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    / Pfizer


    Active Ingredient
    Linezolid 600 mg, 2 mg/ml

    Status in Israel
    RX

    Presentation and Status in Health Basket

    Presentation Basket Yarpa Pharmasoft

    Tablets

    10 X 600 mg

    not in the basket chart 54453 26116

    Solution for Infusion

    300 ml X 2 mg/ml

    not in the basket chart

    Related information


    Dosage

    Linezolid solution for infusion and film coated tablets may be used as initial therapy. Patients who commence treatment on the parenteral formulation may be switched to either oral presentation when clinically indicated. In such circumstances, no dose adjustment is required as linezolid has an oral bioavailability of approximately 100%. The solution for infusion should be administered over a period of 30 to 120 minutes. The film coated tablets may be taken with or without food. The recommended linezolid dosage should be administered IV or orally twice daily.
    Complicated skin and skin structure infections, Community-acquired pneumonia, including concurrent bacteremia, Nosocomial pneumonia:
    Pediatric Patients(Birth through 11 Years of Age), Adults and Adolescents (12 Years and Older): 10 mg/kg IV or oralq8h, recommended duration of treatment – 10 to 14 consecutive  days.
    Vancomycin-resistant Enterococcus faecium infections, including concurrent bacteremia:
    Pediatric Patients(Birth through 11 Years of Age), Adults and Adolescents (12 Years and Older): 10 mg/kg IV or oralq8h, recommended duration of treatment – 14to 28 consecutive days.
    Uncomplicated skin and skin structure infections:
    Pediatric Patients† (Birth through 11 Years of Age): <5 yrs: 10 mg/kg oral‡ q8h  5-11 yrs: 10 mg/kg oral q12h  – 10 to 14 consecutive  days.
    Adults and Adolescents (12 Years and Older): Adults: 400 mg oral q12h. Adolescents: 600 mg oralq12h-  – 10 to 14 consecutive  days.
    Due to the designated pathogens.

    Neonates <7 days: Most pre-term neonates < 7 days of age (gestational age < 34 weeks) have lower systemic linezolid clearance values and larger AUC values than many full-term neonates and older infants. These neonates should be initiated with a dosing regimen of 10 mg/kg q12h. Consideration may be given to the use of 10 mg/kg q8h regimen in neonates with a sub-optimal clinical response. All neonatal patients should receive 10 mg/kg q8h by 7 days of life. ‡ Oral dosing using linezolid Tablet.
    Adult patients with infection due to MRSA should be treated with Linezolid q12h.
    In limited clinical experience, 5 out of 6 (83%) pediatric patients with infections due to Gram-positive pathogens with MICs of 4 μg/mL treated with Linezolid had clinical cures. However, pediatric patients exhibit wider variability in linezolid clearance and systemic exposure (AUC) compared with adults. In pediatric patients with a sub-optimal clinical response, particularly those with pathogens with MIC of 4 μg/mL, lower systemic exposure, site and severity of infection, and the underlying medical condition should be considered when assessing clinical response.
    In controlled clinical trials, the protocol-defined duration of treatment for all infections ranged from 7 to 28 days. Total treatment duration was determined by the treating physician based on site and severity of the infection, and on the patient’s clinical response.
    No dose adjustment is necessary when switching from intravenous to oral administration. Patients whose therapy is started with I.V. Injection may be switched to Tablets at the discretion of the physician, when clinically indicated.
    Elderly patients: No dose adjustment is required.
    Female patients: No dose adjustment is required.
    Patients with renal insufficiency: No dose adjustment is required .
    Patients with mild to moderate renal insufficiency: (ie CLCR> 30 ml/min}: No dose adjustment is required.
    Patients with severe renal insufficiency CLCR < 30 ml/min): No dose adjustment is required. Due to the unknown clinical significance of higher exposure (up to 10 fold) to the two primary metabolites of linezolid in patients with severe renal insufficiency, linezolid should be used with special caution in these patients and only when the anticipated benefit is considered to outweigh the theoretical risk. As approximately 30% of a linezolid dose is removed during 3 hours of hemodialysis, linezolid should be given after dialysis in patients receiving such treatment. The primary metabolites of linezolid are removed to some extent by hemodialysis, but the concentrations of these metabolites are still very considerably higher following dialysis than those observed in patients with normal renal function or mild to moderate renal insufficiency. Therefore, linezolid should be used with special caution in patients with severe renal insufficiency who are undergoing dialysis and only when the anticipated benefit is considered to outweigh the theoretical risk. To date, there is no experience of linezolid administration to patients undergoing continuous ambulatory peritoneal dialysis (CAPD) or alternative treatments for renal failure (other than haemodialysis).
    Patients with impaired hepatic function: No dose adjustment is required. However, there are no pharmacokinetic data and limited clinical experience of linezolid in patients with severe hepatic insufficiency. Linezolid should be used with special caution in patients with severe hepatic insufficiency and only when the anticipated benefit is considered to outweight the theoretical risk.


