ArticleBritish journal of pharmacology2006
No proarrhythmic properties of the antibiotics Moxifloxacin or Azithromycin in anaesthetized dogs with chronic-AV block.
Article in British journal of pharmacology, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 34 papers.
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Who cites it
34 citing papers in PubMed, 81 citations in OpenAlex.
- The effects of apocynin on ciprofloxacin-induced oxidative stress-related cardiotoxicity.Scientific reports · 2025Article
- A novel mutation in hERG gene associated with azithromycin-induced acquired long QT syndrome.Molecular biology reports · 2024Article
- Azithromycin Mitigates Cisplatin-Induced Lung Oxidative Stress, Inflammation and Necroptosis by Upregulating SIRT1, PPARγ, and Nrf2/HO-1 Signaling.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Pharmacokinetic Optimization of Small Molecule Janus Kinase 3 Inhibitors to Target Immune Cells.ACS pharmacology & translational science · 2022Article
- Delivering macrolide antibiotics to heal a broken heart - And other inflammatory conditions.Advanced drug delivery reviews · 2022Review
- The canine chronic atrioventricular block model in cardiovascular preclinical drug research.British journal of pharmacology · 2022Review
- Article
- Quantifying arrhythmic long QT effects of hydroxychloroquine and azithromycin with whole-heart optical mapping and simulations.Heart rhythm O2 · 2021Article
- The Weight of Evidence From Electrophysiology, Observational, and Cardiovascular End Point Studies Demonstrates the Safety of Azithromycin.Clinical and translational science · 2021Review
- Azithromycin: The First Broad-spectrum Therapeutic.European journal of medicinal chemistry · 2020Review
- Azithromycin: The First Broad-spectrum Therapeutic.Journal of translational autoimmunity · 2020Review
- Azithromycin in COVID-19 Patients: Pharmacological Mechanism, Clinical Evidence and Prescribing Guidelines.Drug safety · 2020Review
- Macrolides and viral infections: focus on azithromycin in COVID-19 pathology.International journal of antimicrobial agents · 2020Review
- A Computational Pipeline to Predict Cardiotoxicity: From the Atom to the Rhythm.Circulation research · 2020Article
- Transgenic Rabbit Models in Proarrhythmia Research.Frontiers in pharmacology · 2020Review
- Evaluation of a Fully Automatic Measurement of Short-Term Variability of Repolarization on Intracardiac Electrograms in the Chronic Atrioventricular Block Dog.Frontiers in physiology · 2020Article
- Cardiovascular safety of prokinetic agents: A focus on drug-induced arrhythmias.Neurogastroenterology and motility · 2018Review
- Towards Bridging Translational Gap in Cardiotoxicity Prediction: an Application of Progressive Cardiac Risk Assessment Strategy in TdP Risk Assessment of Moxifloxacin.The AAPS journal · 2018Article
- The anaesthetized rabbit with acute atrioventricular block provides a new model for detecting drug-induced Torsade de Pointes.British journal of pharmacology · 2017Article
- Drug-induced proarrhythmia: risk factors and electrophysiological mechanisms.Nature reviews. Cardiology · 2016Review
Corrections and comments
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Authors and funding
7 authors at 4 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
BACKGROUND & PURPOSE: The therapeutically available quinolone antibiotic moxifloxacin has been used as a positive control for prolonging the QT interval in both clinical and non-clinical studies designed to assess the potential of new drugs to delay cardiac repolarization. Despite moxifloxacin prolonging QT, it has not been shown to cause torsades de pointes arrhythmias (TdP). Azithromycin is a macrolide antibiotic that has rarely been associated, clinically, with cases of proarrhythmia. As there is a lack of clinical data available, the cardiac safety of these drugs was assessed in a TdP-susceptible animal model by evaluating their repolarization and proarrhythmia effects. EXPERIMENTAL APPROACH & KEY
resultsIn transfected HEK cells, the IC(50)s for I (hERG) were 45+/-6 and 856+/-259 microg ml(-1) for moxifloxacin and azithromycin, respectively. Intravenous administration of 2 and 8 mg kg(-1) moxifloxacin (total peak-plasma concentrations 4.6+/-1.5 and 22.9+/-6.8 microg ml(-1)) prolonged the QT(c) in 6 anaesthetized dogs with chronic AV block by 7+/-3 and 21+/-19%, respectively. Similar intravenous doses of azithromycin (total peak-plasma concentrations 5.4+/-1.3 and 20.8+/-4.9 microg ml(-1)) had no electrophysiological effects in the same dogs. The reference compound, dofetilide (25 microg kg(-1) i.v.) caused QT(c) prolongation (29+/-15%) and TdP in all dogs. Beat-to-beat variability of repolarization (BVR), quantified as short-term variability of the left ventricular monophasic action potential duration, was only increased after dofetilide (1.8+/-0.7 to 3.8+/-1.5 ms; P<0.05). CONCLUSION & IMPLICATIONS: As neither moxifloxacin nor azithromycin caused TdP or an increase in the BVR, we conclude that both drugs can be used safely in clinical situations.
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