Kurs “ Allgemeine und systematische Pharmakologie und Toxikologie”

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  • Kurs Allgemeine und systematische Pharmakologie und Toxikologie WS 2017/2018

    Seminarthema IV: Mediatoren Der Inhalt bzw. die Gliederung der Referate ist frhzeitig mit der/dem zustndigen Dozentin/en abzusprechen. Alle Referate sollten max. 15 Minuten dauern und den Einsatz von Hilfsmitteln (Powerpoint-Prsentation) umfassen. Bei Wiederverwendung von Prsentationen von Kolleginnen/en vorangegangener Seminare werden keine Creditpunkte (siehe Link "Creditpunkte") vergeben. Dr. Claudia Walliser (Pharmakologie/Toxikologie) N26-5201 500-65520/65508 Referat 1: H1-Antihistaminika (erster Termin)

    Simons, F. Estelle R. und Simons, K. J: Histamine and H1-antihistamines: Celebrating a century of progress. J Allergy Clin Immunol (2011) 128: 1139-1150.e4

    Yanai, K., Yoshikawa, T., Yanai, A., Nakamura, T., Iida, T., Leurs, R. and Tashiro, M.: The clinical pharmacology of non-sedating antihistamines. Pharmacology & Therapeutics (2017) 178: 148-156

    Dittmann, A. und Mohr, K.: H1-Antihistaminika: Pharmakologische Grundlagen der Wirkung. Pharm. Unserer Zeit (2004) 2: 100-105

    Haen, E.: Arzneiwechselwirkungen mit H1-Antihistaminika. Pharm. Unserer Zeit (2004) 2: 106-107

    Ihr Referat sollte folgende Punkte beinhalten: Wirkungen, Einsatzmglichkeiten und unerwnschte Wirkungen der H1-Antihistaminika der 1. und der 2. Generation mit Beispielen. Die Wirkungen, Nebenwirkungen und Kontraindikationen sollen anhand der pharmakodynamischen und pharmakokinetischen Eigenschaften dieser Substanzen diskutiert werden. Referat 2: Migrne (zweiter Termin)

    Antonaci, F., Ghiotto, N., Wu, S., Pucci, E. and Costa, A.: Recent advances in migraine therapy. SpringerPlus (2016) 5:637, 1-14

    Diener, H.-C.: aktuelle Leitlinie zur Therapie der Migrne (2013-2017), Deutsche Gesellschaft fr Neurologie

    Loder E.: Triptan therapy in migraine. N ENGL J MED (2010) 363: 63-70

    In Ihrem Referat sollten Sie die akute und die prophylaktische medikamentse Therapie der Migrne darstellen. Auf die Wirkungsmechanismen und Nebenwirkungen der Serotonin-Rezeptoragonisten (Triptane) sollten Sie genauer eingehen. Wann ist eine Migrneprophylaxe indiziert? Geben Sie eine kurze Zusammenfassung ber die Mglichkeiten der Migrneprophylaxe der ersten Wahl. Die Epidemiologie, Symptome und Pathogenese der Migrne sind nicht Gegenstand ihres Referates.

    Referat 3: Antileukotriene (zweiter Termin)

    Scott, J. P. and Peters-Golden, M.: Antileukotriene agents for the treatment of lung disease. Am J Respir Crit Care Med (2013) 188: 538-544

    Dahlen S-E.: Treatment of asthma with antileukotrienes: First line or last resort therapy? European Journal of Pharmacology (2006) 533: 40-56 + neueste Fachinfo zu Montelukast

    http://www.asthma.versorgungsleitlinien.de; Montelukast in der Asthma-Stufentherapie von Erwachsenen und Kindern; siehe S. 32 + 33 in der Langfassung

    In Ihrem Referat sollten Sie auf die pathophysiologischen Effekte der Leukotriene, speziell bei Asthma, eingehen. Erklren Sie die Wirkmechanismen der Antileukotriene jeweils mit Beispielen. Beschreiben Sie die Wirkungen der CysLT1-Rezeptor-Antagonisten bei der Behandlung von Asthma, die Vorteile der Kombinationstherapie und nennen Sie weitere Einsatzmglichkeiten dieser Substanzen. Die Biosynthese und der Metabolismus der Leukotriene sind nicht Gegenstand Ihres Referats.

  • Clinical reviews in allergy and immunology

    Series editors: Donald Y. M. Leung, MD, PhD, and Dennis K. Ledford, MD

    Histamine and H1-antihistamines: Celebrating a century ofprogress

    F. Estelle R. Simons, MD, FRCPC,a and Keith J. Simons, PhDb Winnipeg, Manitoba, CanadaINFORMATION FOR CATEGORY 1 CME CREDIT

    Credit can now be obtained, free for a limited time, by reading the review

    articles in this issue. Please note the following instructions.

    Method of Physician Participation in Learning Process: The corema-

    terial for these activities can be read in this issue of the Journal or online at the

    JACIWebsite:www.jacionline.org. The accompanying testsmayonlybe sub-

    mitted online at www.jacionline.org. Fax or other copies will not be accepted.

    Date of Original Release: December 2011. Credit may be obtained for

    these courses until November 30, 2013.

