Polyfunctional antiallergic potencies of Д-antihistamine levocetirizine



Cite item

Full Text

Open Access Open Access
Restricted Access Access granted
Restricted Access Subscription or Fee Access

Abstract

The burden of allergic diseases worldwide is such that it represents a serious public health problem that attracts considerable efforts to identify effective and safe therapies. Antihistamines are an important part of the therapeutic options for allergic diseases. Levocetirizine is the R-enantiomer of cetirizine with pharmacokinetically and pharmacodynamically favourable characteristics. It is a potent inverse agonist of H 1-receptors with anti-inflammatory/anti-allergic properties. It appears to have grater in vivo H 1-receptor occupancy comparatively with other 2 nd generation H 1-antihistamines. This may confer an advantageous efficacy and safety profile. clinical trials indicate that it is safe and effective for the treatment of allergic rhinitis, chronic urticaria and some other allergic conditions in adults and children with a minimal number of untoward reactions. It is also becoming clearer that, in addition to its being a potent antihistamine, levocetirizine has several anti-inflammatory/anti-allergic effects that are observed at clinically relevant concentrations that may enhance its therapeutic benefit.

Full Text

Restricted Access

About the authors

I S Gushchin

Institute of Immunology

Email: igushchin@yandex.ru
Moscow, Russia

References

  1. Church M.K., Church D.S. Pharmacology of antihistamines. Indian J. Dermatol. 2013, v. 58, p. 219-224.
  2. Staub A.M., Bovet D. Action de la thymoxyethyldiethylamine (929 F) et des ethers phenoliques sur le choc anaphylactique. C.R. Soc. Biol. 1937, v. 125, p. 818-821.
  3. Гущин И.С. Аллергическое воспаление и его фармакологический контроль. М., «Фармарус Принт». 1998, 252 с.
  4. Гущин И.С. Кардиотоксическое действие антагонистов Н1-гистаминовых рецепторов. Клинич. фармакол. и тер. 1999, № 3, с. 82-86.
  5. Church M.K., Mauer M., Simons F.E.R. et al. Risk of first-generation H1-antihistamines: a GA2LEN position paper. Allergy. 2010, v. 615, p. 459-466.
  6. Гущин И.С. Спонтанная («конститутивная») активность и обратный агонизм на Н1-рецепторах. Рос. Аллергол. Журн. 2006, № 1, с. 21-32.
  7. Criado P.R., Criadо R.F., Maruta C.W., Machado Filho C. Histamine, histamine receptors and antihistamines: new concepts. An. Bras. Dermatol. 2010, v. 85, p. 195-210.
  8. Walsh G.M. The anti-inflammatory effects of levocetirizine - are they clinically relevant or just an interesting additional effect? Allergy Asthma Clin. Immunol. 2009, v. 5: http:/www. aacijournal.com.
  9. Thomson L., Blaylock M.G., Sexton D.W. et al. Cetirizine and levocetirizine inhibit eotaxin-induced eosinophil transendothelial migration through human dermal or lung microvascular endothelial cells. Clin. Exp. Allergy. 2002, v. 32, p. 1187-1192.
  10. Wu P., Mitchel S., Walsh G.M. et al. A new antihistamine levocetirizine inhibits eosinophil adhesion to vascular cell adhesion molecule-1 under flow conditions. Clin. Exp. Allergy. 2005, v. 35, p. 1073-1079.
  11. Menzies-Gow A., Ying S., Phipps S., Kay A.B. Interactions between eotaxin, histamine and mast cells in early microvascular events associated with eosinophil recruitment to the site of allergic skin reactions in human. Clin. Exp. Allergy. 2004, v. 34, p. 1276.
  12. Giustizieri M.L., Albanesi C., Tluhr J. et al. H1-histamine receptor mediates inflammatory responses in human keratinocytes. J. Allergy Clin. Immunol. 2004, v. 114, р. 1176-2282.
  13. Jang Y.J., Wang J.H., Kim J.S. et al. Levocetirizine inhibits rhinovirus-induced ICAM-1 and cytokine expression and viral replication in airway epithelial cells. Antiviral Res. 2009, v. 81, p. 226-233.
