astemizole

Summary

Summary: Antihistamine drug now withdrawn from the market in many countries because of rare but potentially fatal side effects.

Top Publications

  1. García Ferreiro R, Kerschensteiner D, Major F, Monje F, Stuhmer W, Pardo L. Mechanism of block of hEag1 K+ channels by imipramine and astemizole. J Gen Physiol. 2004;124:301-17 pubmed
    ..The tricyclic antidepressant imipramine and the antihistamine astemizole inhibit the current through Eag1 channels and reduce the proliferation of cancer cells...
  2. Karapetyan Y, Sferrazza G, Zhou M, Ottenberg G, Spicer T, Chase P, et al. Unique drug screening approach for prion diseases identifies tacrolimus and astemizole as antiprion agents. Proc Natl Acad Sci U S A. 2013;110:7044-9 pubmed publisher
    ..We screened a collection of drugs approved for human use and identified astemizole and tacrolimus, which reduced cell-surface PrP and inhibited prion replication in neuroblastoma cells...
  3. Chong C, Chen X, Shi L, Liu J, Sullivan D. A clinical drug library screen identifies astemizole as an antimalarial agent. Nat Chem Biol. 2006;2:415-6 pubmed
    ..The antihistamine astemizole and its principal human metabolite are promising new inhibitors of chloroquine-sensitive and multidrug-resistant ..
  4. Ficker E, Obejero Paz C, Zhao S, Brown A. The binding site for channel blockers that rescue misprocessed human long QT syndrome type 2 ether-a-gogo-related gene (HERG) mutations. J Biol Chem. 2002;277:4989-98 pubmed
    ..Our findings represent a first step toward the design of pharmacological chaperones that will rescue HERG K(+) channels without block. ..
  5. Gardner T, Sander B, Larsen M, Kunselman A, Tenhave T, Lund Andersen H, et al. An extension of the Early Treatment Diabetic Retinopathy Study (ETDRS) system for grading of diabetic macular edema in the Astemizole Retinopathy Trial. Curr Eye Res. 2006;31:535-47 pubmed
    To compare the effects of astemizole, an antihistamine, versus placebo on the 1-year course of diabetic macular edema (DME) and to illustrate use of a modified ETDRS system for grading areas of retinal thickening and hard exudates that ..
  6. Chiu P, Marcoe K, Bounds S, Lin C, Feng J, Lin A, et al. Validation of a [3H]astemizole binding assay in HEK293 cells expressing HERG K+ channels. J Pharmacol Sci. 2004;95:311-9 pubmed
    ..Pharmacological characterization of the [(3)H]astemizole binding assay for HERG K(+) channels was performed using HERG-expressing HEK293 cells...
  7. Musonda C, Whitlock G, Witty M, Brun R, Kaiser M. Chloroquine-astemizole hybrids with potent in vitro and in vivo antiplasmodial activity. Bioorg Med Chem Lett. 2009;19:481-4 pubmed publisher
    ..to form hybrid molecules of two known antimalarial drugs, chloroquine (CQ) and the non-sedating H1 antagonist astemizole. A variety of linkers were investigated to conjugate the two agents into one molecule...
  8. García Quiroz J, Camacho J. Astemizole: an old anti-histamine as a new promising anti-cancer drug. Anticancer Agents Med Chem. 2011;11:307-14 pubmed
    ..Histamine favors the proliferation of normal and malignant cells. Several anti-histamine drugs, including astemizole, can inhibit tumor cell proliferation...
  9. Matsumoto S, Yamazoe Y. Involvement of multiple human cytochromes P450 in the liver microsomal metabolism of astemizole and a comparison with terfenadine. Br J Clin Pharmacol. 2001;51:133-42 pubmed
    The aims of the present study were to investigate the metabolism of astemizole in human liver microsomes, to assess possible pharmacokinetic drug-interactions with astemizole and to compare its metabolism with terfenadine, a typical H1 ..

More Information

Publications90

  1. Yamamoto K, Tamura T, Imai R, Yamamoto M. Acute canine model for drug-induced Torsades de Pointes in drug safety evaluation-influences of anesthesia and validation with quinidine and astemizole. Toxicol Sci. 2001;60:165-76 pubmed
    ..To further validate this model, astemizole was administered intravenously to other dogs under halothane anesthesia. Astemizole at 0...
  2. García Quiroz J, García Becerra R, Barrera D, Santos N, Avila E, Ordaz Rosado D, et al. Astemizole synergizes calcitriol antiproliferative activity by inhibiting CYP24A1 and upregulating VDR: a novel approach for breast cancer therapy. PLoS ONE. 2012;7:e45063 pubmed publisher
    ..b>Astemizole, a new promising antineoplastic drug, targets Eag1 by blocking ion currents...
