Poly-functional anti-allergic activities of anti-histamine drug - rupatadine



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Abstract

Rupatadine is a new agent for the management of diseases with allergic inflammatory conditions. Rupatadine is a dual inhibitor of H 1- and platelet-activating factor (PAF)-receptors and possesses a broader profile of antiallergic properties inhibiting allergy target cells and secretion of different mediators involved in the early- and late-phase of allergic response. Rupatadine is a real example of poly-functional anti-allergic remedy.

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About the authors

I S Gushchin

Institute of Immunology, Moscow

Email: igushchin@yandex.ru

References

  1. Гущин И.С. Об элементах биологической целесообразности аллергической реактивности. Пат. физиол. 1979, № 4, с. 3-11.
  2. Гущин И.С., Курбачева О.М. Аллергия и аллергенспецифическая иммунотерапия. М., «Фармарус Принт Медиа». 2010, 228 с.
  3. Гущин И.С., Каминка М.Э., Дерюгин И.Л. Торможение антигистаминными препаратами нецитотоксического высвобождения гистамина из изолированных тучных клеток крыс. Бюлл. экспер. биол. 1978, № 10, с. 471-474.
  4. Гущин И.С., Зебрев А.И., Читаева В.Г. и соавт. Полифункциональные антиаллергические соединения, сочетающие антигистаминную активность со стабилизацией тучных клеток и базофилов. Хим.-фарм. журнал. 1987, № 11, с. 1313-1318.
  5. Гущин И.С. Аллергическое воспаление и его фармакологический контроль. М., «Фармарус Принт». 1998, 252 с.
  6. Beneviste J., Henson P.M., Cochrane C.G. Leukocyte-dependent histamine release from rabbit platelets. The role of IgE, basophils, and a platelet-activating factor. J. Exp. Med. 1972, v. 136, p. 1356-1377.
  7. Nasser S.M.S., Lee TH. Lipid mediators — leukotrienes, prostanoids and platelet-activating factor. In: Allergy and Allergic Diseases. Ed. by A.B. Kay. Blackwell Science. Lond. 1997, v. 1, p. 380-418.
  8. Stafforini D.M., McIntyre T.M., Zimmerman G.A., Prescott S.M. Platelet-activating factor, a pleiotrophic mediator of physiological and pathological processes. Crit. Rev. Clin. Lab. Sci. 2003, v. 40, p. 643-472.
  9. Uhlig S., Goggel R., Engel S. Mechanisms of platelet-activating factor (PAF)-mediated responses in the lung. Pharmacological Reports. 2005, v. 57, suppl., p. 206-221.
  10. Yost C.Y., Weyrich A.C., Zimmerman G.A. The platelet activating factor (PAF) signaling cascade in systemic inflammatory responses. Biochemie. 2010, v. 92, p. 692-697.
  11. Kajiwara N., Sasaki T., Bradding P. et al. Activation of human mast cells through the platelet-activating factor receptor. J.Allergy Clin. Immunol. 2010, v. 125, p. 1137-1145.
  12. Dyer K.D., Percopo C.M., Xie Z. et al. Mouse and human eosinophils degranulate in response to platelet-activating factor (PAF) and lysoPAF via a PAF-receptor-independent mechanism: evidence for a novel receptor. J. Immunol. 2010, v. 184, p. 6327-6334.
  13. Ishii S., Nagase T., Shindou H. et al. Platelet-activating factor receptor develops airway hyperresponsiveness independently of airway inflammation in a murine asthma model. J.Immunol. 2004, v. 172, p. 7095-7102.
  14. Chung K.F., Dent G., McCusker M. et al. Effect of a ginkgolide mixture (BN 52063) in antagonizing skin and platelet responses to platelet activating factor in man. Lancet. 1987, v. 1 (N 8527), p. 248-251.
  15. Roberts N.M., Page C.P., Chung K.F., Barnes P.J. Effect of PAF antagonist, BN 52063, on antigen-induced, acute, and late-onset cutaneous responses in atopic subjects. J. Allergy Clin. Immunol. 1988, v. 82, p. 236-241.
  16. Abraham W.M., Stevenson J.S., Garrido R. A possible role for PAF in allergen-induced late responses: modification by a selective antagonist. J. Appl. Physiol. 1989, v. 66, p. 2351-2357.
