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Clinical Pharmacology of the Anti-Tuberculosis Drugs
Published in Lloyd N. Friedman, Martin Dedicoat, Peter D. O. Davies, Clinical Tuberculosis, 2020
Gerry Davies, Charles Peloquin
Moxifloxacin (MFX) is a moderately water-soluble weak acid (log P 0.01, pKa 5.69–9.42, MW 401.43). It is a synthetic fourth-generation fluoroquinolone with an 8-methoxy substitution. Fluoroquinolones inhibit the enzymes DNA gyrase and Topoisomerase IV (though the latter is lacking in M. tuberculosis), which are responsible for supercoiling of DNA, resulting in disruption of packing of the bacterial chromosome.5In vitro MIC99s for wild-type organisms range from 0.03 to 0.5 μg/mL.111 Spontaneous mutation frequency (determined in Mycobacterium fortuitum) is 4 × 10−957 with mutations in both the gyrA (particularly codons 90 and 94) and less commonly gyrB genes conferring resistance.5
Gemifloxacin
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
Fluoroquinolones act on the bacterial cell by interference with processes mediated by the two topoisomerase enzymes, DNA gyrase and topoisomerase IV (see Chapter 101, Ciprofloxacin). DNA gyrase mediates negative supercoiling of DNA, which is involved in DNA replication and transcription; topoisomerase IV allows decatenation of intertwined DNA strands after replication (Drlica and Hooper, 2003). Fluoroquinolones stabilize the enzyme–DNA cleavage complex formed during activity of these enzymes and block replication, which is believed to ultimately result in cell death (Yague et al., 2002). Mutations affecting one or both subunits of these two enzymes, as well as enhanced drug efflux, contribute to fluoroquinolone resistance.
Complications in Mohs Surgery
Published in Alexander Berlin, Mohs and Cutaneous Surgery, 2014
Jordan B. Slutsky, Scott W. Fosko
The ear is a unique site that may become painful due to chondritis, either infectious or inflammatory, particularly when cartilage is traumatized. Nonsteroidal anti-inflammatory drugs (NSAIDs) may alleviate the pain of chondritis, but infection should be ruled out, as the ear is often colonized by the Gram-negative bacterium Pseudomonas aeruginosa (Figure 4.12). Fluoroquinolones, such as ciprofloxacin or levofloxacin, are typically used for Pseudomonas infections. Although a more detailed discussion of potential medication side effects is outside the scope of this chapter, it should be noted that fluoroquinolones pose a risk for tendonitis or tendon rupture and have an FDA black box warning stating that this risk is increased in patients more than 60 years old; patients on corticosteroids; and patients with kidney, heart, or lung transplants.
Investigation of the effects of three different generations of fluoroquinolone derivatives on antioxidant and immunotoxic enzyme levels in different rat tissues
Published in Drug and Chemical Toxicology, 2022
Fluoroquinolones (FQs) are synthetic derivatives of nalidixic acid with a bactericidal action against both gram-positive and gram-negative pathogens (Dönmez et al.2018). FQs prevent DNA replication by targeting DNA gyrase and topoisomerase IV in bacteria (Gibson et al.2018). Classification of FQs is made by considering their antimicrobial spectrum and clinical indications. Drugs in each group are similar in their antimicrobial activity. In each successive generation, a new and important group of pathogens is added, while also covering the previous generation (Ezelarab et al.2018). FQs are generally classified into four generations according to their activity and spectrum (Mimouni et al.2019). Although many FQs have been developed so far, moxifloxacin (MXF), ciprofloxacin (CIP), gemifloxacin, levofloxacin (LVX), delafloxacin, and ofloxacin have been approved by the U.S. Food and Drug Administration (FDA). Fluoroquinolones are used in the treatment of urinary tract infections, prostatitis, respiratory tract infections, prosthetic joint infections, intra-abdominal infections, skin and skin structure infections, osteomyelitis, and sexually transmitted diseases (Kim and Hooper 2014, Richards et al.2019). In addition, ciprofloxacin, levofloxacin, and moxifloxacin are used against the SARS-CoV-2 threat due to their potential antiviral effects (Karampela and Dalamaga 2020, Scroggs et al.2021).
Colony stimulating factors for prophylaxis of chemotherapy-induced neutropenia in children
Published in Expert Review of Clinical Pharmacology, 2022
The first-line treatment of febrile neutropenia is antibiotic therapy and the identification of infection. Pediatric patients have a narrower choice of antibacterial agents compared to adults due to limited data and safety concerns. For example, there are controversies around the use of fluoroquinolones in children. Based on animal studies conducted in the 1970s, there is a perception that fluoroquinolones have potential toxicity to developing cartilage [46]. Although the American Academy of Pediatrics released a statement in 2011 about how fluoroquinolones are reasonably safe in children, fluoroquinolones are not as frequently prescribed in children compared in adults. Another concern in regards to antibiotic use in children is drug resistance. Antibiotics are the most commonly prescribed medications to children across all age groups [47].]It is necessary to assess the risk versus benefit of using empiric antibiotic therapy versus G-CSFs in children for primary prophylaxis of febrile neutropenia.
Role of dalbavancin as combination therapy: evidence from the literature and clinical scenarios
Published in Expert Review of Anti-infective Therapy, 2022
Bruno Cacopardo, Dario Cattaneo, Francesco Cortese, Mariagrazia Di Luca, Marco Falcone, Giulia Marchetti, Carlo Tascini, Giusy Tiseo, Mario Venditti
In the retrospective study by Morata and colleagues including patients with osteoarticular infection, dalbavancin was associated with high cure rates [36]. Of note, 45 patients had implant-associated infections, while 19 osteomyelitis, septic arthritis, or spondylodiscitis [36]. In the majority of cases, dalbavancin was administered at the dosage of 500 mg once weekly for a median of five doses, and in one case four doses of 1500 mg were administered biweekly. In patients with prosthetic joint infection, 15 (33.3%) patients received dalbavancin in combination with rifampin or other antibiotics, while in patients without implants 31.5% received a combination therapy of dalbavancin plus other antibiotics [36]. Moreover, although the number of patients that received rifampin concomitantly with dalbavancin was low, the success rate was as high as 70%, suggesting that this combination is not subjected to PK interactions and might be a valid alternative to the traditional regimen of levofloxacin plus rifampin for orthopedic implant infections [36]. Remarkably, this option may be crucial to reduce side effects of long-term therapy with fluoroquinolones and to reduce selective pressure and risk of increasing multi-drug resistance [37].