Linezolid: its role in the treatment of gram-positive, drug-resistant bacterial infections (original) (raw)
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Linezolid: a promising option in the treatment of Gram-positives
Journal of Antimicrobial Chemotherapy, 2016
Linezolid, an oxazolidinone antimicrobial agent that acts by inhibiting protein synthesis in a unique fashion, is used in the treatment of community-acquired pneumonia, skin and soft-tissue infections and other infections caused by Gram-positive bacteria including VRE and methicillin-resistant staphylococci. Currently, linezolid resistance among these pathogens remains low, commonly <1.0%, although the prevalence of antibiotic resistance is increasing in many countries. Therefore, the development of resistance by clinical isolates should prompt increased attention of clinical laboratories to routinely perform linezolid susceptibility testing for this important agent and should be taken into account when considering its therapeutic use. Considering the importance of linezolid in the treatment of infections caused by Gram-positive bacteria, this review was undertaken to optimize the clinical use of this antibiotic.
Linezolid use in Medicin Therapy against Multiresistant Bacteria-A Review
Journal of Bacteriology & Parasitology, 2017
After the description of an element with ability to combat the infectious processes originating from bacteria, starts a race for survival between the interrelationship of species, bacterial and human. With the evolution scientifictechnical, the man was able to synthesize new antibacterial substances, on the other hand the mechanisms of gene evolution enabled the emergence of multidrug-resistant bacteria. Some of this organisms are frequent on hospital environment and have high adaptability to new drugs, such as Staphylococcus aureus and Enterococcus spp. resistant to oxacillin and vancomycin, considered drugs of choice against multidrug-resistant microorganisms. So, a new antibiotics class was developed, superior to vancomycin and oxazolidinone, the linezolid. Thus, the present study aimed at understanding the use of linezolid in drug therapy against multi-resistant bacteria. To perform this study, a literature review of last 10 years was performed. In 2002, after the liberation of the use of linezolid as treatment for infectious processes against gram-positive bacteria, this drug was commonly used throughout the world. Similarly, the pressure of natural selection stood out, and there were records of resistant strains to linezolid. As prospects for control of infections caused by these resistant strains, was approved by the FDA in 2014 the use of drugs with linezolid resistant anti-strains activity. However, we conclude that, in addition to natural selection and genetic variation process, human behavior regarding the use of antibiotics, increases the selection of resistant microorganisms to antibiotic, including linezolid.
Linezolid and its derivatives: the promising therapeutic challenge to multidrug-resistant pathogens
2018
Linezolid is the main drug representative of the oxazolidinones, widely used in the clinical practice to treat severe Gram-positive infections for some decades. The uniquely particular mechanism of action of Linezolid, with a block of ribosomal assembling before the initiation of bacterial protein synthesis has been studied in various bacteria and linked mainly to mutations in the ribosomal 50S subunit. Over the years, a large amount of clinical and pharmacokinetic data have been accumulated, relating to linezolid use in different patient groups (obesity, enteral feeding, renal failure, neonates, and paediatrics) and in different clinical conditions (sepsis syndrome, skin and soft tissue infection, diabetic foot infection, pneumonia, bone and joint infection, infection of the central nervous system, eye infection, and neutropenic sepsis). In 2001 Linezolid resistance started emerging in Staphylococcus aureus and Enterococcus faecium clinical isolates and once again the attention of ...
