Oral Availability of Bilastine

Sádaba, Belén; Gomez-Guiu, Almundena; Azanza, J. R.; Ortega, Ignacio; Valiente, Román

doi:10.1007/s40261-013-0076-y

Cited by 36 publications

(32 citation statements)

References 8 publications

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“…The drug is rapidly absorbed after oral administration with a time to maximum plasma concentration of around 1 hour following administration [ 13 ]. The mean value of bilastine oral bioavailability was found to be about 60% [ 14 ]. The maximum plasma concentration (220 ng/mL) of bilastine 20 mg was detected 1.3 hours after administration, the half time was 14.5 hours, and plasma protein binding was 84–90% [ 13 , 14 ].…”

Section: Reviewmentioning

confidence: 99%

Bilastine: new insight into antihistamine treatment

et al. 2015

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Bilastine is a new second generation H1-antihistamine recently approved for the symptomatic treatment of allergic rhinitis (AR) and chronic urticaria (CU). Bilastine epitomizes the evolution of research on antihistamines concerning both efficacy and safety. In AR treatment, a number of large controlled clinical trials documented its efficacy, as assessed by improvement of all nasal and ocular symptoms and quality of life. These outcomes show that bilastine meets current EAACI/ARIA criteria for medications used in the treatment of AR. Also in CU, the review of the literature indicates that once-daily treatment with bilastine 20 mg was effective in managing symptoms and improving patient’s quality of life. Concerning safety and tolerability, the profile of bilastine is very similar to placebo and in particular the adverse effects on central nervous system are insignificant. The balance of efficacy and safety of bilastine is particularly helpful when dosages higher than standard are needed to control the symptoms, as frequently occurs in patients with urticaria, in whom antihistamines doses up to four times the standard dose may be administered.

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Section: Reviewmentioning

confidence: 99%

Bilastine: new insight into antihistamine treatment

et al. 2015

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“…Absorption of bilastine is rapid and proportional to dose, with its oral bioavailability being reduced by foods and grapefruit juice [1]. Absolute oral bioavailability of bilastine is 60.67 % [2]. No accumulation pattern was shown for bilastine after repeated dosing in a 14-day PK study of escalating daily doses from 10 to 100 mg [3].…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics, Pharmacodynamics and Population Pharmacokinetic/Pharmacodynamic Modelling of Bilastine, a Second-Generation Antihistamine, in Healthy Japanese Subjects

Togawa

Yamaya

Rodríguez³

et al. 2016

Clin Drug Investig

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Background and objectivesBilastine is a novel second-generation antihistamine for the symptomatic treatment of allergic rhinitis and urticaria. The objective of this study was to evaluate the pharmacokinetics, pharmacodynamics, and tolerability of bilastine following single and multiple oral doses in healthy Japanese subjects. The pharmacokinetic and pharmacodynamic profiles were compared with those reported in Caucasian subjects.MethodsIn a single-blind, randomized, placebo-controlled, parallel-group, single- and multiple-ascending dose study, bilastine tablets were administered at single doses of 10, 20, and 50 mg (Part I), and once daily for 14 days at 20 and 50 mg (Part II).ResultsAfter single oral doses, maximum plasma concentrations (C max) were reached at 1.0–1.5 h postdose. Plasma exposure [C max and area under the plasma concentration-time curve (AUC)] increased dose-proportionally at single doses of 10–50 mg. In repeated-dose administration, no remarkable differences were observed between Day 1 and Day 14 for C max or AUC. For inhibitory effects on wheal and flare response, bilastine 20 and 50 mg showed significant inhibition from 1.5 h after administration as compared with placebo, and the significant effect persisted for 24 h after administration. The rates of adverse events (AEs) were comparable between bilastine and placebo in both Part I and Part II. In addition, no dose- or administration period-dependent tendency of increase in rate of AEs or worsening of severity was observed.ConclusionBilastine exhibits similar single- and multiple-dose pharmacokinetic and pharmacodynamic characteristics in healthy Japanese subjects compared with those observed in Caucasian subjects in previous studies.Electronic supplementary materialThe online version of this article (doi:10.1007/s40261-016-0447-2) contains supplementary material, which is available to authorized users.

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“…Bilastine is administered orally once daily. It is rapidly absorbed after oral administration, achieving maximum plasma concentrations after 1-1.5 hours 12,15,16 . Concurrent food intake reduces the bioavailability of bilastine.…”

Section: Bilastine: Pharmacological Profilementioning

confidence: 99%

“…Once steady-state was reached at 4 days, food had no significant effect on the wheal response at any time 17 . Mean oral bioavailability is about 60% and it is 84-90% bound to plasma proteins 12,16,18 . It does not undergo significant hepatic metabolism and approximately 95% is excreted unchanged in either the faeces (67%) or urine (33%) 19 .…”

Section: Bilastine: Pharmacological Profilementioning

confidence: 99%

Bilastine: a lifetime companion for the treatment of allergies

Church

Tiongco-Recto

Ridolo

et al. 2019

Current Medical Research and Opinion

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Objective: Bilastine is a potent and highly selective H 1 -antihistamine approved for the treatment of allergic rhinoconjunctivitis and urticaria. This article summarizes available data on the use of bilastine in the treatment of allergic disorders in different age groups, including younger and older adults, and school-age children and adolescents. Methods: A PubMed literature search ("bilastine") was conducted on 25 February 2019. Additional literature known to the authors and identified from the reference lists of cited publications was included. Results: Bilastine is administered orally at a dose of 20 mg once daily in adults and adolescents aged 12 years and 10 mg once daily in children aged 6 to <12 years. Clinical trials have demonstrated its efficacy at improving nasal and ocular symptoms in patients with allergic rhinitis, and wheals and itching in patients with urticaria. It has a rapid onset of action and long duration of action. Bilastine does not undergo significant metabolism and does not interact with the CYP450 system, which limits its potential for drug-drug interactions. No dosage adjustments are required in patients with renal or hepatic impairment, or in the elderly. Bilastine is generally well tolerated, even when administered at above-standard doses. It does not exhibit anticholinergic effects or cardiotoxic effects, shows no central nervous system penetration and has minimal sedative properties. It has been shown to improve health-related quality of life. Conclusions: Bilastine is a suitable option for the treatment of patients with allergic rhinoconjunctivitis or urticaria across age groups from school-age children to elderly patients.

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Oral Availability of Bilastine

Abstract: The absorption of bilastine after oral administration to healthy subjects was rapid. The absolute oral bioavailability was moderate.

Cited by 36 publications

References 8 publications

Bilastine: new insight into antihistamine treatment

Bilastine: new insight into antihistamine treatment

Pharmacokinetics, Pharmacodynamics and Population Pharmacokinetic/Pharmacodynamic Modelling of Bilastine, a Second-Generation Antihistamine, in Healthy Japanese Subjects

Bilastine: a lifetime companion for the treatment of allergies

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