Drugs

, Volume 40, Issue 5, pp 762–781

Cetirizine

A Review of its Pharmacological Properties and Clinical Potential in Allergic Rhinitis, Pollen-Induced Asthma, and Chronic Urticaria
  • Deborah M. Campoli-Richards
  • Micaela M.-T. Buckley
  • Andrew Fitton
Drug Evaluation

Summary

Synopsis

Cetirizine, a piperazine derivative and carboxylated metabolite of hydroxyzine, is a potent histamine H1-receptor antagonist with antiallergic properties. It has marked affinity for peripheral histamine H1-receptors and, at the standard dose of 10mg daily, lacks the CNS depressant effects of standard antihistamines. In addition, it inhibits histamine release and eosinophil chemotaxis during the secondary phase of the allergic response. Results from controlled clinical trials indicate that cetirizine is an effective and well tolerated treatment of seasonal and perennial allergic rhinitis and chronic idiopathic urticaria. Cetirizine appears to be as effective as conventional dosages ofterfenadine, chlorpheniramine and hydroxyzine in relieving symptoms associated with these disorders and produces a markedly lower incidence of sedation than chlorpheniramine, hydroxyzine and several other standard antihistamines. Thus, cetirizine appears to provide a useful alternative to other ‘nonsedating’ antihistamines; cetirizine may also have a future role in the treatment of allergic asthma and certain forms of physical urticaria.

Pharmacodynamic Properties

Cetirizine demonstrates similar affinity to terfenadine for in vitro binding to peripheral histamine H1-receptors. However, it is highly selective for histamine H1-receptors, possessing less affinity than terfenadine or hydroxyzine for calcium channel receptors, adrenergic α1-, dopamine D2-, serotonin 5-HT2 receptors and muscarinic receptors. Standard tests of antihistaminic activity in animals have shown cetirizine to have greater potency on a weight-to-weight basis than other antihistamines such as clemastine, mepyramine, terfenadine and hydroxyzine. In human studies, suppression of the weal esponse to intradermally injected histamine was greater with cetirizine 10mg than with placebo, peaking at 4 to 8 hours and lasting up to 24 hours. Cetirizine 10mg had a similar potency to diphenhydramine 50mg, hydroxyzine 25mg and terfenadine 180mg, but was more potent than terfenadine 60mg with a more rapid onset and longer duration of action, more potent than loratadine 10mg, chlorpheniramine 6mg or mequitazine 5mg, and more rapid in onset than astemizole 10mg.

Cetirizine 5 to 20mg also provided a dose-dependent protective effect from bronchospasrn induced by inhaled histamine in asthmatics: a 20mg dose was superior in activity; o hydroxyzine 25mg.

Antiallergic activity has been shown in models using allergens and other inflammatory agents. Cetirizine had little effect on mast cells and the release of mediators of immediate hypersensitivity. However, eosinophil chemotaxis in response to allergens was inhibited in atopic subjects. An inhibitory effect on the responses of neutrophils and platelets in allergy has also been demonstrated in experimental models and human volunteers.

In psychomotor performance studies, cetirizine 10mg did not significantly affect subjective or objective assessments of drowsiness, or objective assessments of cognitive impairment in volunteers.

Pharmacokinetic Properties

Cetirizine is rapidly absorbed, reaching peak plasma concentrations of 257 μg/L within 1 hour of administration of 10mg oral doses to healthy volunteers (980 μg/L in children); AUC was 2.87 mg/L · h with this dose (6.37 mg/L · h in children). Plasma concentrations and AUC increase linearly with dose. Food does not affect the extent of absorption, but may slightly reduce the rate.

The volume of distribution of cetirizine at steady-state is 30 to 40L. Animal studies indicate that peak concentrations in the brain are less than 10% of plasma concentrations.

