, Volume 66, Issue 18, pp 2309–2319 | Cite as

Selecting the Optimal Oral Antihistamine for Patients with Allergic Rhinitis

Therapy In Practice


Allergic rhinitis (AR) is now recognised as a global health problem that affects 10–30% of adults and up to 40% of children. Each year, millions of patients seek treatment from their healthcare provider. However, the prevalence of AR maybe significantly underestimated because of misdiagnosis, under diagnosis and failure of patients to seek medical attention. In addition to the classical symptoms such as sneezing, nasal pruritus, congestion and rhinorrhoea, it is now recognised that AR has a significant impact on quality of life (QOL). This condition can lead to sleep disturbance as a result of nasal congestion, which leads to significant impairment in daily activities such as work and school. Traditionally, AR has been subdivided into seasonal AR (SAR) or perennial AR (PAR). SAR symptoms usually appear during a specific season in which aeroallergens are present in the outdoor air such as tree and grass pollen in the spring and summer and weed pollens in the autumn (fall); and PAR symptoms are present year-round and are triggered by dust mite, animal dander, indoor molds and cockroaches. Oral histamine H1-receptor antagonists (H1 antihistamines) are one of the most commonly prescribed medications for the treatment of AR. There are several oral H1 antihistamines available and it is important to know the pharmacology, such as administration interval, onset of action, metabolism and conditions that require administration adjustments. When prescribing oral H1 antihistamines, the healthcare provider must take into account the clinical efficacy and weigh this against the risk of adverse effects from the agent. In addition to the clinical efficacy, potential for improvement in QOL with a particular treatment should also be considered.


  1. 1.
    Dykewicz MS, Fineman S, Skoner DP, et al. Diagnosis and management of rhinitis: complete guidelines of the Joint Task Force on Practice Parameters in Allergy, Asthma and Immunology. American Academy of Allergy, Asthma and Immunology. Ann Allergy Asthma Immunol 1998 Nov; 81 (5): 478–518PubMedCrossRefGoogle Scholar
  2. 2.
    Gandhi RK, Blaiss MS. Current concepts and therapeutic strategies for allergic rhinitis. Otorinolaringol 2005; 55 (3): 187–201Google Scholar
  3. 3.
    Skoner DP. Allergic rhinitis: definition, epidemiology, pathophysiology, detection, and diagnosis. J Allergy Clin Immunol 2001 Jul; 108 (1): S2–8PubMedCrossRefGoogle Scholar
  4. 4.
    Bousquet J, Neukirch F, Bousquet PJ, et al. Severity and impairment of allergic rhinitis in patients consulting in primary care. J Allergy Clin Immunol 2006 Jan; 117 (1): 158–62PubMedCrossRefGoogle Scholar
  5. 5.
    Bousquet J, Van Cauwenberge P, Khaltaev N. Allergic rhinitis and its impact on asthma. J Allergy Clin Immunol 2001 Nov; 108 Suppl. 5: S147–334PubMedCrossRefGoogle Scholar
  6. 6.
    Leynaert B, Neukirch C, Laird R, et al. Quality of life in allergic rhinitis and asthma: a population-based study of young adults. Am J Respir Crit Care Med 2000 Oct; 162 (4): 1391–6PubMedGoogle Scholar
  7. 7.
    Craig TJ, McCann JL, Gurevich F, et al. The correlation between allergic rhinitis and sleep disturbance. J Allergy Clin Immunol 2004 Nov; 114 (5): S139–45PubMedCrossRefGoogle Scholar
  8. 8.
    Huse DM, Hartz SE, Russell MW, et al. Allergic rhinitis may worsen asthma symptoms in children: the international asthma outcomes registry [abstract]. Am J Respir Crit Care Med 1996; 153: A860Google Scholar
  9. 9.
    Corren J, Adinoff AD, Irvin CG. Changes in bronchial responsiveness following nasal provocation with allergen. J Allergy Clin Immunol 1992; 89: 611–8PubMedCrossRefGoogle Scholar
  10. 10.
