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Chemical Compound Review

Astemina     1-[(4-fluorophenyl)methyl]-N- [1-[2-(4...

Synonyms: Hismanal, Alermizol, Astesen, Esmacen, Laridal, ...
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Disease relevance of Retolen


Psychiatry related information on Retolen


High impact information on Retolen

  • Astemizole in the treatment of granulocyte colony-stimulating factor-induced bone pain [11].
  • The data on central nervous system effects of astemizole are limited and were not evaluated [6].
  • Cytochrome P450 3A4 metabolizes terfenadine, astemizole, carbamazepine, alprazolam, triazolam, and other benzodiazepines [12].
  • Even if both drugs differ in their affinity for hEag1 channels (IC50s are approximately 2 microM for imipramine and approximately 200 nM for astemizole) and in their blocking kinetics, both drugs permeate the membrane and inhibit the hEag1 current by selectively binding to open channels [13].
  • However, as astemizole competes with imipramine and intracellular TEA for binding to the channel, it is proposed to interact with an overlapping intracellular binding site [13].

Chemical compound and disease context of Retolen


Biological context of Retolen


Anatomical context of Retolen


Associations of Retolen with other chemical compounds


Gene context of Retolen

  • Experiments with recombinant P450s and antibodies indicate a negligible role for CYP3A4 on the main metabolic route of astemizole, i.e. formation of DES-AST, although CYP3A4 may mediate the relatively minor metabolic routes to 6OH-AST and NOR-AST [30].
  • These results indicate the involvement of CYP2J2 in the presystemic elimination of astemizole in the human small intestine [31].
  • These results suggest that blockade of HERG channels by terfenadine and astemizole might contribute to the cardiac side effects of these compounds [32].
  • During the course of the P450 identification study, higher activities of the astemizole O-demethylation in the rabbit small intestine than in the liver (about 3-fold) were found [31].
  • Effect of the nonsedative H1-receptor antagonist astemizole in perennial allergic and nonallergic rhinitis [33].

