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Fluoroquinolones
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Fluoroquinolones

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Pharmacology".

Deadline for manuscript submissions: 25 July 2025 | Viewed by 12167

Special Issue Editors

Dr. Cecilia Bove

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Guest Editor
Department of Biological Sciences, York College of Pennsylvania, 17403 York, PA, USA
Interests: vagus nerve; neurogastroenterology; fluoroquinolones
Dr. Nuno Manuel Xavier

E-Mail Website
Guest Editor
Centro de Química Estrutural, Institute of Molecular Sciences, Departamento de Química e Bioquímica, Faculdade de Ciências, Universidade de Lisboa, Lisboa, Portugal
Interests: organic chemistry; medicinal chemistry; carbohydrate and nucleos(t)ide chemistry; bioactive molecules; enzyme inhibitors; anticancer agents; antimicrobial agents; anti-Alzheimer’s agents
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

You are invited to submit a manuscript for a Special Issue of Pharmaceuticals on fluoroquinolones.

Fluoroquinolones are a class of antibiotics widely used to treat various bacterial infections due to their broad spectrum of activity. They are effective against many types of bacteria, including those causing respiratory, urinary tract, gastrointestinal, and skin infections. Common fluoroquinolones include ciprofloxacin, levofloxacin, and moxifloxacin.

While fluoroquinolones are generally effective and well-tolerated, they are associated with a rare but serious side effect known as fluoroquinolone-associated disability (FQAD). FQAD encompasses a range of symptoms that can persist long after discontinuation of the medication. These symptoms may include severe fatigue, muscle weakness, joint pain, nerve damage, cognitive difficulties, and psychiatric disturbances. Since the discovery of FQAD, fluoroquinolones have received a “Black Box” label, warning clinicians worldwide to prescribe these antibiotics for uncommon infections or for infections that have not resolved with the utilization of other antibiotic drugs; yet, fluoroquinolones are still among the most prescribed antibiotics worldwide.

The exact mechanism behind FQAD is not fully understood, but it is believed to involve mitochondrial dysfunction, oxidative stress, and damage to connective tissues and nerves. Certain individuals may be predisposed to developing FQAD due to genetic factors or underlying health conditions.

The risk of FQAD is generally higher in older adults, those with a history of tendon disorders, and individuals taking corticosteroids or concurrently using other medications that affect the central nervous system. Symptoms of FQAD can range from mild discomfort to debilitating disability, severely impacting the quality of life of affected individuals.

Dr. Cecilia Bove
Dr. Nuno Manuel Xavier
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • fluoroquinolones
  • fluoroquinolone-associated disability
  • antibiotic safety
  • fluoroquinolone toxicity
  • antibiotic stewardship

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Published Papers (6 papers)