    Corren J. Allergic rhinitis and asthma: how important is the link? J Allergy Clin Immunol 1997; 99: S781–6PubMedCrossRefGoogle Scholar
  11. 11.
    Blaiss M. Current concepts and therapeutic strategies for allergic rhinitis in school-age children. Clin Ther 2004; 26 (11): 1876–89PubMedCrossRefGoogle Scholar
  12. 12.
    Naclerio RM. Allergic rhinitis. N Engl J Med 1991 Sep; 325 (12): 860–9PubMedCrossRefGoogle Scholar
  13. 13.
    Meltzer EO. Evaluation of the optimal oral antihistamine for patients with allergic rhinitis. Mayo Clin Proc 2005 Sep; 80 (9): 1170–6PubMedCrossRefGoogle Scholar
  14. 14.
    Naclerio RM, Proud D, Togias AG, et al. Inflammatory mediators in late antigen-induced rhinitis. N Engl J Med 1985 Jul; 313 (2): 65–70PubMedCrossRefGoogle Scholar
  15. 15.
    Bascom R, Pipkorn U, Lichtenstein LM, et al. The influx of inflammatory cells into nasal washings during the late response to antigen challenge: effect of systemic steroid pretreatment. Am Rev Respir Dis 1988; 138: 406–12PubMedGoogle Scholar
  16. 16.
    Ash ASF, Schild HO. Receptors mediating some actions of histamine. Br J Pharmacol 1966; 27: 427–39Google Scholar
  17. 17.
    Simons FER, Simons KJ. The pharmacology and use of H1-receptor-antagonist drags. N Engl J Med 1994; 330: 1663–70PubMedCrossRefGoogle Scholar
  18. 18.
    Anthes J, Eckel S, Richard C, et al. Characterization of [3H] desloratadine at the human H1 receptor [abstract no. 526]. J Allergy Clin Immunol 2001; 107 Suppl. 2: 160CrossRefGoogle Scholar
  19. 19.
    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: 229–37PubMedCrossRefGoogle Scholar
  20. 20.
    Snyder SH, Snowman AM. Receptor effects of cetirizine. Ann Allergy 1987; 59 (6 Pt 2): 4–8PubMedGoogle Scholar
  21. 21.
    Weiland K, Ter Laak AM, Smit MJ, et al. Mutational analysis of the antagonist-binding site of the histamine H1 receptor. J Biol Chem 1999; 274: 29994–30000CrossRefGoogle Scholar
  22. 22.
    Bakker RA, Schoonus SB, Smit MJ, et al. Histamine H1-receptor activation of nuclear factor-kappa B: roles for G beta gamma- and G alpha(q/11)-subunits in constitutive and agonist-mediated signaling. Mol Pharmacol 2001; 60: 1133–42PubMedGoogle Scholar
  23. 23.
    Leurs R, Church MK, Taglialatela M. H1-antihistamines: inverse agonism, anti-inflammatory actions and cardiac effects. Clin Exp Allergy 2002; 32: 489–98PubMedCrossRefGoogle Scholar
  24. 24.
    Rimmer SJ, Church MK. The pharmacology and mechanisms of action of histamine H1-antagonists. Clin Exp Allergy 1990 Aug; 20 Suppl. 2: 3–17PubMedCrossRefGoogle Scholar
  25. 25.
    Naclerio RM. The effect of antihistamines on the immediate allergic response: a comparative review. Otolaryngol Head Neck Surg 1993 Jun; 108 (6): 723–30PubMedGoogle Scholar
  26. 26.
    Ciprandi G, Passalacqua G, Canonica GW. Effects of H1 antihistamines on adhesion molecules: a possible rationale for long-term treatment. Clin Exp Allergy 1999; 29 Suppl. 3: 49–53PubMedGoogle Scholar
  27. 27.
    Schroeder JT, Schleimer RP, Lichtenstein LM, et al. Inhibition of cytokine generation and mediator release by human basophils treated with desloratadine. Clin Exp Allergy 2001; 31: 1369–77PubMedCrossRefGoogle Scholar
  28. 28.
