nach oben

Erschienen in:

09.05.2014 | Übersicht

Rupatadin — Wirksamkeit und Sicherheit eines nichtsedierenden Antihistaminikums mit PAF-antagonisierender Wirkung

verfasst von: Soja Shamizadeh, Knut Brockow, Prof. Dr. Dr. Johannes Ring

Erschienen in: Allergo Journal | Ausgabe 3/2014

Einloggen, um Zugang zu erhalten

Zusammenfassung

Rupatadin ist ein modernes, nichtsedierendes H1-Antihistaminikum mit zusätzlicher, Plättchenaktivierender-Faktor (PAF)-antagonisierender Wirkung. Rupatadin ist unter den Handelsnamen Rupafin® und Urtimed® in Deutschland zur Behandlung der Rhinitis allergica und der Urtikaria für Erwachsene und Jugendliche ab zwölf Jahren zugelassen. In der folgenden Übersicht wird die bisher verfügbare Literatur zum pharmakologischen Profil und der klinischen Anwendung von Rupatadin zusammengefasst und mit konventionellen Antihistaminika verglichen. Schlussendlich werden die Nebenwirkungen, die Sicherheit sowie die Wechselwirkungen von Rupatadin betrachtet. Aufgrund des Cytochrome-P450-Metabolismus sollte eine Verabreichung von Rupatadin zusammen mit Erythromycin, Ketoconazol und Grapefruitsaft vermieden werden. In zahlreichen Studien konnte die klinische Wirksamkeit und Sicherheit von Rupatadin bei saisonaler, perennialer und persistierender Rhinitis sowie chronisch idiopathischer Urtikaria bestätigt werden.

Simons FE, Simons KJ. Histamine and H1-antihistamines: celebrating a century of progress. J Allergy Clin Immunol 2011; 128: 1139–50PubMedCrossRef

Merlos M, Giral M, Balsa D, Ferrando R, Queralt M, Puigdemont A et al. Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF). J Pharmacol Exp Ther 1997; 280: 114–21

Vuurman E, Theunissen E, Oers A van, Leeuwen C van, Jolles J. Lack of effects between rupatadine 10 mg and placebo on actual driving performance of healthy volunteers. Hum Psychopharmacol 2007; 22: 289–97PubMedCrossRef

Izquierdo I, Merlos M, García-Rafanell J. Rupatadine: a new selective histamine H1 receptor and platelet-activating factor (PAF) antagonist. A review of pharmacological profile and clinical management of allergic rhinitis. Drugs Today (Barc) 2003; 39: 451–68CrossRef

Merckle Recordati GmbH (Hrsg). Rupafin® Fachinformation; 2009

Cuvillo A del, Mullol J, Bartra J, Dávila I, Jáuregui I, Montoro J et al. Comparative pharmacology of the H1 antihistamines. J Investig Allergol Clin Immunol 2006; 16: 3–12PubMed

Katiyar S, Prakash S. Pharmacological profile, efficacy and safety of rupatadine in allergic rhinitis. Prim Care Respir J 2009; 18: 57–68PubMed

Mullol J, Bousquet J, Bachert C, Canonica WG, Gimenez-Arnau A, Kowalski ML et al. Rupatadine in allergic rhinitis and chronic urticaria. Allergy 2008; 63 (Suppl 87): 5–28PubMedCrossRef

Izquierdo I, Nieto C, Ramis J, Cooper M, Dewland P, Forn J. Pharmacokinetics and dose linearity of rupatadine fumarate in healthy volunteers. Methods Find Exp Clin Pharmacol 1997; 19 (Suppl A): 189–203

10.

Ring J. Angewandte Allergologie. 3. Aufl. München: Urban & Vogel; 2004

11.

Ring J, Brockow K, Ollert M, Engst R. Antihistamines in urticaria. Clin Exp Allergy 1999; 29 (Suppl 1): 31–7PubMedCrossRef

12.

