title: Bilastine: an environmental risk assessment.
abstract: BACKGROUND
  Bilastine is a new oral selective, non-sedating histamine H1 antagonist for the symptomatic treatment of allergic rhinoconjunctivitis and urticaria. The European Medicines Agency requires an Environmental Risk Assessment (ERA) for all novel medicines for human use.
  
  
  OBJECTIVE
  To calculate the bilastine predicted environmental concentration in surface water (PECsw; phase I ERA), and to determine the effects of bilastine on aquatic systems (phase II [tier A]).
  
  
  METHODS
  Bilastine PECsw was calculated using the maximum daily dosage (20 mg), assuming that all administered bilastine was released into the aquatic environment. A persistence, bioaccumulation and toxicity assessment was conducted using the log Kow from the molecular structure. In phase II (tier A), a ready biodegradability test was performed, and bilastine's potential toxicity to various aquatic and sediment-dwelling micro-organisms was evaluated.
  
  
  RESULTS
  Bilastine PECSW was calculated as 0.1 μg L(-1), and the compound was not readily biodegradable. Bilastine had no significant effects on Chironomus riparius midges, or on the respiration rate of activated sludge. For green algae, the bilastine no observed effect concentration (NOEC) was 22 mg L(-1); bilastine had no effect on zebra fish development, or on the reproduction rate of daphnids.
  
  
  CONCLUSIONS
  Bilastine NOEC values against zebra fish, algae, daphnids, and aerobic organisms in activated sludge were at least 130 000-fold greater than the calculated PECSW value.
  
  
  CONCLUSIONS
  No environmental concerns exist from bilastine use in patients with allergic rhinoconjunctivitis or urticaria.
authors.affiliation: a FAES Farma , S.A. , Leioa-Bizkaia , Spain and.
authors.forename: María Luisa
authors.initials: ML
authors.lastname: Lucero
authors.affiliation: b Harlan Laboratories Ltd , Itingen , Switzerland.
authors.forename: Armin
authors.initials: A
authors.lastname: Peither
authors.affiliation: a FAES Farma , S.A. , Leioa-Bizkaia , Spain and.
authors.forename: Francisco
authors.initials: F
authors.lastname: Ledo
mesh_terms: D000818:Animals; D001562:Benzimidazoles / Q000008:administration & dosage / Q000633:toxicity*; D002683:Chironomidae / Q000187:drug effects; D000460:Chlorophyta / Q000187:drug effects; D003621:Daphnia / Q000187:drug effects; D004784:Environmental Monitoring / Q000379:methods*; D005260:Female; D039563:Histamine H1 Antagonists, Non-Sedating / Q000008:administration & dosage / Q000633:toxicity*; D008297:Male; D019055:No-Observed-Adverse-Effect Level; D010880:Piperidines / Q000008:administration & dosage / Q000633:toxicity*; D018570:Risk Assessment / Q000379:methods; D012722:Sewage / Q000382:microbiology; D014874:Water Pollutants, Chemical / Q000633:toxicity*; D015027:Zebrafish
chemical_list: D001562:Benzimidazoles; D039563:Histamine H1 Antagonists, Non-Sedating; D010880:Piperidines; D012722:Sewage; D014874:Water Pollutants, Chemical; C445659:bilastine
keywords: Antihistamine; biodegradability; ecotoxicology; toxicology