    Kay GG. The effects of antihistamines on cognition and performance. J Allergy Clin Immunol 2000 Jun; 105 (6): S622–7PubMedCrossRefGoogle Scholar
  29. 29.
    van Cauwenberge P, Bachert C, Passalacqua G, et al. European Academy of Allergology and Clinical Immunology. Consensus statement on the treatment of allergic rhinitis. Allergy 2000; 55: 116–34PubMedCrossRefGoogle Scholar
  30. 30.
    International Rhinitis Management Working Group. International Consensus Report on the diagnosis and management of rhinitis. Allergy 1994; 49 Suppl. 19: 1–34Google Scholar
  31. 31.
    Passalacqua G, Bousquet J, Bachert C, et al. The clinical safety of H1-receptor antagonists: an EAACI position paper. Allergy 1996 Oct; 51 (10): 666–75PubMedGoogle Scholar
  32. 32.
    Simons FER, Simons KJ. Clinical pharmacology of new histamine H1 receptor antagonists. Clin Pharmacokinet 1999; 36: 329–52PubMedCrossRefGoogle Scholar
  33. 33.
    Baltes E, Coupez R, Giezek H, et al. Absorption and disposition of levocetirizine, the eutomer of cetirizine, administered alone or as cetirizine to healthy volunteers. Fundam Clin Pharmacol 2001; 15: 269–77PubMedCrossRefGoogle Scholar
  34. 34.
    Simons FER, Simons KJ. Peripheral H1-blockade effect of fexofenadine. Ann Allergy Asthma Immunol 1997; 79: 530–2PubMedCrossRefGoogle Scholar
  35. 35.
    Simons FER. Advances in H1-antihistamines. N Engl J Med 2004 Nov; 351 (21): 2203–17PubMedCrossRefGoogle Scholar
  36. 36.
    Hindmarch I, Johnson S, Meadows R, et al. The acute and subchronic effects of levocetirizine, cetirizine, loratadine, promethazine and placebo on cognitive function, psychomotor performance, and weal and flare. Curr Med Res Opin 2001; 17: 241–55PubMedGoogle Scholar
  37. 37.
    van Steekelenburg J, Clement PAR, Beel MHL. Comparison of five new antihistamines (H1-receptor antagonists) in patients with allergic rhinitis using nasal provocation studies and skin tests. Allergy 2002 Apr; 57: 346–50PubMedCrossRefGoogle Scholar
  38. 38.
    Geha RS, Meltzer EO. Desloratadine: a new nonsedating, oral antihistamine. J Allergy Clin Immunol 2001 Apr; 107: 751–62PubMedCrossRefGoogle Scholar
  39. 39.
    Simons FER, Silver NA, Gu X, et al. Skin concentrations of H1-receptor antagonists. J Allergy Clin Immunol 2001; 107: 526–30PubMedCrossRefGoogle Scholar
  40. 40.
    Passalacqua G, Canonica GW. A review of evidence from comparative studies of levocetirizine and desloratadine for symptoms of allergic rhinitis. Clin Ther 2005 Jul; 27 (7): 979–92PubMedCrossRefGoogle Scholar
  41. 41.
    Du Buske LM. Clinical comparison of histamine H1-receptor antagonist drags. J Allergy Clin Immunol 1996 Dec; 98 (6 Pt 3): S307–18PubMedCrossRefGoogle Scholar
  42. 42.
    Golightly LK, Greos LS. Second-generation antihistamines: actions and efficacy in the management of allergic disorders. Drugs 2005; 65 (3): 341–84PubMedCrossRefGoogle Scholar
  43. 43.
    Blaiss MS. Quality of life in allergic rhinitis. Ann Allergy Asthma Immunol 1999; 83: 449–54PubMedCrossRefGoogle Scholar
  44. 44.
    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 Units (EEU). Int J Clin Pract 2004; 59: 109–18CrossRefGoogle Scholar
  45. 45.