  3. Vu K, Gelli A. Astemizole and an analogue promote fungicidal activity of fluconazole against Cryptococcus neoformans var. grubii and Cryptococcus gattii. Med Mycol. 2010;48:255-62 pubmed publisher
    ..Here we report that astemizole and a closely related analog (A2) promoted in vitro fungicidal activity of fluconazole against Cryptococcus ..
  4. Ouadid Ahidouch H, Le Bourhis X, Roudbaraki M, Toillon R, Delcourt P, Prevarskaya N. Changes in the K+ current-density of MCF-7 cells during progression through the cell cycle: possible involvement of a h-ether.a-gogo K+ channel. Receptors Channels. 2001;7:345-56 pubmed
    ..9 mV; n = 35 and IK-density = 30.2 +/- 8.5 pA/pF; n = 76). IK was highly sensitive to Mg2+, astemizole and TEA (10 mM)...
  5. Guba W, Green L, Martin R, Roche O, Kratochwil N, Mauser H, et al. From astemizole to a novel hit series of small-molecule somatostatin 5 receptor antagonists via GPCR affinity profiling. J Med Chem. 2007;50:6295-8 pubmed
    The H1R antagonist astemizole was identified as a somatostatin 5 (SST5) receptor antagonist by a comparative sequence analysis of the consensus drug binding pocket of GPCRs...
  6. Gomez Varela D, Contreras Jurado C, Furini S, García Ferreiro R, Stuhmer W, Pardo L. Different relevance of inactivation and F468 residue in the mechanisms of hEag1 channel blockage by astemizole, imipramine and dofetilide. FEBS Lett. 2006;580:5059-66 pubmed
    ..end of the S6 helix (F468) and the introduction of C-type inactivation in the blockage of hEag1 channels by astemizole, imipramine and dofetilide was tested...
  7. Rojo L, Alzate Morales J, Saavedra I, Davies P, Maccioni R. Selective interaction of lansoprazole and astemizole with tau polymers: potential new clinical use in diagnosis of Alzheimer's disease. J Alzheimers Dis. 2010;19:573-89 pubmed publisher
    We describe the interactions of two benzimidazole derivatives, astemizole (AST) and lansoprazole (LNS), with anomalous aggregates of tau protein (neurofibrillary tangles)...
  8. Jakhar R, Paul S, Bhardwaj M, Kang S. Astemizole-Histamine induces Beclin-1-independent autophagy by targeting p53-dependent crosstalk between autophagy and apoptosis. Cancer Lett. 2016;372:89-100 pubmed publisher
    ..In conclusion, these findings indicate that AST-HIS-induced apoptosis and autophagy can be regulated by ROS-mediated signaling pathways. ..
  9. Jeon Y, Kim J, Hwang G, Wu Z, Han H, Park S, et al. Inhibition of cytochrome P450 2J2 by tanshinone IIA induces apoptotic cell death in hepatocellular carcinoma HepG2 cells. Eur J Pharmacol. 2015;764:480-8 pubmed publisher
    ..To identify CYP2J2 inhibitors, 10 terpenoids obtained from plants were screened using astemizole as a CYP2J2 probe substrate in human liver microsomes (HLMs)...
  10. Lee E, Oh J, Park H, Kim D, Lee J, Kim C, et al. Simultaneous gene expression signature of heart and peripheral blood mononuclear cells in astemizole-treated rats. Arch Toxicol. 2010;84:609-18 pubmed publisher
    We investigated the effects of astemizole, a second-generation antihistamine, on the heart and peripheral blood mononuclear cells (PBMCs) and identified the early markers of its cardiotoxicity using gene expression profiling...
  11. Phuc N, Wu Z, O Y, Lee J, Oh S, Song G, et al. LKY-047: First Selective Inhibitor of Cytochrome P450 2J2. Drug Metab Dispos. 2017;45:765-769 pubmed publisher
    ..LKY-047 was demonstrated to be a strong competitive inhibitor of CYP2J2-mediated astemizole O-demethylase and terfenadine hydroxylase activity, with Ki values of 0.96 and 2...
  12. Garg V, Sachse F, Sanguinetti M. Tuning of EAG K(+) channel inactivation: molecular determinants of amplification by mutations and a small molecule. J Gen Physiol. 2012;140:307-24 pubmed publisher
    ..for current inhibition and channel activation are predicted to overlap, as we demonstrate for clofilium and astemizole. The mutation Y464A in the S6 segment also induced inactivation of EAG1, with a time course and voltage ..