The terminal phase elimination half-life is 7 to 10 hours. Approximately 70% of a dose of cetirizine is excreted in the urine, mainly as unchanged drug, although small amounts of unidentified metabolites are found. Approximately 10% of the total dose is excreted in the faeces. The apparent total body clearance is 0.04 to 0.05 L/h/kg (0.06 to 0.07 L/h/kg in children).

In patients with even mild impairment of renal function, the terminal elimination half-life of cetirizine is increased to approximately 20 hours. Half-life is also prolonged in elderly volunteers, an effect independent of age per se, but dependent on renal function. The elimination half-life is somewhat shorter in children, being 6 to 7 hours.

Therapeutic Efficacy

A number of randomised double-blind studies, most placebo controlled and many crossover in design, have established the efficacy of cetirizine 5mg to 20mg daily in the treatment of seasonal and perennial allergic rhinitis, and chronic idiopathic urticaria. In addition, several reports suggest a role for cetirizine 15 to 20mg daily, administered in 2 divided doses, in the treatment of pollen-associated asthma in atopic individuals. Comparisons with other histamine H1-receptor antagonists generally indicate similar symptomatic control, as well as patient and investigator acceptance, between cetirizine 5mg to 10mg daily, terfenadine 60mg twice daily and chlorpheniramine 8mg twice daily in seasonal allergic rhinitis; cetirizine 10mg daily and terfenadine 60mg twice daily in perennial allergic rhinitis; and cetirizine 5mg to 20mg daily, terfenadine 60mg twice daily and hydroxyzine 25mg once to 3 times daily in chronic idiopathic urticaria. A single brief report indicated that cetirizine 10mg twice daily alleviated asthmatic symptoms more successfully than did terfenadine 60mg twice daily in patients with pollen-associated asthma.

Adverse Effects

In the comparative studies discussed above, the incidence of sedation and/or somnolence was generally similar between cetirizine and terfenadine, and not significantly different from that reported with placebo. In contrast, the incidence reported with chlorpheniramine 8mg twice daily in patients with seasonal allergic rhinitis, and with hydroxyzine 25mg to 75mg daily in patients with chronic idiopathic urticaria, was significantly greater than that reported with placebo. Collated results from 1502 patients who received cetirizine 10mg in double-blind placebo-controlled clinical trials conducted in Europe indicate an incidence of sedation similar to that of other ‘nonsedating’ antihistamines, such as astemizole and terfenadine, and substantially less than that with ketotifen, clemastine, chlorpheniramine or mequitazine. In these collated results, there was no significant difference between cetirizine and placebo treatment in the incidence of headache, gastrointestinal disturbance, anticholinergic effects, dizziness or cardiovascular effects.

Dosage and Administration

The recommended dosage of cetirizine in adults and children over the age of 12 is one 10mg tablet daily (Europe) or one 5 or 10mg tablet daily, up to a maximum of 20mg once daily (USA and Canada). In the elderly and in patients with even a mild degree of renal impairment dosage should be reduced.

