Histamine and H1-Antihistamines in Allergic Disease, Second Edition, (Clinical Allergy and Immunology)

517 Pages·2002·1.81 MB·English

by  F. Estelle R. Simons

Histamine and H -Antihistamines
1
in Allergic Disease
Second Edition
Revised and Expanded
edited by
F. Estelle R. Simons
University of Manitoba
Winnipeg,Manitoba,Canada
Marcel Dekker, Inc. New York Basel
•
TM
Copyright ©2002 by Marcel Dekker,Inc. All Rights Reserved.
The first edition was published as Histamine and H-Receptor Antagonists in Allergic
1
Disease (MarcelDekker,1996).
ISBN:0-8247-0628-5
This bookisprintedonacid-freepaper.
Headquarters
MarcelDekker,Inc.
270 MadisonAvenue,NewYork,NY10016
tel:[phone];fax:[phone]
Eastern HemisphereDistribution
MarcelDekkerAG
Hutgasse4,Postfach 812,CH-4001 Basel,Switzerland
tel:[phone];fax:[phone]
WorldWideWeb
http://www.dekker.com
The publisher offers discounts on this book when ordered in bulk quantities. For more
information, write to Special Sales/Professional Marketing at the headquarters address
above.
Copyright 2002byMarcelDekker,Inc. AllRightsReserved.
Neitherthisbooknoranypartmaybereproducedortransmittedinanyformorbyany
means, electronic or mechanical, including photocopying, microfilming, and recording,
or by any information storage and retrieval system, without permission in writing from
the publisher.
Current printing(lastdigit):
10 9 8 7 6 5 4 3 2 1
PRINTEDINTHEUNITEDSTATESOFAMERICA
Dedicated with deepest gratitude to my father,
Francis Raymond Edward Davies
(1910–1995)

Series Introduction
Although 60 years have passed since antihistamines were first developed, new
and exciting observations are still coming forward, new antihistamines are still
being developed, and new uses for existing products are still being established.
Thus, it is timely to produce the second edition of this very successful
volumebyF.EstelleR.Simons,M.D.Dr.Simonsiswidelyconsideredtheclini-
cal expert in the use of antihistamines, and she warrants being the creator and
editorof thisusefulbook. Thisrevisededition containsnewchapters, newcon-
cepts, and information about new products. This book will be exciting reading
for those interested in the study of allergy.
Michael A. Kaliner, M.D.
v

Preface
‘‘Yetallexperienceisanarchwherethro’
Gleamsthatuntravell’dworld...’’
Tennyson
Sincethefirsteditionofthissuccessfulmedicaltextbookwaspublishedin1996,
high-levelinterestinhistamineasachemicalmediatorofinflammationhascon-
tinued,andH-antihistaminessuchascetirizine,fexofenadine,andloratadinere-
1
mainthemostwidelyusedmedicationsworldwideforallergicdisorders,particu-
larly for allergic rhinoconjunctivitis and urticaria.
Several new second-generation, nonsedating H-antihistamines have been
1
approvedforuseduringthepastfewyears.Thesemedicationsincludeebastine,
mizolastine,desloratadine,andlevocetirizine,soontobefollowedbyepinastine,
tecastemizole, and others. New topical H-antihistamine formulations such as
1
azelastine, levocabastine, ketotifen, emedastine, and olopatadine have also been
introducedforintranasalandocularuse.TwoH-antihistamines,astemizoleand
1
terfenadine, which are no longer approved by regulatory agencies due to their
potentialcardiactoxicity,havenowalmostentirelydisappearedfromthescene.
Histamine and H-Antihistamines in Allergic Disease, Second Edition,
1
RevisedandExpanded,reflectstheseimportantdevelopments.Itprovidesanup-
to-date,comprehensiveanalysisofthebenefitsofthisimportantclassofmedica-
tions, including their broad antiallergic effects, and it contrasts the excellent
safetyprofilesoftherelativelynonsedatingsecond-generationH-antihistamines
1
with those of the sedating first-generation H-antihistamines.
1
We sincerelythank thescientists and clinicianscientists who havehelped
to makethisneweditionareality—not onlyfortheir contributionsto thebook,
butalsofortheirsustainedcontributionstoimprovingtheevidencebaseforH-
1
antihistamine use in the treatment of allergic disease.
F. Estelle R. Simons
University of Manitoba
Winnipeg, Manitoba, Canada
vii

Contents
Series Introduction v
Preface vii
Contributors xi
Introduction xiii
Part I. Histamine and Histamine Receptors
1. Histamine in Health and Disease 1
M. Susana Repka-Ramirez and James M. Baraniuk
2. Histamine Receptors: Specific Ligands, Receptor Biochemistry,
and Signal Transduction 27
Remko A. Bakker, Hendrik Timmerman, and Rob Leurs
Part II. H-Antihistamines: Basic Science
1
3. Structure and Classification of H-Antihistamines and Overview
1
of Their Activities 65
Giovanni Passalacqua, G. Walter Canonica,
and Jean Bousquet
4. Antiallergic Anti-Inflammatory Effects of H-Antihistamines
1
in Humans 101
Paraya Assanasen and Robert M. Naclerio
5. Clinical Pharmacology of H-Antihistamines 141
1
F. Estelle R. Simons and Keith J. Simons
ix