  13. Sawayama A, Chen M, Kulanthaivel P, Kuo M, Hemmerle H, Arnold F. A panel of cytochrome P450 BM3 variants to produce drug metabolites and diversify lead compounds. Chemistry. 2009;15:11723-9 pubmed publisher
    ..of reactivity of human P450s by producing 12 of 13 mammalian metabolites for two marketed drugs, verapamil and astemizole, and one research compound...
  14. Viramontes Madrid J, Jerjes Sánchez C, Pelaez Ballestas I, Aguilar Chiu A, Hernández Garduño A. [Risk of drug interactions. Combinations of drugs associated with ventricular arrhythmias]. Rev Invest Clin. 2002;54:192-7 pubmed
    To determine the frequency of concurrent use of cisapride, astemizole and terfenadine with macrolides and azole antimitotics, drug combinations that have been reported in the literature as producing a pharmacological interaction ..
  15. Kim J, Choi Y, Lee B, Lee D. Surface-patterned SU-8 cantilever arrays for preliminary screening of cardiac toxicity. Biosens Bioelectron. 2016;80:456-462 pubmed publisher
    ..Following preliminary experiments, Isoproterenol, Verapamil, and Astemizole were used to investigate the effect of drug toxicity on the physiology of cardiomyocytes...
  16. Ho M, Ring N, Amaral K, Doshi U, Li A. Human Enterocytes as an In Vitro Model for the Evaluation of Intestinal Drug Metabolism: Characterization of Drug-Metabolizing Enzyme Activities of Cryopreserved Human Enterocytes from Twenty-Four Donors. Drug Metab Dispos. 2017;45:686-691 pubmed publisher
    ..6-hydroxylation), CYP3A4 (midazolam 1'-hydroxylation and testosterone 6β-hydroxylation), CYP2J2 (astemizole O-demethylation), UDP-glucuronosyltransferase (UGT; 7-hydroxycoumarin glucuronidation), sulfotransferase (SULT; ..
  17. Poluzzi E, Diemberger I, De Ridder M, Koci A, Clo M, Oteri A, et al. Use of antihistamines and risk of ventricular tachyarrhythmia: a nested case-control study in five European countries from the ARITMO project. Eur J Clin Pharmacol. 2017;73:1499-1510 pubmed publisher
    After regulatory restrictions for terfenadine and astemizole in '90s, only scarce evidence on proarrhythmic potential of antihistamines has been published...
  18. Zeng H, Roman M, Lis E, Lagrutta A, Sannajust F. Use of FDSS/?Cell imaging platform for preclinical cardiac electrophysiology safety screening of compounds in human induced pluripotent stem cell-derived cardiomyocytes. J Pharmacol Toxicol Methods. 2016;81:217-22 pubmed publisher
    ..Other drugs, such as astemizole, solifenacin, and moxifloxacin, exhibited similar arrhythmias at 30nM, 3?M and 300?M, respectively...
  19. Margulis M, Sorota S, Chu I, Soares A, Priestley T, Nomeir A. Protein binding-dependent decreases in hERG channel blocker potency assessed by whole-cell voltage clamp in serum. J Cardiovasc Pharmacol. 2010;55:368-76 pubmed publisher
    ..These data suggest that for highly bound compounds, direct measurement of IC50s in the presence of 100% serum may provide a more accurate estimate of in vivo potencies than the approach based on calculated serum shifts. ..
  20. Danielsson B, Danielsson C, Nilsson M. Embryonic cardiac arrhythmia and generation of reactive oxygen species: common teratogenic mechanism for IKr blocking drugs. Reprod Toxicol. 2007;24:42-56 pubmed
    ..Drugs blocking the IKr channel, such as almokalant, dofetilide, phenytoin, cisapride and astemizole, do all produce a similar pattern of hypoxia-related malformations...
  21. Weissenburger J. A lingering mistake. CMAJ. 2006;174:664 pubmed
  22. Tani E, Rekka E, Kourounakis P. Modification of lipid peroxidation by some known substituted imidazole derivatives. An attempt to correlate their antioxidant activity with lipophilicity. Pharmazie. 1991;46:118-9 pubmed
    The antioxidant activity of two antiallergic agents, oxatomide, astemizole and two neuroleptic drugs, penfluridol, pimozide, structurally related, was tested, using heat-inactivated rat hepatic microsomal fraction and linoleic acid...
  23. Swiader M, Chwalczuk K, Wielosz M, Czuczwar S. Influence of chronic treatment with H1 receptor antagonists on the anticonvulsant activity of antiepileptic drugs. Pol J Pharmacol. 2001;53:93-6 pubmed
    The aim of this study was to evaluate the effects of chronic astemizole and ketotifen administration on the anticonvulsant activity of antiepileptic drugs against maximal electroshock-induced convulsions in mice...