Brockow K, Kiehn M, Riethmüller C, Vieluf D, Berger J, Ring J. Efficacy of antihistamine treatment in the prevention of adverse reactions to Hymenoptera immunotherapy: a prospective, randomized, placebo-controlled trial. J Allergy Clin Immunol 1997; 100: 458–63PubMedCrossRef

13.

Church MK. Efficacy and tolerability of rupatadine at four times the recommended dose against histamine- and platelet- activating factor-induced flare responses and ex vivo platelet aggregation in healthy males. Br J Dermatol 2010; 163: 1330–2PubMedCrossRef

14.

Queralt M, Brazís P, Merlos M, Puigdemont A. Inhibitory effects of rupatadine on mast cell histamine release and skin wheal development induced by Ascaris suum in hypersensitive dogs. Drug Development Research 1998; 44: 49–55CrossRef

15.

Merlos M, Ramis I, Balsa D, Queralt M, Brazis P, Puigdemont A. Inhibitory effect of rupatadine on TNF alpha release from human monocytes and mast cell line MHC-1. Allergy Clin Immunol 2000; 105: s62CrossRef

16.

Queralt M, Merlos M, Giral M, Puigdemont A. Dual effect of a new compound, rupatadine, on edema induced by platelet-activating factor and histamine in dogs: comparison with antihistamines and PAF antagonists. Drug Dev Res 1996; 39: 12–18CrossRef

17.

Merlos M, Balsa D, Giral M, Ferrando R, Garcia-Rafanell J, Forn J. Inhibition of rat peritoneal mast cell exocytosis by rupatadine fumarate: a study with different secretagogues. Methods Find Exp Clín Pharmacol 1997; 19 (Suppl A): 148

18.

Queralt M, Brazís P, Merlos M, De Mora F, Puigdemont A. In vitro inhibitory effect of rupatadine on histamine and TNF-α release from dispersed canine skin mast cells and the human mast cell line HMC-I. lnflamm Res 2000; 49: 355–60CrossRef

19.

Merlos M, Ramis I, Balsa D, Queralt M, Brazis P, Pugidemont A. Inhibitory effect of rupatadine on TNF-α release from human monocytes and mast cell line HMC-1. J Allergy Clin lmmunol 2000; 105 (Suppl 1): S62CrossRef

20.

Barrón S, Ramis I, Merlos M. Rupatadine inhibits the inflammatory component of allergic response: cytokine release, adhesion molecule expression and inflammatory cell recruitment. In: Proceedings of the 23rd EAACI Congress, 12–16 June 2004, Amsterdam

21.

Ramis I, Giral M, Ferrando R, Merlos M. Inhibition of PAFand LTB4-induced human neutrophil chemotaxis by rupatadine using a new fluorescent chemotaxis assay. Allergy 2000; 55 (Suppl 63): 94–5

22.

Barrón S, Roman J, Michelena P, Ramis I, Merlos M. Rupatadine inhibits cytokine production and NF-κB activity by histamine H1 receptor-dependent mechanism. Rev Rinol 2006; 6: 18

23.

Bousquet J, Van Cauwenberge P, Bachert C, Canonica GW, Demoly P, Durham R et al. Requirements for medications commonly used in the treatment of allergic rhinitis. Allergy 2003; 58: 192–7PubMedCrossRef

24.

Bousquet J, Van Cauwenberge P, Khaled NA, Bachert C, Baena-Cagnani CE, Bouchard J et al. Pharmacologic and anti-IgE treatment of allergic rhinitis (ARIA) update (in collaboration with GA2LEN). Allergy 2006; 61: 1086–96PubMedCrossRef

25.

Izquierdo I, Valero A, García O, Pérez I, Mullol J, Van Cauwenberge P. Clinical efficacy of rupatadine in allergic rhinitis under ARIA criteria: pooled analysis. Allergy Clin Immunol Int 2005; 1: 271

26.

