Torsade de Pointes with an antihistamine metabolite: Potassium channel blockade with desmethylastemizole
| Autor: | Craig T. January, Timothy J. Hoon, Christian Studenik, Zhengfeng Zhou, V.R. Vorperian, Saeed Mohammad |
|---|---|
| Rok vydání: | 1996 |
| Předmět: |
medicine.medical_specialty
Potassium Channels medicine.drug_class Voltage clamp Metabolite medicine.medical_treatment QT interval Afterdepolarization Electrocardiography chemistry.chemical_compound Torsades de Pointes Internal medicine medicine Animals Humans Aged Aged 80 and over business.industry Heart Astemizole Receptor antagonist Potassium channel Heart Arrest Endocrinology chemistry Histamine H1 Antagonists Female Antihistamine Rabbits business Cardiology and Cardiovascular Medicine medicine.drug |
| Zdroj: | Journal of the American College of Cardiology. 28(6):1556-1561 |
| ISSN: | 0735-1097 |
| DOI: | 10.1016/s0735-1097(96)00352-x |
| Popis: | Objectives. Proarrhythmic effects have been observed with the selective histamine1 (H1) receptor antagonist drug astemizole, a widely prescribed antihistamine. The metabolites of astemizole and those of other antihistamine compounds have not been implicated as causative agents of cardiac arrhythmias. The purpose of this study was to examine whether desmethylastemizole, the principal metabolite of astemizole, blocks delayed rectifier potassium (K+) channels.Background. 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. Astemizole undergoes extensive first-pass metabolism, and its dominant metabolite, desmethylastemizole, has a markedly prolonged elimination time. We report the clinical observation of QT prolongation and torsade de pointes in a patient with undetectable serum concentrations of astemizole ( |
| Databáze: | OpenAIRE |
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