Lucero María Luisa, Peither Armin, Ledo Francisco
a FAES Farma , S.A. , Leioa-Bizkaia , Spain and.
b Harlan Laboratories Ltd , Itingen , Switzerland.
Drug Chem Toxicol. 2015 Oct;38(4):460-8. doi: 10.3109/01480545.2014.992438. Epub 2015 Jan 22.
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.
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]).
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.
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.
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.
No environmental concerns exist from bilastine use in patients with allergic rhinoconjunctivitis or urticaria.
比拉斯汀是一种新型口服选择性非镇静组胺H1拮抗剂，用于对症治疗变应性鼻结膜炎和荨麻疹。欧洲药品管理局要求对所有新型人用药品进行环境风险评估（ERA）。
计算比拉斯汀在地表水中的预测环境浓度（PECsw；第一阶段ERA），并确定比拉斯汀对水生系统的影响（第二阶段[A层级]）。
使用最大日剂量（20毫克）计算比拉斯汀的PECsw，假设所有给药的比拉斯汀都释放到水生环境中。利用分子结构的辛醇/水分配系数对其持久性、生物累积性和毒性进行评估。在第二阶段（A层级），进行了快速生物降解性试验，并评估了比拉斯汀对各种水生和底栖微生物的潜在毒性。
比拉斯汀的PECsw计算值为0.1微克/升，该化合物不易生物降解。比拉斯汀对摇蚊或活性污泥的呼吸速率没有显著影响。对于绿藻，比拉斯汀的未观察到效应浓度（NOEC）为22毫克/升；比拉斯汀对斑马鱼发育或水蚤繁殖率没有影响。
比拉斯汀对斑马鱼、藻类、水蚤和活性污泥中的需氧生物的NOEC值比对计算出的PECsw值至少大130000倍。
变应性鼻结膜炎或荨麻疹患者使用比拉斯汀不存在环境问题。
