Chaejin Kim, Valentina Lo Re, Monica Rodriguez, John C Lukas, Nerea Leal, Cristina Campo, Aintzane Garcia-Bea, Elena Suarez, Stephan Schmidt, Valvanera Vozmediano
CPT Pharmacometrics Syst Pharmacol . 2021 Jun 22. doi: 10.1002/psp4.12671. Online ahead of print.
Bilastine is a second-generation H1-selective antihistamine for the treatment of allergic conditions in adults and children. It has a rapid onset and a long duration of action. Its pharmacokinetic and pharmacodynamic properties are favorable for all ages, although there’s a lack of studies in older adults, who are heterogenous in different aspects, namely age, comorbidities and comedication.
The aim of this study was to assess the recommendation of the dose of bilastine in older adults.
This was done by integration of bilastine in vitro and in vivo physicochemical data from young adults and studying the effect of aging with two different approaches: a physiologically based pharmacokinetic (PBPK) model and a semi-mechanistic population pharmacokinetic model (Senescence). The PBPK model used intestinal apical efflux and basolateral influx transporters to capture the results from young adults after single IV (10 mg) and 20 mg oral doses, which supports the hypothesis of gut transporters involvement on secretion. The Senescence model was developed from a published PopPK model adding up declining functions on different physiological systems and body composition changes with age.
Both models were then qualified using data from 16 older adults, mean age 68,7 years. The PBPK model was also used to assess the dose in older people (80 years old).
Both models showed that a daily dose of 20 mg is safe and effective in older people, supporting the existing information in this age group.