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Chemical Compound Review

Mistalin     2-[[1-[1-[(4-fluorophenyl) methyl]benzoimid...

Synonyms: Mizollen, Zolistam, Zolistan, Mistamine, Mizolen, ...
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Disease relevance of Mizolastine


Psychiatry related information on Mizolastine


High impact information on Mizolastine


Chemical compound and disease context of Mizolastine


Biological context of Mizolastine

  • Significant increases in theophylline Cmin and AUC were observed after coadministration with mizolastine [2].
  • In this paper we present an overview of five clinical pharmacology studies which were carried out with a view to assessing mizolastine effects on psychomotor and skilled performances, and on cognitive functions in young and aged subjects [3].
  • Furthermore, with long-term use of mizolastine over 1 year, a reduction in pruritus and the number of urticarial episodes was maintained with no evidence of tachyphylaxis or tolerance [10].
  • A population analysis of the kinetics of mizolastine was performed from concentrations on 449 allergic patients, using the nonparametric maximum likelihood method (NPML) [11].
  • CONCLUSION: PKC-mediated phosphorylation of Akt can be blocked by mizolastine [12].

Anatomical context of Mizolastine


Associations of Mizolastine with other chemical compounds


Gene context of Mizolastine

  • CONCLUSIONS: This study demonstrated that mizolastine is able to selectively downregulate CD54 expression on stimulated stromal but not epithelial cells without impairing the immune system effectors [15].
  • Moreover, HaCaT keratinocytes were incubated with mizolastine under various UV treatment modalities in vitro to study its effect on the release of inflammatory cytokines, i.e. interleukin (IL)-1 alpha, IL-6 and tumor necrosis factor alpha (TNF-alpha) [8].
  • An inhibitory effect in vitro of 10 nM mizolastine upon UV-induced cytokine release from HaCaT keratinocytes was observed for IL-1 alpha at 24 h after 10 J/cm2 UVA1, for IL-6 at 48 h after 10 J/cm2 UVA1 and 30 mJ/cm2 UVB, and also for TNF-alpha at 4 h after 10 J/cm2 UVA, 10 J/cm2 UVA1 and 30 mJ/cm2 UVB, respectively [8].
  • Cells were stimulated with interferon (IFN)-gamma (500 IU/ml) in the presence of various mizolastine concentrations (6 x 10(-8)-6 x 10(-6) M) for 24 h and the expression of CD106, CD54, CD58 and HLA class I was evaluated [15].
  • An interaction of desloratadine with P-gp has been suggested in mice, whereas the information on mizolastine is very poor [17].

Analytical, diagnostic and therapeutic context of Mizolastine

  • METHODS: Fifteen healthy volunteers participated in this double-blind crossover study and randomly received single doses of 5, 10, 15, and 20 mg of mizolastine and placebo at 1 week intervals [18].
  • In addition, mizolastine displays low lipophilicity and consequently low cardiac tissue fixation [19].
  • The efficacy of mizolastine, a new non-sedating H1 antagonist, has been evaluated in several placebo-controlled and comparative clinical trials [20].
  • CONCLUSION: ECG monitoring of volunteers and patients included in clinical studies conducted with mizolastine showed no significant effect of mizolastine on cardiac repolarization [21].
  • The highest dose of mizolastine (6 x 10(-6) M), corresponding to 10-fold the peak plasma level after a single oral administration of 10 mg, was able to act on fibroblasts, significantly downregulating the expression of CD54 (p<0.05) [15].