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References

  1. Aaronson D, Goldberg S, Klein G, Boggs P, Hawrylko E, et al. Placebo-controlled comparison of cetirizine and hydroxyzine in chronic urticaria. Scientific Exhibition of the American Academy of Allergy and Immunology, March, 1989Google Scholar
  2. Alomar A, De la Cuadra J, Fernandez J. Cetirizine (C) versus astemizole (A) in the treatment of chronic idiopathic urticaria. Abstract. Clinical and Experimental Allergy 20 (Suppl.l): 55, 1990CrossRefGoogle Scholar
  3. Awni WM, Yeh J, Halstenson CE, Opsahl JA, Chung M, et al. Effect of haemodialysis on the pharmacokinetics of cetirizine. European Journal of Clinical Pharmacology 38: 67–69, 1990PubMedCrossRefGoogle Scholar
  4. Ayars GH, Altman LC, Gleich GJ, Loegering DA, Baker CB. Eosinophil- and eosinophil granule-mediated pneumocyte injury. Journal of Allergy and Clinical Immunology 76: 595–604, 1985PubMedCrossRefGoogle Scholar
  5. Backhouse CI, Renton R, Rosenberg RM. Multicentre double-blind comparison of terfenadine and cetirizine in patients with seasonal allergic rhinitis. British Journal of Clinical Practice 44: 88–91, 1990PubMedGoogle Scholar
  6. Baltes EL. Pharmacokinetics of cetirizine. Allergy Forum, London, June 27, 1988. pp. 7–9, 1988Google Scholar
  7. Baltes E, Brouwers L, Gobert J. Pharmacokinetics of cetirizine in animal species and in man. Symposium Proceedings, Cetirizine: a new era in allergotherapy, Brussels, March 27–30, 1987, pp. 45–50, 1987Google Scholar
  8. Baltes E, Coupez R, Brouwers L, Gobert J. Gas Chromatographic method for the determination of cetirizine in plasma. Journal of Chromatography 430: 149–155, 1988PubMedCrossRefGoogle Scholar
  9. Berman B, Buchman E, Dockhorn R, Lees P, Mansmann H, et al. Cetirizine therapy of perennial allergic rhinitis. Abstract. Journal of Allergy and Clinical Immunology 81: 177, 1988CrossRefGoogle Scholar
  10. Boniver R, Arendt C. Evaluation de la cetirizine et de la terfenadine dans le traitment de la rhinite allergique perannuelle. Acta Oto-Rhino-Laryngologica Belgica 43: 75–81, 1989PubMedGoogle Scholar
  11. Bousquet J, Chanez P, Lacoste JY, Barnéon G, Ghavanian N, et al. Eosinophilic inflammation in asthma. New England Journal of Medicine 323: 1033–1039, 1990PubMedCrossRefGoogle Scholar
  12. Brik A, Tashkin DP, Gong Jr H, Dauphinee B, Lee E. Effect of cetirizine, a new histamine H1antagonist, on airway dynamics and responsiveness to inhaled histamine in mild asthma. Journal of Allergy and Clinical Immunology 80: 51–56, 1987PubMedCrossRefGoogle Scholar
  13. Broide DH, Love S, Altman R, Wasserman SI. Evaluation of cetirizine in the treatment of patients with seasonal allergic rhinitis. Journal of Allergy and Clinical Immunology 81: 176, 1988CrossRefGoogle Scholar
  14. Bruttmann G, Arendt C, Bernheim J. Double-blind, placebo controlled comparison of cetirizine 2HC1 and terfenadine in atopic perennial rhinitis. Acta Therapeutica 15: 99–109, 1989Google Scholar
  15. Bruttmann G, Pedrali P. The antiallergic effectiveness of cetirizine 2HCl in patients suffering from hay fever and pollinic asthma. Symposium Proceedings, Cetirizine: a new era in allergotherapy, Brussels, March 27–30, 1987, pp. 77–81, 1987Google Scholar
  16. Bruttmann G, Pedrali P, Arendt C, Rihoux JP. Protective effect of cetirizine in patients suffering from pollen asthma. Annals of Allergy 64: 224–228, 1990PubMedGoogle Scholar