  24. Phan H, Moeller M, Nahata M. Treatment of allergic rhinitis in infants and children: efficacy and safety of second-generation antihistamines and the leukotriene receptor antagonist montelukast. Drugs. 2009;69:2541-76 pubmed publisher
    ..Unlike their predecessors, such as astemizole and terfenadine, the newer second-generation antihistamines and montelukast appear to be well tolerated, with ..
  25. Swiader M, Łuszczki J, Wielosz M, Czuczwar S. Effect of histamine receptor antagonists on aminophylline-induced seizures and lethality in mice. Pharmacol Rep. 2005;57:531-5 pubmed
    The aim of this study was to evaluate the effects of H(1) (antazoline and astemizole) or H(2) (cimetidine and famotidine) histamine receptor antagonists on the clonic phase, tonic seizures and morality of mice challenged with ..
  26. Ellegaard A, Dehlendorff C, Vind A, Anand A, Cederkvist L, Petersen N, et al. Repurposing Cationic Amphiphilic Antihistamines for Cancer Treatment. EBioMedicine. 2016;9:130-139 pubmed publisher
    ..Of the less frequently described CAD antihistamines, astemizole showed a similar significant association with reduced mortality as loratadine among patients with any non-..
  27. Clements M, Millar V, Williams A, Kalinka S. Bridging Functional and Structural Cardiotoxicity Assays Using Human Embryonic Stem Cell-Derived Cardiomyocytes for a More Comprehensive Risk Assessment. Toxicol Sci. 2015;148:241-60 pubmed publisher
    ..structure) we profiled a panel of 13 drugs with well characterized cardiac liabilities (Amiodarone, Aspirin, Astemizole, Axitinib, AZT, Bepridil, Doxorubicin, E-4031, Mexiletine, Rosiglitazone, Sunitinib, Sibutramine, and Verapamil)...
  28. Benedetto S, Sloan A, Duncan B. Impact of interventions designed to increase market share and prescribing of fexofenadine at HMOs. Am J Health Syst Pharm. 2000;57:1778-85 pubmed
    ..period at four HMOs were analyzed to identify all new and refill prescriptions for loratadine, fexofenadine, astemizole, and cetirizine...
  29. Gutierrez Castrellon P, Ramirez Mayans J, López Pérez G. [Efficacy and safety of astemizole in the treatment of allergic rhinitis and urticaria: a systematic review with meta-analysis]. Rev Alerg Mex. 2005;52:113-26 pubmed
    To compare astemizole with other first or second generation antihistaminics in the treatment of allergic rhinitis or urticaria. Systematic revision of clinical, controlled and randomized tests...
  30. Borowiec A, Hague F, Gouilleux Gruart V, Lassoued K, Ouadid Ahidouch H. Regulation of IGF-1-dependent cyclin D1 and E expression by hEag1 channels in MCF-7 cells: the critical role of hEag1 channels in G1 phase progression. Biochim Biophys Acta. 2011;1813:723-30 pubmed publisher
    ..Interestingly, astemizole, a blocker of hEag1 channels, but not E4031, a blocker of HERG channels, inhibited the expression of both ..
  31. Fischer M, Paulussen J, de Mol N, Janssen L. 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. Biochem Pharmacol. 1998;55:1255-62 pubmed
    The antiallergic drugs astemizole and norastemizole inhibit exocytosis in mast cells, which might be relevant for their therapeutic action. From previous studies, it appeared that the drugs inhibited 45Ca2+ influx...
  32. Watanabe H, Honda Y, Deguchi J, Yamada T, Bando K. Usefulness of cardiotoxicity assessment using calcium transient in human induced pluripotent stem cell-derived cardiomyocytes. J Toxicol Sci. 2017;42:519-527 pubmed publisher
    ..Using these approaches would allow selection of compounds with low cardiotoxic potential at the early stage of drug discovery. ..
  33. Nomura F, Kaneko T, Hattori A, Yasuda K. On-chip constructive cell-network study (II): on-chip quasi-in vivo cardiac toxicity assay for ventricular tachycardia/fibrillation measurement using ring-shaped closed circuit microelectrode with lined-up cardiomyocyte cell network. J Nanobiotechnology. 2011;9:39 pubmed publisher
    ..FP duration prolongation and its fluctuation increase was also observed according to the increase of Astemizole concentration...
  34. Lever R, Hefni A, Moffatt J, Paul W, Page C. Effect of tecastemizole on pulmonary and cutaneous allergic inflammatory responses. Clin Exp Allergy. 2007;37:909-17 pubmed
    Tecastemizole, a major metabolite of astemizole, is a potent and selective H1 receptor antagonist...