Stuebner P, Horak F, Zieglmayer R, Arnáiz E, Leuratti C, Pérez I et al. Effects of rupatadine vs placebo on allergen-induced symptoms in patients exposed to aeroallergens in the Vienna Challenge Chamber. Ann Allergy Asthma Immunol 2006; 96: 37–44PubMedCrossRef

27.

Valero A, Bartra J, Serrano C, Donado E, Gracia O, Izquierdo I. Rupatadine reduces nasal obstruction in allergen-induced rhinitis. Allergy 2007; 62: 137–8CrossRef

28.

Izquierdo I, Paredes I, Lurigados C, Sospedra E, Cooper M, Thomas H. A dose ranging study of rupatadine fumarate in patients with seasonal allergic rhinitis. Allergy 2000; 55: 275

29.

Guadaño EM, Serra-Batlles J, Meseguer J, Castillo JA, De Molina M, Valero A et al. Rupatadine 10 mg and ebastine 10 mg in seasonal allergic rhinitis: a comparison study. Allergy 2004; 59: 766–71PubMedCrossRef

30.

Maiti R, Rahman J, Jaida J, Allala U, Palani A. Rupatadine and levocetirizine for seasonal allergic rhinitis: a comparative study of efficacy and safety. Arch Otolaryngol Head Neck Surg 2010; 136: 796–800PubMedCrossRef

31.

Martínez-Cócera C, De Molina M, Martí-Guadaño E, Pola J, Conde J, Borja J et al. Rupatadine 10 mg and cetirizine 10 mg in seasonal allergic rhinitis: A randomised, doubleblind parallel study. J Invest Allergol Clin Immunol 2005; 15: 22–9

32.

Fantin S, Maspero J, Bisbal C, Agache I, Donado E, Borja J et al. A 12-week placebo-controlled study of rupatadine 10 mg once daily compared with cetirizine 10 mg once daily, in the treatment of persistent allergic rhinitis. Allergy 2008; 63: 924–31PubMedCrossRef

33.

Saint-Martin F, Dumur JP, Pérez I, Izquierdo I. A randomized, double-blind, parallel-group study, comparing the efficacy and safety of rupatadine (20 and 10 mg), a new PAF and H1 receptor-specific histamine antagonist, to loratadine 10 mg in the treatment of seasonal allergic rhinitis. J Investig Allergol Clin Immunol 2004; 14: 34–40PubMed

34.

Maiti R, Jaida J, Rahman J, Gaddam R, Palani A. Olopatadine hydrochloride and rupatadine fumarate in seasonal allergic rhinitis: a comparative study of efficacy and safety. J Pharmacol Pharmacother 2011; 2: 270–6PubMedCentralPubMedCrossRef

35.

Perez I, De La Cruz G, Villa M, Iz-Quierdo I. Rupatadine in allergic rhinitis: pooled analysis of efficacy data. Allergy 2002; 57: 245

36.

Marmouz F, Giralt J, Izquierdo I. Morning and evening efficacy evaluation of rupatadine (10 and 20 mg), compared with cetirizine 10 mg in perennial allergic rhinitis: a randomized, double-blind, placebo-controlled trial. J Asthma Allergy 2011; 4: 27–35PubMedCentralPubMed

37.

Fantin S, Maspero J, Bisbal C, Agache I, Donado E, Borja J et al; international Rupatadine study group. A 12-week placebo-controlled study of rupatadine 10 mg once daily compared with cetirizine 10 mg once daily, in the treatment of persistent allergic rhinitis. Allergy 2008; 63: 924–31PubMedCrossRef

38.

Mion Ode G, Campos RA, Antila M, Rapoport PB, Rosario N, Mello Junior JF deet al. Futura study: evaluation of efficacy and safety of rupatadine fumarate in the treatment of persistent allergic rhinitis. Braz J Otorhinolaryngol 2009; 75: 673–9PubMedCrossRef

39.

