The long duration of action of the second generation antihistamine bilastine coincides with its long residence time at the histamine H1 receptor

European Journal of Pharmacology

Volume 838, 5 November 2018, Pages 107-111

Full length article

Author links open overlay panelReggieBosmaaJellevan den BoraHenry F.VischeraLuisLabeagabRobLeursa

https://doi.org/10.1016/j.ejphar.2018.09.011

open access

Abstract

Drug-target binding kinetics has recently attracted considerable interest in view of the potential predictive power for in vivo drug efficacy. The recently introduced antihistamine bilastine has a long duration of in vivo drug action, which outlasts pharmacological active bilastine concentrations in blood. To provide a molecular basis for the long duration of action, we explored the kinetics of bilastine binding to the human histamine H1 receptor using [3H]mepyramine binding studies and compared its pharmacodynamics properties to the reference compounds fexofenadine and diphenhydramine, which have a long (60 ± 20 min) and short (0.41 ± 0.1 min) residence time, respectively. Bilastine shows a long drug-target residence time at the H1 receptor (73 ± 5 min) and this results in a prolonged H1 receptor antagonism in vitro (Ca2+ mobilization in Fluo-4 loaded HeLa cells), following a washout of unbound antagonist. Hence, the long residence time of bilastine can explain the observed long duration of drug action in vivo.

Article PDF

Oral immunotherapy with the ingestion of house dust mite extract in a murine model of allergic asthma

• Research
• Open Access

• Yao-Tung Wang†,
• Hsu-Chung Liu†,
• Hui-Chen Chen,
• Yen-Ching Lee,
• Tung-Chou Tsai,
• Hsiao-Ling Chen,
• Hueng-Chuen FanEmail author and
• Chuan-Mu ChenEmail author

†Contributed equally

Allergy, Asthma & Clinical Immunology201814:43

https://doi.org/10.1186/s13223-018-0269-2

Abstract

Background

Allergen-specific immunotherapy (ASIT) has the potential to modify allergic diseases, and it is also considered a potential therapy for allergic asthma. House dust mite (HDM) allergens, a common source of airborne allergen in human diseases, have been developed as an immunotherapy for patients with allergic asthma via the subcutaneous and sublingual routes. Oral immunotherapy with repeated allergen ingestion is emerging as another potential modality of ASIT. The aim of this study was to evaluate the therapeutic efficacy of the oral ingestion of HDM extracts in a murine model of allergic asthma.

Staphylococcus aureus from patients with chronic rhinosinusitis show minimal genetic association between polyp and non-polyp phenotypes

• Research article
• Open Access
• Open Peer Review
• 
  

• • 
    
• • 
    
  Jake Jervis BardyEmail author,
• Derek S Sarovich,
• Erin P Price,
• Eike Steinig,
• Steven Tong,
• Amanda Drilling,
• Judy Ou,
• Sarah Vreugde,
• Peter-John Wormald and
• Alkis J Psaltis

BMC Ear, Nose and Throat Disorders201818:16

https://doi.org/10.1186/s12901-018-0064-1

Open Peer Review reports

Abstract

Background

Staphylococcus aureus has a high prevalence in chronic rhinosinusitis (CRS) patients and is suggested to play a more etiopathogenic role in CRS patients with nasal polyps (CRSwNP), a severe form of the CRS spectrum with poorer surgical outcomes. We performed a microbial genome-wide association study (mGWAS) to investigate whether S. aureus isolates from CRS patients have particular genetic markers associated with CRS with nasal polyps (CRSwNP) or CRS without nasal polyps (CRSsNP).

Highlights of eosinophilic chronic rhinosinusitis with nasal polypsin definition, prognosis, and advancement

REVIEW ARTICLE 

Open Access

Hongfei Lou MD, PhD 

 

Nan Zhang MD, PhD 

 

Claus Bachert MD, PhD 

 

Luo Zhang MD, PhD

https://doi.org/10.1002/alr.22214

Abstract

Background

Tissue eosinophils are characteristic of inflammation in most but not all patients with chronic rhinosinusitis with nasal polyps (CRSwNP) and may be useful for defining subgroups and making treatment choices. However, no consistent diagnostic criteria for CRSwNP with eosinophilic inflammation have been established.

