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Chemical Compound Review

Cetiderm     2-[2-[4-[(4-chlorophenyl)- phenyl...

Synonyms: Alerlisin, Benaday, Cetirizin, Virlix, Zirtek, ...
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Disease relevance of cetirizine

  • Two agents recently marketed in the United States, Ioratidine and cetirizine, appear to lack the ability to prolong repolarization and induce torsades de pointes [1].
  • RESULTS: Acute urticaria occurred in 16.2% of the placebo-treated children and in 5.8% of the children treated with cetirizine (P <.001) [2].
  • A double-blinded, 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 [3].
  • Early treatment of perennial rhinitis with budesonide or cetirizine and its effect on long-term outcome [4].
  • The ability of cetirizine (and perhaps other antihistamines) to inhibit these responses at usual therapeutic doses may be useful in investigating the late allergic reaction [5].

Psychiatry related information on cetirizine


High impact information on cetirizine


Chemical compound and disease context of cetirizine


Biological context of cetirizine


Anatomical context of cetirizine


Associations of cetirizine with other chemical compounds


Gene context of cetirizine

  • Pre-incubation with cetirizine diminished the IL-8 release from cells activated with TNF-alpha or PMA in a significant manner [32].
  • RESULTS: Cetirizine at high concentrations (10(2)-10(3) microM) markedly inhibited IFNgamma-induced expression of membrane ICAM-1, HLA-DR and up-regulation of MHC class I, but had no effect on CD40 expression [33].
  • Finally, cetirizine, but not hydrocortisone, inhibited the release of MCP-1 and RANTES from IFNgamma-stimulated keratinocytes [33].
  • In contrast, nonsedating H1-antagonists cetirizine, loratadine, and desloratadine are P-gp substrates [34].
  • In group A, ICAM-1-positive cells decreased from 75.8 (SE +/- 15.12) to 38.8 (SE +/- 7.57) ICAM-3-positive cells decreased from 61.7 (SE +/- 12.72) to 45.2 (SE +/- 9.44) and LFA-1 decreased from 103.9 (SE +/- 17.34) to 66.5 (SE +/- 8.63) after cetirizine treatment (p = 0.02) [35].