    Meltzer EO, Weiler JM, Widlitz MD. Comparative outdoor study of the efficacy, onset and duration of action, and safety of cetirizine, loratadine, and placebo for seasonal allergic rhinitis. J Allergy Clin Immunol 1996; 97: 617–6PubMedCrossRefGoogle Scholar
  46. 46.
    Ciprandi G, Passalacqua G, Mincarini M, et al. Continuous versus on demand treatment with cetirizine for allergic rhinitis. Ann Allergy Asthma Immunol 1997; 79: 507–11PubMedCrossRefGoogle Scholar
  47. 47.
    Ciprandi G, Tosca M, Ricca V, et al. Cetirizine treatment of rhinitis in children with pollen allergy: evidence of its antiallergic activity. Clin Exp Allergy 1997; 27: 1160–6PubMedCrossRefGoogle Scholar
  48. 48.
    Pearlman DS, Lumry WR, Winder JA, et al. Once-daily cetirizine effective in the treatment of seasonal allergic rhinitis in children aged 6 to 11 years: a randomized, double-blind, placebo-controlled study. Clin Pediatr 1997; 36: 209–15CrossRefGoogle Scholar
  49. 49.
    Sabbah A, Daele J, Wade AG, et al. Comparison of the efficacy, safety, and onset of action of mizolastine, cetirizine, and placebo in the management of seasonal allergic rhinoconjunctivitis. Ann Allergy Asthma Immunol 1999; 83: 319–25PubMedCrossRefGoogle Scholar
  50. 50.
    Murray JJ, Nathan RA, Bronsky EA, et al. Comprehensive evaluation of cetirizine in the management of seasonal allergic rhinitis: impact on symptoms, quality of life, productivity, and activity impairment. Allergy Asthma Proc 2002; 23: 391–8PubMedGoogle Scholar
  51. 51.
    Noonan MJ, Raphael GD, Nayak A, et al. The health-related quality of life effects of once-daily cetirizine HCl in patients with seasonal allergic rhinitis: a randomized double-blind, placebo-controlled trial. Clin Exp Allergy 2003; 33: 351–8PubMedCrossRefGoogle Scholar
  52. 52.
    Horak F, Stiibner UP, Zieglmayer R, et al. Controlled comparison of the efficacy and safety of cetirizine 10mg od and fexofenadine 120mg od in reducing symptoms of seasonal allergic rhinitis. Int Arch Allergy Immunol 2001; 125: 73–9PubMedCrossRefGoogle Scholar
  53. 53.
    Howarth PH, Stern MA, Roi L, et al. Double-blind, placebo-controlled study comparing the efficacy and safety of fexofenadine hydrochloride (120 and 180mg once daily) and cetirizine in seasonal allergic rhinitis. J Allergy Clin Immunol 1999; 104: 927–33PubMedCrossRefGoogle Scholar
  54. 54.
    Hampel F, Ratner P, Mansfield L, et al. Fexofenadine hydrochloride, 180 mg, exhibits equivalent efficacy to cetirizine, 10 mg, with less drowsiness in patients with moderate-to-severe seasonal allergic rhinitis. Ann Allergy Asthma Immunol 2003; 91: 354–61PubMedCrossRefGoogle Scholar
  55. 55.
    Day JH, Briscoe MP, Clark RH, et al. Onset of action and efficacy of terfenadine, astemizole, cetirizine, and loratadine for the relief of symptoms of allergic rhinitis. Ann Asthma Allergy Immunol 1997; 79: 163–72CrossRefGoogle Scholar
  56. 56.
    Day JH, Briscoe M, Widlitz MD. Cetirizine, loratadine, or placebo in subjects with seasonal allergic rhinitis: effects after controlled ragweed pollen challenge in an environmental exposure unit. J Allergy Clin Immunol 1998; 101: 638–45PubMedCrossRefGoogle Scholar
  57. 57.
    Nayak AS, Schenkel E. Desloratadine reduces nasal congestion in patients with intermittent allergic rhinitis. Allergy 2001; 56: 1077–80PubMedCrossRefGoogle Scholar
  58. 58.
