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Chemical Compound Review

Ebastina     4-(4-benzhydryloxy-1- piperidyl)-1-(4-tert...

Synonyms: ebastine, Ebastel, Ebastin, Ebastinum, Estivan, ...
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Disease relevance of C12925

  • OBJECTIVE: We compared the efficacy and safety of ebastine 20 mg and 10 mg, loratadine 10 mg, and placebo administered once daily for 4 weeks in controlling the symptoms of seasonal allergic rhinitis (SAR) [1].
  • CONCLUSION: Ebastine 20 mg given once daily was significantly superior to loratadine 10 mg given once daily at improving the rhinitis total symptom score throughout the day and at awakening over a 4-week period [1].
  • Thus, these results, which show ebastine to be an effective and well tolerated agent, indicated that the drug should be considered for the first-line therapy of chronic urticaria [2].
  • Finally, no apparent difference was noted in the safety of ebastine between patients with hepatic insufficiency and healthy subjects as assessed by evaluation of adverse events, vital signs and laboratory parameters [3].
  • Furthermore, ebastine showed no clinically relevant effects in a complete set of regulatory-required toxicity tests (including acute, chronic, reproductive, mutagenic and carcinogenic protocols) at doses giving blood concentrations representing high multiples of clinical exposure [4].

Psychiatry related information on C12925


High impact information on C12925


Chemical compound and disease context of C12925


Biological context of C12925

  • Their functional impact toward ebastine hydroxylation was evaluated using heterologous expression in Saccharomyces cerevisiae cells of site-directed mutated cDNA variants [13].
  • The electrocardiographic effects of ebastine and its active metabolite, carebastine, have been studied alone and in relevant drug-interaction studies in various patient populations [14].
  • The increase in QTcB with ebastine most likely resulted from overcorrection of the small drug-induced increase in heart rate [15].
  • The overall effect after single and repeated 5-day dose, expressed as the AUC of reduction of wheal and flare area (%/h), showed the following order of magnitude: ebastine 20 mg>fexofenadine 120 mg>placebo [16].
  • A double-blind placebo-controlled study of the efficacy and tolerability of ebastine against hayfever in general practice patients [17].

Anatomical context of C12925


Associations of C12925 with other chemical compounds


Gene context of C12925


Analytical, diagnostic and therapeutic context of C12925

  • Ebastine is without effects on the central nervous and cardiovascular systems, even after oral administration of high doses, and does not interact pharmacologically with a wide range of other drugs covering most areas of potential coadministration [4].
  • In 3 randomised double-blind, multicentre clinical trials in patients with SAR, ebastine 10 and 20mg once daily for 2 to 3 weeks significantly reduced symptoms (nasal discharge, stuffiness, sneezing, itchy nose, itchy/watery eyes) when compared with placebo [28].
  • Pooled data from clinical efficacy trials of ebastine 1-30 mg/day administered for 2-3 weeks showed no clinically relevant cardiac effects as assessed by serial electrocardiographs and Holter monitoring [29].
  • 1. We have given 12 healthy subjects the H1-antihistamine ebastine (20 mg) or placebo in a randomized double-blind and crossover study for 1 week each [30].
  • Venous blood was sampled daily during the maintenance and during each testing round for the assay of plasma carebastine (the active metabolite of ebastine) by high pressure liquid chromatography and plasma diazepam by radioreceptor assay [30].


