Pharmacokinetic-Pharmacodynamic Modelling of the Antihistaminic (H1) Effect of Bilastine

Jauregizar, Nerea; Fuente, L de la; Lucero, Maria Luisa; Sologuren, Ander; Leal, Nerea; Rodríguez, M.

doi:10.2165/11317180-000000000-00000

Cited by 53 publications

(77 citation statements)

References 12 publications

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“… CL apparent total clearance of the drug from plasma, ka first-order absorption rate constant, Q intercompartmental clearance, Vc central compartment volume of distribution, Vp peripheral compartment volume of distribution, SEE standard error of estimate a Population pharmacokinetic parameters estimated from Japanese data in this study ( n = 45, 1022 plasma observations) b Caucasian data originated from a previous report [5] ( n = 310, 8429 plasma observations), permission obtained from Springer Science + Business Media…”

Section: Resultsmentioning

confidence: 99%

“…A mixed effects (population) PK and PK/PD model was applied starting with structures similar to the existing model for bilastine [5]. Briefly, the PK model was built first by applying a mixed effects model using Part I and II data, and a PK/PD model describing the drug effect was then developed using Part I data according to an indirect response model.…”

Section: Methodsmentioning

confidence: 99%

“…In the mass-balance study, bilastine was not significantly metabolized in humans and is largely eliminated unchanged both in urine (33.1 %) and feces (67 %) [4]. Population PK modeling with an indirect response model based on data from 310 healthy volunteers suggested that bilastine PK follows a two-compartmental model with first-order absorption and elimination [5]. …”

Section: Introductionmentioning

confidence: 99%

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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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Section: Resultsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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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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“…Plasma was separated by centrifugation and frozen at -20°C prior to determining drug concentrations by LC/MS/MS [18].…”

Section: Study Protocol and Methodsmentioning

confidence: 99%

Comparative inhibition by bilastine and cetirizine of histamine-induced wheal and flare responses in humans

Church

2011

Inflamm. Res.

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“…None of the conducted clinical trials showed any influence of bilastine on the morphology of the ECG signal and QTc interval. Thus, it could be stated that the cardiovascular safety of bilastine is very high, and the influence of the drug on morphology of the ECG signal and cardiac muscle repolarization is the same as that of placebo [10,15,[32][33][34][35][36][37][38][39][40][41][42][43][44].…”

Section: Cardiovascular Safety Of Antihistaminesmentioning

confidence: 99%

The role and choice criteria of antihistamines in allergy management – Expert opinion

Kuna

Jurkiewicz

Czarnecka‐Operacz

et al. 2017

Alergologia Polska - Polish Journal of Allergology

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A b s t r a c tAllergic diseases are the most common chronic conditions lasting throughout the patient's life. They not only cause significant deterioration in the quality of life of patients but also lead to significant absenteeism and reduced productivity, resulting in very high costs for society. Effective and safe treatment of allergic diseases is therefore one of the main challenges for public health and should be carried out by all the specialists in family medicine, internists and paediatricians in collaboration with allergists, otorhinolaryngologists and dermatologists. Antihistamines are most commonly used in the treatment of allergies. Several dozen drugs are available on the pharmaceutical market, and their generic forms are advertised widely as very effective drugs for the treatment of allergic diseases. What is the truth? What are the data from clinical trials and observational studies? Are all drugs equally effective and safe for the patient? According to a panel of experts representing various fields of medicine, inappropriate treatment of allergies can be very risky for patients, and seemingly equally acting medications may differ greatly. Therefore, a panel of experts gathered the latest data from the entire scientific literature and analysed the latest standards and recommendations prepared by scientific societies. This paper provides a summary of these studies and highlights the importance for the patient of the proper choice of drug to treat his allergies.Key words: antihistamines, bilastin, allergic rhinitis, urticaria, allergy. Which antihistamines should be chosen according to current standards and recommendations?In the last few decades the incidence of allergic diseases has grown to epidemic status. According to the current data, more than 600 million people suffer from allergic rhinitis worldwide, approximately 25% of them in Europe. In the ECAP trial (Epidemiology of Allergic Diseases in Poland) as many as 30% of respondents reported allergic rhinitis, less than 7% mentioned urticaria, but over 40% of patients had positive skin tests with common inhaled allergens (e.g. plant pollen, dust mites, mould and animal hair). Despite this huge number of patients, these data are frequently underestimated, since allergic diseases are generally believed to be trivial and non-hazardous. However, it has already been proven that allergic rhinitis, asthma and urticaria are associated with a significant socioeconomic burden all over the world -regardless of region, development level and financial status. The total cost of allergic diseases brings both reduced quality of life and also direct costs of drugs and health services as well as indirect social costs such as the absence from work; it also decreases productivity and concentration and generates learning disorders and

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Pharmacokinetic-Pharmacodynamic Modelling of the Antihistaminic (H1) Effect of Bilastine

Abstract: Pharmacokinetic and pharmacodynamic relationships of bilastine were reliably described with the use of an indirect response pharmacodynamic model; this led to an accurate prediction of the pharmacodynamic activity of bilastine.

Cited by 53 publications

References 12 publications

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

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

Comparative inhibition by bilastine and cetirizine of histamine-induced wheal and flare responses in humans

The role and choice criteria of antihistamines in allergy management – Expert opinion

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