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Research

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15 pages, 4463 KiB  
Article
Norfloxacin Derivative with Carbazole at C-7 FQB-1 Induces Cytotoxic, Antiproliferative, and Antitumor Effects in an Experimental Lung Carcinoma Model
by Alondra Bocanegra-Zapata, Hiram Hernández-López, Socorro Leyva-Ramos, Rodolfo Daniel Cervantes-Villagrana, Marisol Galván-Valencia, L. Angel Veyna-Hurtado, Norma Guadalupe Ramírez Tovar, Damaris Albores-García, Juan Armando Flores de la Torre and Alberto Rafael Cervantes-Villagrana
Pharmaceuticals 2025, 18(5), 664; https://doi.org/10.3390/ph18050664 - 30 Apr 2025
Viewed by 2338
Abstract
Background: Cancer remains a leading cause of morbidity and mortality worldwide. According to the World Health Organization (WHO), lung cancer is the most prevalent type of cancer among both men and women. Despite the various pharmacological and biological treatments available for lung cancer, [...] Read more.
Background: Cancer remains a leading cause of morbidity and mortality worldwide. According to the World Health Organization (WHO), lung cancer is the most prevalent type of cancer among both men and women. Despite the various pharmacological and biological treatments available for lung cancer, their effectiveness has often fallen short, and the side effects can be severe. Therefore, there is an ongoing need to identify and develop novel compounds with enhanced anti-tumor efficacy and improved safety profiles. Research has shown that fluoroquinolone derivatives exhibit a broad cytotoxic spectrum comparable to other drugs used in clinical chemotherapy. Objective: The aim of this work was to synthesize and evaluate the cytotoxic, anti-proliferative, and anti-tumor effects of FQB-1, a novel fluoroquinolone derivative. Results: In silico molecular docking analysis demonstrated a strong interaction between FQB-1 and human topoisomerase, with a binding affinity score of –9.8 kcal/mol. In vitro cytotoxicity and anti-proliferative assays were conducted using the Lewis Lung Carcinoma (LLC) cell line. FQB-1 was tested at concentrations of 2.5, 5.0, 25.0, 50.0, 100.0, and 150.0 µg/mL. Significant cytotoxic and anti-proliferative effects were observed at concentrations of 50–150 µg/mL after 24 h of treatment. To evaluate FQB-1′s efficacy in vivo, a syngeneic tumor model was established in C57BL/6 mice. Treatment with FQB-1 (100 mg/kg) resulted in a marked reduction in tumor volume compared to the untreated control group. Histopathological analysis of tumor tissues from treated animals revealed a decrease in mitotic index and an increase in necrotic regions, indicating compromised tumor viability. Conclusions: FQB-1 exhibits cytotoxic and anti-proliferative effects and can reduce tumor growth while compromising tumor viability. Full article
(This article belongs to the Special Issue Fluoroquinolones)
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16 pages, 3371 KiB  
Article
A Prospective Randomized Pilot Study on the Efficacy of a Dietary Supplementation Regimen of Vitamin E and Selenium for the Prevention of Fluoroquinolone-Induced Tendinopathy
by Oana-Maria Mișcă, Liviu-Coriolan Mișcă, Bogdan Huzum, Andreea-Adriana Neamţu, Simona Cerbu, Daniel-Raul Chioibaș, Petrișor Zorin Crăiniceanu and Andrei Gheorghe Marius Motoc
Pharmaceuticals 2025, 18(4), 575; https://doi.org/10.3390/ph18040575 - 15 Apr 2025
Viewed by 505
Abstract
Background: Fluoroquinolone-induced tendinopathy is a clinically significant adverse effect associated with this class of antibiotics, particularly affecting the Achilles tendon. Despite its growing recognition, the precise pathophysiological mechanisms remain incompletely understood, with hypotheses referencing increased matrix metalloproteinase activity, collagen degradation, and oxidative [...] Read more.
Background: Fluoroquinolone-induced tendinopathy is a clinically significant adverse effect associated with this class of antibiotics, particularly affecting the Achilles tendon. Despite its growing recognition, the precise pathophysiological mechanisms remain incompletely understood, with hypotheses referencing increased matrix metalloproteinase activity, collagen degradation, and oxidative stress. Methods: This prospective randomized pilot study evaluates the potential protective effectiveness of vitamin E and selenium supplementation in mitigating fluoroquinolone-induced tendinopathy. The study was conducted on 25 patients receiving 500 mg/day levofloxacin antibiotherapy, randomly divided into a control group and an experimental group—vitamin E (400 IU/day) and selenium (200 µg/day), oral supplementation for 28 days. Clinical assessment of the pain level through the VAS score and of functionality through the VISA-A score was performed, alongside ultrasound imaging of the Achilles tendon. To assess potential toxicity and ensure adherence to the supplementation protocol, serial biochemical analyses of serum vitamin E and selenium were performed at predetermined intervals. Results: A significant improvement was observed in pain scores (p = 0.0120) and functional outcomes (p = 0.0340) when comparing the control and experimental groups at the three-month follow-up. Ultrasound analysis revealed reduced tendon thickness and neovascularization, supporting structural recovery. Although the incidence of tendinopathy was lower in the interventional group (13.3% vs. 40%), statistical significance was not reached, possibly due to the small sample size. Conclusions: These findings suggest that antioxidant supplementation with vitamin E and selenium may provide a protective effect against fluoroquinolone-induced tendinopathy, warranting further investigation in larger randomized clinical trials. Full article
(This article belongs to the Special Issue Fluoroquinolones)
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Review