  35. Declercq L, Celen S, Lecina J, Ahamed M, Tousseyn T, Moechars D, et al. Comparison of New Tau PET-Tracer Candidates With [18F]T808 and [18F]T807. Mol Imaging. 2016;15: pubmed publisher
    ..affinity and selectivity for tau of the reported radiolabeled tracers BF-158, BF-170, THK5105, lansoprazole, astemizole, and novel tau positron emission tomography ligands against T807 and T808...
  36. Fischer M, Paulussen J, Horbach D, Roelofsen E, van Miltenburg J, de Mol N, et al. Inhibition of mediator release in RBL-2H3 cells by some H1-antagonist derived anti-allergic drugs: relation to lipophilicity and membrane effects. Inflamm Res. 1995;44:92-7 pubmed
    ..This could affect several membrane related processes, which are abundant in the early phases of the IgE-mediated signal transduction process. ..
  37. Tripathi S, Griyappanavar C, Lal A, Biswas K, Biswas N, Sankaranarayanan A, et al. Evaluation of antimuscarinic activity in human volunteers: a teaching aid in clinical pharmacology. Indian J Physiol Pharmacol. 1995;39:163-5 pubmed
    The antimuscarinic activity of oxyphenonium bromide, diphenhydramine hydrochloride and astemizole were evaluated in six volunteers. The parameters used were salivary secretion, heart rate and pupillary size...
  38. Dabhi J, Mehta A. QT prolongation and safety in the Indian population. Curr Drug Saf. 2007;2:200-3 pubmed
    ..This article will focus on recommendation of study on the normal limits of QT interval in Indian population and preparation of the database, which can be helpful in withdrawal of drugs from the market that produces QT prolongation. ..
  39. Tsutsui H, Higashijima S, Miyawaki A, Okamura Y. Visualizing voltage dynamics in zebrafish heart. J Physiol. 2010;588:2017-21 pubmed publisher
    ..Application of the anti-allergy compound astemizole resulted in aberrant propagation of excitation, which accounted for a lack of ventricular contraction...
  40. Van Wauwe J, Goossens J. Arabinogalactan- and dextran-induced ear inflammation in mice: differential inhibition by H1-antihistamines, 5-HT-serotonin antagonists and lipoxygenase blockers. Agents Actions. 1989;28:78-82 pubmed
    ..and dextran responses were inhibited by aprotinin, a kallikrein inhibitor, and the mixed H1/5-HT antagonists astemizole and azatadine...
  41. Neubauer D, Kuhar M, Ravnik I. Antihistamine responsive cluster headache in a teenaged girl. Headache. 1997;37:296-8 pubmed
    ..Thorough investigations failed to prove any definite cause. Antihistamine prophylaxis, first with astemizole and then with loratadine, proved to be very effective...
  42. Bilgili S, Karadag A, Calka O, Ozdemir S, Kosem M. A case of generalized lichen nitidus successfully treated with narrow-band ultraviolet B treatment. Photodermatol Photoimmunol Photomed. 2013;29:215-7 pubmed publisher
    ..There is no consensus on treatment. Corticosteroid, astemizole, phototherapy has been used; however, the results are controversial...
  43. de Guadalupe Chávez López M, Pérez Carreón J, Zuñiga García V, Díaz Chávez J, Herrera L, Caro Sánchez C, et al. Astemizole-based anticancer therapy for hepatocellular carcinoma (HCC), and Eag1 channels as potential early-stage markers of HCC. Tumour Biol. 2015;36:6149-58 pubmed publisher
    Hepatocellular carcinoma (HCC) has very poor prognosis. Astemizole has gained great interest as a potential anticancer drug because it targets several proteins involved in cancer including the Eag1 (ether à-go-go-1) potassium channel ..
  44. Fano S, Caliskan G, Heinemann U. Differential effects of blockade of ERG channels on gamma oscillations and excitability in rat hippocampal slices. Eur J Neurosci. 2012;36:3628-35 pubmed publisher
    Agents such as sertindole and astemizole affect heart action by inducing long-QT syndrome, suggesting that apart from their neuronal actions through histamine receptors, 5-HT2 serotonin receptors and D2 dopamine receptors they also affect ..
  45. Taglialatela M, Secondo A, Fresi A, Rosati B, Pannaccione A, Castaldo P, et al. Inhibition of depolarization-induced [3H]noradrenaline release from SH-SY5Y human neuroblastoma cells by some second-generation H(1) receptor antagonists through blockade of store-operated Ca(2+) channels (SOCs). Biochem Pharmacol. 2001;62:1229-38 pubmed
    ..The second-generation H(1) receptor blockers astemizole, terfenadine, and loratadine, as well as the first-generation compound hydroxyzine, inhibited [3H]NE release ..
