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High-Performance Liquid Chromatography
Published in Adorjan Aszalos, Modern Analysis of Antibiotics, 2020
Joel J. Kirschbaum, Adorjan Aszalos
Rosoxacin was determined in serum, urine, and prostatic tissue using an octadecylsilane column with a mobile phase of acetonitrile-0.2 M aqueous phosphoric acid (37.5:82.5 for serum and 32:68 for urine and tissue) flowing at 1.5 ml/min into a detector set to 280 nm [469]. Cinoxacin was used as internal standard.
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
In December 2016, the Food and Drug Administration (FDA) issued a Drug Safety Communication advising that the use of fluoroquinolone antibiotics be restricted for uncomplicated infections when there are alternative treatment options [50]. This was based on safety review showing that the systemic use of fluoroquinolones was associated with disabling and potentially permanent serious side effects involving tendons, muscles, joints, nerves, and the CNS. More recently, in November 2018, the European Medicines Agency suspended their marketing authorization for medicines containing cinoxacin, flumequine, nalidixic acid, and pipemidic acid [51]. They also recommended restricting the use of all other fluoroquinolones. Specifically, they should not be used for the following: (i) infections that might improve without treatment or that are not severe (e.g. throat infections); (ii) non-bacterial infections (e.g. non-bacterial chronic prostatitis); (iii) traveler’s diarrhea or recurring lower urinary tract infections; or (iv) mild or moderate bacterial infections, unless other antibacterial medicines commonly recommended for these infections cannot be used. They also reminded prescribers that fluoroquinolones should be avoided in patients who have previously experienced these serious side effects, and that caution should be exercised in groups at higher risk of tendon injury (e.g. the elderly, corticosteroid users, patients with kidney disease, and organ transplant recipients).
Delafloxacin: a novel fluoroquinolone with activity against methicillin-resistant Staphylococcus aureus (MRSA) and Pseudomonas aeruginosa
Published in Expert Review of Anti-infective Therapy, 2018
Eric R. Ocheretyaner, Tae Eun Park
The quinolones were first developed in the 1960s, including nalidixic acid, cinoxacin, and oxolinic acid. Addition of fluorine to quinolones yielded fluoroquinolones such as ofloxacin, ciprofloxacin, norfloxacin, pefloxacin, levofloxacin, moxifloxacin, gatifloxacin, and gemifloxacin. The substituents added to certain parts of the quinolone ring (e.g. fluorine) led to an increase in the potency of antibacterial agents. The fluoroquinolones exhibit the antibacterial effects through inhibition of bacterial topoisomerase IV and DNA gyrase (topoisomerase II) enzymes. Quinolones function as a cellular poison by stabilizing the enzyme–DNA complexes after strand breakage, which the cell is able to repair poorly. Therefore, quinolones bind to the DNA gyrase and DNA complex rather than the DNA gyrase alone. The primary mechanism of resistance to fluoroquinolones is alteration in the primary target enzyme of the fluoroquinolones; however, active efflux pumps can also be observed decreasing the fluoroquinolone susceptibility [1]. There has been a focus to identify new fluoroquinolones to combat the growing resistance. Several other fluoroquinolones currently in the pipeline are avarofloxacin (JNJ-Q2), finafloxacin (BAY35–3377), zabofloxacin (DW224a), and non-fluorinated nemonoxacin (TG-873870) [3].
Unresolved gustatory, olfactory and auditory adverse drug reactions to antibiotic drugs: a survey of spontaneous reporting to Eudravigilance
Published in Expert Opinion on Drug Safety, 2019
Sara Ferraro, Irma Convertino, Luca Leonardi, Corrado Blandizzi, Marco Tuccori
Irreversible or persistent mild to moderate disabilities can be an important consequence of adverse drug reactions (ADRs) that strongly affect the quality of life. In 2017, the European Medicine Agency (EMA) started a review of the safety of fluoroquinolone and quinolone antibiotics, with a particular focus on the rare disabling, long-lasting and potentially permanent ADRs, mainly involving muscles, tendons, bones and the nervous system, including sensory ADRs. In November 2018, this review culminated with the recommendation by the Pharmacovigilance Risk Assessment Committee (PRAC) to suspend the marketing authorization of medicines containing quinolones (cinoxacin, flumequine, nalidixic acid, and pipemidic acid) and to restrict the use of fluoroquinolones[1].