Analytical, diagnostic and therapeutic context of cetirizine


  1. Cardiac actions of antihistamines. Woosley, R.L. Annu. Rev. Pharmacol. Toxicol. (1996) [Pubmed]
  2. Prevention of acute urticaria in young children with atopic dermatitis. Simons, F.E. J. Allergy Clin. Immunol. (2001) [Pubmed]
  3. A double-blinded, 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. Warner, J.O. J. Allergy Clin. Immunol. (2001) [Pubmed]
  4. Early treatment of perennial rhinitis with budesonide or cetirizine and its effect on long-term outcome. Rinne, J., Simola, M., Malmberg, H., Haahtela, T. J. Allergy Clin. Immunol. (2002) [Pubmed]
  5. Antiallergic properties of the second-generation H1 antihistamines during the early and late reactions to antigen. Townley, R.G. J. Allergy Clin. Immunol. (1992) [Pubmed]
  6. Sedation and performance issues in the treatment of allergic conditions. Adelsberg, B.R. Arch. Intern. Med. (1997) [Pubmed]
  7. Binding characteristics of cetirizine and levocetirizine to human H(1) histamine receptors: contribution of Lys(191) and Thr(194). Gillard, M., Van Der Perren, C., Moguilevsky, N., Massingham, R., Chatelain, P. Mol. Pharmacol. (2002) [Pubmed]
  8. A dose-ranging study of the effects of mequitazine on actual driving, memory and psychomotor performance as compared to dexchlorpheniramine, cetirizine and placebo. Theunissen, E.L., Vermeeren, A., van Oers, A.C., van Maris, I., Ramaekers, J.G. Clin. Exp. Allergy (2004) [Pubmed]
  9. Specific review of the psychometric effects of cetirizine. Volkerts, E.R., van Laar, M. Allergy (1995) [Pubmed]
  10. Dissociable effects of histamine H1 antagonists on reaction-time performance in rats. Blokland, A., Scholtissen, B., Vermeeren, A., Ramaekers, J. Pharmacol. Biochem. Behav. (2001) [Pubmed]
  11. Enhanced cancer growth in mice administered daily human-equivalent doses of some H1-antihistamines: predictive in vitro correlates. Brandes, L.J., Warrington, R.C., Arron, R.J., Bogdanovic, R.P., Fang, W., Queen, G.M., Stein, D.A., Tong, J., Zaborniak, C.L., LaBella, F.S. J. Natl. Cancer Inst. (1994) [Pubmed]
  12. Severe arrhythmia as a result of the interaction of cetirizine and pilsicainide in a patient with renal insufficiency: first case presentation showing competition for excretion via renal multidrug resistance protein 1 and organic cation transporter 2. Tsuruoka, S., Ioka, T., Wakaumi, M., Sakamoto, K., Ookami, H., Fujimura, A. Clin. Pharmacol. Ther. (2006) [Pubmed]
  13. Comment on severe arrhythmia as a result of the interaction of cetirizine and pilsicainide in a patient with renal insufficiency. Whomsley, R., Strolin-Benedetti, M., Baltes, E. Clin. Pharmacol. Ther. (2006) [Pubmed]
  14. Prospects for antihistamines in the treatment of asthma. Nelson, H.S. J. Allergy Clin. Immunol. (2003) [Pubmed]
  15. Inhibiting effect of cetirizine on histamine-induced and 48/80-induced wheals and flares, experimental dermographism, and cold-induced urticaria. Juhlin, L., de Vos, C., Rihoux, J.P. J. Allergy Clin. Immunol. (1987) [Pubmed]
  16. Urticaria: clinical efficacy of cetirizine in comparison with hydroxyzine and placebo. Kalivas, J., Breneman, D., Tharp, M., Bruce, S., Bigby, M. J. Allergy Clin. Immunol. (1990) [Pubmed]
  17. Effect of cetirizine, a new H1 antihistamine, on the early and late allergic reactions in a bronchial provocation test with allergen. Wasserfallen, J.B., Leuenberger, P., Pécoud, A. J. Allergy Clin. Immunol. (1993) [Pubmed]
  18. Effect of the H2-antagonist cimetidine on the pharmacokinetics and pharmacodynamics of the H1-antagonists hydroxyzine and cetirizine in patients with chronic urticaria. Simons, F.E., Sussman, G.L., Simons, K.J. J. Allergy Clin. Immunol. (1995) [Pubmed]
  19. Pharmacokinetics and pharmacodynamics of cetirizine in infants and toddlers. Spicák, V., Dab, I., Hulhoven, R., Desager, J.P., Klánová, M., de Longueville, M., Harvengt, C. Clin. Pharmacol. Ther. (1997) [Pubmed]
