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astemizole and Torsade de Pointes

astemizole has been researched along with Torsade de Pointes in 28 studies

Astemizole: Antihistamine drug now withdrawn from the market in many countries because of rare but potentially fatal side effects.
astemizole : A piperidine compound having a 2-(4-methoxyphenyl)ethyl group at the 1-position and an N-[(4-fluorobenzyl)benzimidazol-2-yl]amino group at the 4-position.

Research Excerpts

ExcerptRelevanceReference
"Since astemizole in an oral dose of 50 mg/kg/day was recently reported to exert anti-cancer effect in mice, we evaluated its proarrhythmic potential using the atrioventricular block dogs in order to clarify its cardiac safety profile."7.83Possibility as an anti-cancer drug of astemizole: Evaluation of arrhythmogenicity by the chronic atrioventricular block canine model. ( Ando, K; Cao, X; Izumi-Nakaseko, H; Nakamura, Y; Sugiyama, A; Wada, T, 2016)
" In order to study the effects of anesthetic agents on the inducibility of TdP, arrhythmias were induced by programmed electrical stimulation (PES) before and after cumulative intravenous administration of quinidine under anesthesia with sodium pentobarbital, halothane, or isoflurane."7.71Acute canine model for drug-induced Torsades de Pointes in drug safety evaluation-influences of anesthesia and validation with quinidine and astemizole. ( Imai, R; Tamura, T; Yamamoto, K; Yamamoto, M, 2001)
"QT interval prolongation and torsade de pointes are associated with astemizole intake and have been ascribed to block the repolarizing K+ currents, specifically the rapidly activating component of the delayed rectifier iKr."7.69Torsade de pointes with an antihistamine metabolite: potassium channel blockade with desmethylastemizole. ( Hoon, TJ; January, CT; Mohammad, S; Studenik, C; Vorperian, VR; Zhou, Z, 1996)
"Prolongation of the QT interval and torsade de pointes has been reported in patients with an overdose of astemizole."5.30Combined use of astemizole and ketoconazole resulting in torsade de pointes. ( Chen, JH; Tsai, LM; Tsai, WC, 1997)
"The possible occurrence of torsade de pointes in astemizole overdose, and the long elimination time of astemizole and hydroxylated metabolites, makes it necessary to maintain ECG monitoring until QT interval has returned to normal."5.29Prolonged QT interval and torsade de pointes following astemizole overdose. ( Danel, V; Dixmerias, F; Saviuc, P, 1993)
"Astemizole (Hismanal-Janssen, New Brunswick, NJ) is a nonsedating antihistamine that has the advantage of a once-daily dosage schedule."5.29Torsade de pointes associated with Astemizole overdose treated with magnesium sulfate. ( Hasan, RA; Nolan, BM; Zureikat, GY, 1993)
"Since astemizole in an oral dose of 50 mg/kg/day was recently reported to exert anti-cancer effect in mice, we evaluated its proarrhythmic potential using the atrioventricular block dogs in order to clarify its cardiac safety profile."3.83Possibility as an anti-cancer drug of astemizole: Evaluation of arrhythmogenicity by the chronic atrioventricular block canine model. ( Ando, K; Cao, X; Izumi-Nakaseko, H; Nakamura, Y; Sugiyama, A; Wada, T, 2016)
" In order to study the effects of anesthetic agents on the inducibility of TdP, arrhythmias were induced by programmed electrical stimulation (PES) before and after cumulative intravenous administration of quinidine under anesthesia with sodium pentobarbital, halothane, or isoflurane."3.71Acute canine model for drug-induced Torsades de Pointes in drug safety evaluation-influences of anesthesia and validation with quinidine and astemizole. ( Imai, R; Tamura, T; Yamamoto, K; Yamamoto, M, 2001)
"Astemizole is a potent histamine H1-antagonist that has been associated with cases of life-threatening cardiac arrhythmias, including torsade de pointes and atrioventricular (AV) block."3.69Electrophysiological and arrhythmogenic effects of the histamine type 1-receptor antagonist astemizole on rabbit Purkinje fibers: clinical relevance. ( Adamantidis, MM; Caron, JF; Dupuis, BA; Lacroix, DL, 1995)
"QT interval prolongation and torsade de pointes are associated with astemizole intake and have been ascribed to block the repolarizing K+ currents, specifically the rapidly activating component of the delayed rectifier iKr."3.69Torsade de pointes with an antihistamine metabolite: potassium channel blockade with desmethylastemizole. ( Hoon, TJ; January, CT; Mohammad, S; Studenik, C; Vorperian, VR; Zhou, Z, 1996)
"Ebastine also inhibit potassium channels, cloned human Kv 1."2.41[The effect of second generation histamine antagonists on the heart]. ( Górska, M; Grzelewska-Rzymowska, I; Pietrzkowicz, M, 2001)
" This paper reviews the pharmacokinetic properties of these second-generation agents and is intended to provide comparisons that help explain differences in dosing profiles and drug interactions for members of this class of drugs."2.40Pharmacokinetic overview of oral second-generation H1 antihistamines. ( Estes, KS; González, MA, 1998)
" The primary difference between traditional (first-generation) and nonsedating (second-generation) histamine1-receptor antagonists is the incidence and severity of adverse reactions."2.39Cardiovascular toxicity of antihistamines. ( Smith, SJ, 1994)
"Treatment of astemizole-induced torsades de pointes includes discontinuing use of astemizole, intravenous administration of magnesium sulfate and isoproterenol, temporary cardiac pacing, and, when necessary, direct current cardioversion."2.39Torsades de pointes ventricular tachycardia associated with overdose of astemizole. ( Adlakha, A; Meloy, TD; Rao, KA; Stanton, MS; Verma-Ansil, B, 1994)
" The lessons learned from the experiences with these drugs hold implications for the future development of agents that prolong the QT interval and suggest the need for dose-response relation data and metabolic evaluations to define the subpopulations at particular risk."1.29Is QT interval prolongation harmful? A regulatory perspective. ( Botstein, P, 1993)
"The possible occurrence of torsade de pointes in astemizole overdose, and the long elimination time of astemizole and hydroxylated metabolites, makes it necessary to maintain ECG monitoring until QT interval has returned to normal."1.29Prolonged QT interval and torsade de pointes following astemizole overdose. ( Danel, V; Dixmerias, F; Saviuc, P, 1993)
"Astemizole (Hismanal-Janssen, New Brunswick, NJ) is a nonsedating antihistamine that has the advantage of a once-daily dosage schedule."1.29Torsade de pointes associated with Astemizole overdose treated with magnesium sulfate. ( Hasan, RA; Nolan, BM; Zureikat, GY, 1993)