  17. Narita S., Asakura K. The effects of anti-PAF and other agents on the nasal symptoms in sensitized guinea pigs. Auris Nasus Larynx. 1993, v. 20, p. 175-183.
  18. Adamus W.S., Heuer H.O., Meade C.J., Schilling J.C. Inhibitory effects of the new PAF acether antagonist WEB-2086 on pharmacologic changes induced by PAF inhalation in human beings. Clin. Pharmacol. Ther. 1990, v. 47, p. 456-462.
  19. Johnson P.R., Armour C.L., Black J.L. The action of platelet activating factor and its antagonism by WEB 2086 on human isolated airways. Eur. Resp. J. 1990, v. 3, p. 55-60.
  20. Freitag A., Watson R.M., Matsos G. et al. Effect of a platelet activating factor antagonist, WEB 2086, on allergen induced asthmatic responses. Thorax. 1993, v. 48, p. 594-598.
  21. O’Connor B.J., Uden S., Carty T.J. et al. Inhibitory effect of UK74, 505, a potent and specific oral platelet activating factor (PAF) receptor antagonist, on airway and systemic responses to inhaled PAF in humans. Am. J. Resp. Crit. Care Med. 1994, v. 150, p. 35-40.
  22. Kuitert L.M., Hui K.P., Uthayarkumar S.E. et al. Effect of platelet-activating factor antagonist UK-74, 505 on the early and late response to allergen. Am. Rev. Resp. Dis. 1993, v. 147, p. 82-86.
  23. Merlos M., Giral M., Balsa D. et al. Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF). J. Pharmacol. Exp. Ther. 1997, v. 280, p. 114-121.
  24. Izquierdo I., Merlos M., Garcia-Rafanell J. Rupatadine. A new selective histamine H1-receptor and platelet-activating factor (PAF) antagonist. Drugs Today. 2003, v. 39, p. 451-468.
  25. Keam S.J., Plosker G.L. Rupatadine: a review of its use in the management of allergen disorders. Drugs. 2007, v. 67, p. 457-474.
  26. Mullol J., Bousquet J., Bachert C. et al. Rupatadine in allergic rhinitis and chronic urticaria. Allergy. 2008, v. 63 (suppl. 87), p. 5-28.
  27. Katiyar S., Prakash S. Pharmacological profile, efficacy and safety of rupatadine in allergic rhinitis. Primary Care Resp. J. 2009, v. 18, p. 57-68.
  28. Church M.K. 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, v. 163, p. 1330-1332.
  29. Srinivas N.R. Unsuspected polymorphic metabolism of rupatadine via its primary metabolite, desloratadine. Primary Care Resp. J. 2009, v. 18, p. 118-119.
  30. Solans A., Isquierdo I., Donado E. et al. Pharmacokinetic and safety profile of rupatadine when coadministered, open-label, two way, crossover, phase I study. Clin. Ther. 2008, v. 30, p. 1639-1650.
  31. Solans A., Carbo M., Pena J. et al. Influence of food on the oral bioavailability of rupatadine tablets in healthy volunteers: a single dose, randomized, open-label, two-way crossover study. Clin. Ther. 2007, v.29, p.900-908
  32. Kalokasidis K., Molyva D., Mirtsou V. et al. The effect of rupatadine on histamine-induced oedema formation and TNF-α gene expression in the rat paw. Rev. Clin. Pharmacol. Pharmacokin. Intern. Edition. 2008, v. 22, p. 173-175.
  33. Barbanoj M.J., Garcia-Gea C., Morte A. et al. Central and peripheral evaluation of rupatadine, a new antihistamine/platelet-activating factor antagonist, at different doses in healthy volunteers. Neuropsychobiology. 2004, v. 50, p. 311-321.
  34. Queralt M., Brazis 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 Dev. Res. 1998, v. 44, p. 49-55.
  35. Queralt M., Brazis P., Merlos M. et al. In vitro inhibitory effect of rupatadine on histamine and TNF α release from dispersed canine skin mast cells and human mast cell line HMC-I. Inflamm. Res. 2000, v. 49, p. 355-360.
  36. Barron S., Roman J., Michelena P. et al. Rupatadine inhibits cytokine production and NF-κB activity by histamine H1-receptor-dependent mechanism. Rev. Rinol. 2006, v. 6, p. 18.
  37. Stuebner P., Horak F., Zieglmayer R. 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, v. 96, p. 37-44.

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