MODERN ANTIHISTAMINES: CHOICE IN ABUNDANCE OF DRUGS


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Abstract

The article presents the review of current data for pharmacodynamics, pharmacokinetics, clinical efficacy and side effects of new 2-nd generation antihistamines. Desloratadine (Lordestin) has the highest selectivity and affinity for the H1-receptor, has a properties of antagonist and inverse agonist, does not cross the blood-brain barrier and has minimal sedative effect. 2-nd generation drugs have antiinflammatory action that is not associated with H1-blockade and is based on suppression of the release of inflammatory mediators and suppression of cellular response (adhesion, chemotaxis, etc.). Desloratadine has favorable pharmacokinetics and the largest half-life; despite the presence of metabolism, drug interactions are absent. Clinical trials and postmarketing studies have shown high efficacy of desloratadine in relief of symptoms of allergic rhinitis and recurrent urticaria and in improvement of quality of life; drug was well tolerated.

References

  1. Devillier P, Roche N, Faisy C. Clinical pharmacokinetics and pharmacodynamics of desloratadine, fexofenadine and levocetirizine: a comparative review. Clin Pharmacokinet 2008;47(4):217-30.
  2. Simons FE. Advances in H1-antigistamines. N Eng J Med 2004;351:2203-17.
  3. Kreutner W, Hey JA, Anthes J, et al. Preclinical pharmacology of desloratadine, a selective and nonsedating histamine H1 receptor antagonist. 1st communication: receptor selectivity, antihistaminic activity, and antiallergenic effects. Arzneimittelforschung 2000;50:345-52.
  4. Anthes JC, Gilchrest H, Richard C, et al. Biochemical characterization of desloratadine, a potent antagonist of the human histamine H1 receptor. Eur J Pharmacol 2002;449:229-37.
  5. Wu RL, Anthes JC, Kreutner W, et al. Desloratadine inhibits constitutive and histamine-stimulated nuclear factor-kB activity consistent with inverse agonism at the histamine H1 receptor. Int Arch Allergy Immunol 2004;135:313-8.
  6. Hayashi S, Hashimoto S. Anti-unflammatory actions of new antihistamines. Clin Exp Allergy 1999;29:1593-96.
  7. Walsh GM. The clinical relevance of the anti-inflammatory properties of antihistamines. Allergy 2000;55(60);53-61.
  8. Schroeder JT, Schleimer RP, Lichtenstein LM, et al. Inhibition of cytokine generation and mediator release by human basophils treated with desloratadine. Exp Allergy 2001;31:1369-77.
  9. Agrawal DK. Anti-inflammatory properties of desloratadine. Clin Exp Allergy 2004;34:1342-48.
  10. Bakker RA, Schoonus SBJ, Smit MJ, et al. Histamine H1-receptor activation of nuclear factor-kB: roles for Gβγ- and Gα(q/11)-subunits in constitutive and agonist-mediated signaling. Mol Pharmacol 2001;60:1133-42.
  11. Liu H, Farley JM. Effects of first and second generation antihistamines on muscarinic induced mucus gland cell ion transport. BMC Pharmacology 2005;5:8.
  12. Cardelus I, Anton F, Beleta J, et al. Anticholinergic effects of desloratadine, the major metabolite of loratadine, in rabbit and guinea-pig iris smooth muscle. Eur J Pharmacol 1999;374:249-54.
  13. Lehman JM, Blaiss MS. Selecting the optimal oral antihistamine for patients with allergic rhinitis. Drugs 2006;66(18):2309-19.
  14. DuBuske LM. Review of desloratadine for the treatment of allergic rhinitis, chronic idiopatic urticaria and allergic inflammatory disorders. Expert Opin Pharmacother 2005;6(14):2511-23.
  15. Golightly LK, Greos LS. Second-generation antihistamines: actions and efficacy in the management of allergic disorders. Drugs 2005;65(3):341-84.
  16. Day JH, Briscoe MP, Rafeiro E, et al. Comparative clinical efficacy, onset and duration of action of levocetirizine and desloratadine for symptoms of seasonal allergic rhinitis in subjects evaluated in the Environmental Exposure Unit (EEU). Int J Clin Pract 2004;58:109-18.
  17. Timmerman H. Why are non-sedating antihistamines non-sedating? Clin Exp Allergy 1999;29(3):13-8.
  18. Chen C, Hanson E, Watson JW, et al. P-glycoprotein limits the brain penetration of nonsedating but not sedating H1-antagonists. Drug Metab Dispos 2003;31(3):312-8.
  19. Layton D, Wilton LV, Boshier A, et al. Comparison of the risk of drowsiness and sedation between levocetirizine and desloratadine: a prescription-event monitoring study in England. Drug Saf 2006;29:897-909.
  20. Wilken JA, Kane RL, Ellis AK, et al. A comparison of the effect of diphenhydramine and desloratadine on vigilance and cognitive function during treatment of ragweed-induced allergic rhinitis. Ann Allergy Asthma Immunol 2003;91:375-85.
  21. Shedden A. Impact of nasal congestion on quality of life and work productivity in allergic rhinitis: findings from a large online survey. Threat Respir Med 2005;4:439-46.
  22. Bachert C. A Review of the efficacy of desloratadine, fexofenadine, and levocetirizine in the treatment of nasal congestion in patients with allergic rhinitis. Clin Ther 2009;31(5):921-44.
  23. Canonica GW, Tarantini F, Compalati E, et al. Efficacy of desloratadine in the treatment of allergic rhinitis: A meta-analysis of randomized, double-blind, controlled trials. Allergy 2007;62:359-66.
  24. Bousquet J, Khaltaev N, Cruz AA, et al, for the World Health Organization, GA(2)LEN, and AllerGen. Allergic Rhinitis and its Impact on Asthma (ARIA) 2008 update (in collaboration with the World Health Organization, GA(2)LEN and AllerGen). Allergy 2008;63(86):8-160.
  25. O'Donnell BF, Lawlor F, Simpson J, et al. The impact of chronic urticaria on the quality of life. Br J Dermatol 1997;136(2):197-201.
  26. DuBuske L. Desloratadine for chronic idiopathic urticaria: a review of clinical efficacy. Am J Clin Dermatol 2007;8(5):271-83.
  27. Ring J, Hein R, Gauger A, et al. for the Desloratadine Study Group. Once-daily desloratadine improves the signs and symptoms of chronic idiopathic urticaria: a randomized, double-blind, placebo-controlled study. Int J Dermatol 2001;40(1):72-76.
  28. Lachapelle JM, Decroix J, Henrijean A, et al. Desloratadine 5 mg once daily improves the quality of life of patients with chronic idiopathic urticaria. J Eur Acad Dermatol Venereol 2006;20(3):288-92.
  29. Bachert C, Maurer M. Safety and efficacy of desloratadine in subjects with seasonal allergic rhinitis or chronic urticaria results of four postmarketing surveillance studies. Clin Drug Investig 2010;30(2):109-22.

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