  20. Cetirizine inhibits the in vitro and ex vivo chemotactic response of T lymphocytes and monocytes. Jinquan, T., Reimert, C.M., Deleuran, B., Zachariae, C., Simonsen, C., Thestrup-Pedersen, K. J. Allergy Clin. Immunol. (1995) [Pubmed]
  21. Effects of oral cetirizine, a selective H1 antagonist, on allergen- and exercise-induced bronchoconstriction in subjects with asthma. Gong, H., Tashkin, D.P., Dauphinee, B., Djahed, B., Wu, T.C. J. Allergy Clin. Immunol. (1990) [Pubmed]
  22. Cetirizine, loratadine, or placebo in subjects with seasonal allergic rhinitis: effects after controlled ragweed pollen challenge in an environmental exposure unit. Day, J.H., Briscoe, M., Widlitz, M.D. J. Allergy Clin. Immunol. (1998) [Pubmed]
  23. In vivo effects of cetirizine on cutaneous reactivity and eosinophil migration induced by platelet-activating factor (PAF-acether) in man. Fadel, R., David, B., Herpin-Richard, N., Borgnon, A., Rassemont, R., Rihoux, J.P. J. Allergy Clin. Immunol. (1990) [Pubmed]
  24. Antihistamines in the treatment of clinical asthma. Rafferty, P. J. Allergy Clin. Immunol. (1990) [Pubmed]
  25. Safety of cetirizine in infants 6 to 11 months of age: a randomized, double-blind, placebo-controlled study. Simons, F.E., Silas, P., Portnoy, J.M., Catuogno, J., Chapman, D., Olufade, A.O., Pharmd, n.u.l.l. J. Allergy Clin. Immunol. (2003) [Pubmed]
  26. Cetirizine: actions on neurotransmitter receptors. Snowman, A.M., Snyder, S.H. J. Allergy Clin. Immunol. (1990) [Pubmed]
  27. Recent advances in H1-receptor antagonist treatment. Simons, F.E. J. Allergy Clin. Immunol. (1990) [Pubmed]
  28. Effect of cetirizine on histamine- and leukotriene D4-induced bronchoconstriction in patients with atopic asthma. Ghosh, S.K., De Vos, C., McIlroy, I., Patel, K.R. J. Allergy Clin. Immunol. (1991) [Pubmed]
  29. Levocetirizine better protects than desloratadine in a nasal provocation with allergen. Deruaz, C., Leimgruber, A., Berney, M., Pradervand, E., Spertini, F. J. Allergy Clin. Immunol. (2004) [Pubmed]
  30. Inhibitory effect of cetirizine on the bronchial eosinophil recruitment induced by allergen inhalation challenge in allergic patients with asthma. Rédier, H., Chanez, P., De Vos, C., Rifaï, N., Clauzel, A.M., Michel, F.B., Godard, P. J. Allergy Clin. Immunol. (1992) [Pubmed]
  31. Inhibitory effect of oral cetirizine on in vivo antigen-induced histamine and PAF-acether release and eosinophil recruitment in human skin. Michel, L., De Vos, C., Rihoux, J.P., Burtin, C., Benveniste, J., Dubertret, L. J. Allergy Clin. Immunol. (1988) [Pubmed]
  32. Cetirizine counter-regulates interleukin-8 release from human epithelial cells (A549). Arnold, R., Rihoux, J., König, W. Clin. Exp. Allergy (1999) [Pubmed]
  33. Cetirizine and hydrocortisone differentially regulate ICAM-1 expression and chemokine release in cultured human keratinocytes. Albanesi, C., Pastore, S., Fanales-Belasio, E., Girolomoni, G. Clin. Exp. Allergy (1998) [Pubmed]
  34. P-glycoprotein limits the brain penetration of nonsedating but not sedating H1-antagonists. Chen, C., Hanson, E., Watson, J.W., Lee, J.S. Drug Metab. Dispos. (2003) [Pubmed]
  35. Cetirizine modulates adhesion molecule expression in a double-blind controlled study conducted in psoriatic patients. Pestelli, E., Floriani, I., Fabbri, P., Caproni, M. International journal of tissue reactions. (2003) [Pubmed]
  36. Cetirizine reduces inflammatory cell recruitment and ICAM-1 (or CD54) expression on conjunctival epithelium in both early- and late-phase reactions after allergen-specific challenge. Ciprandi, G., Buscaglia, S., Pesce, G., Passalacqua, G., Rihoux, J.P., Bagnasco, M., Canonica, G.W. J. Allergy Clin. Immunol. (1995) [Pubmed]
  37. Comparison between nasal provocation tests and skin tests in patients treated with loratadine and cetirizine. Persi, L., Demoly, P., Harris, A.G., Tisserand, B., Michel, F.B., Bousquet, J. J. Allergy Clin. Immunol. (1999) [Pubmed]
  38. Inhibition of mediator release during the early reaction to antigen. Naclerio, R.M. J. Allergy Clin. Immunol. (1992) [Pubmed]
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