Beclomethasone dipropionate (BDP) nasal aerosol is the first nonaqueous, hydrofluoroalkane-propelled intranasal corticosteroid approved for patients in the United States to treat PAR and seasonal allergic rhinitis.
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Beclomethasone dipropionate is a prodrug that is rapidly activated by hydrolysis to the active monoester 17-beclomethasone monopropionate, which has an affinity for the glucocorticoid receptor that is 25 times that of the parent compound.
Beclometasone controls the rate of protein synthesis, depresses the migration of polymorphonuclear leukocytes, fibroblasts, reverses capillary permeability and lysosomal stabilisation at the cellular level to prevent or control inflammation. Respiratory inhalant use: Control of bronchial asthma that requires corticosteroids along with other therapy
Brand Name: Apo-Beclomethasone (CAN), Beconase AQ, Propaderm (CAN), QVAR Adult: Apply a 0.025% cream/ointment onto affected area. Adult: 100 mcg bid or 50 mcg 3-4 times daily in each nostril.
There is a three-fold range in the dosages of beclomethasone that have been reported to be effective for the treatment of RAO ( Ammann et al 1998, Rush et al 1998a, b ).
The most frequent adverse events were worsening asthma (9%) and nausea (6%) with roflumilast and worsening asthma (4%) and upper respiratory tract infections (4%) with beclomethasone dipropionate. Most of the adverse events were mild to moderate in intensity.
Beclomethasone dipropionate is a prodrug that is rapidly activated by hydrolysis to the active monoester 17-beclomethasone monopropionate. The active metabolite has an affinity for the glucocorticoid receptor that is 25 times that of the parent compound. Ciclesonide is an inactive prodrug that is converted to an active metabolite desisobutyrylciclesonide in the lung. Much (40%–90%) of an inhaled corticosteroid is swallowed and therefore available for systemic absorption (and potential systemic side effects). Thus a low oral bioavailability of inhaled corticosteroids is desirable, ranging from 1% for fluticasone propionate to 26% for 17-beclomethasone monopropionate. In contrast to oral absorption, most drug deposited in the lung will be absorbed systemically and is not subjected to first-pass hepatic metabolism. Deposition and thus absorption from the lung is more a function of the efficiency of the delivery device than the properties of the drug itself. Fluticasone has only 1% oral bioavailability owing to first-pass metabolism but when delivered to the lung by dry powder inhalers or MDIs, total systemic bioavailability is 17% and 25%, respectively. 42 The transition from chlorofluorocarbons- to hydrofluoroalkane (HFA)-powered MDIs has resulted in unanticipated improvement in the delivery of smaller particles deposited deeper in the lung with less oropharnygeal deposition and thus less systemic absorption (see “ Emerging Developments ”). Most of the inhaled corticosteroids are (~70%) bound to plasma proteins and have half-lives of 3 to 8 hours owing to high extraction and metabolism by the liver.