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Discontinued Fluoroquinolones
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Grepafloxacin has intermediate activity against anaerobes, generally having MICs in relation to anaerobes one or two doubling dilutions lower than those obtained with ciprofloxacin. Against a broad range of anaerobes the MIC50 and MIC90 of grepafloxacin are 2 and 16 µg/ml, respectively. Using a breakpoint of 2 µg/ml, grepafloxacin inhibits 83% of Bacteroides fragilis spp., compared with 6% for ciprofloxacin. However, against other B. fragilis group anaerobes, grepafloxacin inhibits only 39% of strains (Spangler et al., 1994; Wexler et al., 1994a; Appelbaum, 1995). Grepafloxacin is 2- to 20-fold more active in vitro than norfloxacin, ofloxacin, tosufloxacin, and ciprofloxacin against a wide variety of common and rare Nocardia species, with MIC90 values in relation to these species of 0.6 to 20 µg/ml (Yazawa and Mikami, 1995). The clinical efficacy of grepafloxacin in the treatment of Nocardia infections is uncertain.
Luminescent Lanthanide Probes as Diagnostic and Therapeutic Tools
Published in Astrid Sigel, Helmut Sigel, Metal Ions in Biological Systems, 2004
Grepafloxacin is a drug administrated to patients with urinary, respiratory or cutaneous infections; it is a synthetic fluorinated quinolone derivative having activity against gram-positive and gram-negative bacteria. Callejon and co-workers have developed an analytical method based on luminescence of the terbium-grepafloxacin complex to quantify its concentration in human urine and serum [35]. Average recoveries were around 90% and dynamic range between 10 and 500 ng/mL. It is noteworthy that this analysis is much simpler than the previously described ones in that terbium chloride is let to interact with the drug in the presence of sodium dodecylsulfate. The measurement technique (TRS) is, however, the same.
The safety of antimicrobials for the treatment of community-acquired pneumonia
Published in Expert Opinion on Drug Safety, 2020
Carla Bastida, Dolors Soy, Antoni Torres
Preclinical studies with fluoroquinolones have demonstrated cardiovascular side effects like hypotension or tachycardia after rapid intravenous administration. In addition, certain quinolones can prolong the QT interval by blocking the human Ether-a-go-go Related Gene that encodes the rapid component of the delayed rectifier potassium current (Ikr). This blockade results in the accumulation of potassium within myocytes, which in turn, delays cardiac repolarization [15]. QT prolongation can potentially lead to life-threatening arrhythmias like torsades de pointes. Their use has been associated with a statistically significant 85% increased odds of arrhythmia (odds ratio [OR] 1.85; 95% CI 1.22–2.81) and a 71% increased odds of cardiovascular mortality (OR 1.71; 95% CI 1.39–2.09) [47]. Quinolones do interact with the Ikr current and some of require dose adjustments in cases of renal insufficiency to avoid excessive concentrations, but most drug-induced cases of torsades de pointes appear to occur in a susceptible population. Among the available fluoroquinolones, moxifloxacin has the highest association with QT prolongation, arrhythmia (P-score 0.99), and cardiovascular mortality (P-score 0.99), followed by levofloxacin and ciprofloxacin [47]. Delafloxacin has only recently been marketed, and although clinical experience is limited, there have been no reports of QT prolongation to date. By contrast, sparfloxacin, grepafloxacin, and gatifloxacin were strongly associated with this adverse event and are no longer available [15].
A novel parameter to predict the effects of antibiotic combinations on the development of Staphylococcus aureus resistance: in vitro model studies at subtherapeutic daptomycin and rifampicin exposures
Published in Journal of Chemotherapy, 2019
Maria V. Golikova, Elena N. Strukova, Yury A. Portnoy, Svetlana A. Dovzhenko, Mikhail B. Kobrin, Stephen H. Zinner, Alexander A. Firsov
Bacterial antibiotic resistance has reached alarming proportions. This might relate in part to the usual antibiotic doses not achieving ‘anti-mutant’ blood concentrations, which could result in pathogen resistance and subsequent therapeutic failure. For example, the mutant prevention concentrations (MPCs) of grepafloxacin, levofloxacin and trovafloxacin against 90% of almost 90 clinical isolates of Streptococcus pneumoniae were close to or below peak serum levels (population pharmacokinetic data) attained with dosing regimens recommended by the manufacturers.1 Similar conclusions were drawn with chloramphenicol, rifampicin, vancomycin, norfloxacin and ofloxacin against Staphylococcus aureus2 and with ciprofloxacin against Escherichia coli.3 Later, the anti-mutant ratios of ciprofloxacin’s area under the curve (AUC) to the MIC established by in vitro simulation of antibiotic pharmacokinetics were found to be 3–9 times (S. aureus), 5–11 times (Pseudomonas aeruginosa), and 16–40 times (Klebsiella pneumoniae) higher than clinically achievable AUC/MICs.4 Clinical AUC/MIC ratios of other agents, e.g. linezolid, also may be insufficient to prevent the enrichment of resistant pathogens during therapy.5,6
Moxifloxacin-induced QT interval prolongation and torsades de pointes: a narrative review
Published in Expert Opinion on Drug Safety, 2018
Fahadullah Khan, Mohammad Ismail, Qasim Khan, Zahid Ali
Moxifloxacin shares the usual adverse drug reactions of fluoroquinolones, but is frequently criticized for its amplified risk of QT interval prolongation (QTIP) and torsades de pointes (TdP) [5,6]. Drug-related TdP is a complex regulatory and clinical problem because of its life-threatening nature, variable clinical course, and poor predictability [7]. In general, fluoroquinolones carry a small risk of TdP [8], but safety warnings have been issued for some member of the fluoroquinolone class (levofloxacin, moxifloxacin) while, others have been withdrawn from the market (sparfloxacin, grepafloxacin) for their risk of cardiac arrhythmia [3].