  14. Ciprandi G., Cirillo I., Vizzaccaro A., Tosca M.A. Levocetirizine improves nasal obstruction and modulates cytokine pattern in patients with seasonal allergic rhinitis: a pilot study. Clin. Exp. Study. 2004, v. 34, p. 958-964.
  15. Mahmoud F., Arifhodzic N., Haines D., Novotney L. Levocetirizine modulates lymphocyte activation in patients with allergic rhinitis. J. Pharmacol. Sci. 2008, v. 108, p. 149-156.
  16. Garcia-Zepeda S., Estrada-Muniz E., Elizondo G. et al. Levocetirizine inhibits migration of immune cells to lymph nodes and induces Treg cells in a murine type I allergic conjunctivitis model. The Open Ophtalmology J. 2012, v. 6, p. 129-136.
  17. Гущин И.С. Обратные агонисты Н1-рецепторов как перспективные противоаллергические средства. Хим.-фарм. журн. 2010, № 1, с. 3-8.
  18. Gillard M., Strolin Benedetti M., Chatelain P., Baltes E. Histamine H1-receptor occupancy and pharmacodynamics of second generation H1-antihistamines. Inflamm. Res. 2005, v. 54, p. 367-369.
  19. Gillman S., Gillard M., Strolin Benedetti M. The concept of receptor occupancy to predict clinical efficacy: a comparison of second generation H1-antihistamines. Allergy Asthma Proc. 2009, v. 30, p. 366-376.
  20. Del Cuvillo A., Millol J., Bartra J. et al. Comparative pharmacology of H1-antihistamines. J. Investig. Allergol. Clin. Immunol. 2006, v. 16, p. 3-12.
  21. Warner J.O., ETAC Study Group. A double blind, randomized, placebo-controlled trial of cetirizine in preventing the onset of asthma in children with atopic dermatitis: 18 months’ treatment and 18 months’ posttreatment follow-up. J. Allergy Clin. Immunol. 2001, v. 108, p. 929-937.
  22. Dharmage S.C., Lowe A.J., Matheson M.C. et al. Atopic dermatitis and the atopic march revisited. Allergy. 2014, v. 69, p. 17-27.
  23. Simons F.E.R. On behalf of the Early Prevention of Asthma in Atopic Children (EPAAC) Study Group. Safety of levoceti-rizine treatment in young atopic children: An 18-month study. Pediatr. Allergy Immunol. 2007, v. 18, p. 535-542.
  24. Simons F.E. Early Prevention of Asthma in Atopic Children Study Group. H1-antihistamine treatment in young atopic children: effect on urticaria. Ann. Allergy Asthma Immunol. 2007, v. 99, p. 261-266.
  25. Астафьева Н.Г., Борзова Е.Ю., Горячкина Л.А. и соавт. Российский национальный согласительный документ «Крапивница и ангиоотек». Рекомендации для практических врачей. Под ред. И.С. Гущина, Н.И. Ильиной. М., «Фармарус Принт Медиа». 2007, 128 с.
  26. Singh-Franco D., Ghin H.L., Robles G.I. et al. Levocetirizine for the treatment of allergic rhinitis and chronic idiopathic urticaria in adults and children. Clin. Therap. 2009, v. 31, p. 1664-1687.
  27. Patel J.G., Modi A.D. Formulation, optimization and evaluation of levocetirizine dihydrochloride oral thin strip. J. Pharm. Bioallied Sci. 2012, v. 4, p. 35-36.
  28. Choudhary D.R., Patel V.A., Chhalotiya U.K. et al. Development and characterization of pharmacokinetic parameters of fast-dissolving films containing levocetirizine. Sci. Pharm. 2012, v. 80, p. 779-787.
  29. Comparative bioavailability study of levocetirizine film-coated 5 mg tablets (EGIS Pharmaceuticals PLC, Hungary) vs. Xyzal film-coated 5 mg tablets (UCB Pharma S.p.a. Italy) in healthy male Caucasian non-smoking volunteers under fasting conditions. - Final Study report. EGIS Doc. No.: 17141/I-V/A.
  30. Note for Guidance on the Investigation of Bioavailability and bioequivalence CPMP/EWP/QWP/1401/98.
  31. Devalia J.L., De Vos C., Hanotte F., Baltes E. A randomized, double-blind, crossover comparison among cetirizine, levocetirizine, and ucb 28557 on histamine-induced cutaneous responses in healthy adult volunteers. Allergy. 2001, v. 56, p. 50-57.