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22 pages, 680 KiB  
Review
Fluoroquinolones for Dermatologists: A Practical Guide to Clinical Use and Risk Management
by Samer Wahood, Omar Alani, Iyla Draw, Lara Shqair, David Wang, Christopher G. Bunick, Giovanni Damiani, Jonathan D. Ho, Sabine Obagi, Hossein Akbarialiabad, Fabrizio Galimberti, Mahmoud Ghannoum and Ayman Grada
Pharmaceuticals 2025, 18(6), 800; https://doi.org/10.3390/ph18060800 - 26 May 2025
Viewed by 193
Abstract
Background: Fluoroquinolones, available in topical and oral formulations, are used to manage bacterial skin and soft tissue infections, including Pseudomonas aeruginosa, atypical mycobacteria, and select multidrug-resistant Gram-negative organisms. Their excellent tissue penetration, bactericidal activity, and convenient dosing make them effective for certain [...] Read more.
Background: Fluoroquinolones, available in topical and oral formulations, are used to manage bacterial skin and soft tissue infections, including Pseudomonas aeruginosa, atypical mycobacteria, and select multidrug-resistant Gram-negative organisms. Their excellent tissue penetration, bactericidal activity, and convenient dosing make them effective for certain skin and soft tissue infections. However, their use is limited by potential safety concerns, including tendinopathy (odds ratio up to 9.1 in corticosteroid users), QT interval prolongation with risk of torsades de pointes, phototoxicity, and rising antimicrobial resistance. Methods: A literature search of PubMed, Scopus, and Web of Science was conducted for articles from January 1985 to April 2025 with the search terms (quinolone OR fluoroquinolone) AND (dermatology OR “skin and soft tissue infection” OR “skin structure infection”). Abstracts and presentations were excluded. A Google search used the same terms for articles from government regulatory agencies. Results: This review provides practical guidance on the clinical use of topical and oral fluoroquinolones in dermatology. Delafloxacin demonstrated over 90% cure rates in trials for complicated skin infections. However, serious safety concerns remain, including a ninefold increase in tendinopathy risk among older adults on corticosteroids and corrected QT intervals exceeding 500 milliseconds in high-risk patients. Phototoxicity varies, with agents like sparfloxacin linked to heightened ultraviolet sensitivity. Resistance to ciprofloxacin exceeds 20 percent in Escherichia coli and P. aeruginosa in some populations. Culture-based prescribing, shorter treatment courses, and preference for topical treatments can reduce risk and preserve efficacy. Conclusions: Fluoroquinolones remain clinically useful in dermatology when prescribed selectively. Their appropriate use requires careful attention to patient risk factors along with their evolving resistance patterns and ongoing stewardship efforts. Full article
(This article belongs to the Special Issue Fluoroquinolones)
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27 pages, 1698 KiB  
Review
Fluoroquinolone-Mediated Tendinopathy and Tendon Rupture
by Ezgi Duman, Sigrid Müller-Deubert, Girish Pattappa, Ioannis Stratos, Stephan A. Sieber, Hauke Clausen-Schaumann, Victoria Sarafian, Chisa Shukunami, Maximilian Rudert and Denitsa Docheva
Pharmaceuticals 2025, 18(2), 184; https://doi.org/10.3390/ph18020184 - 30 Jan 2025
Cited by 1 | Viewed by 2238
Abstract
The fluoroquinolone (FQ) class of antibiotics includes the world’s most prescribed antibiotics such as ciprofloxacin, levofloxacin, and ofloxacin that are known for their low bacterial resistance. This is despite their potential to trigger severe side effects, such as myopathy, hearing loss, tendinopathy, and [...] Read more.
The fluoroquinolone (FQ) class of antibiotics includes the world’s most prescribed antibiotics such as ciprofloxacin, levofloxacin, and ofloxacin that are known for their low bacterial resistance. This is despite their potential to trigger severe side effects, such as myopathy, hearing loss, tendinopathy, and tendon rupture. Thus, healthcare organizations around the world have recommended limiting the prescription of FQs. Tendinopathy is a common name for maladies that cause pain and degeneration in the tendon tissue, which can result in tendon rupture. Whilst there are several identified effects of FQ on tendons, the exact molecular mechanisms behind FQ-mediated tendon rupture are unclear. Previous research studies indicated that FQ-mediated tendinopathy and tendon rupture can be induced by changes in gene expression, metabolism, and function of tendon resident cells, thus leading to alterations in the extracellular matrix. Hence, this review begins with an update on FQs, their mode of action, and their known side effects, as well as summary information on tendon tissue structure and cellular content. Next, how FQs affect the tendon tissue and trigger tendinopathy and tendon rupture is explored in detail. Lastly, possible preventative measures and promising areas for future research are also discussed. Specifically, follow-up studies should focus on understanding the FQ-mediated tendon changes in a more complex manner and integrating in vitro with in vivo models. With respect to in vitro systems, the field should move towards three-dimensional models that reflect the cellular diversity found in the tissue. Full article
