Non sedating antihistamines in children
H1 antihistamines work as inverse agonists that drive the balance toward the inactive side and suppress the effects of histamine.Since these effects are not genuine antagonistic but rather represent a balance displacement between active and inactive forms of H1 receptors, now, the term H1 antihistamine rather than the former “antihistamine antagonist” is used .The biological effects of histamine in the allergic reaction are mediated through H1 receptors that coexist in active and inactive forms of g-protein-coupled receptors which balance each other.Histamine works as an agonist that pushes the balance to the active side leading to effects such as muscular contraction, bronchospasms, upregulation of endothelial permeability, and stimulation of sensory nerves and cough receptors .A Pub Med literature search from January 1, 2000, through April 1, 2013, was conducted to track down randomized controlled studies of clinical efficacy of bilastine.This was supplemented with additional papers on bilastine and abstracts cited in reference lists, obtained from online sources, or supplied by Berlin-Chemie A. The literature search revealed 2 efficacy studies in allergic rhinoconjunctivitis [14, 15], 1 in perennial rhinitis , and 1 in chronic idiopathic urticaria .Though they are helpful in many patients with mild disease, the available non-sedating antihistamines may not be sufficiently efficacious in moderate to severe conditions [1, 2].Therefore, the launch of a recently developed non-sedating oral antihistamine, bilastine, attracts attention .
There is little evidence, if any, that pharmacokinetic differences between specific drugs are important in clinical use.
The aim of this paper is to review the current evidence of bilastine in the treatment of allergic rhinoconjunctivitis and urticaria.
Several mediators are involved in the pathophysiology; however, histamine plays a vital role in the allergic immediate reaction .
Therefore, it is recommended that bilastine is administered at least one hour before or no sooner than two hours after a meal [2, 10].
The maximum plasma concentration (220 ng/m L) of bilastine 20 mg was found 1.3 hours after administration, half time was 14.5 hours, and plasma protein binding was 84–90% .