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Anti-Infective Agents
Published in Radhwan Nidal Al-Zidan, Drugs in Pregnancy, 2020
Risk Summary: The pregnancy experience in humans suggests low risk; however, the authors of one study recommended avoid giving Lomefloxacin during pregnancy because safer alternatives are generally available. However, fluoroquinolones are commonly avoided in the perinatal period because of fears from fetal cartilage damage.
Lomefloxacin
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
Lomefloxacin has antibacterial activity broadly similar to that of norfloxacin, enoxacin, and fleroxacin. Its activity is similar to or inferior to that of ofloxacin, but it is 2 to 8 times less active than ciprofloxacin. It is inferior in spectrum to newer fluoroquinolones such as moxifloxacin or gatifloxacin (Aldridge et al., 1989; Clarke and Zemcov, 1989; Inderlied et al., 1989; Jones et al., 1988; Mayer and Ellal, 1992; Robbins et al., 1989; Shah et al., 1989; Stratton and Weeks, 1989; Sun et al., 1989; Weinstein, 1988; Wise et al., 1988; see Chapter 105, Moxifloxacin, and Chapter 115, Gatifloxacin). The minimum inhibitory concentrations (MICs) of lomefloxacin against some selected bacterial species are shown in Table 116.1, although there have been very little new data since at least 2006.
Design, formulation and optimization of topical ethosomes using full factorial design: in-vitro and ex-vivo characterization
Published in Journal of Liposome Research, 2022
Lomefloxacin HCl (LH), a synthetic second-generation fluoroquinolone antibiotic (Beberok et al.2013, Khalil et al.2017a), has a broad-spectrum activity against a wide range of gram-positive and gram-negative bacteria (Khalil et al.2017b, Sato et al.1996). The fluoroquinolones are effective against a wider variety of infectious diseases (Sato et al.1996, Gomes and Salgado, 2005), including bacterial skin infection, skin burns, eczema, psoriasis and skin allergies. Lomefloxacin possesses excellent activity against E. coli, Neisseria gonorrhoea, S. pneumoniae and Staphylococcus aureus (Khalil et al.2017b). Lomefloxacin is currently available in the market in the oral form; yet, various disadvantages might hinder its oral administration such as; low bioavailability ≃30–40% (Khalil et al.2017a), systemic side effects and frequent dosing. Hence; an alternative topical LH formulation will be developed in the present study. In particular, topical application can enhance the residence time of drugs in the stratum corneum (SC) and epidermis, thereby increasing the skin deposition whereas reducing the systemic absorption, since they act as a rate-limiting membrane (Junyaprasert et al.2012).
In vitro toxicity evaluation of lomefloxacin-loaded MCM-41 mesoporous silica nanoparticles
Published in Drug and Chemical Toxicology, 2021
Virginia Tzankova, Denitsa Aluani, Yordan Yordanov, Massimo Valoti, Maria Frosini, Ivanka Spassova, Daniela Kovacheva, Borislav Tzankov
Here, we developed a new mesoporous silica MCM-41 drug-delivery formulation, loaded with antibacterial agent lomefloxacin. In fact, lomefloxacin is interesting as a model molecule considering the safety point of view. Lomefloxacin is a fluoroquinolone derivative having a broad spectrum of activities against Gram-negative and Gram-positive microorganisms. It is widely used for treating a large number of diseases, such as urinary tract, respiratory, genital, gastrointestinal tract, skin, bone, and joint infections (Sadeek and El-Shwiniy 2010, McEvoy 2016). Recently, pharmacovigilance risk assessment committee (PRAC) of European Medicinal Agency announced new restrictions in the use of fluoroquinolone and quinolone antibiotics, following a critical review of some disabling and potentially long-lasting side effects (European Medicinal Agency 2018). The use of the lomefloxacin is commonly accompanied by adverse effects. Similarly to other quinolone derivatives with antibacterial activity (i.e. sparfloxacin, ciprofloxacin, norfloxacin), lomefloxacin exhibits a high phototoxic potential (Nobuhiko et al.1990, Beberok et al.2013, 2015). The important role of reactive oxygen species (ROS) formation in the mechanism of lomefloxacin induced cytotoxicity has been previously reported (Wagai et al.1989, Wagai and Tawara 1991). The development of new fluoroquinolone formulations is focused on improved drug release and compliance by diminishing the drugs side effects (Li 1985, Qian and Ma 2004, Shen et al. 2004, Cheow and Hadinoto 2011).