  17. Capron A, Ameisen JC, Joseph M, Auriault C, Tonnel AB, et al. New functions for platelets and their pathological implications. International Archives of Allergy and Applied Immunology 77: 107–114, 1985PubMedCrossRefGoogle Scholar
  18. Charlesworth EN, Kagey-Sobotka A, Norman PS, Lichtenstein LM. Effect of cetirizine on mast cell-mediator release and cellular traffic during the cutaneous late-phase reaction. Journal of Allergy and Clinical Immunology 83: 905–912, 1989PubMedCrossRefGoogle Scholar
  19. Coulie P, De Vos C, Ghys L, Rihoux JP. Pharmacological modulation by cetirizine 2HCl and loratidine of the histamine-induced skin reaction in mice and in humans. Drug Development Research 17: 199–206, 1989CrossRefGoogle Scholar
  20. Davies BH, Mullins J, Couch HA. Prophylactic treatment of seasonal allergic rhinitis. A comparison of cetirizine (Zirtek) and terfenadine (Triludan). Clinical Trials Journal 26: 100–107, 1989Google Scholar
  21. De Vos C, Joseph M, Leprevost C, Vorng H, Tomassini M, et al. Inhibition of human eosinophil chemotaxis and of the IgE-dependent stimulation of human blood platelets by cetirizine. International Archives of Allergy and Applied Immunology 88: 212–215, 1989PubMedCrossRefGoogle Scholar
  22. De Vos C, Maleux M-R, Baltes E, Gobert J. Inhibition of histamine and allergen skin wheal by cetirizine in four animal species. Annals of Allergy 59: 278–282, 1987PubMedGoogle Scholar
  23. De Vos C, Maleux M-R, Gobert J. In vitro pharmacological profile of cetirizine 2HCl, a new non sedating anti-allergic drug. Abstract. Revista Española de Alergología e Immunología Clinica 2: 82, 1987Google Scholar
  24. Dijkman JH, Hekking PRM, Molkenboer JF, Nierop G, Van-derschuerens R, et al. Clinical and Experimental Allergy 20: 483–490, 1990PubMedCrossRefGoogle Scholar
  25. Doms M, Vanhulle G, Baelde Y, Coulie P, Dupont P, et al. Lack of potentiation by cetirizine of alcohol-induced psychomotor disturbances. European Journal of Clinical Pharmacology 34: 619–623, 1988PubMedCrossRefGoogle Scholar
  26. Dorsch W, Ring J, Strasser Th, Auch-Dorsch E. Cetirizine suppresses late-phase reactions in human skin after reverse anaphylaxis. XIII International Congress of Allergology and Clinical Immunology, Montreux, October 17, 1988, pp. 18–20, 1988Google Scholar
  27. Durham SR, Kay AB. Eosinophils, bronchial hyperreactivity and late-phase asthmatic reactions. Clinical Allergy 15: 411–418, 1985PubMedCrossRefGoogle Scholar
  28. Fadel F, Herpin-Richard N, Henocq E, Rihoux J-P. Inhibition by cetirizine 2HCl of antigen-induced eosinophil migration in allergic subjects. XIII International Congress of Allergology and Clinical Immunology, Montreux, October 17, 1988, pp. 11–13, 1988Google Scholar
  29. Fadel R, Herpin-Richard N, Rihoux JP, Henocq E. Inhibitory effect of cetirizine 2HCl on eosinophil migration in vivo. Clinical Allergy 17: 373–379, 1987PubMedCrossRefGoogle Scholar
  30. Filley WV, Kephart GM, Holley KE, Gleich GJ. Identification by immunofluorescence of eosinophil granule major basic protein in lung tissues of patients with bronchial asthma. Lancet 2: 11–15, 1982PubMedCrossRefGoogle Scholar
  31. Finnerty JP, Holgate ST, Rihoux JP. The effect of 2 weeks treatment with cetirizine on bronchial reactivity to methacholine in asthma. British Journal of Clinical Pharmacology 29; 79–84, 1990PubMedCrossRefGoogle Scholar