  46. Ma L, Lee S, Lee C, Yin S, Wang J. Molecular cloning and kinetic characterization of an aldehyde dehydrogenase gene in Klebsiella pneumoniae. J Formos Med Assoc. 2005;104:221-30 pubmed
    ..6 mM). The expression of the aldA gene is higher in K. pneumoniae strains from patients with liver abscess. The aldA gene encodes functional ALDH and can use glycolaldehyde and glyceraldehydes as substrates. ..
  47. Lee S, Jeong H, Liu K, Ryu J, Moon T, Yoon C, et al. Identification and functional characterization of novel CYP2J2 variants: G312R variant causes loss of enzyme catalytic activity. Pharmacogenet Genomics. 2005;15:105-13 pubmed
    CYP2J2 plays important roles in the metabolism of therapeutic drugs, such as astemizole and ebastine, as well as endogenous fatty acids...
  48. Guo J, Schofield G. Histamine inhibits KCNQ2/KCNQ3 channel current via recombinant histamine H(1) receptors. Neurosci Lett. 2002;328:285-8 pubmed
    ..09 and was completely abolished by the H(1) receptor selective antagonist, astemizole. Studies of the modulatory effects of histamine on I(M) may aid in elucidating the signal transduction pathway(s)..
  49. Nishimuta H, Sato K, Mizuki Y, Yabuki M, Komuro S. Species differences in intestinal metabolic activities of cytochrome P450 isoforms between cynomolgus monkeys and humans. Drug Metab Pharmacokinet. 2011;26:300-6 pubmed publisher
  50. Ghosal A, Lu X, Penner N, Gao L, Ramanathan R, Chowdhury S, et al. Identification of human liver cytochrome P450 enzymes involved in the metabolism of SCH 530348 (Vorapaxar), a potent oral thrombin protease-activated receptor 1 antagonist. Drug Metab Dispos. 2011;39:30-8 pubmed publisher
    ..Formation of M20 by human liver microsomes was inhibited 89% by ketoconazole, 75% by astemizole (a CYP2J2 inhibitor), and 43% by CYP3A4 monoclonal antibody...
  51. Hsieh Y, Li F, Korfmacher W. Mapping pharmaceuticals in rat brain sections using MALDI imaging mass spectrometry. Methods Mol Biol. 2010;656:147-58 pubmed publisher
    ..As example, MALDI-MS/MS imaging system was employed for visualizing the spatial distribution of astemizole and its primary metabolite in rat brain tissues...
  52. Stanley N, Alford C, Rombaut N, Hindmarch I. Comparison of the effects of astemizole/pseudoephedrine and triprolidine/pseudoephedrine on CNS activity and psychomotor function. Int Clin Psychopharmacol. 1996;11:31-6 pubmed
    The sedative properties of astemizole-D and triprolidine-D were compared in a double-blind, placebo-controlled, repeated-measures design study comprising three experimental treatments, each with a duration of 2 days (n = 12)...
  53. Swiader M, Wielosz M, Czuczwar S. Interaction of astemizole, an H1 receptor antagonist, with conventional antiepileptic drugs in mice. Pharmacol Biochem Behav. 2003;76:169-78 pubmed
    ..The aim of this study was to evaluate the effects of astemizole-given intraperitoneally, singly or for 7 days on the anticonvulsant activity of antiepileptic drugs (AEDs) ..
  54. Goldsmith P, Dowd P. The new H1 antihistamines. Treatment of urticaria and other clinical problems. Dermatol Clin. 1993;11:87-95 pubmed
    ..The efficacy of the new H1 antihistamines in the treatment of itch due to atopic eczema and systemic disease remains uncertain, and further controlled clinical trials are needed to elucidate their possible role in these conditions. ..
  55. Styczynska Soczka K, Zechini L, Zografos L. Validating the Predicted Effect of Astemizole and Ketoconazole Using a Drosophila Model of Parkinson's Disease. Assay Drug Dev Technol. 2017;15:106-112 pubmed publisher
    ..disease, made by expressing human alpha-synuclein in the Drosophila brain, to validate two repurposed compounds: astemizole and ketoconazole...
  56. Waterkeyn C, Laduron P, Meuldermans W, Trouet A, Schneider Y. Uptake, subcellular distribution and biotransformation of 3H-labelled astemizole in cultured rat hepatocytes. Biochem Pharmacol. 1987;36:4129-36 pubmed
    When incubated with 3H-astemizole, a potent antagonist of H1 receptor, cultured rat hepatocytes, which do not express specific receptors for this ligand, avidly take up 3H-label proportionally to the drug concentration...
