Synergic activity of fluoroquinolones and linezolid against Mycobacterium tuberculosis

Dı́az, Juan Carlos Rodrı́guez; Ruiz, Montserrat; López, Manuela; Royo, Gloria

doi:10.1016/s0924-8579(02)00387-4

Cited by 28 publications

(8 citation statements)

References 15 publications

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“…which included MDR and extensively-drug resistant (XDR) M. tuberculosis isolates in their works. Although Rodriguez Díaz et al [22] and Coban et al [23] found no in vitro synergism with RIF/LZD combination, by classic checkerboard method, in RIF-monoresistant and MDR M. tuberculosis isolates, in our study, by a modified checkerboard method, REDCA, which uses resazurin for reading the assay, synergism was observed in 8/39 (20.5%) of local clinical isolate. From these, 2/8 (25%) were INH-monoresistant, 3/8 (37.5%) were MDR and 3/8 (37.5%) were susceptible isolates.…”

Section: Discussioncontrasting

confidence: 78%

Activity of rifampicin and linezolid combination in Mycobacterium tuberculosis

et al. 2017

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By Time Kill Curve Assay, we could observe in M. tuberculosis HRv and susceptible isolates, that LZD alone, at sub inhibitory concentration, has poor effect on the bacillus death. In some cases, the bacillus growth stayed constant while in others showed regrowth at the eighth day of drug exposure. RIF alone exhibits potent concentration-dependent bactericidal activity, and was strongly dependent by the drug exposure time. The RIF/LZD combination accomplished a bacteriostatic effect in the reference strain and susceptible isolates. For the RIF resistant isolates, the RIF/LZD combination did not enhance the effect in killing bacillus. In this sense, additional, in vitro and in vivo studies are needed to evaluate the effect of RIF/LZD combination in order to better understand the adjunctive action of LZD in the treatment of TB and prevent the emergence of mutants with resistance to the available anti-TB drugs.

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Section: Discussioncontrasting

confidence: 78%

Activity of rifampicin and linezolid combination in Mycobacterium tuberculosis

et al. 2017

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“…The target attainment rate should exceed 90%, since when the rate falls below this value the probability of effectiveness of the dosing regimen is significantly decreased [1]. In the case of ␤-lactams and Streptococcus pneumoniae, 33% time above the minimum inhibitory concentration (T > MIC) has been previously used as a bacteriostatic endpoint [2] and 40% T > MIC as the predictive value for clinical cure in humans [3,4]. Therefore, target attainment analysis provides the highest MIC value for which the target attainment exceeds the endpoint value with a probability of ≥90%.…”

Section: Monte Carlo Simulation Describing the Pharmacodynamic Profilmentioning

confidence: 99%

“…The oxazolidinone linezolid has been reported to possess good in vitro antituberculosis activity [1]. Combination of linezolid and fluoroquinolones has been shown to yield synergistic activity against Mycobacterium tuberculosis [2]. It appears that the optimal design of new dosing regimens would benefit from further pharmacokinetic and pharmacodynamic studies.…”

mentioning

confidence: 99%

Post-antibiotic effects of linezolid and other agents against Mycobacterium tuberculosis

Hui

Au-Yeang

Chan

et al. 2008

International Journal of Antimicrobial Agents

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“…55 -57 Further studies also showed that linezolid was synergic with rifampicin in drug-susceptible M. tuberculosis strains and that it had great capacity for restricting the selection of resistant mutants, as defined by a mutant prevention concentration of only 1.2 mg/L. 58,59 Based on these studies, linezolid was first used in a limited number of TB patients to assess its efficacy and tolerability during long-term administration. 60,61 These studies showed that, although linezolid was effective in treating patients with MDR-TB, its prolonged used was associated with toxicity causing anaemia and peripheral neuropathy that persisted after administration of a half-dose of 600 mg once daily.…”

Section: The Case Of Linezolidmentioning

confidence: 99%

Is repositioning of drugs a viable alternative in the treatment of tuberculosis?

Palomino

Martin

2012

Journal of Antimicrobial Chemotherapy

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Antimicrobial resistance is a serious problem because of the scarcity of new antibiotics effective against pathogens such as methicillin-resistant Staphylococcus aureus, β-lactamase-producing Gram-negative bacteria and multidrug-resistant Mycobacterium tuberculosis. Extensively drug resistance is particularly worrying in tuberculosis (TB), since the causative bacteria have become resistant to almost all available first- and second-line drugs and resistance is a threat to achieving control of the disease. Development of new drugs is a lengthy and costly endeavour. This is a particular problem for antibiotics, usage of which is likely to be of limited duration, and is even more true of antibiotics whose use is restricted to the treatment of a disease, such as TB, that is considered to be 'poverty related', and for which the return on the investment is seen as non-attractive. In spite of this, there is an emerging pipeline of new drugs under development that hopefully will bring new anti-TB drugs to the market in the near future. The strategy of drug repurposing, finding new uses for existing approved medicines, has seen unexpected success in other medical areas. More than one blockbuster drug has originated from this strategy. And in the field of TB, there have been several examples in recent years of this approach leading to the use of drugs for which there is undeniable evidence of efficacy in the treatment of the disease, the best example being the fluoroquinolones, which were not developed originally to treat TB. This article reviews some examples of repurposing of drugs in the treatment of TB, newer candidates for repurposing for which there is already preliminary evidence of activity and possible new options that merit further investigation.

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Synergic activity of fluoroquinolones and linezolid against Mycobacterium tuberculosis

Cited by 28 publications

References 15 publications

Activity of rifampicin and linezolid combination in Mycobacterium tuberculosis

Activity of rifampicin and linezolid combination in Mycobacterium tuberculosis

Post-antibiotic effects of linezolid and other agents against Mycobacterium tuberculosis

Is repositioning of drugs a viable alternative in the treatment of tuberculosis?

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