  32. Grant J.A., Riethuisen J., Moulaert B., De Vos C.A. A double-blind, randomized, single-dose, crossover comparison of levocetirizine with ebastine, fexofenadine, loratadine, mizolastine, and placebo: suppression of histamine-induced wheal-and-flare response during 24 hours in healthy male subjects. Ann. Allergy Asthma Immunol. 2002, v. 88, p. 190-197.
  33. Popov T.A., Dumitrascu D., Bachvarova A. et al. A comparison of levocetirizine and desloratadine in the histamine-induced wheal and flare response in human skin in vivo. Inflamm. Res. 2006, v. 55, p. 241-244.
  34. Frossard N., Strolin-Benedetti M., Purohit A., Pauli G. Inhibition of allergen-induced wheal and flare reactions by levocetirizine and desloratadine. Br. J. Clin. Pharmacol. 2008, v. 65, p. 172-179.
  35. Karppinen A., Brummer-Korvenkortio H., Petman L. et al. Levocetirizine for treatment of immediate and delayed mosquito bite reactions. Acta Derm. Venerol. 2006, v. 86, p. 329-331.
  36. Lee D.K., Gray R.D., Wilson A.M. et al. Single and short-term dosing effects of levocetirizine on adenosine monophosphate bronchoprovocation in atopic asthma. Br. J. Clin. Pharmacol. 2004, v. 58, p. 34-39.
  37. Vaidyanathan S., Nair A., Barnes M.L. et al. Effect of levocetirizine on nasal provocation testing with adenosine monophosphate compared with allergen challenge in allergic rhinitis. Clin. Exp. Allergy. 2009, v. 39, p. 409-416.
  38. Walsh G.M. A review of the role of levocetirizine as an effective therapy for allergic disease. Expert Opin. Pharmacother. 2008, v. 9, p. 859-867.
  39. Walsh G.M. Levocetirizine: an update. Curr. Med. Chem. 2006, v. 13, p. 2711-2715.
  40. Mosges R., Konig V., Koberlein J. The effectiveness of levocetirizine in comparison with loratadine in treatment of allergic rhinitis - a meta-analysis. Allergology International. 2011, v. 60, p. 541-546.
  41. Mosges R., Konig V., Koberlein J. The effectiveness of modern antihistamines for treatment of allergic rhinitis - an IPD meta-analysis of 140,853 patients. Allergology International. 2013, v. 62, p. 215-222.
  42. Patou J., De Smedt H., van Couwenberge P., Bachert C. Pathophysiology of nasal obstruction and meta-analysis of early and late effects of levoceterizine. Clin. Exp. Allergy. 2006, v. 36, p. 972-981.
  43. Yonekura S., Okamoto Y., Yamamoto H. et al. Randomized double-blind study of prophylactic treatment with antihistamine for seasonal allergic rhinitis. Int. Arch. Allergy Immunol. 2013, v. 162, p. 71-78.
  44. Nettis E., Calogiuri G.F., Di Leo E. et al. Once daily levocetirizine for the treatment of allergic rhinitis and chronic idiopathic urticaria. J. Asthma and Allergy. 2009, v. 2, p. 17-23.
  45. Belsito D.V. Second-generation antihistamines for the treatment of chronic idiopathic urticaria. J. Drugs Dermatol. 2010, v. 9, p. 503-511.
  46. Kapp A., Wedi B. Chronic urticaria: clinical aspects and focus on a new antihistamine, levocetirizine. J. Drugs Dermatol. 2004, v. 3, p. 632-639.
  47. Nettis E., Colanardi M.C., Barra L. et al. Levocetirizine in the treatment of chronic idiopathic urticaria: a randomized, double-blind, placebo-controlled study. Br. J. Dermatol. 2006, v. 154, p. 533-538.
  48. Kapp A., Pichler W.J. Levocetirizine is an effective treatment in patients suffering from chronic idiopathic urticaria: a randomized, double-blind, placebo-controlled, parallel, multicenter study. Int. J. Dermatol. 2006, v. 45, p. 469-474.
  49. Garg G., Thami G.P Comparative efficacy of cetirizine and levocetirizine in chronic idiopathic urticaria. J. Dermatol. Treat. 2007, v. 18, p. 23-24.