  1. Anaphylaxis to mizolastine. Weidinger, S., Mempel, M., Ollert, M., Elser, I., Rakoski, J., Köhn, F.M., Ring, J. J. Allergy Clin. Immunol. (2004) [Pubmed]
  2. Clinical pharmacokinetics of mizolastine. Lebrun-Vignes, B., Diquet, B., Chosidow, O. Clinical pharmacokinetics. (2001) [Pubmed]
  3. Lack of behavioural toxicity of mizolastine: a review of the clinical pharmacology studies. Rosenzweig, P., Patat, A. Clin. Exp. Allergy (1999) [Pubmed]
  4. Inhibition of HERG1 K(+) channels by the novel second-generation antihistamine mizolastine. Taglialatela, M., Pannaccione, A., Castaldo, P., Giorgio, G., Annunziato, L. Br. J. Pharmacol. (2000) [Pubmed]
  5. Mizolastine in primary acquired cold urticaria. Dubertret, L., Pecquet, C., Murrieta-Aguttes, M., Leynadier, F. J. Am. Acad. Dermatol. (2003) [Pubmed]
  6. Effects of mizolastine, a new antihistamine, on psychomotor performance and memory in elderly subjects. Patat, A., Gram, L.F., Dubruc, C., Brohier, S., Cabanis, M.J., Rosenzweig, P. International clinical psychopharmacology. (1994) [Pubmed]
  7. Mizolastine provides effective symptom relief in patients suffering from perennial allergic rhinitis: a double-blind, placebo-controlled study versus loratadine. Frèche, C., Leynadier, F., Horak, F., Hide, D., Gracia, F.D., Goos, M., Bachert, C., Horvath, A., Antosova, E., Verrecchia, M., Soussen, P.B. Ann. Allergy Asthma Immunol. (2002) [Pubmed]
  8. UV erythema reducing capacity of mizolastine compared to acetylsalicylic acid or both combined in comparison to indomethacin. Grundmann, J.U., Böckelmann, R., Bonnekoh, B., Gollnick, H.P. Photochem. Photobiol. (2001) [Pubmed]
  9. Urticaria to cetirizine. Tella, R., Gaig, P., Bartra, J., Garcia-Ortega, P. Journal of investigational allergology & clinical immunology : official organ of the International Association of Asthmology (INTERASMA) and Sociedad Latinoamericana de Alergia e Inmunología. (2002) [Pubmed]
  10. Clinical advantages of dual activity in urticaria. Kontou-Fili, K. Allergy (2000) [Pubmed]
  11. Population pharmacokinetic analysis of mizolastine and validation from sparse data on patients using the nonparametric maximum likelihood method. Mesnil, F., Mentré, F., Dubruc, C., Thénot, J.P., Mallet, A. Journal of pharmacokinetics and biopharmaceutics. (1998) [Pubmed]
  12. Influence of mizolastine on antigen-induced activation of signalling pathways in murine mast cells. Xia, Q., Zhou, W.M., Yang, S., Zhang, S.Q., Chen, B., Wang, D.B., Wang, Y., Zhang, X.J. Clin. Exp. Dermatol. (2006) [Pubmed]
  13. Differential modulation of mediator release from human basophils and mast cells by mizolastine. Triggiani, M., Giannattasio, G., Balestrieri, B., Granata, F., Gelb, M.H., de Paulis, A., Marone, G. Clin. Exp. Allergy (2004) [Pubmed]
  14. Inhibitory effects of mizolastine on ultraviolet B-induced leukotriene B4 production and 5-lipoxygenase expression in normal human dermal fibroblasts in vitro. Yan, Y., Wang, B., Zuo, Y.G., Qu, T. Photochem. Photobiol. (2006) [Pubmed]
  15. Effects of mizolastine in vitro on human immunocompetent and airway cells: evidence for safety and additional property. Oddera, S., Cagnoni, F., Dellacasa, P., Canonica, G.W. Int. Arch. Allergy Immunol. (2000) [Pubmed]
  16. Comparison of the efficacy, safety, and onset of action of mizolastine, cetirizine, and placebo in the management of seasonal allergic rhinoconjunctivitis. MIZOCET Study Group. Sabbah, A., Daele, J., Wade, A.G., Ben-Soussen, P., Attali, P. Ann. Allergy Asthma Immunol. (1999) [Pubmed]
  17. Comparison of pharmacokinetics and metabolism of desloratadine, fexofenadine, levocetirizine and mizolastine in humans. Molimard, M., Diquet, B., Benedetti, M.S. Fundamental & clinical pharmacology. (2004) [Pubmed]
  18. Pharmacokinetic and pharmacodynamic modeling of mizolastine in healthy volunteers with an indirect response model. Deschamps, C., Dubruc, C., Mentre, F., Rosenzweig, P. Clin. Pharmacol. Ther. (2000) [Pubmed]
  19. The current cardiac safety situation with antihistamines. Yap, Y.G., Camm, A.J. Clin. Exp. Allergy (1999) [Pubmed]
  20. Antihistamines in urticaria. Ring, J., Brockow, K., Ollert, M., Engst, R. Clin. Exp. Allergy (1999) [Pubmed]
  21. QT interval monitoring during clinical studies with mizolastine, a new H1 antihistamine. Delauche-Cavallier, M.C., Chaufour, S., Guérault, E., Lacroux, A., Murrieta, M., Wajman, A. Clin. Exp. Allergy (1999) [Pubmed]
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