Analytical, diagnostic and therapeutic context of Retolen


  1. Astemizole-induced paresthesia. Kaufman, H.S., Chang, P., Chang, G. N. Engl. J. Med. (1990) [Pubmed]
  2. Astemizole-induced torsade de pointes. Simons, F.E., Kesselman, M.S., Giddins, N.G., Pelech, A.N., Simons, K.J. Lancet (1988) [Pubmed]
  3. Regulation of potassium channels by nonsedating antihistamines. Berul, C.I., Morad, M. Circulation (1995) [Pubmed]
  4. Carcinogenicity studies of astemizole in mice and rats. Benze, J., Gypen, L., Vandenberghe, J., Lampo, A., De Coster, R., Bowden, C., Van Cauteren, H. Cancer Res. (1995) [Pubmed]
  5. Giant U waves and associated ventricular tachycardia complicating astemizole overdose: successful therapy with intravenous magnesium. Leor, J., Harman, M., Rabinowitz, B., Mozes, B. Am. J. Med. (1991) [Pubmed]
  6. Sedation and performance issues in the treatment of allergic conditions. Adelsberg, B.R. Arch. Intern. Med. (1997) [Pubmed]
  7. Effects of chlorpheniramine, pyrilamine and astemizole on intracranial self-stimulation in rats. Wauquier, A., Niemegeers, C.J. Eur. J. Pharmacol. (1981) [Pubmed]
  8. Interaction of astemizole, an H1 receptor antagonist, with conventional antiepileptic drugs in mice. Swiader, M., Wielosz, M., Czuczwar, S.J. Pharmacol. Biochem. Behav. (2003) [Pubmed]
  9. Mizolastine, a novel selective histamine H1 receptor antagonist: lack of sedative potential on the EEG in the rodent. Depoortere, H., Decobert, M., Granger, P., Françon, D. Neuropsychobiology (1995) [Pubmed]
  10. A placebo-controlled assessment of mequitazine and astemizole in tests of psychomotor ability. Hindmarch, I., Easton, J.C. International journal of clinical pharmacology research. (1986) [Pubmed]
  11. Astemizole in the treatment of granulocyte colony-stimulating factor-induced bone pain. Gudi, R., Krishnamurthy, M., Pachter, B.R. Ann. Intern. Med. (1995) [Pubmed]
  12. Newer antidepressants and the cytochrome P450 system. Nemeroff, C.B., DeVane, C.L., Pollock, B.G. The American journal of psychiatry. (1996) [Pubmed]
  13. Mechanism of block of hEag1 K+ channels by imipramine and astemizole. García-Ferreiro, R.E., Kerschensteiner, D., Major, F., Monje, F., Stühmer, W., Pardo, L.A. J. Gen. Physiol. (2004) [Pubmed]
  14. The role of antihistamines in the treatment of chronic urticaria. Monroe, E.W. J. Allergy Clin. Immunol. (1990) [Pubmed]
  15. 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]
  16. Efficacy of an oral antihistamine, astemizole, as compared to a nasal steroid spray in hay fever. Salomonsson, P., Gottberg, L., Heilborn, H., Norrlind, K., Pegelow, K.O. Allergy (1988) [Pubmed]
  17. Torsades de pointes ventricular tachycardia associated with overdose of astemizole. Rao, K.A., Adlakha, A., Verma-Ansil, B., Meloy, T.D., Stanton, M.S. Mayo Clin. Proc. (1994) [Pubmed]
  18. Acute canine model for drug-induced Torsades de Pointes in drug safety evaluation-influences of anesthesia and validation with quinidine and astemizole. Yamamoto, K., Tamura, T., Imai, R., Yamamoto, M. Toxicol. Sci. (2001) [Pubmed]
  19. Antihistamines in the treatment of clinical asthma. Rafferty, P. J. Allergy Clin. Immunol. (1990) [Pubmed]
  20. Pharmacokinetic optimisation of histamine H1-receptor antagonist therapy. Simons, F.E., Simons, K.J. Clinical pharmacokinetics. (1991) [Pubmed]
  21. Preclinical in vitro cardiac electrophysiology: a method of predicting arrhythmogenic potential of antihistamines in humans? Cavero, I., Mestre, M., Guillon, J.M., Heuillet, E., Roach, A.G. Drug safety : an international journal of medical toxicology and drug experience. (1999) [Pubmed]
  22. Dual effect of the anti-allergic astemizole on Ca2+ fluxes in rat basophilic leukemia (RBL-2H3) cells: release of Ca2+ from intracellular stores and inhibition of Ca2+ release-activated Ca2+ influx. Fischer, M.J., Paulussen, J.J., de Mol, N.J., Janssen, L.H. Biochem. Pharmacol. (1998) [Pubmed]
  23. Macrolide antibacterials. Drug interactions of clinical significance. von Rosensteil, N.A., Adam, D. Drug safety : an international journal of medical toxicology and drug experience. (1995) [Pubmed]
  24. In vitro and in vivo binding characteristics of a new long-acting histamine H1 antagonist, astemizole. Laduron, P.M., Janssen, P.F., Gommeren, W., Leysen, J.E. Mol. Pharmacol. (1982) [Pubmed]
  25. Safety of antihistamines in children. Ten Eick, A.P., Blumer, J.L., Reed, M.D. Drug safety : an international journal of medical toxicology and drug experience. (2001) [Pubmed]
  26. Uptake, subcellular distribution and biotransformation of 3H-labelled astemizole in cultured rat hepatocytes. Waterkeyn, C., Laduron, P., Meuldermans, W., Trouet, A., Schneider, Y.J. Biochem. Pharmacol. (1987) [Pubmed]
  27. Comparison of triamcinolone acetonide nasal inhaler with astemizole in the treatment of ragweed-induced allergic rhinitis. Bernstein, D.I., Creticos, P.S., Busse, W.W., Cohen, R., Graft, D.F., Howland, W.C., Lumry, W.R., Pedinoff, A.J., Ratner, P.H., Lim, J., Stokes, A., McNally, C. J. Allergy Clin. Immunol. (1996) [Pubmed]
  28. Saquinavir. Clinical pharmacology and efficacy. Vella, S., Floridia, M. Clinical pharmacokinetics. (1998) [Pubmed]
  29. Posttranslational modulation of glucocorticoid feedback inhibition at the pituitary level. Lim, M.C., Shipston, M.J., Antoni, F.A. Endocrinology (2002) [Pubmed]
  30. Involvement of multiple human cytochromes P450 in the liver microsomal metabolism of astemizole and a comparison with terfenadine. Matsumoto, S., Yamazoe, Y. British journal of clinical pharmacology. (2001) [Pubmed]
  31. Involvement of CYP2J2 on the intestinal first-pass metabolism of antihistamine drug, astemizole. Matsumoto, S., Hirama, T., Matsubara, T., Nagata, K., Yamazoe, Y. Drug Metab. Dispos. (2002) [Pubmed]
  32. Blockade of HERG channels expressed in Xenopus oocytes by the histamine receptor antagonists terfenadine and astemizole. Suessbrich, H., Waldegger, S., Lang, F., Busch, A.E. FEBS Lett. (1996) [Pubmed]
  33. Effect of the nonsedative H1-receptor antagonist astemizole in perennial allergic and nonallergic rhinitis. Wihl, J.A., Petersen, B.N., Petersen, L.N., Gundersen, G., Bresson, K., Mygind, N. J. Allergy Clin. Immunol. (1985) [Pubmed]
  34. The treatment of mild to severe chronic idiopathic urticaria with astemizole: double-blind and open trials. Fox, R.W., Lockey, R.F., Bukantz, S.C., Serbousek, D. J. Allergy Clin. Immunol. (1986) [Pubmed]
  35. Comparison of efficacy, safety, and skin test inhibition of cetirizine and astemizole. Berkowitz, R.B., Dockhorn, R., Lockey, R., Findlay, S., Howland, W.C., Mitchell, D.Q., Woehler, T. Ann. Allergy Asthma Immunol. (1996) [Pubmed]
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