  50. Anuradha P., Maiti R., Jyothirmai J. et al. Loratadine versus levocetirizine in chronic idiopathic urticaria: a comparative study of efficacy and safety. Ind. J. Pharmacol. 2010, v. 42, p. 12-16.
  51. Potter P.C., Kapp A., Maurer M. et al. Comparison of the efficacy of levocetirizine 5 mg and desloratadine 5 mg in chronic idiopathic urticaria patients. Allergy. 2009, v. 64, p. 596-604.
  52. Zuberbier T., Oanta A., Bogacka E. et al. Comparison of the efficacy and safety of bilastine 20 mg vs levocetirizine 5 mg for the treatment of chronic idiopathic urticaria: a multi-centre, double-blind, randomized, placebo-controlled study. Allergy. 2009, v. 65, p. 516-528.
  53. Kumar S. Effect of montelukast and levocetirizine for antihistamine resistant chronic urticaria. Allergy. 2010, v. 65, p. 457-458.
  54. Staevska M., Popov T.A., Kralimarkova T. et al. The effectiveness of levocetirizine and desloratadine in up to 4 times conventional doses in difficult-to-treat urticaria. J. Allergy Clin. Immunol. 2010, v. 125, p. 676-682.
  55. O’Donnell B.F., Lawlor F., Simpson J. et al. The impact of chronic urticaria on the quality of life. Br. J. Dermatol. 1997, v. 136, p. 197-201.
  56. Richardson G.S., Roehrs T.A., Rosenthal L. et al. Tolerance to day-time sedative effects of H1-antihistamines. J. Clin. Psychopharmacol. 2002, v. 22, p. 511-515.
  57. Verster J.C., Volkerts E.R. Antihistamines and driving ability: evidence from on-the-road driving studies during normal traffic. Ann. Allergy Asthma Immunol. 2004, v. 92, p. 294-303.
  58. Garcia-Gea C., Martinez-Colomer J., Antonijoan R.M. et al. Comparison of peripheral and central effects of single and repeated oral dose administrations of bilastine, a new H1-antihistamine: a dose-range study in healthy volunteers with hydroxyzine and placebo as control treatments. J. Clin. Psychopharmacol. 2008, v. 28, p. 675-685.
  59. Середенин С.Б. Лекции по фармакогенетике. М., «МИА». 2004, 303 с.
  60. Сычев Д.А., Раменская Г.В., Игнатьев И.В., Кукес В.Г. Клиническая фармакогенетика. Под ред. В.Г Кукеса, Н.П. Бочкова. М., «ГЭОТАР-Медиа». 2007, 248 с.
  61. Фридлянд Д.Г., Гущин И.С., Порошина Ю.А. Индивидуализация выбора Н1-антагонистов для лечения аллергического ринита. Аллергия, астма и клин. иммунол. 2001, № 8, с. 8-17.
  62. Фридлянд Д.Г., Гущин И.С., Порошина Ю.А., Шульженко А.Е. Сравнительное изучение антигистаминной и антиаллергической активности некоторых противогистаминных препаратов. Тер. архив. 2002, № 3, с. 67-72.
  63. Ring J., Alomar A., Bieber T. et al. Guidelines for treatment of atopic eczema (atopic dermatitis). Part I. JEADY. 2012, v. 26, p. 1045-1060.
  64. Murota H., Kitaba S., Tani M. et al. Impact of sedative and non-sedative antihistamines on the impaired productivity and quality of life in patients with pruritic skin diseases. Allergology International. 2010, v. 59, p. 345-354.
  65. Елисютина О.Г., Феденко Е.С., Федоскова Т.Г., Лусс Л.В. Эффективность терапии левоцетиризином у больных с аллергодерматозами. Рос. аллергол. журн. 2012, № 5, с. 69-75.
  66. Pampura A.N., Papadopoulos N.G., Spicak V., Kurzawa R. Evidence for clinical safety, efficacy, and parent and physician perception of levocetirizine for the treatment of children with allergic disease. Int. Arch. Allergy Immunol. 2011, v. 155, p. 367-378.
  67. Ferrer M., Morais-Almeida M., Guizova M., Khanferyan R. Evaluation of treatment satisfaction in children with allergic disease treated with an antihistamine. Clin. Drug Invest. 2010, v. 30, p. 15-34.

Supplementary files

Supplementary Files
Action
1. JATS XML
Download

Copyright © Pharmarus Print Media, 2014



This website uses cookies

You consent to our cookies if you continue to use our website.

About Cookies