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Clinical toxicological aspects of fluoroquinolones
1Institute of Clinical Pharmacology and Toxicology, Freie Universität Berlin, Garystrasse 5, 14195, Germany. stahl@medizin.fu-berlin.de
Abstract:
Reactions of the gastrointestinal tract and the central nervous system are the most often observed adverse effects during therapy with fluoroquinolones. Pathogenesis of the neurotoxic effects of fluoroquinolones could be related to the activation of the NMDA receptor. Animal experiments as well as clinical experience show that the cardiotoxic potentials of sparfloxacin and grepafloxacin are higher than those of the other fluoroquinolones: they cause QT prolongation at rather low doses thus increasing the risk for severe arrhythmia (torsades de pointes). Phototoxicity has been described for all quinolones, but derivatives with a halogen atom at position 8 show the highest potential for such reactions (e.g. clinafloxacin). Chondrotoxicity of quinolones can affect the articular cartilage and the epiphyseal growth plate in immature animals; the use of these drugs in pediatrics should be restricted to carefully selected indications (such as the use of ciprofloxacin in cystic fibrosis). Tendinitis and tendon ruptures can also be induced by quinolones. Overall, quinolones are as well tolerated as most other anti-microbial agents. However, their specific toxic potentials have to be considered when they are chosen for treatment of bacterial infections.
Insights
Fluoroquinolones can cause adverse effects like gastrointestinal and central nervous system reactions. Specific fluoroquinolones carry higher risks for cardiotoxicity, phototoxicity, chondrotoxicity, and tendon issues, requiring careful consideration during treatment.
Area of Science:
- Pharmacology
- Toxicology
- Infectious Diseases
Background:
- Fluoroquinolones are broad-spectrum antibiotics with known adverse effects.
- Gastrointestinal and central nervous system reactions are common.
- Specific fluoroquinolone derivatives exhibit distinct toxicity profiles.
Purpose of the Study:
- To summarize the adverse effects associated with fluoroquinolone therapy.
- To highlight specific toxic potentials including neurotoxicity, cardiotoxicity, phototoxicity, chondrotoxicity, and tendinopathy.
- To inform clinical decision-making regarding fluoroquinolone use.
Main Methods:
- Review of existing literature on fluoroquinolone adverse effects.
- Analysis of animal experiments and clinical data.
- Identification of specific drug properties linked to toxicity.
Main Results:
- Neurotoxic effects may involve NMDA receptor activation.
- Sparfloxacin and grepafloxacin show higher cardiotoxicity, risking QT prolongation and arrhythmia.
- Phototoxicity is more pronounced in 8-halogenated quinolones; chondrotoxicity affects immature cartilage and growth plates.
Conclusions:
- While generally well-tolerated, fluoroquinolones possess specific toxic potentials.
- Cardiotoxicity, neurotoxicity, phototoxicity, chondrotoxicity, and tendon issues are key concerns.
- Careful patient selection and consideration of individual drug toxicities are crucial for safe fluoroquinolone use.