Research

Studies (28)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's19 (67.86)18.2507
2000's6 (21.43)29.6817
2010's2 (7.14)24.3611
2020's1 (3.57)2.80

Authors

AuthorsStudies
Pearlstein, R1
Vaz, R1
Rampe, D1
Kramer, J1
Obejero-Paz, CA1
Myatt, G1
Kuryshev, YA1
Bruening-Wright, A1
Verducci, JS1
Brown, AM1
Goto, A1
Sakamoto, K1
Kambayashi, R1
Izumi-Nakaseko, H2
Kawai, S1
Takei, Y1
Matsumoto, A1
Kanda, Y1
Sugiyama, A2
Nakamura, Y1
Cao, X1
Wada, T1
Ando, K1
Dabhi, J1
Mehta, A1
Adamantidis, MM1
Lacroix, DL1
Caron, JF1
Dupuis, BA1
Kelloway, JS1
Pongowski, MA1
Schoenwetter, WF1
Smith, SJ1
Rao, KA1
Adlakha, A1
Verma-Ansil, B1
Meloy, TD1
Stanton, MS1
Wiley, JF1
Henretig, FM1
Goss, JE1
Ramo, BW1
Blake, K1
Botstein, P1
Herings, RM1
Stricker, BH1
Leufkens, HG1
Bakker, A1
Sturmans, F1
Urquhart, J1
Saviuc, P1
Danel, V1
Dixmerias, F1
Sakemi, H1
VanNatta, B1
Hasan, RA1
Zureikat, GY1
Nolan, BM1
Woosley, RL1
Hsieh, MH1
Chen, SA1
Chiang, CE1
Tai, CT1
Lee, SH1
Wen, ZC1
Chang, MS1
Vorperian, VR1
Zhou, Z1
Mohammad, S1
Hoon, TJ1
Studenik, C1
January, CT1
Tsai, WC1
Tsai, LM1
Chen, JH1
Martin, ES1
Rogalski, K1
Black, JN1
Ikeda, S1
Oka, H1
Matunaga, K1
Kubo, S1
Asai, S1
Miyahara, Y1
Osaka, A1
Kohno, S1
González, MA1
Estes, KS1
DuBuske, LM1
Gilbert, JD1
Cahill, SA1
McCartney, DG1
Lukas, A1
Gross, GJ1
Yamamoto, K1
Tamura, T1
Imai, R1
Yamamoto, M1
Mansfield, RJ1
Thomas, RD1
Grzelewska-Rzymowska, I1
Pietrzkowicz, M1
Górska, M1

