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Chemical Compound Review

Carebastina     2-[4-[4-(4-benzhydryloxy-1...

Synonyms: Carebastine, Carebastinum, CHEMBL67654, SureCN18538, AG-H-72343, ...
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Disease relevance of Carebastine


High impact information on Carebastine

  • Carebastine (10(-7) to 10(-6) mol/L) inhibited this upregulation [3].
  • CONCLUSION: Ebastine can be safely administered to patients with impaired hepatic function, as no clinically important differences can be anticipated from the pharmacokinetics and safety profile of ebastine/carebastine as compared with healthy subjects [1].
  • Therefore, no apparent accumulation of ebastine occurred, and steady-state concentrations of ebastine and carebastine were predictable from single-dose pharmacokinetics both in healthy subjects and in hepatically impaired patients [1].
  • Ebastine is a novel histamine H1 receptor antagonist that combines potency with a rapid onset (fast absorption) and long duration (slow elimination) of action, at least partially mediated via the formation of an acid metabolite (carebastine) that is even more potent as an antihistamine [4].
  • Carebastine inhibited the release of PGD2 (IC30 8.14 mumol/L) but had little effect on cytokine release [5].

Biological context of Carebastine


Anatomical context of Carebastine


Associations of Carebastine with other chemical compounds

  • Ebastine is extensively and rapidly metabolised to its active metabolite; carebastine, has a half-life of approximately 15 hours and duration of action of at least 24 hours [12].

Gene context of Carebastine


Analytical, diagnostic and therapeutic context of Carebastine


  1. 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]
  2. Carebastine Almirall Prodesfarma. Kingham, P. Current opinion in investigational drugs (London, England : 2000) (2000) [Pubmed]
  3. Regulatory effect of histamine H1 receptor antagonist on the expression of messenger RNA encoding CC chemokines in the human nasal mucosa. Fujikura, T., Shimosawa, T., Yakuo, I. J. Allergy Clin. Immunol. (2001) [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. 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]
  6. 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]
  7. N-Dealkylation and hydroxylation of ebastine by human liver cytochrome P450. Hashizume, T., Mise, M., Terauchi, Y., O, L., Fujii, T., Miyazaki, H., Inaba, T. Drug Metab. Dispos. (1998) [Pubmed]
  8. The effect of CYP2J2, CYP3A4, CYP3A5 and the MDR1 polymorphisms and gender on the urinary excretion of the metabolites of the H-receptor antihistamine ebastine: a pilot study. Gervasini, G., Vizcaino, S., Carrillo, J.A., Caballero, M.J., Benitez, J. British journal of clinical pharmacology. (2006) [Pubmed]
  9. Comparative study of different weighting methods in non-linear regression analysis: implications in the parametrization of carebastine after intravenous administration in healthy volunteers. Jansat, J.M., Lastra, C.F., Mariño, E.L. International journal of clinical pharmacology and therapeutics. (1998) [Pubmed]
  10. The effect of food on the bioavailability of ebastine. Pentikis, H.S., Huang, M.Y., Dorr, M.B., Heald, D.L. American journal of therapeutics. (1997) [Pubmed]
  11. 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]
  12. Clinical pharmacology of new histamine H1 receptor antagonists. Simons, F.E., Simons, K.J. Clinical pharmacokinetics. (1999) [Pubmed]
  13. Blood-brain barrier transport of H1-antagonist ebastine and its metabolite carebastine. Tamai, I., Kido, Y., Yamashita, J., Sai, Y., Tsuji, A. Journal of drug targeting. (2000) [Pubmed]
  14. Comparative pharmacokinetics of the histamine H1-receptor antagonist ebastine and its active metabolite carebastine in rats, guinea pigs, dogs and monkeys. Matsuda, M., Sakashita, M., Mizuki, Y., Yamaguchi, T., Fujii, T., Sekine, Y. Arzneimittel-Forschung. (1994) [Pubmed]
  15. Studies on the first-pass metabolism of ebastine in rats. Fujii, T., Matsumoto, S., Hatoyama, T., Miyazaki, H. Arzneimittel-Forschung. (1997) [Pubmed]
  16. Comparative analysis of the cardiotoxicity proclivities of second generation antihistamines in an experimental model predictive of adverse clinical ECG effects. Hey, J.A., del Prado, M., Sherwood, J., Kreutner, W., Egan, R.W. Arzneimittel-Forschung. (1996) [Pubmed]
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