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Review
. 2023 Mar 1;15(3):804.
doi: 10.3390/pharmaceutics15030804.

Overview of Side-Effects of Antibacterial Fluoroquinolones: New Drugs versus Old Drugs, a Step Forward in the Safety Profile?

Aura Rusu  1 , Alexandra-Cristina Munteanu  2 , Eliza-Mihaela Arbănași  1 , Valentina Uivarosi  2
Affiliations
Review

Overview of Side-Effects of Antibacterial Fluoroquinolones: New Drugs versus Old Drugs, a Step Forward in the Safety Profile?

Aura Rusu et al. Pharmaceutics. .

Abstract

Antibacterial fluoroquinolones (FQs) are frequently used in treating infections. However, the value of FQs is debatable due to their association with severe adverse effects (AEs). The Food and Drug Administration (FDA) issued safety warnings concerning their side-effects in 2008, followed by the European Medicine Agency (EMA) and regulatory authorities from other countries. Severe AEs associated with some FQs have been reported, leading to their withdrawal from the market. New systemic FQs have been recently approved. The FDA and EMA approved delafloxacin. Additionally, lascufloxacin, levonadifloxacin, nemonoxacin, sitafloxacin, and zabofloxacin were approved in their origin countries. The relevant AEs of FQs and their mechanisms of occurrence have been approached. New systemic FQs present potent antibacterial activity against many resistant bacteria (including resistance to FQs). Generally, in clinical studies, the new FQs were well-tolerated with mild or moderate AEs. All the new FQs approved in the origin countries require more clinical studies to meet FDA or EMA requirements. Post-marketing surveillance will confirm or infirm the known safety profile of these new antibacterial drugs. The main AEs of the FQs class were addressed, highlighting the existing data for the recently approved ones. In addition, the general management of AEs when they occur and the rational use and caution of modern FQs were outlined.

Keywords: adverse effects; antibacterial quinolones; delafloxacin; fluoroquinolones; lascufloxacin; levonadifloxacin; nemonoxacin; side-effects; sitafloxacin; zabofloxacin.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Key compounds in the discovery of QNs: (a) chloroquine, (b) 7-chloro-l-ethyl-l,4-dihydro-4-oxoquinoline-3-carboxylic acid, (c) nalidixic acid, and (d) general structure of QNs (QNs—antibacterial quinolones).
Figure 2
Figure 2
Chemical structures of FQs used in therapy and approved by the EMA and FDA (EMA—European Medicine Agency, FDA—Food and Drug Administration, FQs—fluoroquinolones).
Figure 3
Figure 3
Chemical structures of the recently approved systemic antibacterial (fluoro)quinolones in the countries where they were produced.
See this image and copyright information in PMC

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