title: Bepotastine besilate for the treatment of pruritus.
abstract: BACKGROUND
  Bepotastine besilate 1.5% is a newly approved second-generation topical antihistamine indicated for the pruritus associated with allergic conjunctivitis. In Japan, the oral formulation is approved to manage pruritus associated with allergic rhinitis and urticaria.
  
  
  METHODS
  Bepotastine is a piperidine derivative that antagonizes H1 receptors with high selectivity. It has been labeled a dual-acting or multiple-acting antiallergic medication, because it inhibits histamine at H1 receptors and stabilizes mast cells to prevent histamine release. Bepotastine may also have other immunoactive properties, such as inhibition of eosinophil migration, interleukin-5 (IL-5), leukotrienes (e.g., LTB4) and platelet-activating factor (PAF). Human clinical trials demonstrate the efficacy and safety of systemic and ophthalmic bepotastine for pruritus relief, limited penetration across the blood-brain-barrier and kinetics suitable for twice-daily administration.
  
  
  CONCLUSIONS
  Bepotastine besilate 1.5% ophthalmic solution is a safe and effective treatment option for allergic conjunctivitis associated pruritus. Side-effect profile is similar to other ocular antihistamine agents. Additional comparative-effectiveness studies would further advance its clinical use. Oral bepotastine is a safe and effective treatment option approved in Japan for allergic rhinitis, urticaria and pruritus associated with skin diseases.
authors.affiliation: Rutgers University/Robert Wood Johnson University Hospital , New Brunswick, NJ 07081 , USA +1 973 912 9817 ; +1 206 333 1884 ; Bielory@Rutgers.edu.
authors.forename: Leonard
authors.initials: L
authors.lastname: Bielory
authors.forename: Shubhasree
authors.initials: S
authors.lastname: Duttachoudhury
authors.forename: Andrea
authors.initials: A
authors.lastname: McMunn
mesh_terms: D000279:Administration, Cutaneous; D000284:Administration, Oral; D000818:Animals; D002986:Clinical Trials as Topic; D003233:Conjunctivitis, Allergic / Q000150:complications / Q000188:drug therapy*; D006634:Histamine H1 Antagonists / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D006801:Humans; D010880:Piperidines / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D011537:Pruritus / Q000150:complications / Q000188:drug therapy*; D011725:Pyridines / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D065631:Rhinitis, Allergic; D012221:Rhinitis, Allergic, Perennial / Q000150:complications / Q000188:drug therapy*; D014581:Urticaria / Q000150:complications / Q000188:drug therapy*
chemical_list: D006634:Histamine H1 Antagonists; D010880:Piperidines; D011725:Pyridines; C511534:bepotastine besilate