Reviews

7 reviews available for astemizole and Torsade de Pointes

ArticleYear
Understanding the structure-activity relationship of the human ether-a-go-go-related gene cardiac K+ channel. A model for bad behavior.
    Journal of medicinal chemistry, 2003, May-22, Volume: 46, Issue:11

    Topics: Cation Transport Proteins; DNA-Binding Proteins; Drug-Related Side Effects and Adverse Reactions; ER

2003
Cardiovascular toxicity of antihistamines.
    Otolaryngology--head and neck surgery : official journal of American Academy of Otolaryngology-Head and Neck Surgery, 1994, Volume: 111, Issue:3 Pt 2

    Topics: Astemizole; Drug Interactions; Heart; Histamine H1 Antagonists; Humans; Terfenadine; Torsades de Poi

1994
Torsades de pointes ventricular tachycardia associated with overdose of astemizole.
    Mayo Clinic proceedings, 1994, Volume: 69, Issue:6

    Topics: Adult; Astemizole; Drug Overdose; Electrocardiography; Female; Humans; Rhinitis, Vasomotor; Torsades

1994
Cardiac actions of antihistamines.
    Annual review of pharmacology and toxicology, 1996, Volume: 36

    Topics: Animals; Astemizole; Cetirizine; Diphenhydramine; Drug Interactions; Histamine H1 Antagonists; Human

1996
Pharmacokinetic overview of oral second-generation H1 antihistamines.
    International journal of clinical pharmacology and therapeutics, 1998, Volume: 36, Issue:5

    Topics: Astemizole; Blood-Brain Barrier; Cetirizine; Histamine H1 Antagonists; Humans; Loratadine; Structure

1998
Second-generation antihistamines: the risk of ventricular arrhythmias.
    Clinical therapeutics, 1999, Volume: 21, Issue:2

    Topics: Animals; Astemizole; Cytochrome P-450 Enzyme System; Drug Interactions; Electrocardiography; Heart;

1999
[The effect of second generation histamine antagonists on the heart].
    Pneumonologia i alergologia polska, 2001, Volume: 69, Issue:3-4

    Topics: Animals; Area Under Curve; Astemizole; Butyrophenones; Electrocardiography; Heart; Histamine H1 Anta

2001

Other Studies

21 other studies available for astemizole and Torsade de Pointes

ArticleYear
MICE models: superior to the HERG model in predicting Torsade de Pointes.
    Scientific reports, 2013, Volume: 3

    Topics: ERG1 Potassium Channel; Ether-A-Go-Go Potassium Channels; Humans; Models, Theoretical; Patch-Clamp T

2013
Validation of Risk-Stratification Method for the Chronic Atrioventricular Block Cynomolgus Monkey Model and Its Mechanistic Interpretation Using 6 Drugs With Pharmacologically Distinct Profile.
    Toxicological sciences : an official journal of the Society of Toxicology, 2022, 10-27, Volume: 190, Issue:1

    Topics: Animals; Astemizole; Atrioventricular Block; DNA-Binding Proteins; Electrocardiography; Haloperidol;

2022
Possibility as an anti-cancer drug of astemizole: Evaluation of arrhythmogenicity by the chronic atrioventricular block canine model.
    Journal of pharmacological sciences, 2016, Volume: 131, Issue:2

    Topics: Animals; Antineoplastic Agents; Astemizole; Atrioventricular Block; Disease Models, Animal; Dogs; Fe

2016
QT prolongation and safety in the Indian population.
    Current drug safety, 2007, Volume: 2, Issue:3

    Topics: Astemizole; Cisapride; Databases, Factual; Drug-Related Side Effects and Adverse Reactions; Electroc

2007
Electrophysiological and arrhythmogenic effects of the histamine type 1-receptor antagonist astemizole on rabbit Purkinje fibers: clinical relevance.
    Journal of cardiovascular pharmacology, 1995, Volume: 26, Issue:2

    Topics: Action Potentials; Animals; Arrhythmias, Cardiac; Astemizole; Dose-Response Relationship, Drug; Hist

1995
Additional causes of torsades de pointes.
    Mayo Clinic proceedings, 1995, Volume: 70, Issue:2

    Topics: Astemizole; Drug Overdose; Humans; Terfenadine; Torsades de Pointes

1995
Torsade de pointes.
    Pediatric emergency care, 1993, Volume: 9, Issue:5

    Topics: Adolescent; Astemizole; Drug Overdose; Humans; Magnesium Sulfate; Torsades de Pointes

