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Toxicity of quinolones
1Institute of Clinical Pharmacology and Toxicology, Department of Toxicology, University Medical Center Benjamin Franklin, Freie Universität Berlin, Germany.
Abstract:
Reactions of the gastrointestinal tract, the CNS and the skin are the most often observed adverse effects during therapy with fluoroquinolones. At least for some of the newer fluoroquinolones a steep dose-response relationship of adverse effects seems to exist. Pathogenesis of the neurotoxic effects of fluoroquinolones is still unknown. Among the newer drugs, trovafloxacin caused mild CNS reactions such as dizziness and lightheadedness in a considerable proportion of patients. Young females seem to be especially sensitive to this effect, which diminishes during treatment or if taken together with food. Cardiotoxic potentials of sparfloxacin and grepafloxacin are higher than those of other fluoroquinolones, but during therapy no clearcut drug-related serious reactions have been reported, apart from a slight prolongation of the QT interval. However, to avoid risks these drugs should not be prescribed to patients with known prolongation of the QT interval (e.g. patients on antiarrhythmics). Phototoxicity has been described for all quinolones, but derivatives with a halogen atom at position 8 show the highest potential for such reactions. Fleroxacin, sparfloxacin, clinafloxacin and lomefloxacin belong to this group of fluoroquinolones. The phototoxic potential of the other new fluoroquinolones is considerably lower, but extensive exposure to UV light should generally be avoided during therapy with all quinolones. Chondrotoxicity of quinolones, as observed in immature animals, can affect articular cartilage and/or the epiphyseal growth plate, depending on the developmental stage. Pathogenesis of chondrotoxicity can probably be explained by the magnesium-chelating properties of these drugs. As juveniles are especially sensitive, use of these drugs in paediatrics should be restricted to carefully selected indications (such as the use of ciprofloxacin in cystic fibrosis). Another manifestation of the toxic effects of quinolones on connective tissue structures are tendopathies. Tendinitis and tendon ruptures have occurred as late as several months after quinolone treatment. Overall, quinolones are well tolerated drugs. Their specific toxic potentials have to be considered when they are chosen for treatment of bacterial infections.
Insights
Fluoroquinolones can cause adverse effects like CNS, skin, and gastrointestinal reactions. Careful consideration of specific toxic potentials, including phototoxicity and chondrotoxicity, is crucial when prescribing these antibiotics.
Area of Science:
- Pharmacology and Toxicology
- Infectious Diseases
Background:
- Fluoroquinolones are broad-spectrum antibiotics used for bacterial infections.
- Adverse effects are a significant concern with fluoroquinolone therapy, particularly with newer agents.
Purpose of the Study:
- To review the adverse effects associated with fluoroquinolone use.
- To highlight specific toxic potentials and risk factors for newer fluoroquinolone drugs.
Main Methods:
- Literature review of reported adverse effects of fluoroquinolones.
- Analysis of dose-response relationships and specific toxicities.
Main Results:
- Common adverse effects include gastrointestinal, CNS, and skin reactions.
- Newer fluoroquinolones like trovafloxacin, sparfloxacin, and grepafloxacin have specific risks such as neurotoxicity, cardiotoxicity (QT prolongation), phototoxicity, and chondrotoxicity.
- Chondrotoxicity is linked to magnesium chelation and is a concern in pediatric patients.
- Tendopathies, including tendon rupture, can occur late after treatment.
Conclusions:
- Fluoroquinolones are generally well-tolerated, but specific toxic potentials must be considered.
- Risk-benefit assessment is essential, especially for patients with pre-existing conditions or in pediatric populations.
- Avoiding concurrent use with drugs prolonging the QT interval is recommended for sparfloxacin and grepafloxacin.