  32. Fireman P, Skoner D, Tanner E, Doyle W. A primate model for the evaluation of antihistamines. Annals of Allergy 59: 9–12, 1987PubMedGoogle Scholar
  33. Fox R, Lockey R, Altman L, Lieberman P, Wasserman S, et al. Cetirizine in the treatment of seasonal rhinitis: a comparison with terfenadine. Journal of Allergy and Clinical Immunology 83: 307, 1989Google Scholar
  34. Frigas E, Loegering DA, Gleich GJ. Cytotoxic effects of the guinea pig eosinophil major basic protein on tracheal epithelium. Laboratory Investigation 42: 35, 1980PubMedGoogle Scholar
  35. Gengo FM, Dabronzo J, Yurchak A, Love S, Miller JK. The relative antihistaminic and psychomotor effects of hydroxyzine and cetirizine. Clinical Pharmacology and Therapeutics 42: 265–272, 1987PubMedCrossRefGoogle Scholar
  36. Gengo FM, Gabos C. Antihistamines, drowsiness, and psychomotor impairment: central nervous system effect of cetirizine. Annals of Allergy 59: 53–57, 1987PubMedGoogle Scholar
  37. Gengo FM, Gabos C, Mechtler L. Quantitative effects of cetirizine and diphenhydramine on mental performance measured using an automobile driving stimulator. Annals of Allergy 64: 520–526, 1990PubMedGoogle Scholar
  38. Ghosh SK, De Vos C, Patel KR. Effect of cetirizine on exercise induced bronchoconstriction in patients with asthma. Abstract. Thorax 45: 332P, 1990Google Scholar
  39. Ghys L, Rihoux J-P. Pharmacological modulation of cutaneous reactivity to histamine: a double-blind acute comparative study between cetirizine, terfenadine and astemizole. Journal of International Medical Research 17: 24–27, 1989PubMedGoogle Scholar
  40. Go MJTh, Wuite J, Arendt C, Bernheim J. Double-blind, placebo controlled comparison of cetirizine and terfenadine in chronic idiopathic urticaria. Acta Therapeutica 15: 77–85, 1989Google Scholar
  41. Gong Jr H, Tashkin DP, Dauphinee B. Effects of single-dose oral cetirizine (UCB-P071), albuterol and placebo on exercise-induced bronchospasm. American Review of Respiratory Disease 137 (Part II): 420, 1988Google Scholar
  42. Gong Jr H, Tashkin DP, Dauphinee B, Djahed B, Wu T-C. Effects of oral cetirizine, a selective H1 antagonist, on allergen-and exercise-induced bronchoconstriction in subjects with asthma. Journal of Allergy and Clinical Immunology 85: 632–641, 1990PubMedCrossRefGoogle Scholar
  43. Herman D, Arnaud A, Dry J, Latil G, Pauli G, et al. Clinical effectiveness and safety of loratadine vs cetirizine in the treatment of seasonal allergic rhinitis.Abstract. Clinical and Experimental Allergy 20 (Suppl. 1): 56, 1990Google Scholar
  44. Howarth P. Clinical tolerance of cetirizine. Allergy Forum, London, June 27, 1988, pp. 24–25, 1988Google Scholar
  45. Hulhoven R, Emonot A, Germouty J, Molina C, Montané F, et al. Double-blind, multi-centric study of cetirizine in grass pollen-induced asthma. Abstract. Journal of Allergy and Clinical Immunology 85 (Part II): 145, 1990Google Scholar
  46. Joseph M, Capron A, Ameisen JC, Capron M, Vorng H, et al. The receptor for IGE on blood platelets. European Journal of Immunology 16: 306–312, 1986PubMedCrossRefGoogle Scholar
  47. Joseph M, Vorng H, Lassalle P, Tsicopoulos A, De Vos C, et al. In vitro activity of cetirizine on platelets. XIII International Congress of Allergology and Clinical Immunology, Montreaux, October 17 1988, pp. 8–10, 1988Google Scholar
