of normal adrenal function and the development of Cushingoid symptoms. Recently beclomethasone-17,21-dipropionate has been used... 

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