[6] It is a second-generation antihistamine and takes effect by selectively inhibiting the histamine H1 receptor, preventing these allergic reactions.
[8] Bilastine was discovered by the Spanish firm FAES Farma[9] and received its first approval in the European Union in 2010 for the symptomatic treatment of allergic rhinoconjunctivitis and urticaria.
[12] Evidence has shown that bilastine is effective in treating skin and eye symptoms of allergic reactions, improving patient's quality of life.
Parameters such as quality of life and discomfort were also assessed, and in the same way the type and frequency of AE, tolerability and general safety of treatment were registered.
[17] In clinical research, bilastine has proven to be well tolerated, with an adverse events profile similar to that of placebo in healthy volunteers, patients with AR and with chronic idiopathic urticaria.
No serious adverse events were reported during the research and there were no clinically significant changes in vital signs, electrocardiography (ECG) or laboratory tests.
In different murine models, bilastine by oral route, antagonizes the effects of histamine in a dose-dependent manner, with potency similar to that of cetirizine and between 5.5 and 10 times greater than that of fexofenadine.
[8][14] Bilastine is most quickly absorbed with the absence of food, and reaches a mean peak plasma concentration of 220 ng/mL approximately 1 h after both single and multiple dosing.
[25] Bilastine has linear pharmacokinetics in the 2.5–220 mg dose range in healthy adult subjects without evidence of accumulation after 14 days of treatment.
[26] Bilastine is a peripherally selective drug, and this is thought to be due to limited brain uptake caused by binding to P-glycoprotein.
[25] Bilastine, or 2-[4-[2-[4-[1-(2-ethoxyethyl) benzimidazol-2-yl] piperidin-1-yl] ethyl] phenyl]-2-methylpropionic acid, is a molecule with a molecular weight of 463.6 daltons and a chemical structure similar to piperidinyl-benzimidazole.
[25] Clinical studies using different dosages were done on histamine-induced wheal and flare reaction over a 24-h period, compared with a single 10 mg oral dose of cetirizine.