Gimenez-Arnau A, Izquierdo I, Maurer M. The use of a responder analysis to identify clinically meaningful differences in chronic urticaria patients following placebo-controlled treatment with rupatadine 10 and 20 mg. J Eur Acad Dermatol Venereol 2009; 23: 1088–91PubMedCrossRef

40.

Gimenez-Arnau A, Pujol RM, Ianosi S, Kaszuba A, Malbran A, Poop G et al. Rupatadine in the treatment of chronic idiopathic urticaria: a double-blind, randomized, placebocontrolled multicentre study. Allergy 2007; 62: 539–46PubMedCrossRef

41.

Dubertret L, Zalupca L, Cristodoulo T, Benea V, Medina I, Fantin S et al. Once-daily rupatadine improves the symptoms of chronic idiopathic urticaria: a randomised, double- blind, placebo-controlled study. Eur J Dermatol 2007; 17: 223–8PubMed

42.

Maiti R, Jaida J, Raghavendra BN, Goud P, Ahmed I, Palani A. Rupatadine and levocetirizine in chronic idiopathic urticaria: a comparative study of efficacy and safety. J Drugs Dermatol 2011; 10: 1444–50PubMed

43.

Kim H, Lynde C. Impact of Desloratadine on symptoms and quality of life in subjects with chronic idiopathic urticaria: a multicenter, practice-based study. Arch Drug Inf 2008; 1: 63–9PubMedCentralPubMedCrossRef

44.

Metz M, Scholz E, Ferran M, Izquierdo I, Giménez-Arnau A, Maurer M. Rupatadine and its effects on symptom control, stimulation time, and temperature thresholds in patients with acquired cold urticaria. Ann Allergy Asthma Immunol 2010; 104: 86–92PubMedCrossRef

45.

Picado C. Rupatadine: pharmacological profile and its use in the treatment of allergic disorders. Expert Opin Pharmacother 2006; 7: 1989–2001PubMedCrossRef

46.

Valero A, Torre F de la, Castillo JA, Rivas P, Cuvillo A del, Antépara I et al. Safety of rupatadine administered over a period of 1 year in the treatment of persistent allergic rhinitis. Drug Safety 2009; 32: 33–42PubMedCrossRef

47.

European Medicines Agency; Committee for Medicinal Products for Human Use (CHMP), eds. Guideline on the clinical development of medicinal products for the treatment of allergic rhinoconjunctivitis. 2004; http://www.ema.europa.eu/docs/en_GB/document_library/Scientific_guideline/2009/09/WC500003554.pdf (access: January 2008)

48.

Fidan V, Fidan T. Fixed drug eruption against rupatadine fumarate. J Craniofac Surg 2011; 22: 1682–3PubMedCrossRef

49.

Dávila I, Sastre J, Bartra J, Cuvillo A del, Jáuregui I, Montoro J et al. Effect of H1 antihistamines upon the cardiovascular system. J Investig Allergol Clin Immunol 2006; 16(Suppl 1): 13–23PubMed

50.

Hove-Madsen L, Llach A, Molina CE, Prat-Vidal C, Farré J, Roura S et al. The proarrhythmic antihistaminic drug terfenadine increases spontaneous calcium release in human atrial myocytes. Eur J Pharmacol 2006; 553: 215–21PubMedCrossRef

51.

Thorn C, Pfaar O, Hörmann K, Klimek L. Rupatadin - Pharmakologie, klinische Wirksamkeit und therapeutische Sicherheit eines neuen Antihistamins mit zusätzlicher, PAFantagonisierender Wirkung. Allergologie 2010; 33: 429–40CrossRef

52.

Keam SJ, Plosker GL. Rupatadine: a review of its use in the management of allergic disorders. Drugs 2007; 67: 457–74PubMedCrossRef

53.

Giral M, Merlos M, Balsa D, Ferrando R, Garcia-Rafanell J, Forn J. Effects of rupatadine on cardiovascular profile in rats and guinea pigs: comparison with other nonsedating antihistamines. Allergy 1997; 52: 44–5CrossRef

54.

