| Customization: | Available |
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| Quality Standard: | USP, Bp |
| Package: | 10 Tablets |
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| Generic Name | Linezolid Tablets |
| Strength | 600mg |
| Packing | 10 Tablets/box |
| Origin | China |
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Product name:
Linezolid Tablets 600mg
Character:
This product is white or white film coating.
Indications:
This product is used to treat the following infections caused by specific microbial sensitive strains:
Hospital-acquired pneumonia, hospital-acquired pneumonia caused by Staphylococcus aureus (methicillin-sensitive and resistant strains) or Streptococcus pneumoniae.
Community-acquired pneumonia, community-acquired pneumonia caused by Streptococcus pneumoniae, including concomitant bacteremia, or community-acquired pneumonia caused by Staphylococcus aureus (only the methicillin-sensitive strain).
Complex skin and skin soft tissue infections, including diabetic foot infections without osteomyelitis, complex skin and skin soft tissue infections caused by Staphylococcus aureus (methicillin-sensitive and resistant strains), Streptococcus pyogenes, or Streptococcus agalactis. There have been no studies on linezolid for the treatment of bedsores.
· Uncomplicated skin and skin soft tissue infections, caused by Staphylococcus aureus (only methicillin-sensitive strains) or Streptococcus pyogenes.
· Vancomycin-resistant enterococcus faecium infections, including concomitant bacteremia.
To reduce the occurrence of bacterial resistance and to ensure the efficacy of linezolid and other antimicrobial agents, Linezolid should only be used to treat or prevent infections caused by confirmed or highly suspected sensitive bacteria. If bacterial culture and drug sensitivity results are available, consideration should be given to selecting or adjusting antimicrobial therapy accordingly. In the absence of such data, local epidemiological data and drug sensitivity status may contribute to the selection of empiric treatment.
In controlled clinical studies, the safety and efficacy of linezolid preparations over 28 days have not been evaluated.
Linezolid is not indicated for the treatment of gram-negative infections. If a combination of gram-negative bacteria is confirmed or suspected, it is important to immediately begin targeted anti-gram-negative therapy (see warnings).
Pharmacology and toxicology:
Linezolid belongs to a new class of synthetic antibiotics, the oxazolidinone class, which can be used to treat infections caused by aerobic gram-positive bacteria. The antibacterial profile of linezolid in vitro also included some gram-negative bacteria and anaerobic bacteria. Linezolid inhibits protein synthesis by bacteria through a different mechanism of action than other antibacterial agents, so cross-resistance between linezolid and other classes of antibacterial agents is unlikely. Linezolid binds to sites on the 23S ribosomal RNA of the bacterial 50S subunit, thereby preventing the formation of the functional 70S initiation complex, which is an important component of bacterial translation. The results of time-bactericidal curve study indicated that linezolid was a bacteriostatic agent for enterococcus and staphylococcus. Linezolid is a fungicide for most streptococcal strains.
In clinical studies, 6 patients infected with Enterococcus faecium developed resistance to linezolid (4 patients received 200mg q12h, lower than the recommended dose; 600mg q12h in 2 cases). In a compassionate application program, resistance to linezolid developed in 8 patients with enterococcus faecium infection and 1 patient with enterococcus faecalis infection. All patients had an unremoved prosthetic device or an undrained abscess. In vitro, the incidence of linezolid resistance ranges from 1×10-9 to 1×10-11. In vitro studies have shown that point mutation of 23SrRNA is associated with the development of linezolid resistance. In the course of clinical administration, there have been reports of linezolid resistance in vancomycin-resistant enterococcus faecium. In one report, there was hospital-based transmission of enterococcus faecium resistant to vancomycin and linezolid. There has also been a report of Staphylococcus aureus resistance (methicillin-resistant) occurring during clinical administration of linezolid. The resistance of these microorganisms to linezolid is associated with a point mutation in 23SrRNA (where the 2576 bits of bird purine are replaced by thymine). When antibiotic-resistant microbes are found in hospitals, it is important to strengthen infection control. No streptococcal resistance to linezolid has been reported, including Streptococcus pneumoniae.
In vitro studies, linezolid has been shown to be additive or unrelated to vancomycin, gentamicin, rifampicin, imipenem-Cilastatin, amtronam, ampicillin, or streptomycin.
In vitro test and clinical application results show that this product has antibacterial activity against most strains of the following microorganisms:
Aerobic and facultative gram-positive pathogens:
Enterococcus faecium (vancomycin-resistant strains only)
Staphylococcus aureus (including methicillin-resistant strains)
Streptococcus agalactis
Streptococcus pneumoniae (including multi-drug resistant strains [MDRSP])
Streptococcus pyogenes
The minimum inhibitory concentration (MIC) in vitro of at least 90% of the following strains was lower than or equal to the sensitive range of linezolid. This data is only from in vitro studies, and its clinical significance is unclear. The safety and effectiveness of linezolid in the clinical treatment of infections caused by these microorganisms has not been confirmed by sufficient and strictly controlled clinical studies.