Bilastine safety in drivers who need antihistamines: new evidence from high-speed simulator driving test on allergic patients

Eur Rev Med Pharmacol Sci 2018; 22 (3): 820-828

DOI: 10.26355/eurrev_201802_14318

A. Demonte, M.B. Guanti, S. Liberati, A. Biffi, F. Fernando, M. Fainello, P. Pepe

Department of Surgical, Medical, Dental and Morphological Sciences with Interest in Transplant, Oncological and Regenerative Medicine; Dermatology Unit; University of Modena and Reggio Emilia, Modena, Italy. patrizia.pepe@unimore.it

---

• PHARMACOLOGY

OBJECTIVE: Bilastine is a highly selective, non-sedating antihistamine, indicated for the symptomatic treatment of allergic rhinoconjunctivitis and urticaria. Available data suggest that bilastine interferes neither with driving ability nor with flying-related performance. However, no data are available on the effect of bilastine on the driving ability in extreme conditions. Here we analyzed the effect of 7 days treatment with 20 mg bilastine in patients with allergic rhinitis and/or chronic urticaria, on psychophysical performance assessed by the Formula One (F1) high-speed simulator-driving test.

Unapproved Pharmaceutical Ingredients Included in Dietary Supplements Associated With US Food and Drug Administration Warnings

Original Investigation 

Public Health

Jenna Tucker, MPH^1,2,3; Tessa Fischer, DVM, MPH^2,3; Laurence Upjohn, PharmD³; et alDavid Mazzera, PhD³; Madhur Kumar, MS, PhD³

Author Affiliations Article Information

JAMA Network Open. 2018;1(6):e183337. doi:10.1001/jamanetworkopen.2018.3337

editorial comment i

Key Points

Question  What are the trends across adulterated dietary supplements associated with a warning released by the US Food and Drug Administration from 2007 through 2016?

Findings  In this quality improvement study, analysis of the US Food and Drug Administration warnings from 2007 through 2016 showed that unapproved pharmaceutical ingredients were identified in 776 dietary supplements, and these products were commonly marketed for sexual enhancement, weight loss, or muscle building. The most common adulterants were sildenafil for sexual enhancement supplements, sibutramine for weight loss supplements, and synthetic steroids or steroid-like ingredients for muscle building supplements, with 157 products (20.2%) containing more than 1 unapproved ingredient.

Rhinosectan® spray (containing xyloglucan) on the ciliary function of the nasal respiratory epithelium; results of an in vitro study

• Research
• Open Access

Allergy, Asthma & Clinical Immunology201814:41

https://doi.org/10.1186/s13223-018-0268-3

• Núria Piqué

and

Barbara De Servi

Abstract

Background

To assess the effects of Rhinosectan® spray, a medical device containing xyloglucan, on nasal ciliary function (in MucilAir™Nasal cells).

Practical guide for allergy and immunology in Canada 2018

Allergy, Asthma & Clinical Immunology

1. Introduction

   Introduction from the Editors

   Authors:Harold Kim, Richard Warrington and Wade Watson

   Citation:Allergy, Asthma & Clinical Immunology 2018 14(Suppl 2):48

   Published on: 12 September 2018

   • ViewFull Text
    
   • ViewPDF
2. Content Type:Review

   An introduction to immunology and immunopathology

   Beyond structural and chemical barriers to pathogens, the immune system has two fundamental lines of defense: innate immunity and adaptive immunity. Innate immunity is the first immunological mechanism for fig...

   Authors:Jean S. Marshall, Richard Warrington, Wade Watson and Harold L. Kim

   Citation:Allergy, Asthma & Clinical Immunology 2018 14(Suppl 2):49

   Published on: 12 September 2018

   • ViewFull Text
    
   • ViewPDF