  57. Paakkari I. Cardiotoxicity of new antihistamines and cisapride. Toxicol Lett. 2002;127:279-84 pubmed
    Although the new second-generation nonsedative antihistamines terfenadine and astemizole were launched as highly selective and specific H(1)-receptor antagonists, they were later found to cause prolongation of the QT-interval and severe ..
  58. Rossignoli P, Rodrigues A, Tinti T, Pereira O, Ellinger F, Chies A. The possible involvement of hyperpolarizing mechanisms in histamine-induced relaxation of the rat portal vein. J Smooth Muscle Res. 2008;44:129-41 pubmed
    ..The histamine-induced relaxation also was not prevented by astemizole (10(-6) M, 10(-5) M and 10(-4) M), cimetidine (10(-5) M, 10(-4) M and 10(-3) M) or thioperamide (10(-6) M, 10(-5)..
  59. Straumann A, Spichtin H, Bernoulli R, Loosli J, Vögtlin J. [Idiopathic eosinophilic esophagitis: a frequently overlooked disease with typical clinical aspects and discrete endoscopic findings]. Schweiz Med Wochenschr. 1994;124:1419-29 pubmed
    ..Prompt diagnosis also avoids further diagnostic procedures and permits rapid remission through treatment with steroids and antihistamines. ..
  60. Doggrell S. Triamcinolone: new and old indications. Expert Opin Pharmacother. 2001;2:1177-86 pubmed
    ..Triamcinolone is used in the treatment of respiratory inflammation, rheumatoid arthritis and a variety of other inflammatory conditions. ..
  61. Taglialatela M, Pannaccione A, Castaldo P, Giorgio G, Annunziato L. Inhibition of HERG1 K(+) channels by the novel second-generation antihistamine mizolastine. Br J Pharmacol. 2000;131:1081-8 pubmed
    ..life-threatening side effects of therapy with the second-generation H(1) receptor antagonists terfenadine and astemizole. Blockade of the K(+) channels encoded by the Human Ether-à-go-go-Related Gene 1 (HERG1) K(+) channels, which ..
  62. Parvez M, Braitenbach K. Astemizole tetrachlorocuprate(II). Acta Crystallogr C. 2000;56 ( Pt 10):1216-7 pubmed
    ..tetrachlorocuprate(II), (C(28)H(33)FN(4)O)[CuCl(4)], contains diprotonated cations of astemizole hydrogen bonded to three Cl atoms in two different CuCl(4)(2-) anions, with Cl.N distances in the range 3...
  63. de Abajo F, Rodriguez L. Risk of ventricular arrhythmias associated with nonsedating antihistamine drugs. Br J Clin Pharmacol. 1999;47:307-13 pubmed
    ..incidence of ventricular arrhythniias associated with the use of five nonsedating antihistamines: acrivastine, astemizole, cetirizine, loratadine and terfenadine...
  64. Masetti M, Cavalli A, Recanatini M. Modeling the hERG potassium channel in a phospholipid bilayer: Molecular dynamics and drug docking studies. J Comput Chem. 2008;29:795-808 pubmed
    ..identify a possible binding mode for the most potent hERG channel blocker so far known, the antihistaminic drug astemizole. We show that the combined use of MD and docking is suitable to identify a possible binding mode of drugs in a ..
  65. Tabo M, Nakamura M, Kimura K, Ito S. QT-RR relationships and suitable QT correction formulas for halothane-anesthetized dogs. J Toxicol Sci. 2006;31:381-90 pubmed
    ..For both Fridericia's and the optimized formula, QT-prolonging drugs (d,l-sotalol, astemizole) showed QTc interval prolongation. A non-QT-prolonging drug (d,l-propranolol) failed to prolong the QTc interval...
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    ..protective dose (PD50S)] as brompheniramine, chlorpheniramine, pyrilamine, and promethazine and superior to astemizole, diphenhydramine, terfenadine, and oxatomide...
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    ..of five in vitro assays in predicting in vivo tumor growth stimulation by the H1-antihistamines loratadine, astemizole, cetirizine, hydroxyzine, and doxylamine...
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    ..antagonist cetirizine has been examined and compared with that of other second-generation antihistamines (astemizole, terfenadine, and loratadine)...
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    ..Terfenadine (3 mg kg(-1) h(-1), i.v.) and astemizole (0.3 and 1 mg kg(-1) h(-1), i.v...
  70. Matsumoto S, Hirama T, Matsubara T, Nagata K, Yamazoe Y. Involvement of CYP2J2 on the intestinal first-pass metabolism of antihistamine drug, astemizole. Drug Metab Dispos. 2002;30:1240-5 pubmed
    Orally administered astemizole is well absorbed but undergoes an extensive first-pass metabolism to O-desmethylastemizole...
