bilastine

No anticholinergic adverse events were observed in the clinical trials with bilastine.

Likewise, Bilastine 20 mg shows a safety and tolerability profile similar to placebo.

Article: Bilastine and quality of life.

Article: Effect of bilastine upon nasal obstruction.

Article: Effect of bilastine upon the ocular symptoms of allergic rhinoconjunctivitis.

Bilastine does not readily cross the blood brain barrier and is not metabolized by the liver.

Additionally, bilastine has been shown to improve quality of life, and all nasal and ocular symptoms related to allergic rhinitis.

Remarkably, 20 and 50 mg of bilastine reduced the wheal and flare reaction significantly more quickly than cetirizine.

The results of this research indicated that bilastine was at least as efficient as cetirizine in reducing histamine-mediated effects in healthy volunteers.

Preclinical data suggest the possibility of interactions between bilastine and drugs or food that are inhibitors or inducers of the P-glycoproteins.

Coadministration of bilastine and grapefruit juice (a known P-glycoprotein-mediated drug transport activator) significantly reduced bilastine systemic exposure.

Pharmacokinetic/pharmacodynamic profiles and studies in special populations indicate that bilastine as dose adjustment is not necessary in elderly patients, or in hepatic or renal insufficiency.

Preclinical investigations demonstrate the affinity and specificity of bilastine for histamine H1-receptors compared with other histamine receptors subtypes and other 30 receptors from different amines.

The clinical efficacy of bilastine in allergic rhinitis (AR) and urticaria has been assessed in 10 perfectly designed clinical assays in which over 4,600 patients were involved.

It was verified that bilastine 20 and 100 mg administered during 4 days, does not induce significant changes in the QT/QTc interval duration in any of the individuals.

Toxicity of bilastine investigated in preclinical toxicology studies in mice, rats and dogs after oral and intravenous administration showed no mortality observed after oral administration of massive doses.

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.

Likewise, coadministration of bilastine 20 mg and ketoconazol 400 mg does not produce any significant prolongation of the QT/QTc interval attributable to bilastine.

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.

In this SAR studies the daily oral administration during 14 days of bilastine 20 mg proves to have the same efficacy than the administration of cetirizine 10 mg or than the administration of desloratadine 5 mg.

Phase II and III studies on AR and urticaria (including the open-label extension phase of 12 months) do not reveal alterations in the ECG, nor significant prolongations of the QTc interval after administration of bilastine 20 mg.

In relation to its antihistamine effect, oral doses of 20 mg daily of bilastine, measured as skin wheal-and-flare surface areas for 24 h, bilastine is capable of inhibiting 50% of the surface areas - throughout the whole administration interval.

Although the tolerance profile of bilastine and levocetirizine or desloratadine were very similar, bilastine was markedly better tolerated than cetirizine in a clinical assay in SAR, with fewer adverse events in the bilastine group.