Association of Pharmacokinetic and Pharmacodynamic Aspects of Linezolid with Infection Outcome
Current Drug Metabolism, 2009
Linezolid is the first antibiotic of a new class (oxazolidinones). It inhibits protein synthesis by binding to the bacterial 23S ribosomal RNA of the 50S subunit, thus blocking the formation of the functional 70S initiation complex, but it does not inhibit peptidyl transferase. Therefore, its mechanism of action is unique and cross resistance is unlikely to occur; however, resistant strains have already been reported, but the rate of resistance is low in surveillance programs. Linezolid has a favorable pharmacokinetic profile. It is rapidly absorbed when administered orally, and it is 100% bioavailable, thus allowing early switch from intravenous to oral administration. The maximum plasma concentration (range between 13.1±1.8 to 19.5±4.5 μg/ml according to the route of administration, studied population and dosages administered to subjects) is achieved 1-2 hours after the first dosage. It penetrates readily to most tissues of the human body at concentrations much higher than that of the minimal inhibitory concentrations of the targeted pathogens. It is metabolized by oxidation in two major inactive metabolites and is eliminated mainly through the kidneys. Linezolid is bacteriostatic for staphylococci and enterococci but bactericidal for pneumococci and kills bacteria in a time-dependent fashion. It has been studied in several randomized controlled trials and has been approved for the treatment of patients with Gram positive bacterial infections (community-acquired and nosocomial pneumonia, skin and soft tissue infections, and infections due to vancomycin-resistant enterococci) including these due to multidrug-resistant strains. Careful and judicious use is warranted to preserve the activity of this important antibiotic.
1999
The emergence of resistance in gram-positive bacteria has necessitated a search for new antimicrobial agents. Linezolid is an oxazolidinone, a new class of antibacterial agents with enhanced activity against pathogens. We compared the activity of linezolid to those of other antimicrobial agents against 3,945 clinical isolates. Linezolid demonstrated potent activity against all isolates tested. For all vancomycin-susceptible enterococci, staphylococci, and streptococci, the activity of linezolid was comparable to that of vancomycin. Against oxacillin-resistant staphylococci and vancomycin-resistant enterococci, linezolid was the most active agent tested. In summary, linezolid appears to be a promising new antimicrobial agent for the treatment of gram-positive infections.
Linezolid resistant Staphylococcus aureus
International Journal of Research in Medical Sciences, 2014
INTRODUCTION Linezolid is the first antibiotic of the oxazolidine class approved for clinical use for resistant Staphylococcus aureus. It was approved by FDA due to the rising incidence of MRSA. 1 It is the only antimicrobial drug available which has proven high activity against multidrug resistant Staphylococcus aureus including the strains with reduced susceptibility to glycopeptides. 2 MECHANISM OF ACTION OF LINEZOLID Linezolid acts by inhibiting bacterial protein synthesis through binding to the peptidyl transferase centre of the 50S ribosomal subunit. 3 Linezolid stops the growth and reproduction of bacteria by disrupting translation of messenger RNA into proteins in the ribosome. It works on the first step of protein synthesis i.e. initiation unlike other protein synthesis inhibitors which inhibit elongation. 4 CLINICAL USE OF LINIZOLID FOR STAPHYLOCOCCUS INFECTIONS It is the only antibiotic with good activity against MRSA available as an oral formulation; making it desirable for outpatient treatment. 5 It is safe and effective for use in children and newborns as well as adults. When administered for short periods, it is a relatively safe drug,
Anti-Microbial Susceptibility Pattern of Linezolid in Various Clinical Isolates
UK Journal of Pharmaceutical Biosciences, 2016
The literature review is suggestive of good efficacy of Linezolid (Oxazolinedione derivative) against gram positive bacteria only. However it is deficient regarding its susceptibility in various clinical isolates. Therefore, the current study was planned to identify the susceptibility pattern of Linezolid in various isolates. Total 748(n) specimens were included in this study. Out of which 144(n) yielded positive growth. For microbiological culture proceedings all recommended CLSI – 2014 (Clinical and laboratory standard institute) guidelines were followed. The linezolid having 30µgm disc potency was used to assess its susceptibility. The clearing zone diameter of >21mm was considered sensitive. Data was recorded and analyzed by using SPSS version 20 for statistical inference. For numerical variables, frequencies were calculated in terms of percentages. The results of current study showed that 84.2% gram-positive and 45.6% gram-negative organisms were sensitive to linezolid. The ...
Linezolid Resistance in Staphylococci
Pharmaceuticals, 2010
Linezolid, the first oxazolidinone to be used clinically, is effective in the treatment of infections caused by various Gram-positive pathogens, including multidrug resistant enterococci and methicillin-resistant Staphylococus aureus. It has been used successfully for the treatment of patients with endocarditis and bacteraemia, osteomyelitis, joint infections and tuberculosis and it is often used for treatment of complicated infections when other therapies have failed.