  71. Matsumoto S, Hirama T, Kim H, Nagata K, Yamazoe Y. In vitro inhibition of human small intestinal and liver microsomal astemizole O-demethylation: different contribution of CYP2J2 in the small intestine and liver. Xenobiotica. 2003;33:615-23 pubmed
    1. The effects of chemical agents on the metabolism of the antihistamine drug astemizole were investigated to evaluate drug-drug interactions. 2...
  72. Shiotani M, Harada T, Abe J, Hamada Y, Horii I. Methodological validation of an existing telemetry system for QT evaluation in conscious guinea pigs. J Pharmacol Toxicol Methods. 2007;55:27-34 pubmed
    ..We believe that the information provided herein will be a quite helpful guide for researchers to evaluate the QT interval reliably and reproducibly in this telemetry guinea pig model. ..
  73. Nicolas J, Whomsley R, Collart P, Roba J. In vitro inhibition of human liver drug metabolizing enzymes by second generation antihistamines. Chem Biol Interact. 1999;123:63-79 pubmed
    Cetirizine, terfenadine, loratadine, astemizole and mizolastine were compared for their ability to inhibit marker activities for CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP3A4 and for some glucuronidation isoenzymes in human liver microsomes...
  74. Pan J, O Neill A, Hancock A, Sullivan J, Brioni J. Histaminergic ligands attenuate barrel rotation in rats following unilateral labyrinthectomy. Methods Find Exp Clin Pharmacol. 1998;20:771-7 pubmed
    ..robust behavioral changes, which was used in further experiments; ii) the clinically used antivertigo agent, astemizole, significantly reduced the rotational behavior in UL rats; iii) the more potent H3 antagonists, thioperamide and ..
  75. Lee C, Jones J, Katayama J, Kaspera R, Jiang Y, Freiwald S, et al. Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity. Drug Metab Dispos. 2012;40:943-51 pubmed publisher
    CYP2J2, an arachidonic acid epoxygenase, is recognized for its role in the first-pass metabolism of astemizole and ebastine...
  76. Al Mutairi N, Hassanein A, Nour Eldin O, Arun J. Generalized lichen nitidus. Pediatr Dermatol. 2005;22:158-60 pubmed
    ..The pigmented macules showed melanin pigmentation on histology. There was no response to oral astemizole treatment for 3 months...
  77. Yao J, Du X, Lu D, Baker R, Daharsh E, Atterson P. Estimation of potency of HERG channel blockers: impact of voltage protocol and temperature. J Pharmacol Toxicol Methods. 2005;52:146-53 pubmed
    ..block the channel in the closed (ketoconazole and BeKm-1), open, and/or inactivated states (E-4031, astemizole, and terfenadine) in HEK293 cells transfected with HERG cDNA at room temperature and near-physiological ..
  78. Roy J, Vantol B, Cowley E, Blay J, Linsdell P. Pharmacological separation of hEAG and hERG K+ channel function in the human mammary carcinoma cell line MCF-7. Oncol Rep. 2008;19:1511-6 pubmed
    Pharmacological inhibitors of the human ether-a-go-go (hEAG) potassium channel, astemizole and imipramine, have been used to demonstrate that hEAG plays a role in cancer cell proliferation...
  79. Borowiec A, Hague F, Harir N, Guénin S, Guerineau F, Gouilleux F, et al. IGF-1 activates hEAG K(+) channels through an Akt-dependent signaling pathway in breast cancer cells: role in cell proliferation. J Cell Physiol. 2007;212:690-701 pubmed
    ..The MCF-7 cell proliferation induced by IGF-1 is inhibited pharmacologically by Astemizole or Quinidine or more specifically using siRNA against hEAG channel...
  80. Simons F, Simons K, Chung M, Yeh J. The comparative pharmacokinetics of H1-receptor antagonists. Ann Allergy. 1987;59:20-4 pubmed
    ..from 20 to 25 hours for hydroxyzine, chlorpheniramine, and brompheniramine; and from 5 to 14 days for astemizole. Few pharmacokinetic studies of H1-receptor antagonists in children have been reported...
  81. Testai L, Breschi M, Martinotti E, Calderone V. QT prolongation in guinea pigs for preliminary screening of torsadogenicity of drugs and drug-candidates. II. J Appl Toxicol. 2007;27:270-5 pubmed
    ..The corresponding RR prolongation is a consequence (not the cause) of this primary effect. Astemizole, haloperidol and terfenadine, torsadogenic in humans, produced in Langendorff perfused guinea pig hearts a ..