  48. Juhlin L, Arendt C. Treatment of chronic urticaria with cetirizine dihydrochloride a non-sedating antihistamine. British Journal of Dermatology 119: 67–72, 1988PubMedCrossRefGoogle Scholar
  49. Juhlin L, de Vos C, Rihoux J-P. Inhibiting effect of cetirizine on histamine-induced and 48/80-induced wheals and flares, experimental dermographism, and cold-induced urticaria. Journal of Allergy and Clinical Immunology 80: 599–602, 1987PubMedCrossRefGoogle Scholar
  50. Kaiser H, Weisberg S, Morris R, Minneapolis MN, Mansmann H, et al. A comparison of cetirizine and chlorpheniramine vs placebo in the treatment of seasonal allergic rhinitis. Journal of Allergy and Clinical Immunology 83: 306, 1989Google Scholar
  51. Kay AB. Eosinophils as effector cells in immunity and hypersensitivity disorders. Clinical and Experimental Immunology 62: 1–12, 1985PubMedGoogle Scholar
  52. Kay AB. Mediators and inflammatory cells in allergic disease. Annals of Allergy 59: 35–42, 1987PubMedGoogle Scholar
  53. Kint A, Constandt L, Arendt C, Bernheim J. Comparative efficacy of cetirizine and terfenadine in the treatment of chronic idiopathic urticaria. Acta Therapeutica 15: 65–73, 1989Google Scholar
  54. Kontou-Fili K, Maniatakou G, Demaka P, Goriakakis M, Paleologos G. Therapeutic effects of eetirizine 2HCl in delayed pressure urticaria. Part I. Effects on weight tests and skin window cytology. Annals of Allergy, in press, 1990Google Scholar
  55. Kontou-Fili K, Maniatakou G, Paleologos G, Arioni K. Cetirizine 2HC1 inhibits delayed pressure urticaria. Part II. Skin biopsy findings. Annals of Allergy, in press, 1990Google Scholar
  56. Kontou-Fili K, Paleologos G, Herakleous M. Suppression of histamine-induced skin reactions by loratadine and cetirizine diHCl. European Journal of Clinical Pharmacology 36: 617–619, 1989PubMedCrossRefGoogle Scholar
  57. Kurzeja A. Comparative study of cetirizine, terfenadine and placebo in the treatment of patients with perennial allergic rhinitis. Symposium Proceedings, Cetirizine: a new era in Allergotherapy, Brussels, March 27–30, 1987, pp. 72–76, 1987Google Scholar
  58. Kurzeja A, Riedelsheimer B, Hulhoven R, Bernheim J. Cetirizine in pollen-associated asthma. Lancet 1: 556, 1989PubMedCrossRefGoogle Scholar
  59. Leprevost C, Capron M, De Vos C, Tomassini M, Capron A. Inhibition of eosinophil chemotaxis by a new antiallergic compound (cetirizine). International Archives of Allergy and Applied Immunology 87: 9–13, 1988PubMedCrossRefGoogle Scholar
  60. Maddox DE, Reed CE. Clinical pharmacodynamics of antihistamines. Annals of Allergy 59: 43–48, 1987PubMedGoogle Scholar
  61. Maniatakou GP, Paleologos GK, Kontou-Fili KH. Lack of tachyphylaxis during chronic administration of cetirizine 2HCl, and antagonist of peripheral H1receptors. Abstract. Clinical and Experimental Allergy 20(Suppl.l): 97, 1990Google Scholar
  62. Matzke GR, Yeh J, Awni WM, Halstenson CE, Chung M. Pharmacokinetics of cetirizine in the elderly and patients with renal insufficiency. Annals of Allergy 59: 25–30, 1987PubMedGoogle Scholar
  63. Michel L, De Vos C, Rihoux J-P, Burtin C, Benveniste J, et al. Inhibitory effect of oral cetirizine on in vivo antigen-induced histamine and PAF-acether release and eosinophil recruitment in human skin. Journal of Allergy and Clinical Immunology 82: 101–109, 1988PubMedCrossRefGoogle Scholar