    Salmun LM, Lorber R, Danzig M, et al. Efficacy and safety of desloratadine in seasonal allergic rhinitis [abstract no. 1123]. J Allergy Clin Immunol 2000; 104 Suppl. 1: 384–5CrossRefGoogle Scholar
  59. 59.
    Heithoff K, Meltzer EO, Mellars L, et al. Desloratadine improves quality of life in patients with seasonal allergic rhinitis [abstract no. 1121]. J Allergy Clin Immunol 2000; 104 Suppl. 1: 383–4CrossRefGoogle Scholar
  60. 60.
    Meltzer EO, Prenner BM, Nayak A. Efficacy and tolerability of once-daily 5mg desloratadine, an H1-receptor antagonist, in patients with seasonal allergic rhinitis: assessment during the spring and fall allergy seasons. Clin Drug Invest 2001; 21: 25–32CrossRefGoogle Scholar
  61. 61.
    Berger WE, Schenkel EJ, Mansfield LE, et al. Safety and efficacy of desloratadine 5mg in asthma patients with seasonal allergic rhinitis and nasal congestion. Ann Allergy Asthma Immunol 2002; 89: 485–91PubMedCrossRefGoogle Scholar
  62. 62.
    Salmun LM, Lorber R. 24-hour efficacy of once-daily desloratadine therapy in patients with seasonal allergic rhinitis. BMC Fam Pract 2002; 3: 14–20PubMedCrossRefGoogle Scholar
  63. 63.
    Wilson AM, Haggart K, Sims EJ, et al. Effects of fexofenadine and desloratadine on subjective and objective measures of nasal congestion in seasonal allergic rhinitis. Clin Exp Allergy 2002; 32: 1504–9PubMedCrossRefGoogle Scholar
  64. 64.
    Day JH, Briscoe MP, Welsh A, et al. Onset of action, efficacy, and safety of a single dose of fexofenadine hydrochloride for ragweed allergy using an environmental exposure unit. Ann Allergy Asthma Immunol 1997; 79: 533–40PubMedCrossRefGoogle Scholar
  65. 65.
    Wahn U, Meltzer EO, Finn AF, et al. Fexofenadine is efficacious and safe in children (aged 6–11 years) with seasonal allergic rhinitis. J Allergy Clin Immunol 2003; 111: 763–9PubMedCrossRefGoogle Scholar
  66. 66.
    Sussman GL, Mason J, Compton D, et al. The efficacy and safety of fexofenadine HCl and pseudoephedrine, alone and in combination, in seasonal allergic rhinitis. J Allergy Clin Immunol 1999; 104: 100–6PubMedCrossRefGoogle Scholar
  67. 67.
    Casale TB, Andrade C, Qu R. Safety and efficacy of once-daily fexofenadine HCl in the treatment of autumn seasonal allergy rhinitis. Allergy Asthma Proc 1999; 20: 193–8PubMedCrossRefGoogle Scholar
  68. 68.
    Bronsky EA, Falliers CJ, Kaiser HB, et al. Effectiveness and safety of fexofenadine, a new nonsedating H1-receptor antagonist, in the treatment of fall allergies. Allergy Asthma Proc 1998; 19: 135–41PubMedCrossRefGoogle Scholar
  69. 69.
    Meltzer EO, Casale TB, Nathan RA, et al. Once-daily fexofenadine HCl improves quality of life and reduces work and activity impairment in patients with seasonal allergic rhinitis. Ann Allergy Asthma Immunol 1999; 83: 311–7PubMedCrossRefGoogle Scholar
  70. 70.
    Bernstein DI, Schoenwetter WF, Nathan RA, et al. Efficacy and safety of fexofenadine hydrochloride for treatment of seasonal allergic rhinitis. Ann Allergy Asthma Immunol 1997; 79: 443–8PubMedCrossRefGoogle Scholar
  71. 71.
    van Cauwenberge P, Juniper EF, Meltzer EO, et al. Comparison of the efficacy, safety and quality of life provided by fexofenadine hydrochloride 120mg, loratadine 10mg and placebo administered once daily for the treatment of seasonal allergic rhinitis. Clin Exp Allergy 2000; 30: 891–9PubMedCrossRefGoogle Scholar
  72. 72.
