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

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.

Safety and Efficacy of Nemonoxacin vs Levofloxacin in Patients With Community-Acquired Pneumonia: A Systematic Review and Meta-Analysis of Randomized Control Trials

“…The cardio-toxic side effects include QT interval prolongation and bundle branch blockage [ 24 ]. According to Pharmacovigilance Working Party (PhVWP) [ 25 ], some fluoroquinolones can cause torsade's de points, especially those that favor QT interval prolongation.…”

A Review of the Development of Multitarget Molecules against HIV-TB Coinfection Pathogens

“…Within this scenario of the constant development of resistant strains and the high toxicity of the drugs used in therapy, the search for new therapeutic options becomes imperative. Many groups have been searching for new anti-MTB drugs [21][22][23][24].…”

“…In 2017, Alexandrova and coworkers reported compounds [102] with chemical structures based on the DUR derivative 21, which had been previously synthesized by Shmalenyuk and coworkers [103]. Alexandrova et al reported hybridization between DUR+AZT (22) and between AZT+5-arylaminouracil (23), as well as the anti-MTB activity of the compounds [104] (Figure 20). Although all the compounds exhibited dual activity in vitro (MT-4 cells) and in ex vivo HIV-1 assays, the hybrid 23 exhibited the highest HIV-1 inhibitory activity, as well as good inhibitory activity against the MS-115 drug-resistant MTB line.…”

Host–Guest Doping Modulated Afterglow Emission of Fluoroquinolones for Their Separation-Free Detection and Discrimination

“…Fluoroquinolones (FQs) are a group of synthetic antibacterial drugs that bear a basic structure of 1,4-dihydro-4-oxoquinoline-3-carboxylic acid. Due to their broad antimicrobial spectrum, good oral absorption, high antibacterial efficiency, and low cost, FQs are heavily used in human health care, animal farming, and aquaculture for bacterial infections, disease prevention, growth promotion, and inhibiting fungal reproduction. − The wide and overuse of FQs also elevate the potential for excessive residues in animal food products, e.g., eggs, milks, and meats, which result in serious adverse effects for human consumers, such as nervous system toxicity, skin reaction, and phototoxicity. − In addition, residues of FQs also lead to antibiotic resistance concerns, whereas the development of new FQs severely lags the rapid proliferation and dissemination of resistance. , Many countries and organizations have set up restrictive maximum residue limits (MRLs) for FQs in edible food products, and some FQs are even prohibited from using. , Therefore, the development of analytical methods for FQ residues is of great significance for food safety and human health. In addition, derivatives of FQs are also produced by modifying the basic 4-quinolone structure at positions of N-1, C-5, C-6, C-7, and C-8.…”