Giral M, Balsa D, Ferrando R, Merlos M, Garcia-Rafanell J, Forn J. CNS activity profile of rupatadine fumarate, a new dual receptor antagonist of platelet-activating factor (PAF) and histamine. Allergy 1998; 53: 131CrossRef

55.

Barbanoj MJ, García-Gea C, Antonijoan R, Izquierdo I, Donado E, Pérez I et al. Evaluation of the cognitive, psychomotor and pharmacokinetic profiles of rupatadine, hydroxyzine and cetirizine, in combination with alcohol, in healthy volunteers. Hum Psychopharmacol 2006; 21: 13–26PubMedCrossRef

56.

Barbanoj MJ, García-Gea C, Morte A, Izquierdo I, Pérez I, Jané F. Central and peripheral evaluation of rupatadine, a new antihistamine/platelet-activating factor antagonist, at different doses in healthy volunteers. Neuropsychobiology 2004; 50: 311–21PubMedCrossRef

57.

Jáuregui I, Mullol J, Bartra J, Cuvillo A del, Dávila I, Montoro J et al. H1 antihistamines: psychomotor performance and driving. J Investig Allergol Clin Immunol 2006; 16: 37–44PubMed

58.

Zuberbier T, Asero R, Bindslev-Jensen C, Walter Canonica G, Church MK, Giménez-Arnau A et al. EAACI/GA(2)LEN/ EDF/WAO guideline: definition, classification and diagnosis of urticaria. Allergy 2009; 64: 1417–26PubMedCrossRef

Titel: Rupatadin — Wirksamkeit und Sicherheit eines nichtsedierenden Antihistaminikums mit PAF-antagonisierender Wirkung
verfasst von: Soja Shamizadeh
Knut Brockow
Prof. Dr. Dr. Johannes Ring
Publikationsdatum: 09.05.2014
Verlag: Urban & Vogel
Erschienen in: Allergo Journal / Ausgabe 3/2014
Print ISSN: 0941-8849
Elektronische ISSN: 2195-6405
DOI: https://doi.org/10.1007/s15007-014-0555-3

Update HNO

Bestellen Sie unseren Fach-Newsletter und bleiben Sie gut informiert – ganz bequem per eMail.

Newsletter bestellen

Live-Webinar "Chronische Unterbauch- und Viszeralschmerzen in der Praxis managen"

Springer Medizin

Rupatadin — Wirksamkeit und Sicherheit eines nichtsedierenden Antihistaminikums mit PAF-antagonisierender Wirkung

Zusammenfassung

Neu im Fachgebiet HNO

Nur selten Nachblutungen nach Abszesstonsillektomie

Rezidivierender Peritonsillarabszess nach Oralsex

Endlich: Zi zeigt, mit welchen PVS Praxen zufrieden sind

Kinder mit anhaltender Sinusitis profitieren häufig von Antibiotika

Update HNO

Live-Webinar "Chronische Unterbauch- und Viszeralschmerzen in der Praxis managen"

Springer Medizin

Zusammenfassung

Bitte loggen Sie sich ein, um Zugang zu diesem Inhalt zu erhalten

Weitere Artikel der Ausgabe 3/2014

Diagnose Nahrungsmittelallergie

Allergologie im Bahnhof

Spezifische Immuntherapie: SLIT mit SCIT gleichgewichtet abgebildet

Allergologie in Klinik und Praxis

Leitlinie zu Akuttherapie und Management der Anaphylaxie

Klosterfrau-Forschungspreis: Genforschungs-Projekte zu Asthma prämiert

Neu im Fachgebiet HNO

Nur selten Nachblutungen nach Abszesstonsillektomie

Rezidivierender Peritonsillarabszess nach Oralsex

Endlich: Zi zeigt, mit welchen PVS Praxen zufrieden sind

Kinder mit anhaltender Sinusitis profitieren häufig von Antibiotika

Update HNO