Pharmacology: Mechanism of action: Arite Beclometasone 50mcg/actuation and 100mcg/actuation Metered Dose Inhaler contains beclometasone dipropionate in solution in propellant HFA-134a resulting in an extrafine aerosol. The aerosol droplets are on average much smaller than the beclometasone dipropionate particles delivered by CFC suspension formulations or dry powder formulations of beclometasone dipropionate. Inhaled beclometasone dipropionate is now well established in the management of asthma. It is a synthetic glucocorticoid and exerts a topical, anti-inflammatory effect on the lungs, with fewer systemic effects than oral corticosteroids. CFC-free beclometasone dipropionate aerosol inhalers shown to exhibit equivalent therapeutic effects, pulmonary function and control of symptoms at lower total daily doses than CFC containing beclometasone dipropionate aerosol inhalers.
Pharmacokinetics: The pharmacokinetic profile shows that the peak serum concentration for total-beclometasone (BOH) (total of any beclometasone OH and beclometasone dipropionate or monopropionate hydrolysed to beclometasone OH) or after single and multiple doses is achieved after 30 minutes. The value at the peak is approximately 2ng/ml after a total daily dose of 800 mcg and the serum levels after 100, 200 and 400mcg are proportional. The principal route of elimination of beclometasone dipropionate and its several metabolites is in the faeces. Between 10% and 15% of an orally administered dose is excreted in the urine, as both conjugated and free metabolites of the drug. Lower total daily doses of CFC-free beclometasone dipropionate aerosol inhalers has shown to achieve the same clinical effect than CFC containing beclometasone dipropionate aerosol inhalers. Pharmacokinetic studies with CFC-free beclometasone dipropionate aerosol inhalers have not been carried out in any special populations.