    Indications

    Therapy is indicated only when an organism resistant to all other antibiotics is suspected. Indicated in adult and pediatric patients for the treatment of infections when known or suspected to be caused by susceptible organisms including those associated with concurrent bacteraemia such as: Pneumonia – community acquired and nosocomial pneumonia including multi drug resistant streptococcus pneumonia (MDRSP). Skin and soft tissue infections including diabetic foot infections. Enterococcal  infections. Combination therapy may be indicated if a concomitant Gram negative pathogen is documented or suspected.


    Contra-Indications

    Hypersensitivity to linezolid or to any of the excipients.
    Oxidase Inhibitors: Linezolid should not be used in patients taking any medicinal product which inhibits monoamine oxidases A or B (e.g. phenelzine, moclobemide) or within two weeks of taking any such medicinal product.
    Potential Interactions Producing Elevation of Blood Pressure: Unless the patients are monitored for increases in blood pressure, linezolid should not be administered to patients with uncontrolled hypertension, pheochromocytoma, thyrotoxicosis and/or patients taking any of the following types of medications: directly and indirectly acting sympathomimetic agents (e.g., pseudoephedrine, phenylpropanolamine), vasopressive agents (e.g., epinephrine, norepinephrine), dopaminergic agents (e.g., dopamine, dobutamine).
    Serotonergic Interactions: Patients are carefully observed for signs and/or symptoms of serotonin syndrome, linezolid not be administered to patients with carcinoid syndrome and/or patients taking any of the following medications: serotonin re-uptake inhibitors, tricyclic antidepressants, serotonin 5–HT1 receptor agonists (triptans), meperidine or buspirone.


    Special Precautions

    Pseudomembranous colitis has been reported with nearly all antibacterial agents including linezolid, and may range in severity from mild to life-threatening. Therefore, it is important to consider this diagnosis in patients who present with diarrhoea subsequent to the administration of any antibacterial agent. Clostridium difficile associated diarrhea (CDAD) has been reported with use of nearly all antibacterial agents, including linezolid, and may range in severity from mild diarrhea to fatal colitis. Treatment with antibacterial agents alters the normal flora of the colon leading to overgrowth of C. difficile. C. difficile produces toxins A and B which contribute to the development of CDAD. Hypertoxin producing strains of C. difficile cause increased morbidity and mortality, as these infections can be refractory to antimicrobial therapy and may require colectomy. CDAD must be considered in all patients who present with diarrhea following antibiotic use. Careful medical history is necessary since CDAD has been reported to occur over two months after the administration of antibacterial agents. If CDAD is suspected or confirmed, ongoing antibiotic use not directed against C. difficile may need to be discontinued. Appropriate fluid and electrolyte management, protein supplementation, antibiotic treatment of C. difficile , and surgical evaluation should be instituted as clinically indicated. The use of antibiotics may occasionally result in an overgrowth of non-susceptible organisms. Should superinfection occur during therapy, appropriate measures should be taken.
    Myelosuppression: including anaemia, leucopenia(including anemia, leucopenia, pancytopenia and thrombocytopenia has been reported in patients receiving linezolid. In cases where the outcome is parameters have hematologic known, when linezolid was discontinued, the affected risen toward pretreatment levels.
    See prescribing information for full details.


    Side Effects

    Abdominal pain/cramps/distension, diarrhea, nausea, vomiting.
    See prescribing information for full details.


    Drug interactions

    Linezolid is not detectably metabolised by the cytochrome P450 (CYP) enzyme system and it doesn’t  induse or inhibit  the activities of clinically significant human CYP Isoforms (lA2, 2C9, 2C19, 2D6, 2El, 3A4).
    See prescribing information for full details.  


    Pregnancy and Lactation

    Pregnancy: There are no adequate data from the use of linezolid in pregnant women.
    Lactation: Breast feeding should be discontinued prior to administration of linezolid.
    See prescribing information for full details.


    Overdose

    No cases of overdose have been reported. However, the following information may prove useful: Supportive care is advised together with maintenance of glomerular filtration. Approximately 30% of a linezolid dose is removed during 3 hours of haemodialysis, but no data are available for the removal of linezolid by peritoneal dialysis or haemoperfusion. The primary metabolites of linezolid are also removed by haemodialysis. Signs of toxicity in rats following doses of 3000 mg/kg/day linezolid were decreased activity and ataxia whilst dogs treated with 2000 mg/kg/day experienced vomiting and tremors.


    Important notes

    Storage: Solution for injection: store below 25°C.


    Manufacturer
    Fresenius Kabi Pfizer Pharmaceuticals Ltd
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