    Mösges R, van Cauwenberg P, Purello-D’Ambrosio F, et al. Fexofenadine and loratadine exhibit rapid relief, but only fexofenadine maintains efficacy over a 2-week period [abstract no. 1005]. Allergy 2000; 55 Suppl. 63: 281Google Scholar
  73. 73.
    Ricard N, Kind P, Christian S, et al. Link between preferences and treatment outcomes in seasonal allergic rhinitis: an empiric investigation. Clin Ther 1999; 20: 268–77CrossRefGoogle Scholar
  74. 74.
    Serra HA, Alves O, Rizzo LFL, et al. Loratadinepseudoephedrine in children with allergic rhinitis, a controlled double-blind trial. Br J Clin Pharmacol 1998; 45: 147–50PubMedCrossRefGoogle Scholar
  75. 75.
    Druce HM, Thoden WR, Mure P, et al. Brompheniramine, loratadine, and placebo in allergic rhinitis: a placebo-controlled comparative trial. J Clin Pharmacol 1998; 38: 382–9PubMedGoogle Scholar
  76. 76.
    Pagliara A, Testa B, Carrupt P-A, et al. Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist. J Med Chem 1998; 41: 853–63PubMedCrossRefGoogle Scholar
  77. 77.
    Best CH, Dale HH, Dudley HW, et al. The nature of the vasodilator constituents of certain tissue extracts. J Physiol 1927; 62: 397–417PubMedGoogle Scholar
  78. 78.
    Zyrtec® (cetirizine hydrochloride) tablets and syrup: package insert. New York: Pfizer Inc., 2002Google Scholar
  79. 79.
    Mohler SR, Nicholson A, Harvey RP, et al. The use of antihistamines in safety-critical jobs: a meeting report. Curr Med Res Opin 2002; 18: 332–7PubMedCrossRefGoogle Scholar
  80. 80.
    Lai DS, Lue KH, Hsieh JC, et al. The comparison of the efficacy and safety of cetirizine, oxatomide, ketotifen, and a placebo for the treatment of childhood perennial allergic rhinitis. Ann Allergy Asthma Immunol 2002; 89: 589–98PubMedCrossRefGoogle Scholar
  81. 81.
    Burtin B, Duchateau J, Pignat JC, et al. Further improvement of quality of life by cetirizine in perennial allergic rhinitis as a function of treatment duration. Invest Allergol Clin Immunol 2000; 10: 66–70Google Scholar
  82. 82.
    Ciprandi G, Tosca MA, Cosentino C, et al. Effects of fexofenadine and other antihistamines on components of the allergic response: adhesion molecules. J Allergy Clin Immunol 2003 Oct; 112 (4 Suppl.): S78–82PubMedCrossRefGoogle Scholar
  83. 83.
    Kay GG, Berman B, Mockoviak SH, et al. Initial and steady-state effects of diphenhydramine and loratadine on sedation, cognition, mood, and psychomotor performance. Arch Intern Med 1997; 157: 2350–6PubMedCrossRefGoogle Scholar
  84. 84.
    Hindmarch I, Shamsi Z. Antihistamines: models to assess sedative properties, assessment of sedation, safety and other side-effects. Clin Exp Allergy 1999; 29 Suppl. 3: 133–42PubMedCrossRefGoogle Scholar
  85. 85.
    Bielory L, Lien KW, Bigelsen S. Efficacy and tolerability of newer antihistamines in the treatment of allergic conjunctivitis. Drugs 2005; 65 (2): 215–28PubMedCrossRefGoogle Scholar
  86. 86.
    Paolieri F, Battifora M, Riccio A, et al. Terfenadine and fexofenadine reduce in vitro ICAM-1 expression on human continuous cell lines. Ann Allergy Asthma Immunol 1998; 81: 601–7PubMedCrossRefGoogle Scholar
  87. 87.
