Bexitrol
Bexitrol is a long-acting beta2-adrenergic receptor agonist drug that is currently prescribed for the treatment of asthma and chronic obstructive pulmonary disease COPD.
Bexitrol is a long-acting beta2-adrenergic receptor agonist drug that is currently prescribed for the treatment of asthma and chronic obstructive pulmonary disease COPD.
Therapeutic Class
Dosage Form & Composition
Inhaler: Bexitrol 25 mcg, Fluticasone proprionate 250 mcg; suspended in propellant HFA-134a
Pack size: Available in canisters containing 120 metered doses.
Bexitrol contains Salmeterol Xinafoate which is a long-acting beta2-adrenergic agonist. In vitro and in vivo pharmacologic studies demonstrate that Bexitrolis selective for beta2-adrenoceptors compared with isoproterenol, which has approximately equal agonist activity on beta1- and beta2-adrenoceptors. In vitro studies show Bexitrol to be at least 50 times more selective for beta2-adrenoceptors than Salbutamol (Albuterol). Although beta2-adrenoceptors are the predominant adrenergic receptors in bronchial smooth muscle and beta1-adrenoceptors are the predominant receptors in the heart, there are also beta2-adrenoceptors in the human heart comprising 10% to 50% of the total beta-adrenoceptors. The precise function of these receptors has not been established, but their presence raises the possibility that even selective beta2-agonists may have cardiac effects.
The pharmacologic effects of beta2-adrenoceptor agonist drugs, including Bexitrol, are at least in part attributable to stimulation of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3′,5′-adenosine monophosphate (cyclic AMP). Increased cyclic AMP levels cause relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells.
In vitro tests show that Bexitrol is a potent and long-lasting inhibitor of the release of mast cell mediators, such as histamine, leukotrienes, and prostaglandin D2, from human lungs. Bexitrol inhibits histamine-induced plasma protein extravasation and inhibits platelet activating factor-induced eosinophil accumulation in the lungs of guinea pigs when administered by the inhaled route.
In humans, single doses of Bexitrol administered via inhalation aerosol attenuate allergen-induced bronchial hyper-responsiveness.
Indications
It is indicated in the regular treatment of asthma, where use of a combination (long-acting beta2-agonist and inhaled corticosteroid) has been found to be appropriate; also indicated in patients with severe COPD.
Contra-indications
Bexitrol is contraindicated in the primary treatment of status asthmaticus or other acute episodes of asthma where intensive measures are required.
Hypersensitivity to any of the ingredients of these preparations contraindicates their use.
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