(This article belongs to the Special Issue Fluoroquinolones)
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31 pages, 3989 KiB  
Review
Fluoroquinolones and Biofilm: A Narrative Review
by Nicholas Geremia, Federico Giovagnorio, Agnese Colpani, Andrea De Vito, Alexandru Botan, Giacomo Stroffolini, Dan-Alexandru Toc, Verena Zerbato, Luigi Principe, Giordano Madeddu, Roberto Luzzati, Saverio Giuseppe Parisi and Stefano Di Bella
Pharmaceuticals 2024, 17(12), 1673; https://doi.org/10.3390/ph17121673 - 11 Dec 2024
Cited by 4 | Viewed by 3403
Abstract
Background: Biofilm-associated infections frequently span multiple body sites and represent a significant clinical challenge, often requiring a multidisciplinary approach involving surgery and antimicrobial therapy. These infections are commonly healthcare-associated and frequently related to internal or external medical devices. The formation of biofilms [...] Read more.
Background: Biofilm-associated infections frequently span multiple body sites and represent a significant clinical challenge, often requiring a multidisciplinary approach involving surgery and antimicrobial therapy. These infections are commonly healthcare-associated and frequently related to internal or external medical devices. The formation of biofilms complicates treatment, as they create environments that are difficult for most antimicrobial agents to penetrate. Fluoroquinolones play a critical role in the eradication of biofilm-related infections. Numerous studies have investigated the synergistic potential of combining fluoroquinolones with other chemical agents to augment their efficacy while minimizing potential toxicity. Comparative research suggests that the antibiofilm activity of fluoroquinolones is superior to that of beta-lactams and glycopeptides. However, their activity remains less effective than that of minocycline and fosfomycin. Noteworthy combinations include fluoroquinolones with fosfomycin and aminoglycosides for enhanced activity against Gram-negative organisms and fluoroquinolones with minocycline and rifampin for more effective treatment of Gram-positive infections. Despite the limitations of fluoroquinolones due to the intrinsic characteristics of this antibiotic, they remain fundamental in this setting thanks to their bioavailability and synergisms with other drugs. Methods: A comprehensive literature search was conducted using online databases (PubMed/MEDLINE/Google Scholar) and books written by experts in microbiology and infectious diseases to identify relevant studies on fluoroquinolones and biofilm. Results: This review critically assesses the role of fluoroquinolones in managing biofilm-associated infections in various clinical settings while also exploring the potential benefits of combination therapy with these antibiotics. Conclusions: The literature predominantly consists of in vitro studies, with limited in vivo investigations. Although real world data are scarce, they are in accordance with fluoroquinolones’ effectiveness in managing early biofilm-associated infections. Also, future perspectives of newer treatment options to be placed alongside fluoroquinolones are discussed. This review underscores the role of fluoroquinolones in the setting of biofilm-associated infections, providing a comprehensive guide for physicians regarding the best use of this class of antibiotics while highlighting the existing critical issues. Full article
(This article belongs to the Special Issue Fluoroquinolones)
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16 pages, 1043 KiB  
Review
Antibacterial Mechanisms and Clinical Impact of Sitafloxacin
by Elian M. A. Kuhn, Levy A. Sominsky, Marco Chittò, Edward M. Schwarz and T. Fintan Moriarty
Pharmaceuticals 2024, 17(11), 1537; https://doi.org/10.3390/ph17111537 - 16 Nov 2024
Cited by 3 | Viewed by 2514
Abstract
Sitafloxacin is a 4th generation fluoroquinolone antibiotic with broad activity against a wide range of Gram-negative and Gram-positive bacteria. It is approved in Japan and used to treat pneumonia and urinary tract infections (UTIs) as well as other upper and lower respiratory infections, [...] Read more.
Sitafloxacin is a 4th generation fluoroquinolone antibiotic with broad activity against a wide range of Gram-negative and Gram-positive bacteria. It is approved in Japan and used to treat pneumonia and urinary tract infections (UTIs) as well as other upper and lower respiratory infections, genitourinary infections, oral infections and otitis media. Compared to other fluoroquinolones, sitafloxacin displays a low minimal inhibitory concentration (MIC) for many bacterial species but also activity against anaerobes, intracellular bacteria, and persisters. Furthermore, it has also shown strong activity against biofilms of P. aeruginosa and S. aureus in vitro, which was recently validated in vivo with murine models of S. aureus implant-associated bone infection. Although limited in scale at present, the published literature supports the further evaluation of sitafloxacin in implant-related infections and other biofilm-related infections. The aim of this review is to summarize the chemical-positioning-based mechanisms, activity, resistance profile, and future clinical potential of sitafloxacin. Full article
(This article belongs to the Special Issue Fluoroquinolones)
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