  64. Michel L, Jean-Louis F, Burtin C. Maclouf J, De Vos C, Dubertret L. Measurement of cetirizine effects on protein diffusion, mediator release, and eosinophil recruitment during in vivo anaphylactic cutaneous reactions. XIII International Congress of Allergology and Clinical Immunology, Montreux, October 17, 1988, pp. 14–17, 1988Google Scholar
  65. Mühlethaler K, Wüthrich B, Helfenstein U, Ghys L, Rihoux J-P. Pharmacological modulation of the skin reaction induced by histamine and allergen in atopic subjects of cetirizine and terfenadine. Allergologie 12: 412–418, 1989Google Scholar
  66. Müller FO, deK Botha JJ, van Dyk M, Luus HG, Groenewoud G. Attenuation of cutaneous reactivity to histamine by cetirizine and dexchlorpheniramine. European Journal of Clinical Pharmacology 35: 319–321, 1988PubMedCrossRefGoogle Scholar
  67. Naclerio RM, Proud D, Ragey-Sobotka A, Freidhoff L, Norman PS, et al. The effect of cetirizine on early allergic response. Laryngoscope 99: 596–599, 1989PubMedCrossRefGoogle Scholar
  68. Panayotopoulos SM, Panayotopoulou ES. The efficacy of cetirizine in the treatment of pollinosis: a correlation with the daily pollen count of atmospheric air a double-blind placebo controlled study. Acta Therapeutica 14: 347–352, 1988Google Scholar
  69. Panayotopoulos SM, Panayotopoulou ES. Efficacy of cetirizine in the treatment of seasonal allergic rhinoconjunctivitis. Annals of Allergy 65: 146–148, 1990PubMedGoogle Scholar
  70. Pechadre JC, Vernay D, Trolese JF, Bloom M, Dupont P, et al. Comparison of the central and peripheral effects of cetirizine and terfenadine. Journal of Clinical Pharmacology 35: 255–259, 1988CrossRefGoogle Scholar
  71. Pedrali P, Arendt C. The preventive effect of cetirizine 10mg bid in the treatment of seasonal allergic asthma: a double-blind placebo-controlled study. XIII International Congress of Allergology and Clinical Immunology, Montreux, October 17, 1988, pp. 31–32, 1988Google Scholar
  72. Raptopoulou-Gigi M, Sichletidis L, Orphanou-Koumerkeridou H, Pechlivanidis J, Printgis S, et al. Cetirizine therapy of allergic rhinitis and bronchial asthma: immunological evaluation. Acta Therapeutica 16: 61–69, 1990Google Scholar
  73. Riedel WJ, Van Veggel L, O’Hanlon JF. Cetirizine 10 and 20mg impair psychomotor performance. Abstract. Clinical and Experimental Allergy 20 (Suppl. 1): 97, 1990CrossRefGoogle Scholar
  74. Rihoux J-P, Dupont P. Comparative study of the peripheral and central effects of terfenadine and cetirizine 2HCl. Annals of Allergy 59: 235–238, 1987PubMedGoogle Scholar
  75. Rihoux J-P, Dupont P. Pharmacological modulation by astemizole and cetirizine 2 HCl of the skin reactivity to histamine. Acta Therapeutica 15: 265–270, 1989Google Scholar
  76. Rihoux J-P, Ghys L, Coulie P. Compared peripheral H1inhibiting effects of cetirizine 2HCl and loratadine. Annals of Allergy 65: 139–142, 1990PubMedGoogle Scholar
  77. Rihoux J-P, Van Neste DJJ. Quantitative time course study of the skin response to histamine and the effect of H1 blockers: a 3-week crossover double-blind comparative trial of cetirizine and terfenadine. Dermatologica 179: 129–134, 1989PubMedCrossRefGoogle Scholar
  78. Rijntjes E, Ghys L, Rihoux J-P. Astemizole and cetirizine in the treatment of seasonal allergic rhinitis: a comparative double-blind, multicentre study. Journal of International Medical Research 18: 219–224, 1990PubMedGoogle Scholar
  79. Schmeisser KJ, Arendt C, Bernheim J. Double-blind comparison of two effective treatments of perennial rhinoconjunctivitis. Acta Therapeutica 15: 87–98, 1989Google Scholar