Aerobic and facultative gram-positive pathogenic bacteria
Enterococcus faecalis (including vancomycin resistant strains)
Enterococcus faecium (Vancomycin sensitive strain)
Staphylococcus epidermidis (including methicillin-resistant strains)
Staphylococcus haemolyticus
Streptococcus viridis
Aerobic and facultative gram-negative pathogenic bacteria
Pasteurella multocida
Toxicological study
The toxic target organs of linezolid were similar in juvenile and adult rats and dogs. The effect on myelosuppression is time - and dose-dependent, with reduced bone marrow cells, reduced extramedullary blood cell production in the spleen and liver, and decreased red blood cell, white blood cell, and platelet levels in peripheral blood in animal studies. Lymphoid tissue loss occurred in the thymus, lymph nodes and spleen. In summary, signs of lymphatic tissue are associated with the possible observed loss of appetite, weight loss, and suppression of weight gain.
After oral administration of linezolid for 6 months, the sciatic nerve of male animals in the 80mg/kg/day group showed irreversible, mild to mild axial degeneration. In this dose group, slight degeneration of sciatic nerve was also found in 1 male animal at mid-3 months autopsy. Sensitive morphological assessment of perfusion fixation tissue was performed to investigate evidence of optic nerve degeneration. After 6 months of administration, mild to moderate optic nerve degeneration was observed in 2 male rats, but the direct correlation with the drug was unclear because the abnormality was acute and asymmetrically distributed. This neurodegeneration found on microscopic examination is similar to spontaneous unilateral optic degeneration in older rats and may be an intensification of common background changes.
These doses are comparable to those observed in some human subjects. The effects on the hemogram and lymphatic system, although not fully recovered during the recovery period in some studies, are reversible.
Carcinogenicity, genotoxicity, reproductive toxicity
carcinogenicity
No lifetime survival studies in animals were conducted to assess the potential carcinogenicity of linezolid.
genotoxicity
Linezolid has not been found to be teratogenic or mutagenic in gene mutation tests (Ames bacterial retromutation test and Chinese hamster ovarian cell chromosome aberration test), in vitro unconventional DNA synthesis (UDS) test, in vitro chromosome defect analysis of human lymphocytes and in vivo micronucleus test in mice.
Reproductive toxicity
Linezolid did not affect fecundity or reproductive behavior in adult female rats. When administered to adult male rats at a dose of ≥50mg/kg/day (which, according to AUC, is equivalent to or greater than the dose given to humans), it can reversibly reduce the fertility and reproductive behavior of male rats. Reversible effects on reproductive function are mediated by alterations in sperm production. The affected sperm cells contain mitochondria with abnormal morphology and orientation and are inactive. The observed hypertrophy and proliferation of epithelial cells in the epididymis is associated with reduced fecundity. No similar epididymal changes were seen in dogs.
Adolescent male rats were given linezolid (50mg/kg/day, from days 7-36; 100mg/kg/day from 37 to 55 days of birth, according to the average AUC, equivalent to 1.7 times the dose given to human children aged 3 months to 11 years), was found to slightly reduce the fecundity of sexually mature male rats. No effect of shorter treatment periods on fertility was observed during conception and the early neonatal period (equivalent to day 6 to day 5 postnatal), during the neonatal period (days 5 to 21 postnatal), or during adolescence (days 22 to 35 postnatal). Rats were given the drug between days 22 and 35 of birth and a reversible reduction in sperm motility and changes in sperm morphology were observed.
pregnancy
Teratogenic effect, pregnancy classification C: According to AUC, no teratogenic effect was observed in mice, rats or rabbits when the exposure to linezolid was 6.5 times the expected human exposure (mice), or equivalent (rats) or 0.06 times (rabbits), respectively. However, fetal and fetal toxicity can be seen (see non-teratogenic effects). Adequate and well-controlled studies have not been conducted in pregnant women. Linezolid should only be used in pregnant women if the benefits outweigh the potential risks to the fetus.
Non-teratogenic effect
In mice, embryonic and fetal toxicity was detected only at doses that resulted in maternal toxicity (clinical symptoms and decreased weight gain). At a dose of 450mg/kg/day (6.5 times the estimated human exposure based on AUC), increased embryo death was observed after implantation, including whole litter loss, decreased fetal weight, and increased incidence of costocondral fusion.
In rats, mild fetal toxicity was observed at doses of 15 mg/kg/day and 50mg/kg/day (based on AUC, exposure levels approximately 0.22 times the estimated human exposure, respectively). The effects included lower fetal weight and lower sternal ossification, which is often associated with lower fetal weight. At doses of 50mg/kg/day, mild maternal toxicity was observed, manifested by decreased weight gain.
In domestic rabbits, fetal weight loss occurred only at doses of 15mg/kg/day (0.06 times the estimated human exposure based on AUC) and maternal toxicity (clinical signs, decreased weight gain, and decreased food intake).
Female rats given 50mg/kg/day (in AUC terms, equivalent to the human dose) between gestation and lactation experienced a decrease in the number of surviving pups 1-4 days postpartum. An increase in the number of unimplanted embryos is seen when surviving female or male juveniles mate at sexual maturity.
Lactating woman
Linezolid and its metabolites can be secreted in the milk of lactating rats, and the concentration in the milk is similar to that in maternal plasma. It is not known whether linezolid is secreted by human milk. Because many drugs can be secreted by human milk, lactating women should be careful when taking linezolid.
Storage:
Avoid light, seal and store at 15-30 ° C (59-86 ° F).
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