    Allegra® (fexofenadine hydrochloride) capsules and tablets: package insert. Kansas City (MO): Aventis Pharmaceuticals Inc., 2003Google Scholar
  88. 88.
    Clarinex® (desloratadine) tablets: package insert. Kenilworth (NJ): Schering Corporation, 2002Google Scholar
  89. 89.
    Bower EA, Moore JL, Moss M, et al. The effects of single-dose fexofenadine, diphenhydramine, and placebo on cognitive performance in flight personnel. Aviat Space Environ Med 2003; 74: 145–52PubMedGoogle Scholar
  90. 90.
    Thomson L, Blaylock MG, Sexton DW, et al. Cetirizine and levocetirizine inhibit eotaxin-induced eosinophil transendothelial migration through human dermal or lung microvascular endothelial cells. Clin Exp Allergy 2002; 32: 1187PubMedCrossRefGoogle Scholar
  91. 91.
    Simons FER, Prenner BM, Finn A. Efficacy and safety of desloratadine in the treatment of perennial allergic rhinitis. J Allergy Clin Immunol 2003; 111: 617–22PubMedCrossRefGoogle Scholar
  92. 92.
    Xyzal® (levocetirizine) tablets: package insert. Brussels: UCB Pharma Ltd, 2003Google Scholar
  93. 93.
    de Blic J, Wahn U, Billard E. Levocetirizine in children: evidenced efficacy and safety in a 6-week randomized seasonal allergic rhinitis trial. Pediatr Allergy Immunol 2005 May; 16 (3): 267–75PubMedCrossRefGoogle Scholar
  94. 94.
    Lee DK, Gardiner M, Haggart K, et al. Comaprative effects of desloratadine, fexofenadine, and levocetirizine on nasal adenosine monophosphate challenge in patients with perennial allergic rhinitis. Clin Exp Allergy 2004; 34: 650–3PubMedCrossRefGoogle Scholar
  95. 95.
    Taglialatela M, Timmerman H, Annunziato L. Cardiotoxic potential and CNS effects of first-generation antihistamines. Trends Pharmacol Sci 2000; 21: 52–6PubMedCrossRefGoogle Scholar
  96. 96.
    Bockholdt B, Klug E, Schneider V. Suicide through doxylamine poisoning. Forensic Sci Int 2001; 119: 138–40PubMedCrossRefGoogle Scholar
  97. 97.
    Baker AM, Johnson DG, Levisky JA, et al. Fatal diphenhydramine intoxication in infants. J Forensic Sci 2003; 48: 425–8PubMedGoogle Scholar
  98. 98.
    Claritin® (loratadine) tablets, syrup, and rapidly-disintegrating tablets: package insert. Kenilworth (NJ): Schering Corporation, 2000Google Scholar
  99. 99.
    Timmerman H. Factors involved in the absence of sedative effects by second-generation antihistamines. Allergy 2000; 55 Suppl. 60: 5–10PubMedCrossRefGoogle Scholar
  100. 100.
    Simons FER, Fraser TG, Maher J, et al. Central nervous system effects of H1-receptor antagonists in the elderly. Ann Allergy Asthma Immunol 1999; 82: 157–60PubMedCrossRefGoogle Scholar
  101. 101.
    Simons FER, Fraser TG, Reggin JD, et al. Comparison of the central nervous system effects produced by six H1-receptor antagonists. Clin Exp Allergy 1996; 26: 1092–7PubMedCrossRefGoogle Scholar
  102. 102.
    Scharf MB, Kay G, Rikken G, et al. Desloratadine has no effect on wakefulness or psychomotor performance [abstract no. 1001]. Allergy 2000; 55 Suppl. 63: 280Google Scholar
  103. 103.
    Tashiro M, Sakurada Y, Iwabuchi K, et al. Central effects of fexofenadine and cetirizine: measurement of psychomotor performance, subjective sleepiness, and brain histamine H1-receptor occupancy using 11C-doxepin positron emission tomography. J Clin Pharmacol 2004; 44: 890–900PubMedCrossRefGoogle Scholar
  104. 104.
