title: Bilastine: a new antihistamine with an optimal benefit-to-risk ratio for safety during driving.
abstract: BACKGROUND
  Rational selection of a second-generation H1-antihistamine requires efficacy and safety considerations, particularly regarding central nervous system (CNS) effects (cognitive and psychomotor function), potential for driving impairment, minimal sedative effects and a lack of interactions. This review evaluates the key safety features of the non-sedating antihistamine, bilastine, during driving and in preventing road traffic accidents.
  
  
  METHODS
  Among the second-generation H1-antihistamines, sedative effects which can affect cognitive and psychomotor performance, and possibly driving ability, may not be similar. Bilastine is absorbed rapidly, undergoes no hepatic metabolism or cytochrome P450 interaction (minimal drug-drug interaction potential), and is a substrate for P-glycoprotein (limiting CNS entry). Positron emission tomography showed that, compared with other second-generation H1-antihistamines, bilastine has the lowest cerebral histamine H1-receptor occupancy. Bilastine 20 mg once daily (therapeutic dose) is non-sedating, does not enhance the effects of alcohol or CNS sedatives, does not impair driving performance and has at least similar efficacy as other second-generation H1-antihistamines in the treatment of allergic rhinoconjunctivitis and urticaria.
  
  
  CONCLUSIONS
  Current evidence shows that bilastine has an optimal benefit-to-risk ratio, meeting all conditions for contributing to safety in drivers who need antihistamines, and hence for being considered as an antihistamine of choice for drivers.
authors.affiliation: a Allergy Department , Basurto University Hospital , Bilbao 48013 , Spain.
authors.forename: Ignacio
authors.initials: I
authors.lastname: Jáuregui
authors.affiliation: b Department of Neuropsychology and Psychopharmacology, Faculty of Psychology and Neuroscience , Maastricht University , Maastricht , The Netherlands.
authors.forename: Johannes G
authors.initials: JG
authors.lastname: Ramaekers
authors.affiliation: c Department of Pharmacology , Tohoku University Graduate School of Medicine , Sendai , Japan.
authors.forename: Kazuhiko
authors.initials: K
authors.lastname: Yanai
authors.affiliation: d Clinical Pharmacology Unit , Hospital Universitari Germans Trias i Pujol-IGTP, Hospital del Mar Medical Research Institute-IMIM, and Universidad Autónoma de Barcelona-UAB , Barcelona , Spain.
authors.forename: Magí
authors.initials: M
authors.lastname: Farré
authors.affiliation: e Coordinadora del Grupo de Trabajo de Actividades Preventivas de SEMERGEN , International Health Center , Madrid , Spain.
authors.forename: Esther
authors.initials: E
authors.lastname: Redondo
authors.affiliation: f Medical and Clinical Department , FAES FARMA S. A. , Leioa , Spain.
authors.forename: Román
authors.initials: R
authors.lastname: Valiente
authors.affiliation: f Medical and Clinical Department , FAES FARMA S. A. , Leioa , Spain.
authors.forename: Luis
authors.initials: L
authors.lastname: Labeaga
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism; D001334:Automobile Driving; D001562:Benzimidazoles / Q000008:administration & dosage / Q000009:adverse effects* / Q000493:pharmacokinetics; D004347:Drug Interactions; D039563:Histamine H1 Antagonists, Non-Sedating / Q000008:administration & dosage / Q000009:adverse effects* / Q000493:pharmacokinetics; D006801:Humans; D010880:Piperidines / Q000008:administration & dosage / Q000009:adverse effects* / Q000493:pharmacokinetics
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D001562:Benzimidazoles; D039563:Histamine H1 Antagonists, Non-Sedating; D010880:Piperidines; C445659:bilastine
keywords: antihistamine; bilastine; driving; non-sedating; safety