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Sparfloxacin
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
Sparfloxacin has also been used successfully in the treatment of skin and soft tissue infections, typhoid fever, and an abscess in the pituitary gland (Lipsky et al., 1999b; Ohnishi et al., 2000; Uchida et al., 2008). Sparfloxacin alone and with pentoxifylline have been used for prophylaxis of spontaneous bacterial peritonitis in cirrhotic patients (Mostafa et al., 2014). In some parts of the world, sparfloxacin is available as eye drops and has been successfully used to treat cases of conjunctivitis or corneal infection (Vyas et al., 2002).
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].
Current treatment options for Mycobacterium marinum cutaneous infections
Published in Expert Opinion on Pharmacotherapy, 2023
Marina Medel-Plaza, Jaime Esteban
In conclusion, rifampicin and rifabutin had the lowest MICs among the antibiotics studied. The MICs (Table 2) of minocycline, doxycycline, clarithromycin, imipenem, and amikacin were close to their breakpoints. Among the studied fluoroquinolones, the MICs of sparfloxacin and moxifloxacin were 4–8 times lower than those of levofloxacin ciprofloxacin, and ofloxacin. However, sparfloxacin and moxifloxacin in vivo efficacy for M. marinum have yet to be demonstrated, as well as linezolid [5]. Routine susceptibility testing of M. marinum in vitro is not recommended and is reserved only for relapse cases [21]. However, in areas with high resistance rates, we believe that antimicrobial susceptibility testing in vitro should be performed in all cases.
Design and evaluation of dental films of PEGylated rosin derivatives containing sparfloxacin for periodontitis
Published in Drug Development and Industrial Pharmacy, 2018
Dinesh M. Morkhade, Vishwanath S. Nande, Umesh V. Barabde, Arun T. Patil, Siddheshwar B. Joshi
In a series of papers from our laboratory, we demonstrated that PEGylated rosin derivatives (PRDs) (containing rosin, PEG 400, and maleic anhydride) are the improved in series ester-adduct derivatives of rosin having an excellent film-forming propensity [15–19]. These could be used successfully as a coating, matrixing, and microencapsulating materials for sustained drug release [15–19]. Furthermore, PRDs are biocompatible and degrade slowly in vivo over a period of time [20], which make them suitable candidates for designing sustained-release films/implants for the treatment of periodontitis. In view of this, present study was undertaken with an objective to investigate the application of PRDs to produce sustained-release antibacterial films containing sparfloxacin for periodontitis. Sparfloxacin occurs as a yellow crystalline powder that is sparingly soluble in glacial acetic acid or chloroform, very slightly soluble in ethanol, and practically insoluble in water [21]. The mean elimination half-life (t1/2) of sparfloxacin is 20 h; the t1/2 is independent of the dose suggesting that sparfloxacin elimination kinetics are linear. It is a synthetic, orally administered member of quinoline class of broad-spectrum antibacterial agent, which is particularly active against anaerobes such as Prevotella melaninogenicus, Bacteroides fragilis, Actinobacillus actinomycetem comitans, and aerobic isolates such as Spirochaetes, Pseudomonas aeruginosa, Escherichia coli, and Streptococus salivarius. These isolates are often found in the patients suffering from periodontitis. Therefore, sparfloxacin was selected as a model drug for the present study.