    Ramaekers JG, Uiterwijk MMC, O’Hanlon JF. Effects of loratadine and cetirizine on actual driving and psychometric test performance, and EEG during driving. Eur J Clin Pharmacol 1992; 42: 363–9PubMedGoogle Scholar
  105. 105.
    Vermeeren A, Ramaekers JG, O’Hanlon JF. Effects of emedastine and cetirizine, alone and with alcohol, on actual driving of males and females. J Psychopharmacol 2002; 16: 57–64PubMedCrossRefGoogle Scholar
  106. 106.
    Gengo FM, Gabos C, Mechtler L. Quantitative effects of cetirizine and diphenhydramine on mental performance measured using an automobile driving simulator. Ann Allergy 1990; 64: 520–6PubMedGoogle Scholar
  107. 107.
    Gengo FM, Gabos C. Antihistamines, drowsiness, and psychomotor impairment: central nervous system effect of cetirizine. Ann Allergy 1987; 59 (6 Pt 2): 53–7PubMedGoogle Scholar
  108. 108.
    Walsh JK, Muehlbach MJ, Schweitzer PK. Simulated assembly line performance following ingestion of cetirizine or hydroxyzine. Ann Allergy 1992; 69: 195–200PubMedGoogle Scholar
  109. 109.
    Vuurman EFPM, Rikken GH, Muntjewerff ND, et al. Effects of desloratadine, diphenhydramine, and placebo on driving performance and psychomotor performance measurements. Eur J Clin Pharmacol 2004; 60: 307–13PubMedCrossRefGoogle Scholar
  110. 110.
    Hindmarch I, Shamsi Z, Stanley N, et al. A double-blind, placebo-controlled investigation of the effects of fexofenadine, loratadine and promethazine on cognitive and psychomotor function. Br J Clin Pharmacol 1999; 48: 200–6PubMedCrossRefGoogle Scholar
  111. 111.
    Verster JC, Volkerts ER, van Oosterwijck AW, et al. Acute and subchronic effects of levocetirizine and diphenhydramine on memory functioning, psychomotor performance, and mood. J Allergy Clin Immunol 2003 Mar; 111 (3): 623–7PubMedCrossRefGoogle Scholar
  112. 112.
    Taglialatela M, Timmerman H, Annunziato L. Cardiotoxic potential and CNS effects of first-generation antihistamines. Trends Pharmacol Sci 2000; 21: 52–6PubMedCrossRefGoogle Scholar
  113. 113.
    Milne RW, Larson LA, Jorgensen KL, et al. Hepatic disposition of fexofenadine: influence of the inhibitors erythromycin and dibromosulphothalein. Pharm Res 2000; 17: 1511–5PubMedCrossRefGoogle Scholar
  114. 114.
    Ambudkar SV, Dey S, Hrycyna CA, et al. Biochemical, cellular, and pharmacological aspects of the multidrug transporter. Annu Rev Pharmacol Toxicol 1999; 39: 361–98PubMedCrossRefGoogle Scholar
  115. 115.
    Tian R, Koyabu N, Takanaga H, et al. Effects of grapefruit juice and orange juice on the intestinal efflux of P-glycoprotein substrates. Pharm Res 2002; 19: 802–9PubMedCrossRefGoogle Scholar
  116. 116.
    Dresser GK, Bailey DG, Leake BF, et al. Fruit juices inhibit organic anion transporting polypeptide-mediated drug uptake to decrease the oral availability of fexofenadine. Clin Pharmacol Ther 2002; 71: 11–20PubMedCrossRefGoogle Scholar
  117. 117.
    Hamman MA, Bruce MA, Hachner-Daniels BD, et al. The effect of rifampin administration on the disposition of fexofenadine. Clin Pharmacol Ther 2001; 69: 114–21PubMedCrossRefGoogle Scholar

Copyright information

© Adis Data Information BV 2006

Authors and Affiliations

  1. 1.Department of Pediatrics, Division of Clinical Allergy and ImmunologyUniversity of Tennessee Health Science CenterMemphisUSA

Personalised recommendations