  1. Comparison of once-daily ebastine 20 mg, ebastine 10 mg, loratadine 10 mg, and placebo in the treatment of seasonal allergic rhinitis. The Ebastine Study Group. Ratner, P.H., Lim, J.C., Georges, G.C. J. Allergy Clin. Immunol. (2000) [Pubmed]
  2. Double-blind multicentre comparative study of ebastine, terfenadine and placebo in the treatment of chronic idiopathic urticaria in adults. Kalis, B. Drugs (1996) [Pubmed]
  3. Pharmacokinetics and safety of ebastine in patients with impaired hepatic function compared with healthy volunteers: a phase I open-label study. Lasseter, K.C., Dilzer, S.C., Vargas, R., Waldman, S., Noveck, R.J. Clinical pharmacokinetics. (2004) [Pubmed]
  4. A preclinical overview of ebastine. Studies on the pharmacological properties of a novel histamine H1 receptor antagonist. Roberts, D.J. Drugs (1996) [Pubmed]
  5. Ebastine: the effect of a new antihistamine on psychomotor performance and autonomic responses in healthy subjects. Vincent, J., Sumner, D.J., Reid, J.L. British journal of clinical pharmacology. (1988) [Pubmed]
  6. Differential cognitive effects of ebastine and (+)-chlorpheniramine in healthy subjects: correlation between cognitive impairment and plasma drug concentration. Tagawa, M., Kano, M., Okamura, N., Higuchi, M., Matsuda, M., Mizuki, Y., Arai, H., Fujii, T., Komemushi, S., Itoh, M., Sasaki, H., Watanabe, T., Yanai, K. British journal of clinical pharmacology. (2002) [Pubmed]
  7. Comparative pharmacology of H1 antihistamines: clinical relevance. Simons, F.E. Am. J. Med. (2002) [Pubmed]
  8. Ebastine: an update of its use in allergic disorders. Hurst, M., Spencer, C.M. Drugs (2000) [Pubmed]
  9. Overview of allergic mechanisms. Ebastine has more than an antihistamine effect. Campbell, A., Michel, F.B., Bremard-Oury, C., Crampette, L., Bousquet, J. Drugs (1996) [Pubmed]
  10. Comparison of cetirizine, ebastine and loratadine in the treatment of immediate mosquito-bite allergy. Karppinen, A., Kautiainen, H., Petman, L., Burri, P., Reunala, T. Allergy (2002) [Pubmed]
  11. Azelastine tablets in the treatment of chronic idiopathic urticaria. Phase iii, randomised, double-blind, placebo and active controlled multicentric clinical trial. Camarasa, J.M., Aliaga, A., Fernández-Vozmediano, J.M., Fonseca, E., Iglesias, L., Tagarro, I. Skin Pharmacol. Appl. Skin Physiol. (2001) [Pubmed]
  12. The effects of single and repeated administration of ebastine on cognition and psychomotor performance in comparison to triprolidine and placebo in healthy volunteers. Hindmarch, n.u.l.l., Shamsi, Z. Current medical research and opinion. (2001) [Pubmed]
  13. Human CYP4F12 genetic polymorphism: identification and functional characterization of seven variant allozymes. Cauffiez, C., Klinzig, F., Rat, E., Tournel, G., Allorge, D., Chevalier, D., Pottier, N., Lovecchio, T., Colombel, J.F., Lhermitte, M., Lo-Guidice, J.M., Broly, F. Biochem. Pharmacol. (2004) [Pubmed]
  14. Cardiac effects of ebastine and other antihistamines in humans. Moss, A.J., Morganroth, J. Drug safety : an international journal of medical toxicology and drug experience. (1999) [Pubmed]
  15. Effects of supratherapeutic doses of ebastine and terfenadine on the QT interval. Gillen, M.S., Miller, B., Chaikin, P., Morganroth, J. British journal of clinical pharmacology. (2001) [Pubmed]
  16. A study comparing the inhibitory effects of single and repeated oral doses of ebastine and fexofenadine against histamine-induced skin reactivity. Barbanoj, M.J., Antonijoan, R.M., García-Gea, C., Morte, A., Gich, I., Gispert, J., Garcia, E., Esbrí, R., Luria, X. Int. Arch. Allergy Immunol. (2003) [Pubmed]
  17. A double-blind placebo-controlled study of the efficacy and tolerability of ebastine against hayfever in general practice patients. Ankier, S.I., Warrington, S.J. J. Intern. Med. (1989) [Pubmed]
  18. Involvement of CYP2J2 and CYP4F12 in the metabolism of ebastine in human intestinal microsomes. Hashizume, T., Imaoka, S., Mise, M., Terauchi, Y., Fujii, T., Miyazaki, H., Kamataki, T., Funae, Y. J. Pharmacol. Exp. Ther. (2002) [Pubmed]
  19. Ebastine inhibits T cell migration, production of Th2-type cytokines and proinflammatory cytokines. Nori, M., Iwata, S., Munakata, Y., Kobayashi, H., Kobayashi, S., Umezawa, Y., Hosono, O., Kawasaki, H., Dang, N.H., Tanaka, H., Shiohara, T., Morimoto, C. Clin. Exp. Allergy (2003) [Pubmed]
  20. Suppression of mammalian K+ channel family by ebastine. Ko, C.M., Ducic, I., Fan, J., Shuba, Y.M., Morad, M. J. Pharmacol. Exp. Ther. (1997) [Pubmed]
  21. Comparison of the efficacy of ebastine 10mg and 20mg once daily with that of cetirizine 10mg once daily in adults with seasonal allergic rhinitis. A multicentre double-blind study. Cohen, B., Gehanno, P. Drugs (1996) [Pubmed]
  22. Effects of H1 antihistamines on animal models of QTc prolongation. Gras, J., Llenas, J. Drug safety : an international journal of medical toxicology and drug experience. (1999) [Pubmed]
  23. Histamine--a major role in allergy? Bachert, C. Clin. Exp. Allergy (1998) [Pubmed]
  24. Cimetidine does not influence the metabolism of the H1-receptor antagonist ebastine to its active metabolite carebastine. Van Rooij, J., Schoemaker, H.C., Bruno, R., Reinhoudt, J.F., Breimer, D.D., Cohen, A.F. British journal of clinical pharmacology. (1993) [Pubmed]
  25. Characterization of Ebastine, Hydroxyebastine, and Carebastine Metabolism by Human Liver Microsomes and Expressed Cytochrome P450 Enzymes: Major Roles for CYP2J2 and CYP3A. Liu, K.H., Kim, M.G., Lee, D.J., Yoon, Y.J., Kim, M.J., Shon, J.H., Choi, C.S., Choi, Y.K., Desta, Z., Shin, J.G. Drug Metab. Dispos. (2006) [Pubmed]
  26. cDNA cloning and expression of a novel cytochrome p450 (cyp4f12) from human small intestine. Hashizume, T., Imaoka, S., Hiroi, T., Terauchi, Y., Fujii, T., Miyazaki, H., Kamataki, T., Funae, Y. Biochem. Biophys. Res. Commun. (2001) [Pubmed]
  27. A novel cytochrome P450 enzyme responsible for the metabolism of ebastine in monkey small intestine. Hashizume, T., Mise, M., Matsumoto, S., Terauchi, Y., Fujii, T., Imaoka, S., Funae, Y., Kamataki, T., Miyazaki, H. Drug Metab. Dispos. (2001) [Pubmed]
  28. Comparative clinical studies with ebastine: efficacy and tolerability. Luria, X. Drug safety : an international journal of medical toxicology and drug experience. (1999) [Pubmed]
  29. A review of the cardiac systemic side-effects of antihistamines: ebastine. Moss, A.J., Chaikin, P., Garcia, J.D., Gillen, M., Roberts, D.J., Morganroth, J. Clin. Exp. Allergy (1999) [Pubmed]
  30. Diazepam effects on the performance of healthy subjects are not enhanced by treatment with the antihistamine ebastine. Mattila, M.J., Aranko, K., Kuitunen, T. British journal of clinical pharmacology. (1993) [Pubmed]
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