1993
Torsades de pointes associated with astemizole (Hismanal) therapy.
    Archives of internal medicine, 1993, Dec-13, Volume: 153, Issue:23

    Topics: Aged; Aged, 80 and over; Astemizole; Erythromycin; Female; Humans; Hypokalemia; Torsades de Pointes

1993
Is QT interval prolongation harmful? A regulatory perspective.
    The American journal of cardiology, 1993, Aug-26, Volume: 72, Issue:6

    Topics: Astemizole; Butylamines; Electrocardiography; Humans; Terfenadine; Torsades de Pointes; Urinary Inco

1993
Public health problems and the rapid estimation of the size of the population at risk. Torsades de pointes and the use of terfenadine and astemizole in The Netherlands.
    Pharmacy world & science : PWS, 1993, Oct-15, Volume: 15, Issue:5

    Topics: Adolescent; Adult; Aged; Aged, 80 and over; Astemizole; Child; Child, Preschool; Drug Synergism; Dru

1993
Prolonged QT interval and torsade de pointes following astemizole overdose.
    Journal of toxicology. Clinical toxicology, 1993, Volume: 31, Issue:1

    Topics: Adult; Astemizole; Drug Overdose; Electrocardiography; Female; Gastric Lavage; Half-Life; Humans; Is

1993
Torsade de pointes induced by astemizole in a patient with prolongation of the QT interval.
    American heart journal, 1993, Volume: 125, Issue:5 Pt 1

    Topics: Adult; Astemizole; Electrocardiography; Female; Humans; Long QT Syndrome; Torsades de Pointes

1993
Torsade de pointes associated with Astemizole overdose treated with magnesium sulfate.
    Pediatric emergency care, 1993, Volume: 9, Issue:1

    Topics: Adolescent; Astemizole; Drug Overdose; Electrocardiography; Female; Humans; Magnesium Sulfate; Poiso

1993
Drug-induced torsades de pointes in one patient with congenital long QT syndrome.
    International journal of cardiology, 1996, Apr-19, Volume: 54, Issue:1

    Topics: Adult; Anti-Arrhythmia Agents; Anti-Bacterial Agents; Astemizole; Cardiac Pacing, Artificial; Electr

1996
Torsade de pointes with an antihistamine metabolite: potassium channel blockade with desmethylastemizole.
    Journal of the American College of Cardiology, 1996, Nov-15, Volume: 28, Issue:6

    Topics: Aged; Aged, 80 and over; Animals; Astemizole; Electrocardiography; Female; Heart; Heart Arrest; Hist

1996
Combined use of astemizole and ketoconazole resulting in torsade de pointes.
    Journal of the Formosan Medical Association = Taiwan yi zhi, 1997, Volume: 96, Issue:2

    Topics: Antifungal Agents; Astemizole; Drug Interactions; Electrocardiography; Female; Histamine H1 Antagoni

1997
Quinine may trigger torsades de pointes during astemizole therapy.
    Pacing and clinical electrophysiology : PACE, 1997, Volume: 20, Issue:8 Pt 1

    Topics: Adult; Anti-Allergic Agents; Astemizole; Drug Interactions; Drug Therapy, Combination; Female; Hista

1997
Astemizole-induced torsades de pointes in a patient with vasospastic angina.
    Japanese circulation journal, 1998, Volume: 62, Issue:3

    Topics: Aged; Angina Pectoris, Variant; Anti-Allergic Agents; Astemizole; Coronary Vasospasm; Female; Humans

1998
Predictors of torsades de pointes in rabbit ventricles perfused with sedating and nonsedating histamine H1-receptor antagonists.
    Canadian journal of physiology and pharmacology, 2000, Volume: 78, Issue:5

    Topics: Action Potentials; Animals; Arrhythmias, Cardiac; Astemizole; Cetirizine; Electrocardiography; Heart

2000
Acute canine model for drug-induced Torsades de Pointes in drug safety evaluation-influences of anesthesia and validation with quinidine and astemizole.
    Toxicological sciences : an official journal of the Society of Toxicology, 2001, Volume: 60, Issue:1

    Topics: Acute Disease; Anesthesia; Anesthetics, Inhalation; Animals; Astemizole; Atrioventricular Node; Cath

2001
Recurrent syncope. Drug induced long QT syndrome.
    Postgraduate medical journal, 2001, Volume: 77, Issue:907

    Topics: Adult; Anti-Allergic Agents; Antimalarials; Astemizole; Chloroquine; Electrocardiography; Humans; Lo

2001