    Copyright Statement: Copyright 2011-2013. All rights reserved.Overall Purpose/Goal: To provide excellent reviews on key aspects of

    allergic disease to those who research, treat, or manage allergic disease.

    Target Audience: Physicians and researchers within the field of allergic


    Accreditation/Provider Statements and Credit Designation: The

    American Academy of Allergy, Asthma & Immunology (AAAAI) is ac-

    credited by the Accreditation Council for Continuing Medical Education

    (ACCME) to provide continuing medical education for physicians. The

    AAAAI designates these educational activities for a maximum of 1 AMA

    PRA Category 1 Credit. Physicians should only claim credit commensu-rate with the extent of their participation in the activity.

    List of Design Committee Members: F. Estelle R. Simons, MD,

    FRCPC, and Keith J. Simons, PhD

    Activity Objectives

    1. To understand new insights into the mechanism of action of


    2. To know when it is appropriate to use H1-antihistamines.

    3. To list the adverse effects of H1-antihistamines.

    Recognition of Commercial Support: This CME activity has not re-

    ceived external commercial support.

    Disclosure of Significant Relationships with Relevant Commercial

    Companies/Organizations: F. E. R. Simons is a member of the Uriach

    medical advisory board. K. J. Simons declares that he has no relevant con-

    flicts of interest.In this review we celebrate a century of progress since the initialdescription of the physiologic and pathologic roles of histamineand 70 years of progress since the introduction ofH1-antihistamines for clinical use. We discuss histamine andclinically relevant information about the molecular mechanismsof action of H1-antihistamines as inverse agonists (notantagonists or blockers) with immunoregulatory effects. Unlikefirst (old)generation H1-antihistamines introduced from 1942to the mid-1980s, most of the second (new)generationH1-antihistamines introduced subsequently have beeninvestigated extensively with regard to clinical pharmacology,efficacy, and safety; moreover, they are relatively free fromadverse effects and not causally linked with fatalities afteroverdose. Important advances include improved nasal andophthalmic H1-antihistamines with rapid onset of action (inminutes) for allergic rhinitis and allergic conjunctivitistreatment, respectively, and effective and safe use of high (up to4-fold) doses of oral second-generation H1-antihistamines forchronic urticaria treatment. New H1-antihistamines introducedfor clinical use include oral formulations (bilastine andFrom athe Department of Pediatrics & Child Health and the Department of Immunology,

    Faculty ofMedicine, and bthe Faculty of Pharmacy and the Department of Pediatrics &

    Child Health, Faculty of Medicine, University of Manitoba.

    Received for publication June 9, 2011; revised September 6, 2011; accepted for publica-

    tion September 7, 2011.

    Available online October 27, 2011.

    Corresponding author: F. Estelle R. Simons, MD, FRCPC, Room FE125, 820 Sherbrook

    St, Winnipeg, R3A 1R9 Manitoba, Canada. E-mail: lmcniven@hsc.mb.ca.


    2011 American Academy of Allergy, Asthma & Immunologydoi:10.1016/j.jaci.2011.09.005rupatadine), and ophthalmic formulations (alcaftadine andbepotastine). Clinical studies of H3-antihistamines withenhanced decongestant effects have been conducted in patientswith allergic rhinitis. Additional novel compounds being studiedinclude H4-antihistamines with anti-inflammatory effects inallergic rhinitis, atopic dermatitis, and other diseases.Antihistamines have a storied past and a promising future.(J Allergy Clin Immunol 2011;128:1139-50.)

    Key words: Histamine, H1-antihistamine(s), H2-antihistamine(s),H3-antihistamine(s), H4-antihistamine(s), allergic rhinitis, allergicconjunctivitis, urticaria, atopic dermatitis, cetirizine, desloratadine,fexofenadine, levocetirizine, loratadine, rupatadine, bilastine, alcaf-tadine, bepotastine

    In 2010-2011, we celebrate the centenary of the initialdescription of the physiologic and pathologic effects of histamine.In 2012, we celebrate the 70th anniversary of the introduction ofH1-antihistamines for clinical use. These and other importantevents related to histamine, histamine receptors, and H1-antihista-mines are shown in Fig 1.1-18HISTAMINE AND HISTAMINE RECEPTORSHistamine, a structurally simple chemical messenger, is a

    natural body constituent synthesized from the amino acid histi-dine by L-histidine decarboxylase, an enzyme expressed in manydifferent cell types. Histamine plays an important physiologicrole in human health, exerting its diverse effects through 4subtypes of receptors (Table I).11-18 Through the H1-receptor, it1139



    DECEMBER 2011

    1140 SIMONS AND SIMONSAbbreviations usedBBB: Blood-brain barrierCNS: Central nervous systemPET: Positron emission tomographycontributes to regulation of cell proliferation and differentiation,hematopoiesis, embryonic development, regeneration, andwound healing and plays an important role in neurotransmissionin the central nervous system (CNS). It is produced in neuronswith cell bodies in the tuberomamillary nucleus of the posteriorhypothalamus that send their axons throughout the cerebrum,cerebellum, posterior pi