  80. Schoeneich M, Pécoud A. Effect of cetirizine in a conjunctival provocation test with allergens. Clinical and Experimental Allergy 20: 171–174, 1990PubMedCrossRefGoogle Scholar
  81. Seidel WF, Cohen S, Bliwise NG, Dement WC. Cetirizine effects on objective measures of daytime sleepiness and performance. Annals of Allergy 59: 58–62, 1987PubMedGoogle Scholar
  82. Sidiropoulos J, Volonakis M, Kontou-Fili K. Inhibition of histamine-induced wheal and flare reactions by cetirizine 2HCl and mequitazine both in healthy and atopic subjects: a comparative double-blind placebo controlled study. Review of Clinical Pharmacology and Pharmacokinetics, International Edition 6: 110–120, 1988Google Scholar
  83. Simons KJ, McMillan JL, Simons FER. A double-blind, crossover comparison of cetirizine (C), terfenadine (T), and loratadine (L) vs placebo (P): suppressive effects on histamine-induced wheals and flares. Abstract. Journal of Allergy and Clinical Immunology 85 (Suppl): 255, 1990CrossRefGoogle Scholar
  84. Snyder SH, Snowman AM. Receptor effects of cetirizine. Annals of Allergy 59: 4–8, 1987PubMedGoogle Scholar
  85. Spyropoulou-Vlahou M, Stavropoulos-Giokas A, Filippou M, Koyas A, Kontou-Fili K. Clinical and laboratory results confirm the efficacy of cetirizine 2HCl in seasonal allergic rhinitis. Acta Therapeutica 16: 71–78, 1990Google Scholar
  86. Tashkin DP, Brik A, Gong Jr H. Cetirizine inhibition of histamine-induced bronchospasm. Annals of Allergy 59 (Part II): 49–52, 1987PubMedGoogle Scholar
  87. Van Cauwenberge P. Clinical efficacy of cetirizine in seasonal rhinitis. XIII International Congress of Allergology and Clinical Immunology, Montreux, October 17, 1988, pp. 26–27, 1988Google Scholar
  88. Van Cauwenberge PB, Rihoux JP, Doyle WJ, Skoner DP, Tanner E. Effect of cetirizine and cimetidine on the cutaneous reactivity of the rhesus monkey to histamine 48/80, substance P and VIP. Clinical and Experimental Dermatology 12: 149, 1987Google Scholar
  89. Van Epps DE, Kutvirt SG, Potter JW. In vitro effects of cetirizine and histamine on human neutrophil function. Annals of Allergy 59: 13–19, 1987PubMedGoogle Scholar
  90. Wasserman SI. Histamine and the preclinical pharmacology of cetirizine. Annals of Allergy 59: 1–3, 1987PubMedGoogle Scholar
  91. Watson WTA, Chen XY, Simons FER, Simons KJ. The pharmacokinetics and pharmacodynamics of cetirizine (C), a new H1-receptor antagonist, in children with allergic rhinitis. Journal of Allergy and Clinical Immunology 83: 277, 1987Google Scholar
  92. Watson WTA, Simons KJ, Chen XY, Simons FER. Cetirizine: a pharmacokinetic and pharmacodynamic evaluation in children with seasonal allergic rhinitis. Journal of Allergy and Clinical Immunology 84: 457–464, 1989PubMedCrossRefGoogle Scholar
  93. Wood SG, John BA, Chasseaud LF, Yeh J, Chung M. The metabolism and pharmacokinetics of l4C-cetirizine in humans. Annals of Allergy 59 (Part II): 31–34, 1987PubMedGoogle Scholar

Copyright information

© Adis International Limited 1990

Authors and Affiliations

  • Deborah M. Campoli-Richards
    • 1
  • Micaela M.-T. Buckley
    • 1
  • Andrew Fitton
    • 1
  1. 1.Adis Drug Information ServicesAucklandNew Zealand
  2. 2.Adis International LimitedMairangi Bay, AucklandNew Zealand

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